Formulation and characterization of polymeric films containing combinations of antiretrovirals (ARVs) for HIV prevention.
Formulation and characterization of polymeric films containing combinations of antiretrovirals (ARVs) for HIV prevention.
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DOI：
10.1007/s11095-014-1474-4
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发表时间：
2015-02
影响因子：
3.7
通讯作者：
Rohan, Lisa Cencia
中科院分区：
文献类型：
--
作者：
Akil, Ayman;Agashe, Hrushikesh;Dezzutti, Charlene S.;Moncla, Bernard J.;Hillier, Sharon L.;Devlin, Brid;Shi, Yuan;Uranker, Kevin;Rohan, Lisa Cencia
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 was < 10% (w/w). All films delivered the active agents with release of > 50% of film drug content within 30 minutes. 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.
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