Chemistry Division, Solid State Physics Division, Bhabha Atomic Research Centre, Mumbai-400 085, India.
J Phys Chem B. 2010 Dec 16;114(49):16414-21. doi: 10.1021/jp108225r. Epub 2010 Nov 16.
The objective of the present investigation is to develop and characterize anionic mixed micelles of two biocompatible surfactants, Tween 80 (T-80) and sodium deoxycholate (NaDC), and evaluate their potential in the delivery of doxorubicin hydrochloride (DOX), a cationic anticancer drug. The mixed micelles were characterized for their microstructure, intermicellar interactions, and doxorubicin binding ability by dynamic light scattering, small angle neutron scattering (SANS), viscosity, and optical absorption measurements. Salt-induced growth of the mixed micelles at different compositions suggests that both electrostatic interaction of the anionic bile salts and steric repulsion of the ethylene oxide groups in nonionic components are affected by the presence of electrolytes. Addition of bile salt molecules to T-80 micelles suppresses the salt-induced growth of nonionic T-80 micelles. SANS studies indicate that bile salt micelles are prolate ellipsoidal in shape, and the addition of T-80 transforms them toward a spherical shape. The anionic bile salt can successfully bind to the cationic drug doxorubicin. The in vitro cytotoxicity studies in various cancer cell lines revealed that DOX-loaded micelles have greater in vitro anticancer activity as compared to DOX solution, indicating their potential in pharmaceutical applications.
本研究旨在开发和表征两种生物相容性表面活性剂吐温 80（T-80）和脱氧胆酸钠（NaDC）的阴离子混合胶束，并评估其在盐酸阿霉素（DOX）作为阳离子抗癌药物传递中的潜在应用。通过动态光散射、小角中子散射（SANS）、粘度和光吸收测量，对混合胶束的微观结构、胶束间相互作用和阿霉素结合能力进行了表征。不同组成的混合胶束的盐诱导生长表明，阴离子胆汁盐的静电相互作用和非离子成分中氧化乙烯基团的空间排斥均受电解质存在的影响。向 T-80 胶束中添加胆汁盐分子抑制了非离子 T-80 胶束的盐诱导生长。SANS 研究表明，胆汁盐胶束呈扁长椭圆形，添加 T-80 后转变为球形。阴离子胆汁盐可以成功结合阳离子药物阿霉素。在各种癌细胞系中的体外细胞毒性研究表明，与 DOX 溶液相比，载 DOX 的胶束具有更高的体外抗癌活性，表明其在药物应用中的潜力。
