Development of Spray-Dried Cyclodextrin-Based Pediatric Anti-HIV Formulations
- 28 June 2021
- journal article
- research article
- Published by Springer Science and Business Media LLC in AAPS PharmSciTech
- Vol. 22 (5), 1-10
- https://doi.org/10.1208/s12249-021-02068-w
Abstract
The human immunodeficiency virus (HIV) impacts up to 37 million people globally, of which 1.8 million are children. To date, there is no cure for HIV, although treatment options such as antiretroviral therapy (ART) are available. ART, which involves a patient taking a combination of antiretrovirals, is being used to treat HIV clinically. Despite the effectiveness of ART, there is currently no palatable pediatric formulation to treat HIV in children, which has hindered patient compliance and overall treatment efficacy. In addition, anti-HIV therapeutics are often poorly water-soluble, and hence have poor bioavailability. In the present study, we developed a pediatric-friendly formulation for anti-HIV therapeutics with improved dissolution characteristics of the therapeutic agents. Lopinavir (LPV) and ritonavir (RTV), available as FDA-approved fixed-dose combination products, were chosen as model ART drugs, and the formulation and processing parameters of spray-dried cyclodextrin (CD)-based LPV and RTV complexes were studied. Results showed that the spray-dried complexes exhibited enhanced dissolution profiles in comparison to pure drugs, particularly spray-dried β-CD complexes, which showed the most favorable dissolution profiles. This current formulation with enhanced dissolution and taste-masking ability through the use of cyclodextrin has the potential to address the unmet need for the development of suitable pediatric formulations.Keywords
This publication has 25 references indexed in Scilit:
- Drug delivery strategies and systems for HIV/AIDS pre-exposure prophylaxis and treatmentJournal of Controlled Release, 2015
- Enhanced Boosting of Oral Absorption of Lopinavir Through Electrospray Coencapsulation with RitonavirJournal of Pharmaceutical Sciences, 2015
- Stability-enhanced Hot-melt Extruded Amorphous Solid Dispersions via Combinations of Soluplus® and HPMCAS-HFAAPS PharmSciTech, 2015
- Pediatric Drug Formulations: A Review of Challenges and ProgressPublished by American Academy of Pediatrics (AAP) ,2014
- Complexation approach for fixed dose tablet formulation of lopinavir and ritonavir: an anomalous relationship between stability constant, dissolution rate and saturation solubilityJournal of inclusion phenomena and molecular recognition in chemistry, 2011
- Determining association constants from titration experiments in supramolecular chemistryChemical Society Reviews, 2010
- Nanoneuroprotection and Nanoneurotoxicity: Recent Progress and Future PerspectivesNanomedicine, 2010
- The complexation efficiencyJournal of inclusion phenomena and molecular recognition in chemistry, 2007
- Cyclodextrins and their uses: a reviewProcess Biochemistry, 2003
- Antiretroviral-Drug Concentrations in SemenAntimicrobial Agents and Chemotherapy, 2000