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负载布洛芬及其衍生物的乳液基凝胶

Emulsion-Based Gel Loaded with Ibuprofen and Its Derivatives.

作者信息

Agboola Adebukola Abiola, Nowak Anna, Duchnik Wiktoria, Kucharski Łukasz, Story Anna, Story Grzegorz, Struk Łukasz, Antosik Adrian Krzysztof, Ossowicz-Rupniewska Paula

机构信息

Department of Chemical Organic Technology and Polymeric Materials, Faculty of Chemical Technology and Engineering, West Pomeranian University of Technology in Szczecin, Piastów Ave. 42, 71-065 Szczecin, Poland.

Department of Cosmetic and Pharmaceutical Chemistry, Pomeranian Medical University in Szczecin, Powstańców Wielkopolskich Ave. 72, 70-111 Szczecin, Poland.

出版信息

Gels. 2023 May 8;9(5):391. doi: 10.3390/gels9050391.

DOI:10.3390/gels9050391
PMID:37232983
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10217311/
Abstract

The aim of this study was to evaluate the effect of vehicle and chemical modifications of the structure of active compounds on the skin permeation and accumulation of ibuprofen (IBU). As a result, semi-solid formulations in the form of an emulsion-based gel loaded with ibuprofen and its derivatives, such as sodium ibuprofenate (IBUNa) and L-phenylalanine ethyl ester ibuprofenate ([PheOEt][IBU]), were developed. The properties of the obtained formulations were examined, including density, refractive index, viscosity, and particle size distribution. The parameters of release and permeability through the pig skin of the active substances contained in the obtained semi-solid formulations were determined. The results indicate that an emulsion-based gel enhanced the skin penetration of IBU and its derivatives compared to two commercial preparations in the form of a gel and a cream. The average cumulative mass of IBU after a 24 h permeation test from an emulsion-based gel formulation through human skin was 1.6-4.0 times higher than for the commercial products. Ibuprofen derivatives were evaluated as chemical penetration enhancers. After 24 h of penetration, the cumulative mass was 1086.6 ± 245.8 for IBUNa and 948.6 ± 87.5 µg IBU/cm for [PheOEt][IBU], respectively. This study demonstrates the perspective of the transdermal emulsion-based gel vehicle in conjunction with the modification of the drug as a potentially faster drug delivery system.

摘要

本研究的目的是评估活性化合物结构的载体和化学修饰对布洛芬（IBU）皮肤渗透和蓄积的影响。结果，开发了以负载布洛芬及其衍生物（如布洛芬钠（IBUNa）和L-苯丙氨酸乙酯布洛芬酯（[PheOEt][IBU]））的乳液基凝胶形式的半固体制剂。对所得制剂的性质进行了检查，包括密度、折射率、粘度和粒度分布。测定了所得半固体制剂中活性物质通过猪皮的释放和渗透参数。结果表明，与凝胶和乳膏形式的两种市售制剂相比，乳液基凝胶增强了IBU及其衍生物的皮肤渗透。通过人皮肤进行24小时渗透试验后，乳液基凝胶制剂中IBU的平均累积质量比市售产品高1.6 - 4.0倍。布洛芬衍生物被评估为化学渗透促进剂。渗透24小时后，IBUNa的累积质量为1086.6±245.8，[PheOEt][IBU]的累积质量为948.6±87.5μg IBU/cm²。本研究证明了基于透皮乳液的凝胶载体结合药物修饰作为一种潜在更快的药物递送系统的前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/0c7fc3ff6f15/gels-09-00391-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/3021849ba988/gels-09-00391-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/4368a5613499/gels-09-00391-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/8ed12d9f982f/gels-09-00391-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/038c048f7f1d/gels-09-00391-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/5308fa57ec73/gels-09-00391-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/4d1005f409c5/gels-09-00391-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/840dd40ab5b4/gels-09-00391-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/3f38080ddd4d/gels-09-00391-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/0c7fc3ff6f15/gels-09-00391-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/3021849ba988/gels-09-00391-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/4368a5613499/gels-09-00391-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/8ed12d9f982f/gels-09-00391-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/038c048f7f1d/gels-09-00391-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/5308fa57ec73/gels-09-00391-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/4d1005f409c5/gels-09-00391-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/840dd40ab5b4/gels-09-00391-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/3f38080ddd4d/gels-09-00391-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f3d/10217311/0c7fc3ff6f15/gels-09-00391-g008.jpg

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