Results in Asian Journal of Pharmaceutics: 337
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Asian Journal of Pharmaceutics, Volume 16; https://doi.org/10.22377/ajpmds
Aim: The main aim of this study was to Formulation and Characterization of Repaglinide Transdermal Patch Using Natural polymers. Materials and Methods: The Box–Behnken design was used, which has three levels and three factors to investigate the associate impact of significant attributes on tensile strength, In vitro drug release, and Ex vivo drug permeation. Fifteen formulations were developed that differed in the polymer ratio (9:1, 8:1, and 7:1). The permeation of repaglinide through hairless goat ear skin through Ex vivo was found to increase with the help of permeation enhancer d-limonene. Results: As per the experimental data, it is concluded that the R12 is the best formulation in ex vivo permeation, in which we have taken 30% propylene glycol as a plasticizer, 3% d-limonene as a permeation enhancer, and this formulation shown 301.825 μg/cm2 permeation in 24 h. Conclusion: After optimizing all formulations, it concluded that the ratio of polymer in 9:1, 3% of a permeation enhancer, and 30% plasticize was the optimum quantity of different excipients used in the optimized formulation. These findings suggest that transdermal repaglinide delivery may have therapeutic promise, with benefits such as reduced dose frequency, better patient compliance, non-invasive properties, enhanced bioavailability, and ease of medication discontinuation.
Asian Journal of Pharmaceutics, Volume 6; https://doi.org/10.4103/0973-8398.100152
Preparation and characterization of Simvastatin/ Hydroxy propyl beta cyclodextrin (HPBCD) (SV/HPBCD) binary systems by co-grinding technique and formulating the binary system in oral mucoadhesive microcapsules by using hydrophilic sodium alginate (SA) and another plant seed mucilage dillenia (obtained from Dillenia indica, Family, Dilleniaceae) using orifice gelation technique and systematically evaluating in vitro by using scanning electron microscopy (SEM), fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffractometer (XRD). The microcapsules were smooth and elegant in appearance showed no visible cracks as confirmed by SEM; and extended drug release of 72.682% upto 12 hours in phosphate buffer of pH 6.8; showing particle size within the range of 371.5-457 μm, and less angle of repose, Hausner's ratio and Carr's consolidation index; and showed encapsulation efficiency of 63.068 ± 0.002 to 99.083 ± 0.017%. The in vitro release data of optimized batch of microcapsules were plotted in various kinetic equations to understand the mechanisms and kinetics of drug release, which followed zero order kinetics and value of "n," is calculated to be 0.505 and drug release was diffusion controlled. The in vivo antihyperlipidemic activity of formulations in mice was carried out developing hyperlipidemia in mice and then administering the optimized formulations orally, and the formulation showed promising results.
Asian Journal of Pharmaceutics, Volume 6; https://doi.org/10.4103/0973-8398.100148
This study aimed to prepare anti-glaucomatous dorzolamide hydrochloride-(Dorzo) loaded nanoparticles as a controlled release system. Eudragit RS 100 (RS) and/or RL 100 (RL) were used in formulations by an opportunely adapted Quasi-emulsion solvent diffusion technique. The formulations were evaluated in terms of particle size, zeta potential, drug entrapment, and release profile. All formulations showed tiny particle size varying from 114 to 395 nm for RS and 65 to 277 nm for RL. Positive zeta potential was +19 to +32 mV for RS and +23 to +42 mV for RL formulations. It was demonstrated that increasing polymer concentration lead to increase the percentage of drug entrapped in all batches, to a certain extent (drug: polymer 1:4). Nanoparticles prepared using RL showed lower entrapment efficiency than RS. In contrast, increasing the stirring rate resulted in an increase in the percentage of Dorzo entrapped. A prolonged drug release was shown by all the formulations. Increasing the polymer concentration caused a decrease in the release rate. Moreover, it was evident that increasing RL content increased the amount of Dorzo released. Dorzo-loaded nanoparticles could represent promising drug ophthalmic carriers, due to small particle size, positive zeta potential, and sustained release profile; hence, expecting prolonged corneal contact time, more therapeutically efficient, decreased frequency of administration per day, and better patient compliance.
Asian Journal of Pharmaceutics, Volume 6; https://doi.org/10.4103/0973-8398.100146
The purpose of this research work is to prepare novel eatable gel formulations with suitable rheological characteristics, which provide a means of administering salbutamol sulphate to dysphagic and geriatric patients. Gels prepared using a natural polymer silk fibroin of different concentrations was subjected for in vitro characterization. The effect of concentration of the solution on gelation time, viscosity, and drug release was studied. FTIR and DSC spectra reveal that the drug was found compatible with silk fibroin. TGA curves showed weight loss as the temperature increased. Formulations F3, F4, F6, and F9 had thin, nectar like, honey like, and spoon thick viscosity range respectively, which is considered suitable for dysphagia patients as given by National Dysphagia Diet Task Force. Formulations showed shear thinning pseudoplastic behavior. Based on the concentration and viscosity of the polymer, formulation F9 was found to sustain the release of drug up to 90 min (99.4 ± 0.5%), whereas F3 showed release within 5 min (99.2 ± 2.0%). Mechanism of drug release was found to be anomalous transport. All formulations were found stable after 6 months when kept at refrigerated temperature (4°C - 8°C) and room temperature. It can be concluded that the salbutamol sulphate gels prepared are suitable as vehicles for dysphagic patients.
