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白藜芦醇经皮给药系统的比较研究:变形脂质体的高效性。

Comparative study of transdermal drug delivery systems of resveratrol: High efficiency of deformable liposomes.

机构信息

The Research Institute of Theoretical and Applied Physical Chemistry (INIFTA), Universidad Nacional de La Plata, Calle 64 Diag. 113, 1900 La Plata, Buenos Aires, Argentina.

The Research Institute of Theoretical and Applied Physical Chemistry (INIFTA), Universidad Nacional de La Plata, Calle 64 Diag. 113, 1900 La Plata, Buenos Aires, Argentina.

出版信息

Mater Sci Eng C Mater Biol Appl. 2018 Sep 1;90:356-364. doi: 10.1016/j.msec.2018.04.073. Epub 2018 Apr 28.

Abstract

Trans-resveratrol (3, 5, 4' trihydroxystilbene, RSV) is a natural compound that shows antioxidant, cardioprotective, anti-inflammatory and anticancer properties. The transdermal, painless application of RSV is an attractive option to other administration routes owing to its several advantages like avoiding gastrointestinal problems and first pass metabolism. However, its therapeutic potential is limited by its low solubility and low stability in water and the reduced permeability of stratum corneum. To overcome these inconveniences the encapsulation of this compound in a drug delivery system is proposed here. In order to find the best carrier for transdermal application of RSV various liposomal nanoparticulate carriers like conventional liposomes (L-RSV), deformable liposomes (LD-RSV), ultradeformable liposomes (LUD-RSV) and ethosomes (Etho-RSV) were assayed. Transmission electron microscopic (TEM) and dynamic light scattering (DLS) studies were performed to analyze the surface morphology of these carriers. Structural characterization for these formulations was performed by confocal Raman spectroscopy. The spectroscopic results were analysed in conjunction with calorimetric data to identify the conformational changes and stability of formulations in the different nanoparticles induced by the presence of RSV. Comparison of the results obtained with the different carrier systems (L-RSV, LD-RSV, LUD-RSV and Etho-RSV) revealed that the best RSV carrier was LD-RSV. The increase in the fluidity of the bilayers in the region of the hydrophobic chains of the phospholipid by ethanol probably facilitates the accommodation of the RSV in the bilayer and contributes to the improved encapsulation of RSV without affecting the mobility of this carrier.

摘要

反式白藜芦醇(3,5,4' 三羟基二苯乙烯,RSV)是一种天然化合物,具有抗氧化、心脏保护、抗炎和抗癌特性。由于其避免胃肠道问题和首过代谢等多种优势,RSV 的经皮、无痛应用是其他给药途径的一个有吸引力的选择。然而,由于其在水中的低溶解度和低稳定性以及角质层的渗透性降低,其治疗潜力受到限制。为了克服这些不便,提出了将该化合物包封在药物传递系统中。为了找到 RSV 经皮应用的最佳载体,研究了各种脂质体纳米颗粒载体,如常规脂质体(L-RSV)、变形脂质体(LD-RSV)、超变形脂质体(LUD-RSV)和醇质体(Etho-RSV)。进行了透射电子显微镜(TEM)和动态光散射(DLS)研究,以分析这些载体的表面形态。通过共焦拉曼光谱对这些制剂进行了结构特征分析。通过对不同纳米粒子中 RSV 存在引起的制剂构象变化和稳定性的热数据进行分析,对这些制剂进行了结构表征。对不同载体系统(L-RSV、LD-RSV、LUD-RSV 和 Etho-RSV)的结果进行比较,结果表明 RSV 的最佳载体是 LD-RSV。乙醇可能会增加磷脂疏水链区域双层的流动性,从而促进 RSV 进入双层,并有助于改善 RSV 的包封而不影响该载体的流动性。

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