Institute of Pharmacy, Bundelkhand University, Jhansi, UP 284128, India.
Int J Pharm. 2011 Feb 28;405(1-2):203-9. doi: 10.1016/j.ijpharm.2010.12.002. Epub 2010 Dec 9.
The purpose of this investigation was to evaluate the performance of poly (amidoamine) (PAMAM) dendrimers, with three different surface groups, to be used as drug carriers. Drug-dendrimers complexes were investigated for solubility studies, dissolution studies, in vitro drug release studies, and for stability studies. The solubility enhancement was found maximum with PEGylated dendrimers (33 times) followed by amine (23 times) and hydroxyl (17.5 times) dendrimers. The solubility profile of simvastatin-dendrimer complex showed a linear correlation (Higuchi A(L)-type diagram) between solubility and dendrimers concentration. The formation of the complexes between drug molecules and dendrimers were characterized by the FTIR spectra of these complexes, showing the appearance of the bond formed between the functional groups of the drug (OH and COOH) and dendrimers (NH(2) and OH). The drug-dendrimer complexes displayed the controlled release action during in vitro release studies. Pure simvastatin (SMV) was released in 5h whereas the PEGylated dendrimers-SMV complexes released the drug up to 5 days. The non-PEGylated formulations released the drug up to 24h. Formulations with amine and PEGylated dendrimers were subjected to accelerated stability studies. Formulations with amine dendrimers were found to be most stable in dark, low temperature (0°C) whereas the dark, RT was most suitable storage conditions for formulation with PEGylated dendrimers.
本研究旨在评估具有三种不同表面基团的聚酰胺-胺（PAMAM）树枝状大分子作为药物载体的性能。研究了药物-树枝状大分子复合物的溶解度研究、溶解研究、体外药物释放研究和稳定性研究。发现聚乙二醇化树枝状大分子（提高 33 倍）、胺（提高 23 倍）和羟基（提高 17.5 倍）树枝状大分子的增溶效果最大。辛伐他汀-树枝状大分子复合物的溶解度曲线显示了溶解度与树枝状大分子浓度之间的线性相关性（Higuchi A（L）-型图）。药物分子与树枝状大分子之间形成复合物的特征是这些复合物的傅里叶变换红外光谱（FTIR），显示出药物（OH 和 COOH）和树枝状大分子（NH（2）和 OH）的官能团之间形成的键。药物-树枝状大分子复合物在体外释放研究中显示出控制释放作用。纯辛伐他汀（SMV）在 5 小时内释放，而聚乙二醇化树枝状大分子-SMV 复合物则在 5 天内释放药物。非聚乙二醇化制剂在 24 小时内释放药物。对含有胺和聚乙二醇化树枝状大分子的制剂进行了加速稳定性研究。含有胺树枝状大分子的制剂在黑暗、低温（0°C）下最稳定，而含有聚乙二醇化树枝状大分子的制剂在黑暗、RT 下最适合储存。
