2010磷脂纳米粒-口服-5.4.pdf

articles Mechanisms of Phospholipid Complex Loaded Nanoparticles Enhancing the Oral Bioavailability Qiang Peng, Zhi-Rong Zhang, Xun Sun, Jiao Zuo, Dong Zhao, and Tao Gong* Key Laboratory of Drug Targeting and Drug DeliVery Systems, Ministry of Education, West China School of Pharmacy, Sichuan UniVersity, Southern Renmin Road, No. 17, Section 3, Chengdu 610041, P. R. China Received November 5, 2009; Revised Manuscript Received January 19, 2010; Accepted February 18, 2010 Abstract: The purpose of the present study was to study the mechanisms of salvianolic acid B phospholipid complex loaded nanoparticles (SalB-PLC-NPs) enhancing the oral bioavailability of SalB by in situ perfusion model in rats and to evaluate the potential of phospholipid complex loaded nanoparticles (PLC-NPs) serving as an efficient oral delivery system to enhance the bioavailability of highly water-soluble drugs. SalB-PLC-NPs, prepared by a solvent evaporation method, exhibited a spherical shape with a mean particle size and a zeta potential of 112.2 nm and -44.2 mV, respectively. The drug entrapment efficiency and drug loading were 86.19% and 3.21%, respectively. The lyophilized SalB-PLC-NPs, prepared with 10% maltose as the cryoprotectant, presented sustained release profiles in artificial gastric juice (0.1 M HCl with pH 1.2) and intestinal juice (PBS with pH 6.8 and 7.4). The absorption mechanisms were