1.Study on liver targeted drug delivery system of the effective anticancer component from Bolbstemma paniculatum.
Yi-Yi SUN ; Tong-Hui LL ; Chen-Kang TANG ; Zi-Ping ZHU ; Qun CHI ; Shi-Xiang HOU
China Journal of Chinese Materia Medica 2005;30(11):817-821
OBJECTIVETo study the liver targeted drug delivery system of TBMS--the effective anticancer component from Bolbstemma paniculatum, and to discuss the system's function of decreasing toxicity.
METHODBCA was used as carrier material. The preparation through overall feedback dynamic techniques. The properties of preparation and toxicology were also technology of nanoparticles was optimized studied. Thenanoparticles' targeting in mice vivo was observed with transmission electron microscopy. The function of decreasing toxicity was researched by the XXTX-2000 automatic quantitative analysis management system.
RESULTD50 was 0.68 microm. Drug-loading rate and entrapment rate were 37.3% and 88.6% respectively. The release in vitro accorded with Weibull equation. The reaching release balance time and the t 1/2 extended 26 times and 19 times respectively comparing with injection. Nanoparticles mainly distributed in liver tissue. Their toxicity to lung and liver was evidently lower than injection. Nanoparticles' LD50 exceeded injection's by 13.5% and their stimulus was much lower than injection.
CONCLUSIONThe TBMS can be targeted to liver by liver targeted drug delivery system. At the same time, the problem about the toxicity hindering clinical application could be solved, which lays the foundation for the further studies on TBMS.
Animals ; Antineoplastic Agents, Phytogenic ; administration & dosage ; pharmacokinetics ; Cucurbitaceae ; chemistry ; Delayed-Action Preparations ; Drug Compounding ; methods ; Drug Delivery Systems ; Drugs, Chinese Herbal ; administration & dosage ; pharmacokinetics ; Excipients ; Liver ; metabolism ; Mice ; Nanostructures ; Particle Size ; Plants, Medicinal ; chemistry ; Rabbits ; Rhizome ; chemistry ; Tissue Distribution