Department of Applied Chemistry, Government College University, Faisalabad, Pakistan.
Department of Pharmaceutical Chemistry, Government College University, Faisalabad, Pakistan.
AAPS PharmSciTech. 2018 Aug;19(6):2719-2739. doi: 10.1208/s12249-018-1098-9. Epub 2018 Jul 5.
Curcumin is a naturally occurring constituent of turmeric that is a good substitute for synthetic medicines for the treatment of different diseases, due to its comparatively safer profile. However, there are certain shortcomings that limit its use as an ideal therapeutic agent. In order to overcome these drawbacks, we prepared novel curcumin-loaded mixed polymeric micelles using different biocompatible polymers by the thin-film hydration method. We investigated the critical micelle concentration and temperature, drug loading and encapsulation efficiency, and minimum inhibitory concentration by spectrophotometry. Surface morphology, stability, particle size, drug-polymer interaction, and physical state of the prepared formulations were investigated using scanning electron microscopy, zeta potential, particle size analyzer, Fourier-transform infrared spectroscopy, and X-ray diffraction, respectively. The drug loading and entrapment efficiency were significantly increased (P < 0.01) when curcumin was encapsulated with pluronic-based mixed polymeric micelles as compared to that of pluronic-based micelles alone. In vitro studies exhibited that pluronic-based mixed polymeric micelles significantly increased anticancer (P < 0.01), antimicrobial (P < 0.001), antioxidant (P < 0.001), and α-amylase inhibitory (P < 0.001) activities when compared to pure curcumin and/or pluronic-based micelles alone. These findings suggest that the formation of mixed polymeric micelles increases the stability and solubility of curcumin.
姜黄素是姜黄中的一种天然成分,由于其相对更安全的特性,它可以替代合成药物治疗各种疾病。然而,它也存在一些限制其应用的缺点。为了克服这些缺点,我们采用薄膜水化法,使用不同的生物相容性聚合物制备了新型载姜黄素混合聚合物胶束。我们通过分光光度法研究了胶束的临界胶束浓度和温度、载药量和包封率以及最小抑菌浓度。通过扫描电子显微镜、Zeta 电位、粒径分析仪、傅里叶变换红外光谱和 X 射线衍射分别研究了制剂的表面形态、稳定性、粒径、药物-聚合物相互作用和物理状态。与单独使用普朗尼克胶束相比,姜黄素包封在基于普朗尼克的混合聚合物胶束中时,载药量和包封效率显著增加(P<0.01)。体外研究表明,与纯姜黄素和/或单独的普朗尼克胶束相比,基于普朗尼克的混合聚合物胶束显著提高了抗癌(P<0.01)、抗菌(P<0.001)、抗氧化(P<0.001)和α-淀粉酶抑制(P<0.001)活性。这些发现表明,混合聚合物胶束的形成增加了姜黄素的稳定性和溶解度。