| Literature DB >> 22796159 |
Xinxin Zhang1, Shiyan Guo, Rong Fan, Miaorong Yu, Feifei Li, Chunliu Zhu, Yong Gan.
Abstract
The purpose of this study was to design and evaluate the dual-functional liposome (LPG) with synthetic polymeric nano-biomaterial (Gal-P123) that targets cancer cells and reverses multidrug resistance (MDR) in hepatocellular carcinoma (HCC) cells. The mitoxantrone (MX) loaded LPG (MX-LPG) was about 100 nm in diameter, spherically shaped, and had an encapsulation efficiency of 97.3%. The cytotoxicity and cellular uptake of MX-LPG were evaluated in HCC Huh-7 cells. BCRP-overexpressing MDCKII/BCRP cells were used to certify the inhibitory effect of LPG on drug efflux transporter. Compared with MX, MX-LPG had 2.3-fold higher cytotoxicity in Huh-7 cells and a 14.9-fold increase in cellular MX accumulation in MDCKII/BCRP cells. The pharmacokinetic study in rats showed that LPG significantly prolonged the circulation time and enhanced the bioavailability of MX. Moreover, MX-LPG increased antitumor activity and improved selectivity in BALB/c mice bearing orthotopic xenograft HCC tumors.Entities:
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Year: 2012 PMID： 22796159 DOI： 10.1016/j.biomaterials.2012.06.048
Source DB: PubMed Journal: Biomaterials ISSN： 0142-9612 Impact factor: 12.479