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硝酸咪康唑负载传递体的体外与体内特征研究及其在治疗皮肤念珠菌病中的应用。

In vitro and in vivo characterization of Miconazole Nitrate loaded transethosomes for the treatment of Cutaneous Candidiasis.

机构信息

Department of Pharmacy, Quaid-i-Azam University Islamabad 45320, Pakistan.

Department of Pharmacy, Quaid-i-Azam University Islamabad 45320, Pakistan.

出版信息

Int J Pharm. 2023 Nov 25;647:123563. doi: 10.1016/j.ijpharm.2023.123563. Epub 2023 Oct 30.

DOI:10.1016/j.ijpharm.2023.123563
PMID:37907141
Abstract

This study aimed to fabricate Miconazole Nitrate transethosomes (MCZN TESs) embedded in chitosan-based gel for the topical treatment of Cutaneous Candidiasis. A thin film hydration method was employed to formulate MCZN TESs. The prepared MCZN TESs were optimized and analyzed for their physicochemical properties including particle size (PS), polydispersity index (PDI), zeta potential (ZP), entrapment efficiency (%EE), Fourier transform infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC), deformability, and Transmission electron microscopy (TEM). In vitro release, skin permeation and deposition, skin irritation, antifungal assay, and in vivo efficacy against infected rats were evaluated. The optimized MCZN TESs showed PS of 224.8 ± 5.1 nm, ZP 21.1 ± 1.10 mV, PDI 0.207 ± 0.009, and % EE 94.12 ± 0.101 % with sustained drug release profile. Moreover, MCZN TESs Gel exhibited desirable pH, spreadability, and viscosity. Notably, the penetration and deposition capabilities of MCZN TESs Gel showed a 4-fold enhancement compared to MCZN TESs. Importantly, in vitro antifungal assay elaborated MCZN TESs Gel anti-fungal activity was 2.38-fold more compared to MCZN Gel. In vivo, studies showed a 1.5 times reduction in the duration of treatment MCZN TESs Gel treated animal group. Therefore, studies demonstrated that MCZN TESs could be a suitable drug delivery system with higher penetration and good antifungal potential.

摘要

本研究旨在制备硝酸咪康唑(MCZN)传递体(transethosomes)并嵌入壳聚糖凝胶中,用于治疗皮肤念珠菌病。采用薄膜水化法制备 MCZN 传递体。对制备的 MCZN 传递体进行优化,并分析其物理化学性质,包括粒径(PS)、多分散指数(PDI)、Zeta 电位(ZP)、包封率(%EE)、傅里叶变换红外光谱(FTIR)、差示扫描量热法(DSC)、变形性和透射电子显微镜(TEM)。评估了体外释放、皮肤渗透和沉积、皮肤刺激性、抗真菌试验以及对感染大鼠的体内疗效。优化后的 MCZN 传递体的 PS 为 224.8 ± 5.1nm、ZP 为 21.1 ± 1.10mV、PDI 为 0.207 ± 0.009 和 %EE 为 94.12 ± 0.101%,具有持续的药物释放特性。此外,MCZN 传递体凝胶表现出理想的 pH 值、铺展性和粘度。值得注意的是,与 MCZN 传递体相比,MCZN 传递体凝胶的渗透和沉积能力提高了 4 倍。重要的是,体外抗真菌试验详细阐述了 MCZN 传递体凝胶的抗真菌活性是 MCZN 凝胶的 2.38 倍。在体内,研究表明,MCZN 传递体凝胶治疗组的治疗持续时间缩短了 1.5 倍。因此,研究表明 MCZN 传递体可以作为一种合适的药物传递系统,具有更高的渗透和良好的抗真菌潜力。

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