Department of Polymer Science and Technology, School of Chemical Engineering and Technology, Tianjin University, Nankai District, Tianjin, People's Republic of China.
J Mater Sci Mater Med. 2012 Aug;23(8):1913-9. doi: 10.1007/s10856-012-4664-9. Epub 2012 May 9.
Hydrogels with the advantages of prolonging drug release and administration convenience are necessary for intravaginal drug delivery to prevent sexual transmission of human immunodeficiency virus and other vaginal infections. In this study, the thermosensitive hydrogel of methylcellulose modified by stearic acid (MCS) were evaluated in the presence of NaCl and phosphates, which exhibited sol-to-gel transition performance at body temperature or even lower. The in vitro cytotoxicity and in vivo mucosal irritation were investigated and the results showed that MCS hydrogel possessed good biocompatibility similar with hydroxyethyl cellulose (HEC) gel. Significantly, the release studies revealed that MCS hydrogel could control tenofovir sustained release for 10 h without burst release, longer than that from HEC gel or poloxamer 407 hydrogel. Therefore, MCS thermosensitive hydrogel would be a promising carrier for intravaginal delivery of antiviral drugs for long time controlled release.
具有延长药物释放和给药方便优点的水凝胶对于阴道内药物递送是必要的，以防止人类免疫缺陷病毒和其他阴道感染的性传播。在这项研究中，评估了在存在 NaCl 和磷酸盐的情况下由硬脂酸改性的甲基纤维素的温敏水凝胶（MCS），其在体温或更低温度下表现出溶胶-凝胶转变性能。研究了体外细胞毒性和体内黏膜刺激性，结果表明 MCS 水凝胶具有与羟乙基纤维素（HEC）凝胶相似的良好生物相容性。重要的是，释放研究表明 MCS 水凝胶可以控制替诺福韦持续释放 10 小时而无突释，比 HEC 凝胶或泊洛沙姆 407 水凝胶释放时间更长。因此，MCS 温敏水凝胶将成为用于阴道内递抗病毒药物的有前途的载体，可实现长时间的控释。
