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Molecular Inclusion Complex of Curcumin–β-Cyclodextrin Nanoparticle to Enhance Curcumin Skin Permeability from Hydrophilic Matrix Gel

机译:姜黄素-β-环糊精纳米分子的分子包合物可提高亲水性基质凝胶的姜黄素皮肤渗透性

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摘要

Curcumin (CUR) has various pharmacological effects, but its extensive first-pass metabolism and short elimination half-life limit its bioavailability. Therefore, transdermal application has become a potential alternative to delivery CUR. To increase CUR solubility for the development of a transparent homogenous gel and also enhance the permeation rate of CUR into the skin, β-cyclodextrin–curcumin nanoparticle complex (BCD–CUR-N) was developed. CUR encapsulation efficiency was increased by raising the percentage of CUR to BCD up to 20%. The mean particle size of the best CUR loading formula was 156 nm. All evaluation data using infrared spectroscopy, Raman spectroscopy, powder X-ray diffractometry, differential thermal analysis and scanning electron microscopy confirmed the successful formation of the inclusion complex. BCD–CUR-N increased the CUR dissolution rate of 10-fold (p < 0.01). In addition, the improvement of CUR permeability acrossed skin model tissue was observed in gel containing the BCD–CUR-N and was about 1.8-fold when compared with the free CUR gel (p < 0.01). Overall, CUR in the form of the BCD–CUR-N improved the solubility further on the penetration of CUR.
机译:姜黄素(CUR)具有多种药理作用,但其广泛的首过代谢和消除半衰期短限制了其生物利用度。因此,经皮应用已成为递送CUR的潜在替代方法。为了增加CUR的溶解度以形成透明的均质凝胶并提高CUR在皮肤中的渗透率,开发了β-环糊精-姜黄素纳米颗粒复合物(BCD-CUR-N)。通过将BUR中的CUR百分比提高到20%,可以提高CUR封装效率。最佳CUR加载公式的平均粒径为156 nm。所有使用红外光谱,拉曼光谱,粉末X射线衍射,差热分析和扫描电子显微镜的评估数据均证实了包合物的成功形成。 BCD–CUR-N使CUR溶出度提高了10倍(p <0.01)。此外,在含有BCD-CUR-N的凝胶中观察到CUR在整个皮肤模型组织中的渗透性提高,与游离CUR凝胶相比,约为CUR的1.8倍(p <0.01)。总体而言,BCD–CUR-N形式的CUR进一步提高了CUR的渗透性。

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