Laboratory for Nanomedicine, Institute of Life Sciences, Nalco Square, Chandrasekharpur, Bhubaneswar, Orissa, India.
Nanomedicine (Lond). 2010 Apr;5(3):433-49. doi: 10.2217/nnm.10.9.
AIM: To develop a suitable formulation of curcumin-encapsulated methoxy poly(ethylene glycol) (MePEG)/poly-epsilon-caprolactone (PCL) diblock copolymeric micelle by varying the copolymer ratio, for achieving small sized micelles with high encapsulation of curcumin. To evaluate the micelle's aqueous solubility and stability, efficiency of cellular uptake, cell cytotoxicity and ability to induce apoptosis on pancreatic cell lines. METHOD: Amphiphilic diblock copolymers (composed of MePEG and PCL) were used in various ratios for the preparation of curcumin-encapsulated micelles using a modified dialysis method. Physicochemical characterization of the formulation included size and surface charge measurement, transmission electron microscopy characterization, spectroscopic analysis, stability and in vitro release kinetics studies. The anticancer efficacy of the curcumin-encapsulated micelle formulation was compared with unmodified curcumin in terms of cellular uptake, cell cytotoxicity and apoptosis of pancreatic cell lines MIA PaCa-2 and PANC-1. RESULTS: Physiochemical characterization of the formulations revealed that curcumin was efficiently encapsulated in all formulation of MePEG/PCL micelles; however, a 40:60 MePEG:PCL ratio micelle was chosen for experimental studies owing to its high encapsulation (approximately 60%) with size (approximately 110 nm) and negative zeta potential (approximately -16 mV). Curcumin-encapsulated micelles increased the bioavailability of curcumin due to enhanced uptake (2.95 times more compared with unmodified) with comparative cytotoxic activity (by induction of apoptosis) compared with unmodified curcumin at equimolar concentrations. IC(50) values for unmodified curcumin and curcumin micelles were found to be 24.75 microM and 22.8 microM for PANC-1 and 14.96 microM and 13.85 microM for MIA PaCa-2, respectively. Together the results clearly indicate the promise of a micellar system for efficient solubilization, stabilization and controlled delivery of the hydrophobic drug curcumin for cancer therapy.
目的：通过改变共聚物比例，开发一种合适的姜黄素包封甲氧基聚乙二醇（MePEG）/聚己内酯（PCL）两亲嵌段共聚物胶束的配方，以获得具有高姜黄素包封率的小尺寸胶束。评估胶束的水溶解度和稳定性、细胞摄取效率、细胞细胞毒性以及对胰腺细胞系诱导凋亡的能力。
方法：使用不同比例的两亲性嵌段共聚物（由 MePEG 和 PCL 组成），通过改良的透析法制备姜黄素包封胶束。制剂的物理化学性质包括粒径和表面电荷测量、透射电子显微镜表征、光谱分析、稳定性和体外释放动力学研究。在细胞摄取、细胞毒性和胰腺细胞系 MIA PaCa-2 和 PANC-1 的凋亡方面，将姜黄素包封胶束制剂的抗癌效果与未修饰的姜黄素进行了比较。
结果：制剂的物理化学性质分析表明，姜黄素在所有 MePEG/PCL 胶束制剂中均能有效包封；然而，由于其高包封率（约 60%）、粒径（约 110nm）和负 zeta 电位（约-16mV），选择 40:60 MePEG:PCL 比例的胶束用于实验研究。姜黄素包封胶束增加了姜黄素的生物利用度，因为与未修饰的姜黄素相比，摄取量增加了 2.95 倍（在等摩尔浓度下，与未修饰的姜黄素相比，诱导凋亡的细胞毒性活性相当）。未修饰的姜黄素和姜黄素胶束对 PANC-1 的 IC50 值分别为 24.75μM 和 22.8μM，对 MIA PaCa-2 的分别为 14.96μM 和 13.85μM。这些结果清楚地表明，胶束系统在癌症治疗中为疏水性药物姜黄素的有效溶解、稳定和控制释放提供了希望。
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