Suppr超能文献

用于盐酸特比萘芬局部给药的pH响应性泊洛沙姆F127共聚丙烯酸可生物降解纳米凝胶的研制与评价

Development and Evaluation of pH-Responsive Pluronic F 127 Co-Poly- (Acrylic Acid) Biodegradable Nanogels for Topical Delivery of Terbinafine HCL.

作者信息

Hassan Shams Ul, Khalid Ikrima, Hussain Liaqat, Barkat Kashif, Khan Ikram Ullah

机构信息

Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Pakistan.

Department of Pharmacology, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Pakistan.

出版信息

Dose Response. 2022 Apr 26;20(2):15593258221095977. doi: 10.1177/15593258221095977. eCollection 2022 Apr-Jun.

Abstract

Research aimed to develop and evaluate biodegradable, pH-responsive chemically cross-linked Pluronic F127 co-poly- (acrylic acid) nanogels for dermal delivery of Terbinafine HCL (TBH) to increase its permeability and as a new approach to treat skin fungal infections. TBH-loaded nanogels were successfully synthesized from acrylic acid (AA) and Pluronic F127 by free-radical copolymerization technique using N,N'-methylene bisacrylamide (MBA) as crosslinker and ammonium persulphate (APS) as initiator. Prepared nanogels exhibited 93.51% drug entrapment efficiency (DEE), 45 nm particle size, pH-dependent swelling and release behavior. Nanogels were characterized using different physicochemical techniques. The skin retention studies through rat skin showed about 42.34% drug retention from nanogels while 1% Lamisil cream (marketed product) showed about 26.56% drug retention. Moreover, skin irritation studies showed that nanogels were not irritating. Nanogels showed improved antifungal activity against compared to commercial product. studies on rats infected with confirmed superiority of nanogels over 1% Lamisil for eradication of fungal infection. This confirms that TBH loaded in Pluronic F127 co-poly-(acrylic acid) nanogels provided greater targetibility and cure rates of poorly soluble TBH in animal model and hence nanogels could be a potential carrier for effective topical delivery of TBH for skin fungal infection treatment.

摘要

本研究旨在开发和评估可生物降解、pH响应性化学交联的普朗尼克F127共聚丙烯酸纳米凝胶,用于盐酸特比萘芬(TBH)的皮肤给药,以提高其渗透性,并作为治疗皮肤真菌感染的新方法。采用N,N'-亚甲基双丙烯酰胺(MBA)作为交联剂,过硫酸铵(APS)作为引发剂,通过自由基共聚技术,由丙烯酸(AA)和普朗尼克F127成功合成了负载TBH的纳米凝胶。制备的纳米凝胶表现出93.51%的药物包封率(DEE)、45nm的粒径、pH依赖性溶胀和释放行为。使用不同的物理化学技术对纳米凝胶进行了表征。通过大鼠皮肤进行的皮肤滞留研究表明,纳米凝胶的药物滞留率约为42.34%,而1%的兰美抒乳膏(市售产品)的药物滞留率约为26.56%。此外,皮肤刺激性研究表明纳米凝胶无刺激性。与市售产品相比,纳米凝胶对[具体真菌名称未给出]显示出更高的抗真菌活性。对感染[具体真菌名称未给出]的大鼠的研究证实,纳米凝胶在根除真菌感染方面优于1%的兰美抒。这证实了负载在普朗尼克F127共聚丙烯酸纳米凝胶中的TBH在动物模型中提供了更高的靶向性和对难溶性TBH的治愈率,因此纳米凝胶可能是有效局部递送TBH治疗皮肤真菌感染的潜在载体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d31/9087256/43baa04d6098/10.1177_15593258221095977-fig1.jpg

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验