ABSTRACT
<p><b>OBJECTIVE</b>To 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.</p><p><b>METHOD</b>BCA 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.</p><p><b>RESULT</b>D50 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.</p><p><b>CONCLUSION</b>The 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.</p>
Subject(s)
Animals , Mice , Rabbits , Antineoplastic Agents, Phytogenic , Pharmacokinetics , Cucurbitaceae , Chemistry , Delayed-Action Preparations , Drug Compounding , Methods , Drug Delivery Systems , Drugs, Chinese Herbal , Pharmacokinetics , Excipients , Liver , Metabolism , Nanostructures , Particle Size , Plants, Medicinal , Chemistry , Rhizome , Chemistry , Tissue DistributionABSTRACT
<p><b>OBJECTIVE</b>To select the best preparation method of vincristine transfersomes (VCR-T) and predict its possibility of being a new formulation of VCR.</p><p><b>METHOD</b>Orthogonal design was used to optimize the preparation methods on the basis of single factor pretests; and the permeation tests in vitro were performed in modified Franz diffusion cells.</p><p><b>RESULT</b>The optimum formula was: pH was equal to 7.3, the ratio of lecithin to sodium deoxycholate is 70/20, the weight of VCR is 10 mg, hydrating time is 30 minutes. The optimized solution was light yellow and transparent colloid solution. The VCR-T are spherical and smooth with average diameters of 94 nm and an encapsulation ratio of 90%. The test in vitro showed that VCR-T could permeat through mouse skin at zero rate with the cumulative penetrating quality amounting to 63.8%.</p><p><b>CONCLUSION</b>Transfersomes may become a promising carrier of VCR for clinic use.</p>