Mukerjee Anindita, Vishwanatha Jamboor K
Department of Molecular Biology, Institute for Cancer Research, Graduate School of Biomedical Sciences, University of North Texas, Health Science Center, Fort Worth, TX, 76107, USA.
Anticancer Res. 2009 Oct;29(10):3867-75.
Among the potent anticancer agents, curcumin has been found to be very efficacious against many different types of cancer cells. However, the major disadvantage associated with the use of curcumin is its low systemic bioavailability when administered orally due to its poor aqueous solubility. Our present work investigated the efficiency of encapsulation of curcumin in poly (lactic-coglycolic acid) (PLGA) nanospheres using solid/oil/water emulsion solvent evaporation method.
The nanospheres were formulated and then characterized for percent yield, encapsulation efficiency, surface morphology, particle size, drug distribution studies, drug polymer interaction studies and in vitro drug release profiles.
Our studies showed the successful formation of smooth and spherical curcumin-loaded PLGA nanospheres, with an encapsulation efficiency of 90.88+/-0.14%. The particle size distribution showed a range of 35 nm to 100 nm, with the mean particle size being 45 nm. Evaluation of these curcumin-loaded nanospheres was carried out in prostate cancer cell lines. Results showed robust intracellular uptake of the nanospheres in the cells. Cell viability studies revealed that the curcumin-loaded nanospheres were able to exert a more pronounced effect on the cancer cells as compared to free curcumin.
Our studies achieved successful formulation of curcumin loaded PLGA nanospheres, thus indicating that nanoparticle-based formulation of curcumin has high potential as an adjuvant therapy for clinical application in prostate cancer.
在强效抗癌药物中,姜黄素已被发现对许多不同类型的癌细胞非常有效。然而,使用姜黄素的主要缺点是口服给药时由于其水溶性差导致全身生物利用度低。我们目前的工作采用固/油/水乳液溶剂蒸发法研究了姜黄素在聚(乳酸-乙醇酸)(PLGA)纳米球中的包封效率。
制备纳米球,然后对其产率、包封效率、表面形态、粒径、药物分布研究、药物-聚合物相互作用研究和体外药物释放曲线进行表征。
我们的研究表明成功形成了光滑球形的载姜黄素PLGA纳米球,包封效率为90.88±0.14%。粒径分布范围为35nm至100nm,平均粒径为45nm。在前列腺癌细胞系中对这些载姜黄素纳米球进行了评估。结果显示纳米球在细胞内有大量摄取。细胞活力研究表明,与游离姜黄素相比,载姜黄素纳米球对癌细胞能产生更显著的作用。
我们的研究成功制备了载姜黄素PLGA纳米球,表明基于纳米颗粒的姜黄素制剂作为前列腺癌临床应用的辅助治疗具有很大潜力。