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1.
Acta Pharmaceutica Sinica ; (12): 920-925, 2010.
Article in Chinese | WPRIM | ID: wpr-354553

ABSTRACT

To prepare polyrotaxane-camptothecin conjugates and evaluate its anti-tumor effect, polyrotaxane-camptothecin conjugates were successfully synthesized, and the release behavior was performed; MTT assay and cell morphology were used to examine the inhibition of cells' proliferation effect in vitro. The experimental study of the antitumor effect on S180 mice in vivo was also performed to further evaluate the anti-tumor effect of conjugate. The result showed polyrotaxane-camptothecin conjugates can effectively inhibit the proliferation in a dose dependent effect. In vivo study and cell morphology observation of S180 mice showed significant decrease in growth of tumor, degree of tumor infiltration and blood vessel number. The result indicated anti-tumor mechanism may be through affect the angiogenesis and reduced blood supply to tumor cells and then leading to necrosis.


Subject(s)
Animals , Female , Humans , Male , Mice , Antineoplastic Agents, Phytogenic , Pharmacology , Camptothecin , Pharmacology , Cell Line, Tumor , Cell Proliferation , Cyclodextrins , Chemistry , Drug Carriers , Drug Compounding , Mice, Inbred BALB C , Neoplasm Transplantation , Ovarian Neoplasms , Pathology , Poloxamer , Chemistry , Rotaxanes , Chemistry , Sarcoma 180 , Pathology , Tumor Burden
2.
Acta Pharmaceutica Sinica ; (12): 920-5, 2010.
Article in Chinese | WPRIM | ID: wpr-382465

ABSTRACT

To prepare polyrotaxane-camptothecin conjugates and evaluate its anti-tumor effect, polyrotaxane-camptothecin conjugates were successfully synthesized, and the release behavior was performed; MTT assay and cell morphology were used to examine the inhibition of cells' proliferation effect in vitro. The experimental study of the antitumor effect on S180 mice in vivo was also performed to further evaluate the anti-tumor effect of conjugate. The result showed polyrotaxane-camptothecin conjugates can effectively inhibit the proliferation in a dose dependent effect. In vivo study and cell morphology observation of S180 mice showed significant decrease in growth of tumor, degree of tumor infiltration and blood vessel number. The result indicated anti-tumor mechanism may be through affect the angiogenesis and reduced blood supply to tumor cells and then leading to necrosis.

3.
Acta Pharmaceutica Sinica ; (12): 803-808, 2009.
Article in Chinese | WPRIM | ID: wpr-344102

ABSTRACT

To prepare the oral self-microemulsifying drug delivery system (SMEDDS) of GBE50, balance solubility method was used to screen emulsifier and assistant emulsifier; a pseudo-tamary phase diagram was used to prepare microemulsion; and orthogonal design was used to optimize formulation. Self-microemulsifying efficiency, dissolution, stability and pharmacokinetics of the preparation were studied. As a result, GBE50-SMEDDS of IPM, Cremophor EL, 1,2-propanediol and GBE50 could be self emulsified to form stable microemulsion with particle diameter between 20 and 50 nm when emulsifying with water. Its self-microemulsifying efficiency and dissolution are quick with good stability and it has a higher bioavailability than market existing agents Xingling particles. GBE50-SMEDDS is stable and effective.


Subject(s)
Biological Availability , Drug Delivery Systems , Methods , Drugs, Chinese Herbal , Pharmacokinetics , Ginkgolides , Pharmacokinetics , Technology, Pharmaceutical , Methods
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