The depigmentation effect of hydroquinone-loaded nanostructured lipid carriers (NLCs) on the rat skin

IF 0.7 Q4 PHARMACOLOGY & PHARMACY

Journal of Reports in Pharmaceutical Sciences Pub Date : 2022-01-01 DOI:10.4103/jrptps.JRPTPS_74_21

B. Sharifmakhmalzadeh, M. Javadi, A. Salimi

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Abstract

The goal of this research is the localization of hydroquinone (HQ) to the epidermis for the treatment of hyperpigmentation in rat skin. For this purpose, nanostructured lipid carrier (NLC) was selected for the dermal delivery of HQ. A 23 factorial design was used in this study, and eight NLCs were prepared with a cold homogenization technique. HQ entrapment efficiency (EE %), particle size, morphology, thermal behavior of NLCs, and permeability parameters through rat skin with NLC in comparison with HQ aqueous solution (HQ-S) with Franz diffusion cells were evaluated. Based on the optimization technique, the best NLC was selected and in the in vivo experiment, the depigmentation effect of optimized NLC in comparison with that of HQ-S was evaluated. The results showed that the main problem for HQ permeability was fast permeation and low concentration in the site of action. Partitioning from aqueous donor phase into skin rate was the limiting step for drug flux, and this can be solved using NLC. The decrease in maximum flux obtained by NLC was according to formulation 8. Regression analysis suggested a significant and direct effect of the S/L ratio and the percentage of liquid lipids on the drug loading. NLC decreased drug permeation through rat skin basically due to sustained release properties.

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负载对苯二酚的纳米结构脂质载体(NLCs)对大鼠皮肤的脱色作用

本研究的目的是对苯二酚(HQ)在表皮的定位，以治疗大鼠皮肤色素沉着。为此，我们选择了纳米结构脂质载体(NLC)来给药。本研究采用23因子设计，采用冷均质技术制备8个NLCs。评价了NLC与HQ水溶液(HQ- s)在Franz扩散池中的吸附效率(EE %)、粒径、形貌、热行为以及通过大鼠皮肤的渗透性参数。在此基础上，选择了最佳的NLC，并在体内实验中，比较了优化后的NLC与HQ-S的脱色效果。结果表明，HQ渗透的主要问题是渗透速度快，作用部位浓度低。从供水相到皮肤率的分配是药物通量的限制步骤，这可以用NLC来解决。NLC得到的最大通量的减小量按式8计算。回归分析表明，S/L比和液脂百分比对载药量有显著的直接影响。NLC降低药物通过大鼠皮肤的渗透主要是由于其缓释特性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Journal of Reports in Pharmaceutical Sciences Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)

CiteScore

1.40

自引率

0.00%

发文量

期刊介绍： The Journal of Reports in Pharmaceutical Sciences(JRPS) is a biannually peer-reviewed multi-disciplinary pharmaceutical publication to serve as a means for scientific information exchange in the international pharmaceutical forum. It accepts novel findings that contribute to advancement of scientific knowledge in pharmaceutical fields that not published or under consideration for publication anywhere else for publication in JRPS as original research article. all aspects of pharmaceutical sciences consist of medicinal chemistry, molecular modeling, drug design, pharmaceutics, biopharmacy, pharmaceutical nanotechnology, pharmacognosy, natural products, pharmaceutical biotechnology, pharmacology, toxicology and clinical pharmacy.