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

IF 2.3 4区 医学 Q3 PHARMACOLOGY & PHARMACY Dose-Response Pub Date : 2022-04-01 DOI:10.1177/15593258221095977
S. Hassan, Ikrima Khalid, Liaqat Hussain, K. Barkat, I. Khan
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引用次数: 5

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 ex-vivo 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 in-vitro antifungal activity against Candida albicans compared to commercial product. In-vivo studies on rats infected with Candida albicans 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.
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ph响应型Pluronic f127共聚丙烯酸可生物降解纳米凝胶的研制与评价,用于局部递送盐酸特比萘芬
研究旨在开发和评估可生物降解、pH响应性化学交联的Pluronic F127共聚-(丙烯酸)纳米凝胶,用于皮肤递送盐酸特比萘芬(TBH),以增加其渗透性,并作为治疗皮肤真菌感染的新方法。以丙烯酸(AA)和PluronicF127为原料,以N,N′-亚甲基双丙烯酰胺(MBA)为交联剂,过硫酸铵(APS)为引发剂,采用自由基共聚技术成功合成了TBH负载纳米凝胶。制备的纳米凝胶表现出93.51%的药物包封率(DEE)、45nm的粒径、pH依赖性的溶胀和释放行为。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离体皮肤滞留研究显示,纳米凝胶对药物的滞留率约为42.34%,而1%拉米西乳膏(上市产品)显示出约26.56%的药物滞留率。此外,皮肤刺激性研究表明,纳米凝胶没有刺激性。与商业产品相比,纳米凝胶对白色念珠菌的体外抗真菌活性有所提高。对感染白色念珠菌的大鼠进行的体内研究证实,纳米凝胶在根除真菌感染方面优于1%拉米西。这证实了负载在Pluronic 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难溶性TBH的靶向性和治愈率,因此纳米凝胶可能是有效局部递送TBH用于皮肤真菌感染治疗的潜在载体。
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来源期刊
Dose-Response
Dose-Response PHARMACOLOGY & PHARMACY-RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING
CiteScore
4.90
自引率
4.00%
发文量
140
审稿时长
>12 weeks
期刊介绍: Dose-Response is an open access peer-reviewed online journal publishing original findings and commentaries on the occurrence of dose-response relationships across a broad range of disciplines. Particular interest focuses on experimental evidence providing mechanistic understanding of nonlinear dose-response relationships.
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