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LDH 杂化温敏水凝胶用于阴道内递抗 HIV 药物。

LDH hybrid thermosensitive hydrogel for intravaginal delivery of anti-HIV drugs.

机构信息

a Department of Pharmaceutics, School of Pharmacy , Qingdao University , Qingdao , China.

出版信息

Artif Cells Nanomed Biotechnol. 2019 Dec;47(1):1234-1240. doi: 10.1080/21691401.2019.1596935.

Abstract

Microbicides based on hydrogel have become an effective way to prevent the HIV replication and transmission because of their convenience and prolonging drug release. In this study, a hybrid thermo-sensitive hydrogel constituted by nanosized layered double hydroxides and poloxamer 407 (P407) was constructed and co-loaded with both hydrophobic and hydrophilic drug. The LDH-P407 hydrogel could achieve sol-gel transition at body temperature. The in vivo experiment showed that LDH-P407 hydrogel can achieve controlled release of theaflavin and Nile red (hydrophobic drug model) into blood by vaginal drug delivery, meanwhile the hydrogel showed barely mucosal irritation. In addition, ex vivo experiment showed that the nifeviroc-loaded LDH-P407 hydrogel was able to specifically bind co-receptor CCR5 of DCs cells. Therefore, the LDH-P407 hydrogel would be a promising carrier for intravaginal delivery of anti-HIV drugs.

摘要

基于水凝胶的杀微生物剂因其方便性和延长药物释放而成为预防 HIV 复制和传播的有效方法。在这项研究中,构建了由纳米层状双氢氧化物和泊洛沙姆 407(P407)组成的混合温敏水凝胶,并共同负载疏水性和亲水性药物。LDH-P407 水凝胶可以在体温下实现溶胶-凝胶转变。体内实验表明,LDH-P407 水凝胶可以通过阴道给药将茶黄素和尼罗红(疏水性药物模型)控制释放到血液中,同时水凝胶几乎没有粘膜刺激性。此外,离体实验表明,载有 nifeviroc 的 LDH-P407 水凝胶能够特异性结合 DCs 细胞的共受体 CCR5。因此,LDH-P407 水凝胶有望成为阴道内递抗 HIV 药物的载体。

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