用于阴道黏膜给药的纳米胶束复合温敏水凝胶的制备及性能评价

doi:10.11896/cldb.22040117

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Abstract The occurrence of cervical cancer is closely related to infection with human papillomavirus (HPV). Treatment of HPV infection is effective for preventing the development of cervical cancer. Lopinavir (LPV) is an anti-HIV drug approved by FDA, and it was found that LPV has anti-HPV activity. The aim of this study was to develop a nano-micelles composite hydrogel drug delivery system loaded LPV and explore its perfor-mance for local administration through vaginal mucosa. LPV-loaded mixed micelles (TPGS-STDC/LPV) were prepared by the self-assembly of amphiphilic polymer TPGS, penetrant STDC, and LPV, then were dispersed into the thermosensitive hydrogel to form LPV-loaded nano-micelles composite hydrogel (NMCH). The particle size, zeta potential, morphology, entrapment efficiency, drug loading and drug release of TPGS-STDC/LPV were detected. The mucosal adhesion, drug release, transdermal penetration and antiviral activity of NMCH were also tested. The results showed that TPGS-STDC/LPV exhibited high entrapment efficiency and high drug loading, and the cumulative release of LPV achieved (96.82±2.93)% with pH of 4.5 at 72 h, Showing a good acid-response drug release. NMCH had a human temperature sensitive nature and good adhesion to the vaginal epithelial mucosa, and the skin permeation rate of LPV (54.05±2.74)% was observed about 7.4 times that of free LPV, and NMCH displayed good anti-HPV activities. This drug delivery system could be suitable for topical vaginal administration.

Key words： HPV virus lopinavir nano-mixed micelles nano micelles composite thermosensitive hydrogel vaginal topical administration

Published: 10 October 2023 Online: 2023-09-28

CLC number:

O636

Fund:National Natural Science Foundation of China (21562014) and China Tobacco ｜ China Tobacco Guizhou Industry Co., Ltd.(GZZY/KJ/JS/2014_Y005-1).

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	Articles by authors
	HE Xianhui
	YANG Peixin
	LU Xiaoluan
	TANG Luyang
	FU Yangyang
	PENG Qianrong
	YANG Min

Cite this article:

HE Xianhui,YANG Peixin,LU Xiaoluan, et al. Preparation and Evaluation of Nano Micelles Composite Thermosensitive Hydrogels for Vaginal Mucosa Administration[J]. Materials Reports, 2023, 37(19): 22040117-7.

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http://www.mater-rep.com/EN/10.11896/cldb.22040117 OR http://www.mater-rep.com/EN/Y2023/V37/I19/22040117

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