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用于局部应用的曲酸酯基纳米乳液的动力学释放研究、抗菌活性和毒性概况。

kinetic release study, antimicrobial activity and toxicity profile of a kojic acid ester-based nanoemulsion for topical application.

作者信息

Syed Azhar Sharifah Nurfadhlin Afifah, Ashari Siti Efliza, Ahmad Syahida, Salim Norazlinaliza

机构信息

Integrated Chemical BioPhysics Research Centre, Faculty of Science, Universiti Putra Malaysia 43400 UPM Serdang Selangor Malaysia

Centre of Foundation Studies for Agricultural Science, Universiti Putra Malaysia 43400 UPM, Serdang Selangor Malaysia.

出版信息

RSC Adv. 2020 Dec 9;10(71):43894-43903. doi: 10.1039/d0ra04807k. eCollection 2020 Nov 27.

Abstract

Nanoemulsions have emerged as novel vehicles for drug delivery that allow sustained or controlled release for topical application. In this study, kojic acid ester-based nanoemulsion (KAE-NA) was analyzed for permeation evaluation, kinetic release study, antimicrobial activity and toxicity profile on embryonic zebrafish (). Based on KAE-NA permeation evaluation, the percentage of permeation was significantly improved from 4.94% at 1 h to 59.64% at 8 h of application. The permeation rate of KAE-NA at 8 h was 4659.50 μg cm h (initial concentration, = 2000 μg mL) with a permeability coefficient ( ) value of 0.48 cm h. The kinetic release analysis showed the Korsmeyer-Peppas model was the best fitted kinetic model with high linearity [ = 0.9964]. Antimicrobial activity of KAE-NA was studied against the skin pathogen bacteria ATCC 43300. The results indicated that the inhibition zone size of the KAE-NA (8.00 ± 0.0 mm) was slightly bigger than that of its active ingredient, kojic acid ester (6.5 ± 0.0 mm). The toxicity profile of KAE-NA on embryonic zebrafish revealed less toxicity with LC (50% lethal concentration) more than 500 μg mL. The survival rate of the embryonic zebrafish was more than 80% when treated at doses ranging from 7.81-250 μg mL and showed normal development throughout the experiment without any observed deformation. Hence, KAE-NA proved to be less toxic on the embryonic zebrafish.

摘要

纳米乳剂已成为新型药物递送载体,可实现局部应用的持续或控释。在本研究中,对基于曲酸酯的纳米乳剂(KAE-NA)进行了渗透评估、动力学释放研究、抗菌活性以及对斑马鱼胚胎的毒性研究。基于KAE-NA的渗透评估,给药1小时时的渗透率为4.94%,至8小时时显著提高至59.64%。KAE-NA在8小时时的渗透速率为4659.50μg·cm²/h(初始浓度,C₀ = 2000μg/mL),渗透系数(P)值为0.48cm/h。动力学释放分析表明,Korsmeyer-Peppas模型是拟合度最佳的动力学模型,线性度高(R² = 0.9964)。研究了KAE-NA对皮肤病原菌ATCC 43300的抗菌活性。结果表明,KAE-NA的抑菌圈大小(8.00±0.0mm)略大于其活性成分曲酸酯(6.5±0.0mm)。KAE-NA对斑马鱼胚胎的毒性研究显示毒性较小,半数致死浓度(LC)超过500μg/mL。当以7.81 - 250μg/mL的剂量处理时,斑马鱼胚胎的存活率超过80%,且在整个实验过程中发育正常,未观察到任何畸形。因此,KAE-NA对斑马鱼胚胎的毒性较小。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dda1/9058481/047e1b566a01/d0ra04807k-f1.jpg

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