RT Journal Article
T1 Influence of plasticizers on the pH-dependent drug release and cellular interactions of hydroxypropyl methylcellulose/zein vaginal anti-HIV films containing tenofovir
A1 Notario Pérez, Fernando
A1 Cazorla Luna, Raúl
A1 Martín Illana, Araceli
A1 Galante, Joana
A1 Ruiz Caro, Roberto
A1 Sarmento, Bruno
A1 Das Neves, José
A1 Veiga Ochoa, María Dolores
AB 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.
PB American Chemical Society
YR 2021
FD 2021-02-08
LK https://hdl.handle.net/20.500.14352/109840
UL https://hdl.handle.net/20.500.14352/109840
LA eng
NO Notario-Pérez F, Cazorla-Luna R, Martín-Illana A, Galante J, Ruiz-Caro R, Sarmento B, Das Neves J, Veiga MD.Influence of plasticizers on the pH-dependent drug release and cellular interactions of hydroxypropyl methylcellulose/zein vaginal anti-HIV films containing tenofovir. Biomacromolecules. 2021 Feb 8;22(2):938-48.
NO AEI
NO FEDER
NO Fundaca̧o para  a Ciencia e a Tecnologia/Ministério da Ciência, Tecnologia e Ensino Superior
NO Ministerio de Ciencia, Innovación y Universidades (España)
DS Docta Complutense
RD 7 abr 2025