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壳聚糖溶胀行为对替诺福韦从用于预防HIV性传播的粘膜粘附阴道给药系统中控制释放的影响。

Influence of Chitosan Swelling Behaviour on Controlled Release of Tenofovir from Mucoadhesive Vaginal Systems for Prevention of Sexual Transmission of HIV.

作者信息

Notario-Pérez Fernando, Martín-Illana Araceli, Cazorla-Luna Raúl, Ruiz-Caro Roberto, Bedoya Luis-Miguel, Tamayo Aitana, Rubio Juan, Veiga María-Dolores

机构信息

Departamento Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad Complutense de Madrid, 28040 Madrid, Spain.

Departamento Farmacología, Facultad de Farmacia, Universidad Complutense de Madrid, 28040 Madrid, Spain.

出版信息

Mar Drugs. 2017 Feb 21;15(2):50. doi: 10.3390/md15020050.

DOI:10.3390/md15020050
PMID:28230790
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5334630/
Abstract

The main challenges facing efforts to prevent the transmission of human immunodeficiency virus (HIV) are the lack of access to sexual education services and sexual violence against young women and girls. Vaginal formulations for the prevention of sexually transmitted infections are currently gaining importance in drug development. Vaginal mucoadhesive tablets can be developed by including natural polymers that have good binding capacity with mucosal tissues, such as chitosan or guar gum, semisynthetic polymers such as hydroxypropylmethyl cellulose, or synthetic polymers such as Eudragit RS. This paper assesses the potential of chitosan for the development of sustained-release vaginal tablets of Tenofovir and compares it with different polymers. The parameters assessed were the permanence time of the bioadhesion-determined ex vivo using bovine vaginal mucosa as substrate-the drug release profiles from the formulation to the medium (simulated vaginal fluid), and swelling profiles in the same medium. Chitosan can be said to allow the manufacture of tablets that remain adhered to the vaginal mucosa and release the drug in a sustained way, with low toxicity and moderate swelling that ensures the comfort of the patient and may be useful for the prevention of sexual transmission of HIV.

摘要

预防人类免疫缺陷病毒(HIV)传播所面临的主要挑战是缺乏性教育服务以及针对年轻女性和女孩的性暴力。用于预防性传播感染的阴道制剂目前在药物研发中日益重要。阴道黏膜黏附片可以通过加入与黏膜组织具有良好结合能力的天然聚合物(如壳聚糖或瓜尔胶)、半合成聚合物(如羟丙基甲基纤维素)或合成聚合物(如丙烯酸树脂RS)来制备。本文评估了壳聚糖用于开发替诺福韦缓释阴道片的潜力,并将其与不同聚合物进行比较。评估的参数包括以牛阴道黏膜为底物体外测定的生物黏附持久时间、制剂在介质(模拟阴道液)中的药物释放曲线以及在相同介质中的溶胀曲线。可以说,壳聚糖能够制造出可黏附于阴道黏膜并持续释放药物的片剂,其毒性低且溶胀适度,能确保患者的舒适度,可能有助于预防HIV的性传播。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/713b/5334630/f0b1da7387e7/marinedrugs-15-00050-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/713b/5334630/b9fe04a658ae/marinedrugs-15-00050-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/713b/5334630/4d39c04ad22d/marinedrugs-15-00050-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/713b/5334630/7438edd19abd/marinedrugs-15-00050-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/713b/5334630/008b3f154d25/marinedrugs-15-00050-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/713b/5334630/f0b1da7387e7/marinedrugs-15-00050-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/713b/5334630/b9fe04a658ae/marinedrugs-15-00050-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/713b/5334630/2a1b8c44873e/marinedrugs-15-00050-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/713b/5334630/81ac6c426f8f/marinedrugs-15-00050-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/713b/5334630/3eb535611676/marinedrugs-15-00050-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/713b/5334630/4d39c04ad22d/marinedrugs-15-00050-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/713b/5334630/7438edd19abd/marinedrugs-15-00050-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/713b/5334630/008b3f154d25/marinedrugs-15-00050-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/713b/5334630/f0b1da7387e7/marinedrugs-15-00050-g008.jpg

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