Department of Biochemistry and Biotechnology, Annamalai University, Annamalai Nagar 608 002, Tamil Nadu, India.
Colloids Surf B Biointerfaces. 2013 Oct 1;110:313-20. doi: 10.1016/j.colsurfb.2013.03.039. Epub 2013 May 2.
Ellagic acid (EA), a naturally occurring polyphenolic compound is well documented for its anticancer property in numerous pre-clinical models. The properties like poor water solubility and limited oral bio-availability of ellagic acid has hampered its clinical applications. The present study, reports the preparation of ellagic acid encapsulated chitosan nanoparticles (EA@CS-NP) by ionic gelation method as an effective drug delivery for oral cancer treatment. The synthesized ellagic acid nanoparticle is spherical shaped with an average particle size of 176nm. The drug-encapsulation and loading-efficiency of the nanoparticles were 94±1.03% and 33±2.15% respectively. The in vitro drug release profile in the PBS medium shows sustained release of EA from EA@CS-NP. Further, this study evaluates the therapeutic efficacy of EA@CS-NP in human oral cancer cell line (KB) using MTT and DNA fragmentation analysis. EA@CS-NP exhibit significant cytotoxicity in KB cells in a dose-dependent manner with a very low IC50 value compared to the free EA. The results of the present study strengthen our hypothesis and hope that this novel formulation could possibly overcome the current limitations of ellagic acid and can open a new avenue for oral cancer therapy.
鞣花酸（EA）是一种天然存在的多酚化合物，在许多临床前模型中都有其抗癌特性的充分记录。鞣花酸的水溶性差和口服生物利用度有限等特性阻碍了其临床应用。本研究报告了通过离子凝胶化法制备鞣花酸包封壳聚糖纳米粒子（EA@CS-NP）作为口腔癌治疗的有效药物递送系统。合成的鞣花酸纳米粒子呈球形，平均粒径为 176nm。纳米粒子的药物包封率和载药效率分别为 94±1.03%和 33±2.15%。在 PBS 介质中的体外药物释放曲线显示 EA@CS-NP 从纳米粒子中持续释放 EA。此外，本研究使用 MTT 和 DNA 片段分析评估了 EA@CS-NP 在人口腔癌细胞系（KB）中的治疗功效。与游离 EA 相比，EA@CS-NP 以剂量依赖性方式在 KB 细胞中表现出显著的细胞毒性，IC50 值非常低。本研究的结果支持了我们的假设，并希望这种新制剂能够克服鞣花酸的当前局限性，并为口腔癌治疗开辟新途径。
