埃伯康唑负载Niosomes的开发与评价

ECSOC-25 Pub Date : 2021-11-13 DOI:10.3390/ecsoc-25-11664
Priyadarshi Aparajay, A. Dev
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引用次数: 1

摘要

侵袭性真菌感染需要很长的治疗时间;然而,由于耐药性的发展,治疗变得更加麻烦。大多数抗真菌部分在口服给药时显示全身毒性,导致抗真菌部分通过局部途径递送。依伯康唑(Eberconazole, EBZ)是一种溶解度差、渗透性高的BCS类药物。它是一种广谱的咪唑衍生物,通过抑制麦角甾醇的合成而起到杀菌剂和抑菌剂的作用。市场上有各种各样的EBZ外用药膏,但缺乏适当的给药计划和快速去除导致生物利用度差。乳小体是囊状载体,可以捕获亲水和亲脂药物。以非离子表面活性剂Span20和胆固醇为原料,采用薄膜水合(TFH)技术制备了乳质体制剂。在处方前研究中,利用红外光谱法和熔点法确定了EBZ的纯度,并利用紫外可见光谱法制备了标准校准曲线。对所制备的膜体配方进行了形貌、包封效率、粒径和zeta电位的表征。该配方的包封效率为86±0.85%,微观评价时,杂质呈环状结构。进一步的体外和体内释放研究将在未来进行其有效性和抗真菌活性的评估。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development and Evaluation of Eberconazole-Loaded Niosomes
: Invasive fungal infections require a long treatment schedule; however, treatment has become more cumbersome due to the development of resistance. Most antifungal moieties show systemic toxicity upon oral administration, leading to delivery of antifungal moieties via a topical route. Eberconazole (EBZ) is a BCS class II drug that has poor solubility and high permeability. It is a broad-spectrum imidazole derivative, which acts as a both fungicidal and fungistatic drug by inhibiting ergosterol synthesis. Various topical creams of EBZ are available in the market, but the lack of a proper dosing schedule and rapid removal lead to poor bioavailability. Niosomes are vesicular carriers that can entrap both hydrophilic and lipophilic drugs. Niosomal formulations have been prepared using Span20 (nonionic surfactant) and cholesterol by thin-film hydration (TFH) technique. During preformulation studies, the purity of EBZ was ascertained using FT-IR and melting point studies, while the standard calibration curve was prepared using UV-visible spectroscopy. The prepared niosomal formulations were characterized for their morphology, entrapment efficiency, particle size, and zeta potential. The formulation has shown 86 ± 0.85% entrapment efficiency, while the noisome appeared in a ring-like structure during its microscopic evaluation. Further evaluations of in vitro and in vivo release studies will be performed in the future for its efficacy and antifungal activity.
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