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1.
Acta Pharmaceutica Sinica ; (12): 970-975, 2005.
Article in Chinese | WPRIM | ID: wpr-253510

ABSTRACT

<p><b>AIM</b>To study the release and cell uptake characteristics of 9-nitrocamptothecin (9-NC) nanostructured lipid carrier system (NLC) in vitro and its tissue distribution characteristics in vivo.</p><p><b>METHODS</b>Mouse peritoneal macrophages were used to investigate the uptake of nanoparticles by cells in vitro. The tissue distribution of 9-nitrocamptothecin solution and stealth nanostructured lipid carrier system (S-NLC) was determined after intravenous administration to mice at a single dose of 1.5 mg kg(-1). The release and crystalloid characteristics were also investigated.</p><p><b>RESULTS</b>X-ray diffraction spectrum showed that 9-NC probably was amorphous in S-NLC. The liquid lipid did not change the characteristics of the solid matrix in nanoparticles. The in vitro release and cell uptake characteristics of stealth and non-stealth 9-NC-NLC were investigated, separately. The results showed that the stealth 9-NC-NLC had sustained-release characteristics and could resist the absorption effect of the additional plasmas to a certain extent. In addition, the cell uptake percentage of stealth 9-NC-NLC was much lower than that of the non-stealth ones. The tissues distribution results showed that 9-NC in the S-NLC was mainly found in the lung, liver, pancreas and ovary/uterus, while the quantity of 9-NC was much lower in heart and kidney. The AUQ(0-t), of S-NLC in blood, ovary/uterus, pancreas, liver and lung were higher than that of 9-nitrocamptothecin solution. The weight-average drug targeting efficiency (Te*) of S-NLC in liver and lung were significantly higher than that of 9-nitrocamptothecin solution. The mean residence times (MRT) of S-NLC was 44 h, while that of 9-nitrocamptothecin solution was 8 h. Therefore, S-NLC showed obvious targeting effects on liver and lung.</p><p><b>CONCLUSION</b>S-NLC with PEG flexible chains has sustained-release characteristics and can prolong its circulation in blood and have good targeting efficiency on liver and lung.</p>


Subject(s)
Animals , Female , Mice , Antineoplastic Agents , Chemistry , Pharmacokinetics , Camptothecin , Chemistry , Pharmacokinetics , Delayed-Action Preparations , Drug Carriers , Drug Delivery Systems , Hexoses , Chemistry , Liver , Metabolism , Lung , Metabolism , Macrophages, Peritoneal , Physiology , Nanoparticles , Particle Size , Phagocytosis , Phosphatidylcholines , Chemistry , Polyethylene Glycols , Chemistry , Tissue Distribution
2.
Acta Pharmaceutica Sinica ; (12): 859-862, 2003.
Article in Chinese | WPRIM | ID: wpr-266567

ABSTRACT

<p><b>AIM</b>To develop high bioavailability preparations without irritation for Panax notoginsenosides.</p><p><b>METHODS</b>The effects of some additives such as microcrystalline cellulose, beta-cyclodextrin and hydroxypropyl cellulose on drug in the preparations were examined.</p><p><b>RESULTS</b>Saponins of Panax notoginseng (PNS) was absorbed in rabbits more when administered intranasally than through other routines, and the formulations including MCC both gave high bioavailability and low irritation.</p><p><b>CONCLUSION</b>Bioavailability of Panax notoginsenosides can be increased through changing routine of administration and formulations.</p>


Subject(s)
Animals , Female , Male , Rabbits , Rats , Administration, Intranasal , Biological Availability , Bufo bufo , Cellulose , Toxicity , Cyclodextrins , Drug Carriers , Drug Delivery Systems , Ginsenosides , Pharmacokinetics , Nasal Mucosa , Metabolism , Panax , Chemistry , Permeability , beta-Cyclodextrins
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