Asian Journal of Pharmaceutics, Volume 6; https://doi.org/10.4103/0973-8398.100141
The demand for fast disintegrating tablets has been growing during the last decade especially for geriatric and pediatric patients because of swallowing difficulties. Amlodipine besylate is used commonly for the treatment angina pectoris, commonly known as angina, which is chest pain due to ischemia of the heart muscle, generally due to obstruction or spasm of the coronary arteries. Hence, in the present work an attempt has been made to formulate fast dissolving tablets of amlodipine besylate by direct compression technique using various concentration of super disintegrants like cross carmellose sodium (Ac-Di-Sol), polyplasdone R-XL and sodium starch glycolate (SSG). The formulated tablets were evaluated for crushing strength, friability, thickness, diameter, weight variation, drug content, wetting time, water absorption ratio, disintegration time, and percentage of drug release. All formulations showed satisfactory result. Among them formulation F3 containing 3% of Ac-Di-Sol exhibited complete release within 12 minutes and disintegration time was within 10 seconds. Dissolution data was compared with innovator for similarity factor (f2) exhibited an acceptable value >50 (82). Accelerated stability study indicated no significant difference in assay and crushing strength. Hence, three production validation scale batches were designed based on lab scale best batch (F3) and charged for stability. All parameters were within the limit of acceptance. There was no chemical interaction between the drug and excipients during FT-IR study; considered in the present investigation.
Asian Journal of Pharmaceutics, Volume 6; https://doi.org/10.4103/0973-8398.100138
The objective of present work was to incorporate drug-resin complex (DRC) to microspheres to achieve improved drug loading, less leakage, and extended zero order release. Ondensetron hydrochloride (ODH), a model drug was complexed with Indion 244, and incorporated to microspheres of hydroxypropyl methyl cellulose (HPMC), and ethyl cellulose (EC). A 32 full factorial design was used to prepare microspheres using HPMC and EC as independent variables, X1 and X2 respectively. The microspheres obtained were evaluated for yield, topology, micromeritics, drug entrapment, and drug release kinetics. Complexation of ODH with Indion 244 was found to be 28% wt/wt. The incorporation efficiency of DRC to microspheres (DRC1-DRC9) was in the range of 70.41 2.18 to 95.08 0.76% wt/wt. The trend of increase in the drug entrapment (DRC) with high amounts of HPMC and EC was noted for all microspheres. Yield of DRC9 was maximum (84.87% wt/wt), and was lowest for DRC1. Acceptable Hausner's ratio, Carr's compressibility index and angle of repose demonstrated the excellent flowability of microspheres (DRC1 to DRC9). Drug release kinetic studies showed that, ODH dissociation from DRC, and its diffusion through HPMC and EC, both, have contributed for extended zero order release. Especially, from DRC2, maximum extended release was noted up to 19.10 hrs (zero order, R2 = 0.9239). Hence, it can be concluded that, incorporation of DRC to microspheres can overcome poor drug loading, high drug leakage, and poor drug sustainability problems of microspheres. Especially, the zero order release can be achieved by incorporation of DRC to microspheres.
Asian Journal of Pharmaceutics, Volume 6; https://doi.org/10.4103/0973-8398.100136
The main objective of the present study is to prepare floating microsphere of the bromhexine hydrochloride in order to achieve gastro-retention which may result in the improvement of bioavailability and solubility as the bromhexine is soluble up to the pH range of 1-4. The microsphere is prepared by the non-aqueous solvent evaporation method using hydroxyl propyl methyl cellulose and ethyl cellulose in different drug polymer ratios. The in vitro release is studied in the USP dissolution apparatus type I. The percentage yield is more than 60% for the all the batches. The entrapment efficiency increased by increasing the polymer concentration and found to be maximum at 1:4 drug polymer ratios. The drug loading was found to be in the range of the 19.30-33.70%. All the batches show in vitro buoyancy percentage in the range of the 53.3% to 70.13% after 12 h. The in vitro dissolution and permeation studies revealed that the formulations followed zero order release pattern and 'n' values derived from the PEPPAs equation confirmed that the drug release from the floating system was the non-Fickian transport mechanism. The SEM studies revealed that the drug adsorbed on the surface of the microspheres can able to provide the burst effect in order to provide the immediate therapeutic effect. Therefore, the floating microspheres were able to be buoyant up to 12 h, having excellent flow properties, and met the required drug release kinetics for gastro-retentive systems.
Asian Journal of Pharmaceutics, Volume 6; https://doi.org/10.4103/0973-8398.100131
Niacin or nicotinic acid (NA) is used in the treatment of hyperlipidemia. NA immediate release formulation shows undesirable effects like flushing of the face and neck parts. In the present study, NA floating sustained release dosage form was developed to prolong the drug release, to retain the drug delivery system above the site of absorption for the desired period of time, and to reduce the drug release rate compared to conventional formulations in order to minimize the side effects. The preformulation parameters such as flow properties and drug-excipient compatibility studies were performed. The drug excipient compatibility studies were performed using the FTIR study and the results showed that all the polymers used in the study are compatible with the pure drug. The floating sustained release tablets of niacin were prepared by the wet granulation method and the granules were evaluated for various micromeritic properties like bulk density, tapped density, Carr's Index, Hausner's ratio, and angle of repose. The tablets were evaluated for post-compressional parameters like average weight, thickness, hardness, friability, swelling index, floating lag time and total floating time, and in vitro drug release studies. All the formulations showed total floating time >20 hr. The concentration of the effervescent agent and the concentration and type of polymer showed an effect on the floating behavior and drug release. The formulation containing 13% sodium bicarbonate, HPMC (33%) and Eudragit RS PO (4%) showed required drug release up to 20 hr.
