Pharmacy Department, TIFAC-CORE in NDDS, Faculty of Technology and Engineering, G. H. Patel Building, Fateh Gunj, Vadodara 390002, India.
J Biomed Nanotechnol. 2009 Feb;5(1):99-105. doi: 10.1166/jbn.2009.026.
Calcium phosphate is considered as a potential biomaterial for drug and gene delivery because of its excellent features. In this study, we reported the formulation and characterization of calcium phosphate nanoparticle containing anticancer drug, methotrexate (MTX). Calcium phosphate nanoparticles containing MTX (CaPi-MTX) were prepared by reverse micelles technique. CaPi-MTX nanoparticles of average size 262 +/- 47.64 nm with entrapment efficiency of 58.04 +/- 4.09% were obtained. The IR spectrum of CaPi-MTX showed characteristics of composite formation of hydroxyapatite with MTX. X-RD analysis revealed that, CaPi-MTX nanoparticles were crystalline and in hydroxyapatite form. TEM studies showed that CaPi-MTX nanoparticles were spherical in shape. In vitro release study of CaPi-MTX nanoparticles showed slow release of MTX at physiological pH (pH 7.4) while > 90% release was observed within 3-4 hours at endosomal pH (pH 5.5 and pH 6.0). Confocal microscopy was performed using CHO cell lines, showed intracellular localization of FITC-Dextran loaded calcium phosphate nanoparticles. Results indicate that prepared CaPi-MTX nanoparticles could serve the purpose for intracellular drug delivery.
磷酸钙因其优异的特性而被认为是一种潜在的药物和基因传递的生物材料。在这项研究中，我们报道了载有抗癌药物甲氨蝶呤（MTX）的磷酸钙纳米粒子的配方和特性。通过反胶束技术制备了载有 MTX 的磷酸钙纳米粒子（CaPi-MTX）。平均粒径为 262 ± 47.64nm，包封率为 58.04 ± 4.09%。CaPi-MTX 的 IR 光谱显示了羟基磷灰石与 MTX 复合形成的特征。X-RD 分析表明，CaPi-MTX 纳米粒子是结晶的，呈羟基磷灰石形式。TEM 研究表明，CaPi-MTX 纳米粒子呈球形。在生理 pH（pH7.4）下，CaPi-MTX 纳米粒子的体外释放研究表明 MTX 释放缓慢，而在溶酶体 pH（pH5.5 和 pH6.0）下 3-4 小时内释放超过 90%。使用 CHO 细胞系进行共聚焦显微镜检查，显示 FITC-Dextran 负载的磷酸钙纳米粒子的细胞内定位。结果表明，所制备的 CaPi-MTX 纳米粒子可用于细胞内药物传递。
