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(searched for: doi:10.4103/0973-8398.160318)
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Devendra Kumar Bhopte, , Mohan Lal Kori
Biomedical and Pharmacology Journal, Volume 15, pp 2011-2024; https://doi.org/10.13005/bpj/2539

Abstract:
The majority of formulations are available as oral dosage forms. In spite of some pharmaceutical challenges, this route is considered as most suitable way of drug delivery. For that reason it is necessary to optimize dose and dosing frequency to reduce the toxic effects of drug. Therefore, in this study, we have conceptualized the fabrication of floating microspheres of Quinapril Hydrochloride by the solvent evaporation technique with varying ratios of HPMC, Carrageenan, and Poly methyl methacrylate with polyvinyl alcohol that will augment its gastric retention time in conjunction with the sustained pharmacological activity. The formulation process of floating microspheres was optimized for stirring speed (X1) and concentration of polymer ratio (X2) on dependent variables such as percentage entrapment efficiency (Y1), percentage yield (Y2), in vitro buoyancy (Y3), and percentage of drug release (Y4) by using the factorial design. The drug was characterized by Fourier transform infrared spectroscopy, Differential scanning calorimetry was used for the identification of drug polymer blend interaction. The prepared microspheres were characterized by number of parameters including; scanning electron microscopy, percentage yield, particle size, in vitro buoyancy, drug entrapment efficiency, in vitro drug release, and in vivo floating behavior in albino rabbits. The release profile of microspheres prepared with hydrophilic, pore forming material and ion exchange resin combinations was dependent on the layer of pores developed by the fluid present at the absorption site of stomach and the drug release rate was retarded at site of action i.e. GIT.
Safirah Maheen,
Bioinspired, Biomimetic and Nanobiomaterials, Volume 9, pp 202-212; https://doi.org/10.1680/jbibn.19.00065

Abstract:
Lipid based polymers have been proved to be as efficient drug carriers to overcome insufficiencies of conventional formulations. Ceresin wax (CSW) was employed to improve permeability, oral bioavailability and patient compliance by preparing Enalapril (EP) loaded lipospheres with simple solvent evaporation method. Box-behnken design with proposed polynomial equations and quadratic model was applied to statistically investigate and validate collective influence of formulation variables on lipospheres. Spherical smooth surface lipospheres having an average size of 55 µm with excellent micromeritics properties were produced. DSC, X-RD and FTIR findings proved the lack of any possible interaction between formulation components. Zeta potential ranged from –5 mV to –20 mV suggested significant stability of lipospheres. The responses like percentage yield (29–68%,), entrapment efficiency (21–53%) and drug release (42–93%) were found to be greatly affected by concentration of lipids, surfactant and stirring speed. Reduce and sustained EP release from lipospheres may lower treatment cost and enhance hypertensive patients’ compliance.
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