Asian Journal of Pharmaceutics, Volume 6; https://doi.org/10.4103/0973-8398.100127
Helicobacter pylori (H. pylori), the major culprit for peptic ulcer, has a unique way of survival in harsh acidic environment of the stomach by colonizing deep in the gastric mucosal layer. Failure of conventional therapies against H. pylori for complete eradication has major limitations like low residence time of delivery system in stomach, poor penetration of drug in gastric mucosa, acidic degradation of antibiotics, and development of antibiotics resistance. The poor penetration of antibiotics through thick viscoelastic mucosal gel results in incomplete eradication of H. pylori. Various investigators have formulated novel gastro-retentive drug delivery systems such as floating systems, mucoadhesive systems, pH-sensitive gel systems, and muco-penetrating delivery systems for increasing the concentration of antibiotic in close proximity to the site of H. pylori infection. This review summarizes the novel drug delivery approaches investigated during the last few years and suggests that a high eradication rate can be achieved by therapy comprising of muco-penetrating delivery systems of antibiotics against H. pylori.
Asian Journal of Pharmaceutics, Volume 6; https://doi.org/10.4103/0973-8398.100125
The objective of the present study offers an overview of regulatory guidelines for medical devices in India. Medical devices are now a pervasive part of modern medical care. They are in many cases associated with quality of care. In some cases, the use of devices has certainly improved quality. In other cases, devices have been associated with many problems. The approach to quality of devices has depended largely on regulation .Recently introduced guidelines and the amendment in the law will provide adequate guidance for both the manufacturers and competent authorities to manage cases efficiently and appropriately. While these regulations and reforms promise to clarify, unify, and expedite the process of manufacturing and importing medical devices into India, they also pose their own challenges and complications. Understanding the regulatory reforms imminent in India will be crucial for foreign companies looking to enter or expand their business in India's medical markets. It is hoped that the guidelines are implemented and regulated properly with effective outcome. This article highlights current regulations pertaining to applications for medical device registration certificates, medical device clinical trials, and medical device manufacturing/importation licenses.
Asian Journal of Pharmaceutics, Volume 6; https://doi.org/10.4103/0973-8398.100118
Since last two decades the work on oleogels is being exploited in pharmaceutical, cosmetics, and nutraceutical industries for their desired rheological, physical, and chemical stabilities in semisolid formulations. Recently, we had developed a stable and efficacious oleogel containing diclofenac diethylamine for topical application. The present review article deals with the literature of oleogels including its application in various fields from last few decades till date. The literature reveals that the oleogels have simplicity in manufacturing, high physical, chemical, and mechanical stability and better invivo efficacy, which make them appropriate to employ as bases for topical formulations.
Asian Journal of Pharmaceutics, Volume 3; https://doi.org/10.4103/0973-8398.59948
Poly (D, L-lactide-co-glycolide) (PLGA) is approved by the Food and Drug Administration for drug delivery use. The polymeric nanoparticles based on PLGA and its co-polymer are designed for controlled and targeted drug delivery. Also, PLGA and its co-polymer are important in designing nanoparticles with desired characteristics such as biocompatibility, biodegradation, particle size, surface properties, drug release and targetability. This review focuses on the polymer literature, methods for preparation of nanoparticles and recent studies on the nanoparticles based on PLGA and its co-polymer for the conventional and targeted delivery of drugs by various routes.
Asian Journal of Pharmaceutics, Volume 10; https://doi.org/10.22377/ajp.v10i03.755
Asian Journal of Pharmaceutics, Volume 3; https://doi.org/10.4103/0973-8398.56292
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.72125
The aim of the present study was to mask the extremely bitter taste of Tramadol HCL, an opioid analgesic, and to formulate a tablet which can rapidly disintegrate in saliva (rapidly disintegrating tablet). The crucial aspect in the formulation of mouth-dissolving tablets is to mask the bitter taste and to minimize the disintegration time. Taste masking was done using sweetening agent and D-mannitol and taste-masked pellets were prepared by extrusion spheronization technique. Prepared pellets were tested for drug content, taste evaluation in oral cavity and molecular property. Pellet shows significant taste masking, confirmed by in vitro taste evaluation; therefore, it was selected for further study. Pellets were evaluated for density, angle of repose, Carr's index, Hausner's ratio and sphericity while tablets were evaluated for disintegration and in vitro dissolution. A 3 2 full factorial design and statistical models were applied to optimize the effect of two factors, i.e. superdisintegrant sodium starch glycolate and taste-masking agent (D-mannitol). In this study, response surface methodology was used for designing of the experiment, generation of mathematical models and optimization study. Taste evaluation of pellets in human volunteers revealed considerable taste masking with a degree of bitterness below threshold value (2.0) within 10 s, whereas Tramadol HCl was rated intensely bitter with a score of +4 for 10 s. The size of the pellets varied from 0.895 to 1.423 mm for different batch and found to be a spherical. Disintegration time of different formulations varied from 30 to 60 s. It was observed that the responses, i.e. disintegration time and sphericity were affected by both the factors. The statistical models were validated and can be successfully used to prepare optimized taste-masked mouth-dissolving tablets of Tramadol HCl with adequate disintegration and shape.
