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用于芒果苷经皮给药的“多元脂质体”囊泡系统:制剂研究与三维皮肤组织评价

"Plurethosome" as Vesicular System for Cutaneous Administration of Mangiferin: Formulative Study and 3D Skin Tissue Evaluation.

作者信息

Sguizzato Maddalena, Ferrara Francesca, Mariani Paolo, Pepe Alessia, Cortesi Rita, Huang Nicolas, Simelière Fanny, Boldrini Paola, Baldisserotto Anna, Valacchi Giuseppe, Esposito Elisabetta

机构信息

Department of Chemical and Pharmaceutical Sciences, University of Ferrara, I-44121 Ferrara, Italy.

Department of Neurosciences and Rehabilitation, University of Ferrara, I-44121 Ferrara, Italy.

出版信息

Pharmaceutics. 2021 Jul 23;13(8):1124. doi: 10.3390/pharmaceutics13081124.

DOI:10.3390/pharmaceutics13081124
PMID:34452085
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8398752/
Abstract

Human skin is dramatically exposed to toxic pollutants such as ozone. To counteract the skin disorders induced by the air pollution, natural antioxidants such as mangiferin could be employed. A formulative study for the development of vesicular systems for mangiferin based on phosphatidylcholine and the block copolymer pluronic is described. Plurethosomes were designed for mangiferin transdermal administration and compared to ethosome and transethosome. Particularly, the effect of vesicle composition was investigated on size distribution, inner and outer morphology by photon correlation spectroscopy, small angle X-ray diffraction, and transmission electron microscopy. The potential of selected formulations as vehicles for mangiferin was studied, evaluating encapsulation efficiency and in vitro diffusion parameters by Franz cells. The mangiferin antioxidant capacity was verified by the 2,2-diphenyl-1-picrylhydrazyl assay. Vesicle size spanned between 200 and 550 nm, being influenced by phosphatidylcholine concentration and by the presence of polysorbate or pluronic. The vesicle supramolecular structure was multilamellar in the case of ethosome or plurethosome and unilamellar in the case of transethosome. A linear diffusion of mangiferin in the case of ethosome and transethosomes and a biphasic profile in the case of plurethosomes indicated the capability of multilamellar vesicles to retain the drug more efficaciously than the unilamellar ones. The antioxidant and anti-inflammatory potential effect of mangiferin against pollutants was evaluated on 3D human skin models exposed to O. The protective effect exerted by plurethosomes and transethosomes suggests their possible application to enhance the cutaneous antioxidant defense status.

摘要

人类皮肤会大量接触到臭氧等有毒污染物。为了对抗空气污染引起的皮肤疾病,可以使用芒果苷等天然抗氧化剂。本文描述了一项基于磷脂酰胆碱和嵌段共聚物普朗尼克开发芒果苷囊泡系统的配方研究。设计了普朗尼克脂质体用于芒果苷的透皮给药,并与乙醇脂质体和转乙醇脂质体进行比较。特别地,通过光子相关光谱、小角X射线衍射和透射电子显微镜研究了囊泡组成对尺寸分布、内外形态的影响。通过Franz扩散池研究了所选配方作为芒果苷载体的潜力,评估了包封效率和体外扩散参数。通过2,2-二苯基-1-苦基肼自由基测定法验证了芒果苷的抗氧化能力。囊泡大小在200至550纳米之间,受磷脂酰胆碱浓度以及聚山梨酯或普朗尼克的存在影响。乙醇脂质体或普朗尼克脂质体情况下的囊泡超分子结构是多层的,而转乙醇脂质体情况下是单层的。乙醇脂质体和转乙醇脂质体情况下芒果苷呈线性扩散,而普朗尼克脂质体情况下呈双相分布,这表明多层囊泡比单层囊泡更能有效地保留药物。在暴露于臭氧的三维人体皮肤模型上评估了芒果苷对污染物的抗氧化和抗炎潜在作用。普朗尼克脂质体和转乙醇脂质体发挥的保护作用表明它们可能用于增强皮肤抗氧化防御状态。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c7c0/8398752/331f785b5548/pharmaceutics-13-01124-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c7c0/8398752/4bf5b3e9503a/pharmaceutics-13-01124-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c7c0/8398752/b19841ac66e0/pharmaceutics-13-01124-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c7c0/8398752/c60577d20d47/pharmaceutics-13-01124-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c7c0/8398752/de15f7496c87/pharmaceutics-13-01124-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c7c0/8398752/4ab50af0d89e/pharmaceutics-13-01124-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c7c0/8398752/6df3a86c1963/pharmaceutics-13-01124-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c7c0/8398752/331f785b5548/pharmaceutics-13-01124-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c7c0/8398752/4bf5b3e9503a/pharmaceutics-13-01124-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c7c0/8398752/b19841ac66e0/pharmaceutics-13-01124-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c7c0/8398752/c60577d20d47/pharmaceutics-13-01124-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c7c0/8398752/de15f7496c87/pharmaceutics-13-01124-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c7c0/8398752/4ab50af0d89e/pharmaceutics-13-01124-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c7c0/8398752/6df3a86c1963/pharmaceutics-13-01124-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c7c0/8398752/331f785b5548/pharmaceutics-13-01124-g007.jpg

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