Formulation, characterization and evaluation of curcumin-loaded PLGA nanospheres for cancer therapy.
Formulation, characterization and evaluation of curcumin-loaded PLGA nanospheres for cancer therapy.
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发表时间：
2009-10
影响因子：
2
通讯作者：
A. Mukerjee;J. Vishwanatha
中科院分区：
文献类型：
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作者：
A. Mukerjee;J. Vishwanatha
背景技术在有效的抗癌剂中，已发现姜黄素对于许多不同类型的癌细胞非常有效。然而，与使用姜黄素相关的主要缺点是，由于其水溶性差，口服给药时其全身生物利用度较低。我们目前的工作研究了采用固/油/水乳液溶剂蒸发方法将姜黄素封装在聚乳酸-乙醇酸 (PLGA) 纳米球中的效率。材料和方法配制纳米球，然后表征其产率百分比、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。结果我们的研究表明成功形成了光滑、球形的姜黄素负载 PLGA 纳米球，包封率为 90.88+/-0.14%。粒径分布范围为35 nm至100 nm，平均粒径为45 nm。在前列腺癌细胞系中对这些负载姜黄素的纳米球进行了评估。结果显示细胞内纳米球的细胞内摄取强劲。细胞活力研究表明，与游离姜黄素相比，负载姜黄素的纳米球能够对癌细胞发挥更显着的作用。结论 我们的研究成功地制备了负载姜黄素的 PLGA 纳米球，从而表明基于纳米颗粒的姜黄素制剂具有作为前列腺癌临床应用辅助治疗的巨大潜力。
BACKGROUND 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. MATERIALS AND METHODS 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. RESULTS 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. CONCLUSION 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.