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.72124
In the present investigation, newly developed mixed hydrotropic solid dispersion (HSD) technology precludes the use of organic solvent and also decreases the individual concentration of hydrotropic agents, simultaneously decreasing their toxic potential. 'Mixed-hydrotropic solubilization' technique is the phenomenon to increase the solubility of poorly water-soluble drugs in the aqueous solution containing blends of hydrotropic agents, which may give synergistic enhancement effect on solubility of poorly water-soluble drugs and to reduce concentrations of each individual hydrotropic agent to minimize their toxic effects due to high concentration of hydrotropic agents. Maheshwari has made HSD of paracetamol using urea. In the present study, the aqueous solution of hydrotropic blend (20% urea and 10% sodium citrate) has been found to increase aqueous solubility of poorly water-soluble drug, aceclofenac. This mixedhydrotropic blend was used to prepare solid dispersion of aceclofenac. The prepared solid dispersions have been characterized by IR and XRD studies. They have been studied for dissolution rate enhancement effect. The prepared solid dispersions were found very stable (chemically).
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.72123
Nanocapsules are submicroscopic colloidal drug delivery system and are composed of an oily or an aqueous core surrounded by a thin polymeric membrane. Nanocapsules have recently generated lot of interest in the area of controlled release with availability of biocompatible and biodegradable polymers. Nanocapsules of diltiazem were prepared with an objective of achieving controlled release of the drug in order to reduce the frequency of administration of drug, to obtain more uniform plasma concentration, and to improve patient compliance. Diltiazem was chosen as the model drug, as it is widely used in the treatment of chronic conditions such as hypertension and angina which require prolonged therapy. Nanocapsules were prepared by the interfacial deposition technique by taking different concentrations of polymers and phospholipid mixture. Five best formulations were selected based on the encapsulation efficiency. The morphology of nanocapsules was assessed by scanning electron microscope and they were found to be smooth, spherical, and discrete. The particles followed normal size distribution with particle size in the range of 20 to 380 nm. In vitro release studies indicated prolonged release for all polymers for 48 hours, with polycaprolactone as the best polymer releasing about 95 to 98%. The formulations were stable at 4°C but unstable at 25°C, and hence recommended for storage in refrigeration. Thus, it can be concluded that nanocapsules are a useful technology for controlled release of diltiazem.
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.72122
During the past two decades, there has been a steady increase in both the number of antiretroviral medications and the number of possible regimens available to manage human immunodeficiency virus (HIV) and acquired immune deficiency syndrome (AIDS). But still, regimen fails due to some reasons such as toxicity, adverse effects, and consequent difficulties with patient adherence. Stavudine is the Food and Drug Administration approved drug for clinical use for the treatment of HIV infection, AIDS, and AIDS related conditions, either alone or in combination with other antiviral agents. The side effects of Stavudine are dose dependent and a reduction of the total administered dose reduces the severity of the toxicity. To reduce the frequency of administration and to improve patient compliance, a once daily sustained release formulation of Stavudine is desirable. Hence, in the present work, an attempt has been made to develop once daily sustained release matrix tablets of Stavudine using putative hydrophilic matrix materials such as hydroxyl propyl methyl cellulose (HPMC) K4M and Carbopol 974P. The prepared extended release tablets were then evaluated for various physical tests like diameter, thickness, weight variation, hardness, friability, and drug content uniformity. The results of all these tests were found to be satisfactory. Formulation F9 extended the drug release till the end of 24 hours and showed higher r values for zero order plot, indicating that drug release followed zero order kinetics. This finding reveals that above a particular concentration, HPMC K4M and Carbopol 974P are capable of providing almost zero order drug release.
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.72121
Glimepiride (GMP) is poorly water soluble drug, so solubility is the main constraint for oral its bioavailability. An attempt has been made to increase the solubility of this model drug by formulating solid dispersion (SD) using Poloxamer 188 (PXM 188) as polymer and then formulating SDs tablets of the best formulation of SDs. Tablet formulations were prepared by direct compression technique using superdisintegrant croscarmellose sodium in different concentrations. SDs were evaluated for XRD, SEM, in vitro dissolution profiles, and dissolution efficiency, and developed tablet formulations were evaluated for various pharmaceutical characteristics viz. hardness, % friability, weight variation, drug content, disintegration time, in vitro dissolution profiles, and dissolution efficiency. Among different formulations of SDs, SD containing drug is to polymer ratio 1 : 4 gives best dissolution profile and dissolution efficiency and among tablet formulations, formulations containing 5% croscarmellose sodium gives best disintegration and dissolution profiles compared with other formulations. Results showed that poloxamer is a promising polymer for enhancing the solubility of GMP.
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.72119
The main objective of this study was to develop paclitaxel loaded poly (caprolactone) injectable microspheres prepared by solvent evaporation method. Mircoparticles were characterized in terms of particle size and size distribution, surface morphology, drug physical state, and crystalline nature by using master size analyzer, scanning electron microscope, differential scanning calorimetry, and X-ray diffraction. Paclitaxel loading over different concentrations was analyzed by high-performance liquid chromatography. In vitro drug release studies were performed in phosphate buffer saline. Best formulation was selected for in vitro cytotoxic studies by using MCF-7 breast cancer cell lines.
