开发包裹在刺激敏感嵌段共聚物纳米凝胶分散体中的巴龙霉素的皮肤应用。
Developing cutaneous applications of paromomycin entrapped in stimuli-sensitive block copolymer nanogel dispersions.
作者信息
Brugués Alba Pujol, Naveros Beatriz Clares, Calpena Campmany Ana C, Pastor Pilar Hernández, Saladrigas Roser Fisa, Lizandra Cristina Riera
机构信息
Health Microbiology & Parasitology Department, Faculty of Pharmacy, University of Barcelona, Joan XXIII Avenue, 08028 Barcelona, Spain.
出版信息
Nanomedicine (Lond). 2015 Jan;10(2):227-40. doi: 10.2217/nnm.14.102.
AIM
A new paromomycin micellar nanogel based on poloxamer 407 was developed.
MATERIALS & METHODS: In vitro release and ex vivo permeation/retention studies were conducted. In vivo tolerance was assayed by transepidermal water loss. Ex vivo cytotoxicity on RAW and VERO cells and antileishmanial activity on Leishmania promastigotes was tested.
RESULTS
The particle size was 9.19 nm (99% loading efficiency) exhibiting Newtonian behavior at 4°C and was pseudoplastic at 25 and 40°C. Drug release followed a Weibull model and the drug remaining in the skin was 31.652 µg/g/cm(2). In vivo tolerance achieved excellent results with negligible cellular toxicity and the best antileishmanial efficiency.
CONCLUSION
The nanogel provided controlled, effective and safe delivery of paromomycin for the treatment of cutaneous leishmaniasis.
目的
研发一种基于泊洛沙姆407的新型巴龙霉素胶束纳米凝胶。
材料与方法
进行体外释放和离体渗透/滞留研究。通过经表皮水分流失测定体内耐受性。测试纳米凝胶对RAW和VERO细胞的离体细胞毒性以及对利什曼原虫前鞭毛体的抗利什曼活性。
结果
粒径为9.19纳米（负载效率99%），在4°C时表现出牛顿流体行为，在25°C和40°C时为假塑性流体。药物释放遵循威布尔模型，皮肤中残留的药物为31.652微克/克/平方厘米。体内耐受性取得了优异结果，细胞毒性可忽略不计，抗利什曼效果最佳。
结论
该纳米凝胶为巴龙霉素治疗皮肤利什曼病提供了可控、有效且安全的给药方式。
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