Pharmaceutical Sciences and Technology, University Institute of Chemical Technology, Mumbai, India.
Pharm Dev Technol. 2013 May-Jun;18(3):619-25. doi: 10.3109/10837450.2011.649855. Epub 2012 Jan 12.
The purpose of the present study was to develop Tamoxifen loaded β-cyclodextrin nanosponges for oral drug delivery. The three types of Tamoxifen loaded β-cyclodextrin nanosponges were synthesized by varying the molar ratios of β-cyclodextrin to carbonyldiimidazole as a crosslinker viz. 1:2, 1:4 and 1:8. The Tamoxifen nanosponge complex (TNC) with particle size of 400-600 nm was obtained by freeze drying method. Differential scanning calorimetry, Fourier transformed infra-red spectroscopy and X-ray powder diffraction studies confirmed the complexation of Tamoxifen with cyclodextrin nanosponge. AUC and Cmax of TNC formulation (1236.4 ± 16.12 µg · mL(-1) h, 421.156 ± 0.91 µg/mL) after gastric intubation were 1.44 fold and 1.38 fold higher than plain drug (856.079 ± 15.18 µg · mL(-1) h, 298.532 ± 1.15 µg/mL). Cytotoxic studies on MCF-7 cells showed that TNC formulation was more cytotoxic than plain Tamoxifen after 24 and 48 h of incubation.
本研究旨在开发用于口服给药的他莫昔芬负载β-环糊精纳米海绵。通过改变β-环糊精与碳二亚胺作为交联剂的摩尔比（分别为 1:2、1:4 和 1:8），合成了三种类型的他莫昔芬负载β-环糊精纳米海绵。通过冷冻干燥法获得粒径为 400-600nm 的他莫昔芬纳米海绵复合物（TNC）。差示扫描量热法、傅里叶变换红外光谱和 X 射线粉末衍射研究证实了他莫昔芬与环糊精纳米海绵的络合。胃内给药后 TNC 制剂（AUC 和 Cmax 分别为 1236.4±16.12µg·mL(-1)h 和 421.156±0.91µg/mL）的 AUC 和 Cmax 分别比普通药物（856.079±15.18µg·mL(-1)h 和 298.532±1.15µg/mL）高 1.44 倍和 1.38 倍。MCF-7 细胞的细胞毒性研究表明，TNC 制剂在孵育 24 和 48 小时后比普通他莫昔芬更具细胞毒性。
