School of Pharmacy, Bandung Institute of Technology, Ganesha 10, Bandung, 40132, Indonesia,
AAPS PharmSciTech. 2013 Dec;14(4):1303-12. doi: 10.1208/s12249-013-0023-5. Epub 2013 Aug 29.
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.
姜黄素 (CUR) 具有多种药理作用,但由于其广泛的首过代谢和短的消除半衰期,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。为了提高 CUR 的溶解度,以开发透明均相凝胶,并提高 CUR 进入皮肤的渗透速率,开发了β-环糊精-姜黄素纳米颗粒复合物 (BCD-CUR-N)。通过将 CUR 与 BCD 的比例提高到 20%,可以提高 CUR 的包封效率。最佳 CUR 负载配方的平均粒径为 156nm。使用红外光谱、拉曼光谱、粉末 X 射线衍射、差示热分析和扫描电子显微镜的所有评估数据都证实了包合物的成功形成。BCD-CUR-N 将 CUR 的溶解速率提高了 10 倍(p<0.01)。此外,在含有 BCD-CUR-N 的凝胶中观察到 CUR 经皮模型组织渗透性的提高,与游离 CUR 凝胶相比约提高了 1.8 倍(p<0.01)。总体而言,以 BCD-CUR-N 形式存在的 CUR 进一步提高了 CUR 的溶解度和渗透。