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本文引用的文献

1
An Intravaginal Ring for the Simultaneous Delivery of an HIV-1 Maturation Inhibitor and Reverse-Transcriptase Inhibitor for Prophylaxis of HIV Transmission.一种用于同时递送HIV-1成熟抑制剂和逆转录酶抑制剂以预防HIV传播的阴道环。
J Pharm Sci. 2015 Oct;104(10):3426-39. doi: 10.1002/jps.24551. Epub 2015 Jul 6.
2
Engineering a degradable polyurethane intravaginal ring for sustained delivery of dapivirine.工程化一种可降解的聚氨酯阴道环用于持续递送达匹韦林。
Drug Deliv Transl Res. 2011 Jun;1(3):223-37. doi: 10.1007/s13346-011-0027-1.
3
Intravaginal rings: controlled release systems for contraception and prevention of transmission of sexually transmitted infections.阴道环:用于避孕和预防性传播感染的控释系统。
Drug Deliv Transl Res. 2011 Jun;1(3):185-93. doi: 10.1007/s13346-011-0024-4.
4
Cross-Sectional Analysis of Selected Genital Tract Immunological Markers and Molecular Vaginal Microbiota in Sub-Saharan African Women, with Relevance to HIV Risk and Prevention.撒哈拉以南非洲女性特定生殖道免疫标志物与阴道微生物群的横断面分析及其与艾滋病病毒风险和预防的相关性
Clin Vaccine Immunol. 2015 May;22(5):526-38. doi: 10.1128/CVI.00762-14. Epub 2015 Mar 11.
5
Preclinical assessments of vaginal microbicide candidate safety and efficacy.阴道杀微生物剂候选物的临床前安全性和功效评估。
Adv Drug Deliv Rev. 2015 Sep 15;92:27-38. doi: 10.1016/j.addr.2014.12.005. Epub 2014 Dec 24.
6
Development of polyether urethane intravaginal rings for the sustained delivery of hydroxychloroquine.用于持续递送羟氯喹的聚醚聚氨酯阴道环的研发。
Drug Des Devel Ther. 2014 Oct 9;8:1801-15. doi: 10.2147/DDDT.S71352. eCollection 2014.
7
Advanced topical drug delivery system for the management of vaginal candidiasis.用于治疗阴道念珠菌病的先进局部给药系统。
Drug Deliv. 2016;23(2):550-63. doi: 10.3109/10717544.2014.928760. Epub 2014 Jun 24.
8
A 90-day tenofovir reservoir intravaginal ring for mucosal HIV prophylaxis.用于黏膜 HIV 预防的 90 天替诺福韦储库阴道环。
Antimicrob Agents Chemother. 2012 Dec;56(12):6272-83. doi: 10.1128/AAC.01431-12. Epub 2012 Sep 24.
9
A hot-melt extruded intravaginal ring for the sustained delivery of the antiretroviral microbicide UC781.一种热熔挤出阴道内环,用于持续释放抗逆转录病毒微物 UC781。
J Pharm Sci. 2012 Feb;101(2):576-87. doi: 10.1002/jps.22781. Epub 2011 Oct 4.
10
Vaginal microbicide gel for delivery of IQP-0528, a pyrimidinedione analog with a dual mechanism of action against HIV-1.阴道用杀微生物剂凝胶递药系统 IQP-0528,一种嘧啶二酮类似物,具有针对 HIV-1 的双重作用机制。
Antimicrob Agents Chemother. 2011 Apr;55(4):1650-60. doi: 10.1128/AAC.01368-10. Epub 2011 Jan 18.

载有羟氯喹的聚氨酯阴道环对乳酸杆菌的影响。

Impact of Hydroxychloroquine-Loaded Polyurethane Intravaginal Rings on Lactobacilli.

作者信息

Traore Yannick Leandre, Chen Yufei, Bernier Anne-Marie, Ho Emmanuel A

机构信息

Laboratory for Drug Delivery and Biomaterials, College of Pharmacy, Faculty of Health Sciences, University of Manitoba, Winnipeg, Manitoba, Canada.

Department of Biological Sciences, Faculty of Science, Université de Saint-Boniface, Winnipeg, Manitoba, Canada.

出版信息

Antimicrob Agents Chemother. 2015 Dec;59(12):7680-6. doi: 10.1128/AAC.01819-15. Epub 2015 Sep 28.

DOI:10.1128/AAC.01819-15
PMID:26416871
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4649168/
Abstract

The use of polymeric devices for controlled sustained delivery of drugs is a promising approach for the prevention of HIV-1 infection. Unfortunately, certain microbicides, when topically applied vaginally, may be cytotoxic to vaginal epithelial cells and the protective microflora present within the female genital tract. In this study, we evaluated the impact of hydroxychloroquine (HCQ)-loaded, reservoir-type, polyurethane intravaginal rings (IVRs) on the growth of Lactobacillus crispatus and Lactobacillus jensenii and on the viability of vaginal and ectocervical epithelial cells. The IVRs were fabricated using hot-melt injection molding and were capable of providing controlled release of HCQ for 24 days, with mean daily release rates of 17.01 ± 3.6 μg/ml in sodium acetate buffer (pH 4) and 29.45 ± 4.84 μg/ml in MRS broth (pH 6.2). Drug-free IVRs and the released HCQ had no significant effects on bacterial growth or the viability of vaginal or ectocervical epithelial cells. Furthermore, there was no significant impact on the integrity of vaginal epithelial cell monolayers, in comparison with controls, as measured by transepithelial electrical resistance. Overall, this is the first study to evaluate the effects of HCQ-loaded IVRs on the growth of vaginal flora and the integrity of vaginal epithelial cell monolayers.

摘要

使用聚合物装置进行药物的控释持续给药是预防HIV-1感染的一种有前景的方法。不幸的是,某些局部阴道应用的杀微生物剂可能对阴道上皮细胞以及女性生殖道内存在的保护性微生物群具有细胞毒性。在本研究中,我们评估了载有羟氯喹(HCQ)的储库型聚氨酯阴道环(IVR)对卷曲乳杆菌和詹氏乳杆菌生长以及阴道和子宫颈外上皮细胞活力的影响。这些IVR采用热熔注射成型法制造,能够在24天内实现HCQ的控释,在醋酸钠缓冲液(pH 4)中的平均每日释放率为17.01±3.6μg/ml,在MRS肉汤(pH 6.2)中的平均每日释放率为29.45±4.84μg/ml。不含药物的IVR和释放出的HCQ对细菌生长或阴道或子宫颈外上皮细胞的活力没有显著影响。此外,与对照组相比,通过跨上皮电阻测量,对阴道上皮细胞单层的完整性没有显著影响。总体而言,这是第一项评估载有HCQ的IVR对阴道菌群生长和阴道上皮细胞单层完整性影响的研究。