Application and Efficacy of Melatonin Elastic Liposomes in Photoaging Mice

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

doi:10.1155/2022/7135125

Xueqin Hou, Yifan Cong + Show 5 more

Open Access

https://doi.org/10.1155/2022/7135125

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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.

Highlights

Melatonin (N-acetyl-5-methoxytryptamine, MLT), known as pineal gland hormone, is a hormone synthetized in the pineal gland at nighttime through a sequence of well-known reactions from serotonin [1]
The number of collagen fiber bundles in the dermis was increased and thickened, and they displayed an ordered arrangement. These results indicated that the melaskin hydration (%) Naïve control (NC) stratum corneum (SC) Model control (MC) M LT-elastic liposomes (ELs) M LT-C Ls tonin liposome preparation, especially Melatonin Elastic Liposomes (MLT-ELs), had good biocompatibility and it mitigated the structural damage of the skin
A functional MLT-loaded elastic liposome platform was developed through thin-film dispersion approach and applied for delivery of MTL through the skin to achieve antiaging effect caused by UV radiation

Summary

Introduction

Melatonin (N-acetyl-5-methoxytryptamine, MLT), known as pineal gland hormone, is a hormone synthetized in the pineal gland at nighttime through a sequence of well-known reactions from serotonin [1]. MLT is usually supplemented by oral administration, but most drugs are degraded through the liver due to the firstpass effect, and few can be used by the body [2]. It has a short half-life, low solubility, and instability, which limits its absorption in the body and affects the efficacy of ordinary melatonin preparations [2]. It is proposed to change the way of drug delivery and exploit nanodelivery system, so as to increase the solubility of drug, prolong the half-life in vivo, and improve the bioavailability of drug

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