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用于咖啡酸透皮递送的普朗尼克123液体溶致液晶——来自结构研究和药物释放的见解

Pluronic 123 Liquid Lyotropic Crystals for Transdermal Delivery of Caffeic Acid-Insights from Structural Studies and Drug Release.

作者信息

Romeo Martina, Mazzotta Elisabetta, Lovati Francesca, Porto Michele, Rossi Cesare Oliviero, Muzzalupo Rita

机构信息

Department of Pharmacy Health and Nutritional Sciences, University of Calabria, Via P. Bucci, 87036 Arcavacata di Rende, Italy.

Department of Chemistry and Chemical Technologies, Cubo 14/D, University of Calabria, Via P. Bucci, 87036 Arcavacata di Rende, Italy.

出版信息

Gels. 2024 Mar 6;10(3):181. doi: 10.3390/gels10030181.

Abstract

BACKGROUND

This study aims to evaluate the percutaneous permeation profiles of caffeic acid (CA) from the cubic and hexagonal liquid crystalline phases of Pluronic P123/water mixtures.

METHOD

The resulting drug-loaded mesophases were subjected to characterisation through deuterium nuclear magnetic resonance spectroscopy and polarised optical microscopy observations. These analyses aimed to evaluate the structural changes that occurred in the mesophases loading with CA. Additionally, steady and dynamic rheology studies were conducted to further explore their mechanical properties and correlate them to the supramolecular structure. Finally, CA release experiments were carried out at two different temperatures to examine the behaviour of the structured systems in a physiological or hyperthermic state.

RESULTS

As the concentration of the polymer increases, an increase in the viscosity of the gel is noted; however, the addition of caffeic acid increases microstructure fluidity. It is observed that the temperature effect conforms to expectations. The increase in temperature causes a decrease in viscosity and, consequently, an increase in the rate of permeation of caffeic acid.

CONCLUSIONS

The CA permeation profile from the prepared formulations is mostly dependent on the structural organisation and temperature. Cubic mesophase LLC 30/CA showed greater skin permeation with good accumulation in the skin at both tested temperatures.

摘要

背景

本研究旨在评估咖啡酸(CA)从普朗尼克P123/水混合物的立方相和六方相液晶相的经皮渗透情况。

方法

通过氘核磁共振光谱和偏振光学显微镜观察对所得载药中间相进行表征。这些分析旨在评估载有CA的中间相中发生的结构变化。此外,进行了稳态和动态流变学研究,以进一步探索它们的力学性能,并将其与超分子结构相关联。最后,在两个不同温度下进行了CA释放实验,以研究结构化系统在生理或高温状态下的行为。

结果

随着聚合物浓度的增加,凝胶的粘度增加;然而,咖啡酸的加入增加了微观结构的流动性。观察到温度效应符合预期。温度升高导致粘度降低,从而使咖啡酸的渗透速率增加。

结论

所制备制剂的CA渗透情况主要取决于结构组织和温度。立方相液晶脂质体30/CA在两个测试温度下均表现出更大的皮肤渗透性,并在皮肤中具有良好的蓄积性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/428a/10970513/5cf28a534dc1/gels-10-00181-g001.jpg

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