Formulation and Characterization of Polymeric Films Containing Combinations of Antiretrovirals (ARVs) for HIV Prevention
| Autor: | Ayman Akil, Lisa C. Rohan, Kevin Uranker, Charlene S. Dezzutti, Bernard J. Moncla, Hrushikesh Agashe, Sharon L. Hillier, Brid Devlin, Yuan Shi |
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| Rok vydání: | 2014 |
| Předmět: |
Tenofovir
Anti-HIV Agents Polymers Administration Topical Chemistry Pharmaceutical Dapivirine Organophosphonates Human immunodeficiency virus (HIV) Pharmaceutical Science HIV Infections Pharmacology medicine.disease_cause Article chemistry.chemical_compound Drug Delivery Systems immune system diseases Humans Medicine Pharmacology (medical) Maraviroc Drug Carriers business.industry Vaginal microbicide Adenine Organic Chemistry virus diseases Virology Microbicides for sexually transmitted diseases Topical microbicides Administration Intravaginal Drug Combinations Pyrimidines chemistry Vagina HIV-1 Molecular Medicine Female business Drug carrier Biotechnology medicine.drug |
| Zdroj: | Pharmaceutical Research. 32:458-468 |
| ISSN: | 1573-904X 0724-8741 |
| DOI: | 10.1007/s11095-014-1474-4 |
| Popis: | To develop polymeric films containing dual combinations of anti-HIV drug candidate tenofovir, maraviroc and dapivirine for vaginal application as topical microbicides.A solvent casting method was used to manufacture the films. Solid phase solubility was used to identify potential polymers for use in the film formulation. Physical and chemical properties (such as water content, puncture strength and in vitro release) and product stability were determined. The bioactivity of the film products against HIV was assessed using the TZM-bl assay and a cervical explant model.Polymers identified from the solid phase solubility study maintained tenofovir and maraviroc in an amorphous state and prevented drug crystallization. Three combination film products were developed using cellulose polymers and polyvinyl alcohol. The residual water content in all films was10% (w/w). All films delivered the active agents with release of50% of film drug content within 30 min. Stability testing confirmed that the combination film products were stable for 12 months at ambient temperature and 6 months under stressed conditions. Antiviral activity was confirmed in TZM-bl and cervical explant models.Polymeric films can be used as a stable dosage form for the delivery of antiretroviral combinations as microbicides. |
| Databáze: | OpenAIRE |
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