灰黄霉素纳米结构脂质载体凝胶治疗皮肤病的研制与表征

IF 4.6 Q1 CHEMISTRY, APPLIED
Neelam Datt , Rajasekhar Reddy Poonuru , Pankaj K. Yadav
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引用次数: 3

摘要

本研究旨在制备含有灰黄霉素纳米结构脂质载体(nlc)的局部凝胶,并评估其对浅表感染的有效性。采用单硬脂酸甘油、油酸、Pluronic f68和Tween 80等多种脂类和表面活性剂进行药物溶解度研究,并采用Box-Behnken设计(BBD)对脂类、表面活性剂和乳化剂的浓度进行优化。利用超声法制备微乳液。对制备的批(F1 ~ F15)进行分析,发现最佳批(F12)的粒径为209 nm, zeta电位为-44.12 mV,包封率为85.24%,释药率为92.12%。F12为0.2% w/w药物、2% GMS、2% Pluronic F68和Tween 80(比例为1:1)。卡波波尔940,1.5%制备外用凝胶。生化研究结果表明,与标准药物相比,负载灰黄蛋白的纳米凝胶产生了更显著的脂质过氧化降低。体外细胞毒性研究表明纳米凝胶在人角质形成细胞(HaCaT)中的安全性较好。抗真菌活性的结果表明,在21天的时间内,使用红毛霉和狗毛霉菌株对Wistar大鼠的足癣和癣等浅表感染有完全的临床和真菌学治愈。这些临床前研究证明纳米凝胶在治疗上述表面感染方面具有更好的潜力,为现有产品提供了有效的替代方案。
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 characterization of griseofulvin loaded nanostructured lipid carrier gel for treating dermatophytosis

The present investigations were aimed at formulating topical gel containing nanostructured lipid carriers (NLCs) of griseofulvin and assess its effectiveness on superficial infections. The drug solubility studies were executed using various lipids and surfactants like Glyceryl monostearate, Oleic acid, Pluronic F 68, and Tween 80, and the concentrations of lipids, surfactants, and emulsifier were optimized using Box-Behnken design (BBD). Microemulsions were made utilizing sonication. The prepared batches (F1 to F15) were analyzed and observed that the optimized batch (F12), containing 0.2% w/w drug, 2% GMS, 2% Pluronic F68 and Tween 80 (in the ratio of 1:1) showed a particle size of 209 nm, zeta potential of -44.12 mV, entrapment level of 85.24% along with a drug release of 92.12%. Carbopol 940, 1.5% was used to make the topical gel. The results of biochemical studies reflected that griseofulvin-loaded-nanogel produced a more significant decrease in lipid peroxidation as compared to the standard drug. The in-vitro cytotoxicity studies showed better safety of nanogel in human keratinocyte cells (HaCaT). The results of antifungal activity showed complete clinical and mycological cure in a duration of 21 days against superficial infections like Tenia pedis and also ringworm in Wistar rats while using T.rubrum and M.canis fungal strains. These preclinical investigations have proved that the nanogels have a better potential in treating the aforementioned superficial infections providing an effective alternative for currently existing products.

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CiteScore
4.50
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