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.72118
Novel poly (vinyl caprolactam-co-vinyl acetate) microspheres were crosslinked with N', N' methylene bisacrylamide (NNMBA) prepared by free radical emulsion polymerization. This was done by using vinyl caprolactam, vinyl acetate, and NNMBA with varying amounts. 5-Fluorouracil (5-FU) is an anticancer drug which was mixed into these microspheres during in situ polymerization. These microspheres were characterized by using differential scanning calorimetry (DSC), X-ray diffraction (XRD), and scanning electron microscopy (SEM) techniques. XRD and DSC results indicated that there was uniform distribution of 5-FU drug particles in microspheres, and SEM pictures suggest that the microspheres are in spherical shape. Both encapsulation efficiency and release patterns are found to be dependent on the amount of crosslinking agent and amount of drug loaded. From the results of drug release kinetic studies, an anomalous and nonFickian behavior was observed in the present studies. Furthermore, in vitro release studies indicated the release of 5-FU up to 10 hours.
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.72117
The parenteral administration route is the most effective and common form of delivery for active drug substances with poor bioavailability and the drugs with a narrow therapeutic index. Drug delivery technology that can reduce the total number of injection throughout the drug therapy period will be truly advantageous not only in terms of compliance, but also to improve the quality of the therapy. Such reduction in frequency of drug dosing is achieved by the use of specific formulation technologies that guarantee the release of the active drug substance in a slow and predictable manner. The development of new injectable drug delivery system has received considerable attention over the past few years. A number of technological advances have been made in the area of parenteral drug delivery leading to the development of sophisticated systems that allow drug targeting and the sustained or controlled release of parenteral medicines.
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.72116
Control chart is the most successful statistical process control (SPC) tool, originally developed by Walter Shewhart in the early 1920s. A control chart can easily collect, organize and store information, calculate answers and present results in easy to understand graphs. It helps to record data and allows to see when an unusual event, e.g., a very high or low observation compared with "typical" process performance, occurs. Computers accept information typed in manually, read from scanners or manufacturing machines, or imported from other computer databases. The resulting control charts can be examined in greater detail, incorporated into reports, or sent across the internet. A stable process is a basic requirement for process improvement efforts. A computer collecting information in real time can even detect very slight changes in a process, and even warn you in time to prevent process errors before they occur. First, control charts demonstrate how consistently process is performing, and whether you should, or should not, attempt to adjust it. Next, the statistical process control chart compares the process performance to standard pharmaceutical requirements, providing a process capability index as an ongoing, accurate direction for quality improvement. Finally, control charts and its resulting process capability index quickly evaluate the results of quality initiatives designed to improve process consistency. This review focuses on elements of control chart and types of various control charts along with example. Advantages of various control charts are also included.
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.72115
There is considerable interest in the skin as a site of drug application for both local and systemic effect. However, the skin, in particular the stratum corneum, possesses a formidable barrier to drug penetration thereby limiting topical and transdermal bioavailability. Skin penetration enhancement techniques have been developed to improve bioavailability and to increase the range of drugs for which topical and transdermal delivery is a viable option. The permeation of drug through skin can be enhanced by both chemical penetration enhancement and physical methods. In this review, we have discussed the physical and chemical penetration enhancement technology for transdermal drug delivery as well as the probable mechanisms of action.
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.68469
Floating beads are often used for controlled drug release as they have a gastroretentive property without affecting the gastric emptying rate. In the present study mosapride-controlled release beads were prepared with the help of the ionotropic gelation method, using sodium alginate containing KHCO 3 as the gas-forming agent. The physical characterization of the mosapride beads was examined by SEM. The results showed that the shape and texture of the beads were uniform before and after dissolution. The percentage of mosapride drug entrapment efficiency ranged from 97.4 ± 0.08 to 99.1 ± 0.04. The percentage of mosapride content from the beads was determined by high-performance liquid chromatography (HPLC) and ranged from 97.9 ± 0.08 to 99.6 ± 0.01. The in-vitro percentage release of mosapride from the beads at the end of 14 hours ranged from 90.0 ± 0.2 to 99.5 ± 0.12. The formulated beads in formulations 1 and 3 were sealed in vials and kept for 90 days at 40°C / 75% RH. After 90 days of exposure the percentage drug content was found to be 99.2 ± 0.04. The Floating beads designed for the gastroretentive dosage form could be suitable for controlled drug delivery.
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.68468
In view of good skin tolerability, glycofurol was used as a vehicle-based gel and its effect on the topical penetration of Naproxen (NAP) was investigated. The aim of this study was to develop a suitable gel with bioadhesive property, spreadability, and viscosity for a topical anti-inflammatory effect. Three gelling agents were examined: Carbopol 974P, Gantrez AN 119, and Polyvinylpyrroloidone PVP K30. Skin permeation rates and lag times of NAP were evaluated using the Franz-type diffusion cell, in order to optimize gel formulation. The permeation rate of the NAP-based gel across excised rat skin was investigated. A significant increase in permeability parameters such as steady-state flux (Jss), permeability coefficient (Kp), and penetration index (PI) were observed in the optimized formulation containing 2% Transcutol as a permeation enhancer. From the skin irritation test, it was concluded that the optimized novel tetraglycol-based gel formulation was safe to be used for transdermal drug delivery. The developed naproxen / glycofurol-based gel appeared promising for dermal and transdermal delivery of naproxen and could be applicable with water-insoluble drugs, which would circumvent most of the problems associated with drug therapy.
