School of Pharmacy, Yantai University, Yantai, Shandong, PR China.
Drug Dev Ind Pharm. 2010 Sep;36(9):1027-35. doi: 10.3109/03639041003610799.
The aim of this study was to prepare and characterize the complex of puerarin and poly(amidoamine) (PAMAM) dendrimers and to evaluate the complex as an ocular drug delivery system.
The complexes of puerarin and PAMAM dendrimers were prepared at various puerarin-to-dendrimer ratios. The physicochemical properties of the complexes were characterized by differential scanning calorimetry and Fourier transform infrared spectroscopy. The in vitro release studies were performed by dialysis. Corneal permeation was evaluated by Valia-Chien diffusion cell with excised corneas and ocular residence time in rabbits.
The results showed that puerarin-dendrimer complexes formed primarily by hydrogen-bonding interactions. Typically, 43, 56, 125, and 170 molecules of puerarin could be incorporated into G3.5, G4, G4.5, and G5 PAMAM dendrimer molecule. Puerarin was released more slowly from puerarin-dendrimer complexes than free puerarin in deionized water and phosphate buffer solution (pH 6.8). The in vitro release rate of puerarin complexed with full generation dendrimers was lower than that with half generation dendrimers. Furthermore, puerarin-dendrimer complexes produced longer ocular residence times in rabbits compared with puerarin eye drops. No damages to the epithelium or endothelium were observed after the PAMAM dendrimer administration in this corneal permeation study.
Puerarin-dendrimer complexes represent a potential ocular drug delivery system to improve the efficacy of drug treatment.
本研究旨在制备葛根素与聚酰胺-胺（PAMAM）树枝状聚合物复合物，并评价其作为眼部药物传递系统的性能。
在不同的葛根素与树枝状聚合物比例下制备葛根素与 PAMAM 树枝状聚合物的复合物。通过差示扫描量热法和傅里叶变换红外光谱对复合物的理化性质进行表征。通过透析法进行体外释放研究。采用离体角膜瓦利亚-钱氏扩散池评价角膜渗透，并用兔眼停留时间进行评价。
结果表明，葛根素-树枝状聚合物复合物主要通过氢键相互作用形成。通常，43、56、125 和 170 个葛根素分子可以分别结合到 G3.5、G4、G4.5 和 G5 PAMAM 树枝状聚合物分子上。在去离子水和磷酸盐缓冲溶液（pH 6.8）中，葛根素从葛根素-树枝状聚合物复合物中的释放速度比游离葛根素慢。与半代树枝状聚合物相比，全代树枝状聚合物结合的葛根素复合物的体外释放速度更低。此外，与葛根素滴眼液相比，葛根素-树枝状聚合物复合物在兔眼内停留时间更长。在这项角膜渗透研究中，给予 PAMAM 树枝状聚合物后，上皮或内皮没有受到损伤。
葛根素-树枝状聚合物复合物是一种有潜力的眼部药物传递系统，可提高药物治疗效果。
