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用于白藜芦醇经皮递送的优化微乳剂的设计与配方

Design and Formulation of Optimized Microemulsions for Dermal Delivery of Resveratrol.

作者信息

Juškaitė Vaida, Ramanauskienė Kristina, Briedis Vitalis

机构信息

Department of Clinical Pharmacy, Lithuanian University of Health Sciences, Eivenių Street 4, 50161 Kaunas, Lithuania.

出版信息

Evid Based Complement Alternat Med. 2015;2015:540916. doi: 10.1155/2015/540916. Epub 2015 Aug 31.

DOI:10.1155/2015/540916
PMID:26417375
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4568364/
Abstract

The objective of this study was to formulate optimal formulations of microemulsions (MEs) and evaluate their feasibility for delivery of resveratrol into human skin ex vivo. Oil-in-water MEs were formulated using surfactant (S) PEG-8 caprylic/capric glycerides and cosurfactant (CoS) polyglyceryl-6-isostearate. Ethyl oleate was used as an oily phase. MEs were formulated using 5 : 1, 6 : 1, and 7 : 1 surfactant and cosurfactant (S : CoS) weight ratios. Pseudoternary phase diagrams were constructed and optimal compositions of MEs were obtained using Design Expert software. Mean droplet size for optimized ME formulations was determined to be 68.54 ± 1.18 nm, 66.08 ± 0.16 nm, and 66.66 ± 0.56 nm for systems with S : CoS weight ratios 5 : 1, 6 : 1, and 7 : 1, respectively. Resveratrol loading resulted in mean droplet size increase. The distribution of droplet size between fractions changed during storage of formulated MEs. Results demonstrated the increase of number of droplets and relative surface area when S : CoS weight ratios were 6 : 1 and 7 : 1 and the decrease when S : CoS weight ratio was 5 : 1. The highest penetration of resveratrol into the skin ex vivo was determined from ME with S : CoS weight ratio 5 : 1. It was demonstrated that all MEs were similar in their ability to deliver resveratrol into the skin ex vivo.

摘要

本研究的目的是制备微乳（MEs）的最佳配方，并评估其将白藜芦醇离体递送至人皮肤的可行性。采用表面活性剂（S）聚乙二醇-8辛酸/癸酸甘油酯和助表面活性剂（CoS）聚甘油-6-异硬脂酸酯制备水包油型微乳。油酸乙酯用作油相。使用5∶1、6∶1和7∶1的表面活性剂与助表面活性剂（S∶CoS）重量比来制备微乳。构建了拟三元相图，并使用Design Expert软件获得了微乳的最佳组成。对于S∶CoS重量比为5∶1、6∶1和7∶1的体系，优化后的微乳配方的平均液滴尺寸分别确定为68.54±1.18nm、66.08±0.16nm和66.66±0.56nm。负载白藜芦醇导致平均液滴尺寸增加。在配制的微乳储存期间，各组分之间的液滴尺寸分布发生变化。结果表明，当S∶CoS重量比为6∶1和7∶1时，液滴数量和相对表面积增加，而当S∶CoS重量比为5∶1时则减少。从S∶CoS重量比为5∶1的微乳中测定出白藜芦醇在离体皮肤中的最高渗透率。结果表明，所有微乳在将白藜芦醇离体递送至皮肤的能力方面相似。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/68ed/4568364/a241fbb44c87/ECAM2015-540916.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/68ed/4568364/2bde225efafe/ECAM2015-540916.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/68ed/4568364/510c835ba37e/ECAM2015-540916.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/68ed/4568364/ce0d5b8bc6f8/ECAM2015-540916.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/68ed/4568364/a241fbb44c87/ECAM2015-540916.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/68ed/4568364/2bde225efafe/ECAM2015-540916.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/68ed/4568364/510c835ba37e/ECAM2015-540916.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/68ed/4568364/ce0d5b8bc6f8/ECAM2015-540916.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/68ed/4568364/a241fbb44c87/ECAM2015-540916.004.jpg

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