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.68466
Salbutamol sulfate microcapsules with a coat consisting of sodium alginate and mucoadhesive polymer such as sodium carboxy methyl cellulose (NaCMC), methyl cellulose (MC), carbopol-934, and hydroxy propyl methyl cellulose (HPMC) were prepared by ionotropic gelation technique and were evaluated for morphological characters, drug content, loading efficiency, drug-polymer interactions, swelling ratio, mucoadhesive properties, and in vitro release. The resulting microcapsules were discrete, spherical, and free-flowing, and microencapsulation efficiency was 51.28-96.70%. The microcapsules prepared with alginate alone (A4) have exhibited good mucoadhesive property in the in vitro washoff test. The swelling ratio of microcapsules was enhanced with increased alginate concentration. Salbutamol sulfate release from these mucoadhesive microcapsules was slow and extended over a period of 8 h and depends upon the concentration of the alginate. The drug release from alginate-HPMC/carbopol microcapsules followed diffusion-controlled first-order kinetics. The release rate of alginate-HPMC microcapsules (A4H) was higher than other formulations and comparable with commercially available controlled-release capsules. Microcapsules with alginate alone (A4) followed diffusion mechanism. In conclusion, alginate-HPMC/carbopol mucoadhesive microcapsules could be promising vehicle for oral controlled release of salbutamol sulfate.
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.68465
Oral mucoadhesive sustained drug delivery systems of salbutamol sulfate were formulated using an isolated natural agent from the seeds of Caesalpinia pulcherrima. The isolated material was evaluated for various parameters, such as, melting point, viscosity, pH, elemental analysis, swelling index, phytochemical constituents, and solubility studies. The mucoadhesive characters of the isolated substance were identified by a comparative study with hydroxyl propyl cellulose and sodium alginate, by various in vitro methods, such as, Shear stress measurement, Wilhelmy's method, Falling sphere method, and Detachment force measurement. Formulation and evaluation of mucoadhesive oral tablets of salbutamol sulfate (100 mg), using isolated natural materials in different proportions, and in vitro release studies, were carried out for three different formulations according to the U.S.P apparatus two (paddle method). Each 100 mg tablet was taken in 900 ml of acid buffer 1.2 and maintained at 37˚C. After two hours the filtrate was collected and replaced in buffer 7.4. In vitro releases of three different formulations for nine hours were studied, which showed the sustained action of drug release with increasing the concentration of the isolated natural mucoadhesive agent in the formulations.
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.68463
Transdermal systems are ideally suited for diseases that demand chronic treatment. Hence, an anti-diabetic agent of both therapeutic and prophylactic usage has been subjected to transdermal investigation. Gliclazide, a second-generation hypoglycemic agent, faces problems like its poor solubility, poor oral bioavailability with large individual variation and extensive metabolism. In the present work, transdermal matrix-type patches were prepared by film casting techniques on mercury using polymers like HPMC, Eudragit RL-100, and chitosan. Also an attempt was made to increase the permeation rate of drug by preparing an inclusion complex with hydroxypropyl β-cyclodextrin (HP β-CD). The possibility of a synergistic effect of chemical penetration enhancers (CPE) (propylene glycol and oleic acid) on the transdermal transport of the drug was also studied. Folding endurance was found to be high in patches containing higher amount of the Eudragit. There was increase in tensile strength with an increase in Eudragit in the polymer blend. In vitro drug release profile indicates that the drug release is sustained with increasing the amount of Eudragit in patches. The patches containing inclusion complex of drug showed higher permeation flux compared with patches containing plain drug. The result of the synergistic effect indicates that the HP β- CD in conjunction with other CPE showed a higher permeation flux.
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.68461
The purpose of this research was to mask the intensely bitter taste of metoclopramide hydrochloride and to formulate a rapid-disintegrating tablet of the taste-masked drug. Taste masking was done by complexing the drug with ion exchange resin, Indion 204 and Indion 214, in different ratios. The complex loading process was optimized for the concentration of resin, swelling time, stirring time, pH, and temperature for maximum drug loading. Drug-resin complexes (DRC) were tested for flow properties, drug content, in-vitro release in simulated salivary fluid, and in simulated gastric fluid (SGF), taste evaluation by the panel method. Taste evaluation of DRC revealed considerable taste masking with the degree of bitterness below threshold value (40 μg/ml) in 0 to 5 min. Complex of both Indion 204 and Indion 214 masked the taste, but on the basis of the comparative study, resin 214 was selected for taste masking property. Disintegrant croscarmellose (5% wt/wt) gave the minimum disintegration time in comparison to crosspovidone and sodium starch glycolate. The batch of tablet containing Pearlitol SD and Avicel (PH102) in the ratio 60:40 and 5% (wt/wt) Croscarmellose showed faster disintegration i.e. 32 s, as compare to marketed tablet. It also revealed rapid drug release (t 80 , 6 min) in SGF compared with marketed formulation (t 80 , 9 min).
