期刊
BIOMACROMOLECULES
卷 22, 期 2, 页码 938-948出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.biomac.0c01609
关键词
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资金
- Spanish Research Agency [MAT2016-76416-R]
- European Regional Development Fund (AEI/FEDER, UE) [MAT2016-76416-R]
- Portuguese funds through FCT-Fundacao para a Ciencia e a Tecnologia/Ministerio da Ciencia, Tecnologia e Ensino Superior [UID/BIM/04293/2019]
- Spanish Ministry of Science, Innovation and Universities
- Spanish Ministry of Education, Culture and Sport
- Fundacao para a Ciencia e a Tecnologia, Portugal [SFRH/BD/140271/2018]
Vaginal films with pH-dependent release of tenofovir were developed for HIV prevention, achieving optimal drug release by adjusting plasticizer combinations and ratios. The films had potential to reach suitable mucosal TFV levels with low systemic exposure, protecting women from HIV transmission.
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.
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