Abstract
The sustained release of an antiretroviral agent to women mucosa has been proved as an excellent strategy to reduce the sexual transmission of HIV. Hybrid micro-mesoporous particles have been synthesized and functionalized with a silane coupling agent followed by loading the antiretroviral tenofovir. It has been observed that the disposition of the silane molecule on the surface of the particles determines the interaction mechanism with the antiretroviral molecule loaded independently on the surface area of the particles. In this sense, available and free amino groups are required to achieve a smart pH-responsive material, a condition that is only achieved in those materials containing a silane chemisorbed monolayer. Moreover, the modulation of the release kinetics attributed to the presence of the silane monolayer covering the mesopores has been confirmed by fitting the releasing curves to the first order and Weibull models. The developed micro-mesoporous particles have been demonstrated to be excellent smart-release vehicles for antiviral agents and can be safely used in polymer mucoadhesive vaginal gels.
Highlights
The vast majority of new HIV infections are acquired via the genital and rectal mucosa, with an increased risk of infection in women compared to men
Fourier transform infrared (FTIR) spectroscopy was used for the structural characterization of the porous hybrid particles as well as for the determination of the interaction between the silane coupling agent and the surface of the particle
New micro-mesoporous hybrid particles have been proved as successful hosts for the incorporation of TFV used for HIV prevention
Summary
The vast majority of new HIV infections are acquired via the genital and rectal mucosa, with an increased risk of infection in women compared to men. The research in developing microbicides for prevention of mucosal HIV transmission has been focused on using antiretroviral agents in various formulations and dosing strategies. Among the strategies for a sustained release of the antiviral or antiretroviral drugs it stands out the controlled drug delivery systems based on inert materials with high porosity to load the maximum amount of drug. These systems are formed by a support material, organic, inorganic or hybrid where the drug is loaded. Within the inorganic drug delivery systems, it stands out the mesoporous silica, which can exhibit different kind of interaction with organic molecules to develop biopharmaceutical functions [3,4] Among the multiple possibilities of the porous organic materials, drug delivery systems based on polypropylene, polystyrene, poly(α, β-L Malic acid), poly(ethylene glycol)-block-poly (-caprolactone), ethyl cellulose, etc., can be found in the literature [1,2].
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