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.68460
The present research was aimed to formulate and evaluate pH and time-dependent multiparticulate systems for colon-targeted drug delivery of celecoxib (CXB) with maximum drug absorption, reduced peak plasma fluctuations, and minimum potential side effects. Multiple unit delayed release systems of the drug in MCC (Avicel® PH-102) grade were prepared using polymethacrylate polymers (Eudragit® L-100 and RSPO) as a granulating binder by the extrusion-spheronization technique and characterized for their shape, size, size distribution, friability, density, and moisture content. In vitro release studies were performed in 0.1N HCl, for first 2 h then further performed in phosphate buffer (pH 6.8) for 24 h. The resulting pellets were prepared by extrusion spheronization using different grades of polymethacrylate polymers as a granulating binder, showing a substantial decrease in drug release in initial 5 h (16.28-16.7%) and releasing most of the drug in 12-24 h. The geometric and arithmetic mean diameter ranged from (490 to 780 ΅m) and (636 to 734 μm), respectively. The minimum to maximum range for circularity, elongation and rectangle were found to be (0.847±0.009 to 0.965±0.078), (1.036±0.057 to 1.185±0.023), and (0.724±0.041 to 0.791±0.047) respectively showing the proper shape and size of the pellets. The content of CXB in the prepared pellets was observed between 98.70 and 99.47% justifying the uniform drug distribution. The in vitro dissolution studies showed that the retardant effect in initial 5 h and most of the drug release in 24 h depended on the ratio and concentration of different grades of methacrylate polymers used in the formulation. CXB-loaded MUPS prepared by the extrusion-spheronization technique using polymethacrylate polymers showed immense potential for colon-specific drug delivery of the drug.
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.68459
The transdermal route has numerous advantages over the more traditional drug delivery routes. These include high bioavailability, absence of first pass hepatic metabolism, steady drug plasma concentrations, and the fact that therapy is non-invasive. The main obstacle to permeating drug molecules is the outermost layer of the skin, the stratum corneum. Consequently, research into enhancing transdermal drug delivery (TDD) by overcoming this layer, is an area of prime interest. This review article is written to provide a coverage commentary of the recent advancements in TDD enhancement techniques.
Asian Journal of Pharmaceutics, Volume 4; https://doi.org/10.4103/0973-8398.68458
Asian Journal of Pharmaceutics, Volume 6; https://doi.org/10.4103/0973-8398.104837
Asian Journal of Pharmaceutics, Volume 9; https://doi.org/10.4103/0973-8398.160311
Terbutaline sulphate is a selective B2 bronchodilator which is used in the treatment of asthma. Conventional Terbutaline tablets available in the market are not suitable where quick onset of action is required. Terbutaline sulphate sublingual tablets were prepared by using mannitol, microcrystalline cellulose pH102 (F1) and lactose monohydrate, microcrystalline cellulose pH102 (F4) as filler and its combination in different ratio, Crospovidone as superdisintegrant and sodium lauryl Sulphate as permeability enhancers by drug dispersion direct compression method.The formulation F1 found the 93.51% of % drug permeability, 8 seconds disintegration time and 96.95% drug release within one minute. The formulation F4 also found the 98.25% of drug permeability, 13 seconds disintegration time and 90.31% drug release within one minute. It was concluded that the sublingual tablet of Terbutaline sulphate can be formulated for sublingual absorption of drug in emergency treatment of asthma by Mannitol and Microcrystalline cellulose pH 102 in combination (75% and 25% respectively) or lactose monohydrate and Microcrystalline cellulose pH 102 in combination (75% and 25% respectively) as filler, Crospovidone as superdisintegrant, and Sodium Lauryl sulphate as permeability enhancer by direct compression drug dispersion method
Asian Journal of Pharmaceutics, Volume 9; https://doi.org/10.4103/0973-8398.160316
Asian Journal of Pharmaceutics, Volume 9; https://doi.org/10.4103/0973-8398.160319
Asian Journal of Pharmaceutics, Volume 9; https://doi.org/10.4103/0973-8398.160309
Asian Journal of Pharmaceutics, Volume 9; https://doi.org/10.4103/0973-8398.160317
Asian Journal of Pharmaceutics, Volume 9; https://doi.org/10.4103/0973-8398.160318
Asian Journal of Pharmaceutics, Volume 9; https://doi.org/10.4103/0973-8398.160314
The purpose of present research work was to develop spray-dried mucoadhesive microspheres of prochlorperazine (PCPZ) for intranasal administration with an aim to avoid first-pass metabolism and to improve therapeutic effectiveness. A 2 3 factorial design was employed with amount of polymer, feed flow rate and volume of gluteraldehyde as independent variables while particle size of the microspheres and percentage drug entrapment efficiency as dependent variables. The microspheres were evaluated for drug loading, surface morphology, degree of swelling, in-vitro mucoadhesion, drug release, histopathology and stability studies. Particle size of all batches was found to be in the range of 7.32-15.67 μm. The percentage entrapment efficiency was found to be in the range between 84.90 and 96.21. In-vitro mucoadhesion was performed by adhesion number using goat nasal mucosa and was observed in a range from 76.25 to 87.72. The optimum formulation was selected based on the criteria of attaining the minimum value of particle size with substantial entrapment efficiency. Scanning electron microscopy analysis of the microspheres revealed that the microspheres were nearly smooth and spherical. In-vitro diffusion studies showed non-Fickian drug release. The Fourier transform infrared spectrophotometer spectra revealed no interaction between drug and excipients. Optimum formulation was found to be nonirritant in histopathology study carried out on goat nasal mucosa. The prepared microspheres were found to be stable over a period of 3 months even after stored at 40°C. In conclusion, PCPZ loaded mucoadhesive chitosan microspheres were reported for the first time, being suitable for intranasal delivery for the treatment of nausea and vomiting
