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Tenofovir containing thiolated chitosan core/shell nanofibers: in vitro and in vivo evaluations.

Tenofovir containing thiolated chitosan core/shell nanofibers: in vitro and in vivo evaluations.
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Meng J, Agrahari V, Ezoulin MJ, Zhang C, Purohit SS, Molteni A, Dim D, Oyler NA, Youan BB,


Meng J, Agrahari V, Ezoulin MJ, Zhang C, Purohit SS, Molteni A, Dim D, Oyler NA, Youan BB, (click to view)

Meng J, Agrahari V, Ezoulin MJ, Zhang C, Purohit SS, Molteni A, Dim D, Oyler NA, Youan BB,

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Molecular pharmaceutics 2016 Oct 4()

Abstract

It is hypothesized that a thiolated chitosan (TCS) core/shell nanofiber (NF) can enhance the drug loading of tenofovir, a model low molecular weight and highly water soluble drug molecule, improve its mucoadhesivity, and in vivo safety. To test this hypothesis, PEO core with TCS shell NFs are fabricated by a coaxial electrospinning technique. The morphology, drug loading, drug release profiles, cytotoxicity and mucoadhesion of the NFs are analysised using scanning and transmission electron microscopies, liquid chromatography, cytotoxicity assays on VK2/E6E7 and End1/E6E7 cell lines and Lactobacilli crispatus, and periodic acid colorimetric method, respectively. In vivo safety studies are performed in C57BL/6 mice followed by H&E and immunohistochemical (CD45) staining analysis of genital tract. The mean diameters of PEO, PEO/TCS, PEO/TCS-PLA NFs are 118.56, 9.95, and 99.53 nm. The NFs exhibit smooth surface with average diameters. The drug loading (13%-25%, w/w) increased by 10 folds compared to a nanoparticle formulation due to the investigation of the electrospinning technique. The NFs are non-cytotoxic at the concentration of 1 mg/ml. The PEO/TCS-PLA core/shell NFs mostly exhibit a release kinetic following Weibull model (r=0.9914), indicating the drug release from a matrix system.The core/shell NFs are 40-60 fold more bioadhesive than the NFs of PEO only. The NFs are non-toxic and non-inflammatory in vivo after daily treatment for up to 7 days. Owing to their enhanced drug loading and preliminary safety profile, the TCS core/shell NFs are promising candidates for the topical delivery of HIV/AIDS microbicides such as tenofovir.

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