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褪黑素弹性脂质体在光老化小鼠中的应用及疗效

Application and Efficacy of Melatonin Elastic Liposomes in Photoaging Mice.

作者信息

Hou Xueqin, Qiu Xinyu, Wang Yaping, Song Shuangshuang, Cong Yifan, Hao Jifu

机构信息

Institute of Pharmacology, Shandong First Medical University & Shandong Academy of Medical Sciences, Taian, Shandong 271016, China.

College of Pharmacy, Shandong First Medical University & Shandong Academy of Medical Sciences, Taian, Shandong 271016, China.

出版信息

Oxid Med Cell Longev. 2022 Mar 8;2022:7135125. doi: 10.1155/2022/7135125. eCollection 2022.

DOI:10.1155/2022/7135125
PMID:35300175
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8923809/
Abstract

Transdermal drug delivery system is a preferable choice to overcome the low bioavailability of oral medication. Elastic liposomes have shown great effectiveness for percutaneous transport of melatonin (MLT). In this study, the elastic liposomes loaded with MLT were prepared using thin-film dispersion method and optimized through the central composite design (CCD) approach. The physicochemical properties and skin permeation against UV-induced skin photoaging efficacy of the developed MLT-ELs were assessed. The average size of the MLT-ELs was about 49 nm with a spherical shape and high encapsulation efficiency (73.91%) and drug loading (9.92%). The results of FTIR, DSC, and XRD revealed that the chemical structure of MLT was not changed after prepared elastic liposomes, and the drug was successfully encapsulated in the elastic liposome membrane material. In vitro skin permeation evaluation showed that the cumulative penetration of elastic liposomes was 1.5 times higher than that of conventional liposomes, highlighting that the elastic liposomes more easily penetrated into the body. The photoaging experiment results indicated that topical MLT-EL treatment ameliorated the skin elasticity, enhanced the skin hydration level, and preserved the integrity of dermal collagen and elastic fibers. It could be concluded that the elastic liposomes might serve as a promising platform for the transdermal delivery of melatonin.

摘要

经皮给药系统是克服口服药物生物利用度低的一种优选方法。弹性脂质体已显示出对褪黑素（MLT）经皮转运具有显著效果。在本研究中，采用薄膜分散法制备了负载MLT的弹性脂质体，并通过中心复合设计（CCD）方法进行优化。评估了所制备的MLT-ELs的理化性质以及针对紫外线诱导的皮肤光老化功效的皮肤渗透情况。MLT-ELs的平均粒径约为49nm，呈球形，具有较高的包封率（73.91%）和载药量（9.92%）。傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）和X射线衍射（XRD）结果表明，制备弹性脂质体后MLT的化学结构未发生改变，且药物成功包封于弹性脂质体膜材料中。体外皮肤渗透评估显示，弹性脂质体的累积渗透率比传统脂质体高1.5倍，突出表明弹性脂质体更易渗透进入体内。光老化实验结果表明，局部应用MLT-EL可改善皮肤弹性、提高皮肤水合水平，并保持真皮胶原蛋白和弹性纤维的完整性。可以得出结论，弹性脂质体可能是褪黑素经皮递送的一个有前景的平台。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cca4/8923809/2d0f5bbea60d/OMCL2022-7135125.014.jpg
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