Influence of Plasticizers on the pH-Dependent Drug Release and Cellular Interactions of Hydroxypropyl Methylcellulose/Zein Vaginal Anti-HIV Films Containing Tenofovir
| Autor: | Roberto Ruiz-Caro, José Neves, Joana Galante, Fernando Notario-Pérez, Bruno Sarmento, Raúl Cazorla-Luna, Araceli Martín-Illana, María-Dolores Veiga |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
Sexual transmission
Polymers and Plastics Zein Bioengineering 02 engineering and technology Polyethylene glycol 010402 general chemistry 01 natural sciences Biomaterials chemistry.chemical_compound Hypromellose Derivatives Plasticizers PEG ratio Materials Chemistry Glycerol Humans Tenofovir Chromatography Plasticizer Hydrogen-Ion Concentration 021001 nanoscience & nanotechnology 0104 chemical sciences Lactic acid Drug Liberation Oleic acid chemistry Female 0210 nano-technology |
| Zdroj: | Biomacromolecules. 22:938-948 |
| ISSN: | 1526-4602 1525-7797 |
| DOI: | 10.1021/acs.biomac.0c01609 |
| Popis: | Vaginal films featuring the pH-dependent release of tenofovir (TFV) were developed for the prevention of sexual transmission of human immunodeficiency syndrome (HIV). Films based on hydroxypropyl methylcellulose and zein were prepared incorporating different plasticizers [oleic acid, lactic acid, glycerol, and polyethylene glycol 400 (PEG)] and evaluated for in vitro drug release in an acidic simulated vaginal fluid (pH 4.2) and a slightly alkaline mixture of simulated seminal and vaginal fluids (pH 7.5). Results revealed that optimal biphasic TFV release was possible with proper combination of plasticizers (PEG and oleic acid, 1:7 w/w) and by adjusting the plasticizer/matrix-forming material ratio. The films had similar or higher levels of TFV associated with genital epithelial cells (Ca Ski or HEC-1-A cells) but lower drug permeability compared to the free drug. These data confirm that films have the potential to achieve suitable mucosal levels of TFV with low systemic exposure. The films developed could protect women from HIV sexual transmission. |
| Databáze: | OpenAIRE |
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