Asian Journal of Pharmaceutics, Volume 9; https://doi.org/10.4103/0973-8398.160312
In the present investigation iontophoretic permeation of risedronate sodium (RS) through optimized gel based formulation was evaluated with respect to various electrical parameters like Current density and type of current. The study also involved enhancement the iontophoretic permeation of RS in combination with electroporation and chemical penetration enhancers with its in-vivo Pharmacokinetic evaluation. The permeation studies were carried through the human cadaver skin by using modified Franz diffusion cell and microcontroller based devices for iontophoresis and electroporation developed in the laboratory. In-vivo Pharmacokinetic studies were carried out in hairless rats. One way ANOVA followed by Tukey-Kramer test for multiple comparisons. The permeation of RS was significantly increased with iontophoresis at 0.5 mA/Cm 2 current density. The iontophoretic permeation was found depend on current density and ON:OFF ratio. The pulsatile current resulted in high permeation than continuous current. Maximum permeation was obtained at 0.5 mA/cm 2 with 1:1 pulsed current. When iontophoresis was coupled with chemical penetration enhancers and electroporation for 100 ms at 220V, synergistic enhancement in permeation was observed with shortened lag time and high flux. The required flux was achieved with area of application 1.55 cm 2 . In-vivo studies in hairless rats revealed high C max, low t max and increased area under the curve with electroporation, followed by iontophoresis indicated increased bioavailability. Relative bio-availability was 4.6 when calculated in comparison to passive studies
Asian Journal of Pharmaceutics, Volume 9; https://doi.org/10.4103/0973-8398.160315
Asian Journal of Pharmaceutics, Volume 9; https://doi.org/10.4103/0973-8398.160310
Asian Journal of Pharmaceutics, Volume 9; https://doi.org/10.4103/0973-8398.150030
The guanine derivative antiviral drug acyclovir (ACV) is one of the oldest molecules laying successful market until date, being commercially available in various dosage forms for oral, topical and parenteral administrations. Clinical application of this drug is superior to new antiviral agents due to its potential values such as suppression of recurrence, safety profile, minimal drug interactions, and being inexpensive. ACV is slightly water-soluble, less permeable and poorly bioavailable, yet more potential antiviral molecule, the physicochemical modifications and novel dosage form approaches resulted with more than 100 research works within a decade. The survey of literature showed enormous reports on ACV formulation development, which includes modified tablets, particulate drug delivery, vesicular drug delivery, polymeric nanoparticles, bioadhesive systems, floating dosage forms, in situ gelling systems, transdermal delivery, implantable systems, emulsified dosage forms, polymeric films/patches, etc. As the drug could be administered via multiple routes for effective site targeted action at various doses, and attracted the attention of many researches, the review of the current approaches for the delivery of ACV could be more beneficial for the new scientists. This paper is a review of recent researches highlighting the development of newer techniques and novel dosage forms of ACV for better therapeutic efficacy, which were aimed at enhancing its solubility, permeability and bioavailability
Asian Journal of Pharmaceutics, Volume 9; https://doi.org/10.4103/0973-8398.150035
The objective of this study was to formulate topical gel loaded nanoemulsions containing flurbiprofen using volatile oil. The gel released the drug at a controlled rate to the targeted site. Flurbiprofen (log P = 4.09) in generally used for transdermal treatment of rheumatoid arthritis and osteoarthritis. Selection of the oil phase, surfactant, and cosurfactant was done by individual screening method with the aid of pseudo-ternary phase study. International Conference on Harmonisation Q8 guidelines was applied using 3 2 factorial designs coupled with response surface methodology. The formulations were prepared by using spontaneous emulsification method. The selected formulation from various statistical and other studies was investigated. It was found that selected formulation showed an optimum in-vitro data. Later the optimized formulation obtained within the tentative design space was incorporated in the gel and compared with the marketed formulation. The result suggested the optimized formulation with good potential for transdermal delivery of the drug than the marketed formulations
Asian Journal of Pharmaceutics, Volume 9; https://doi.org/10.4103/0973-8398.150032
Asian Journal of Pharmaceutics, Volume 9; https://doi.org/10.4103/0973-8398.150036
Asian Journal of Pharmaceutics, Volume 9; https://doi.org/10.4103/0973-8398.150033
Asian Journal of Pharmaceutics, Volume 9; https://doi.org/10.4103/0973-8398.150041
The objective was to find the factors involve that contributes toward the noncompliance in the patients with cardio-vascular diseases. This was descriptive in nature. Nishter Hospital, Multan. Patients admitted in the cardio ward of the hospital were interviewed during the period of June 6, to August 6, 2013. The information regarding the demographics, level of education, and trust on doctors, medication taking behavior and compliance were taken with the help of questionnaire. Statistical analysis was performed with the help of SPSS 17 (SPSS Inc. Released 2008. SPSS Statistics for Windows, Version 17.0. Chicago: SPSS Inc).Of 200 respondents 65.0% were compliant and 35% were noncompliant