Preparation and characterization of intravenously injectable curcumin nanosuspension

被引:94
作者
Gao, Yan [1 ]
Li, Zhonggang [2 ]
Sun, Min [1 ]
Guo, Chenyu [1 ]
Yu, Aihua [1 ]
Xi, Yanwei [1 ]
Cui, Jing [3 ]
Lou, Hongxiang [4 ]
Zhai, Guangxi [1 ]
机构
[1] Shandong Univ, Coll Pharm, Dept Pharmaceut, Jinan 250012, Peoples R China
[2] Shandong Univ, Ctr New Drugs Evaluat, Jinan 250012, Peoples R China
[3] Shandong Univ, Qilu Hosp, Dept Pharm, Jinan 250012, Peoples R China
[4] Shandong Univ, Coll Pharm, Dept Nat Prod Chem, Jinan 250012, Peoples R China
关键词
Curcumin; nanosuspension; high pressure homogenization; cytotoxicity; vascular irritation; SOLID LIPID NANOPARTICLES; I CLINICAL-TRIAL; ORAL CURCUMIN; SOLUBLE DRUGS; PHARMACOKINETICS; FORMULATION; BIOAVAILABILITY; PARTICULATE; AGENTS; MODEL;
D O I
10.3109/10717544.2010.520353
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The interest in nanosuspensions by the pharmaceutical industry is increasing given several nanosuspension products currently on the market for poorly soluble drugs. In this study, a novel dosage form for curcumin (CUR), CUR nanosuspension (CUR-NS), was successfully prepared by high pressure homogenization to improve CUR's cytotoxicity, as well as improve its application via intravenous injection. Characterization of the CUR-NS was evaluated by morphology, size, zeta potential, solubility, dissolution rate, and crystal state of drug. The nanoparticles for CUR-NS presented a sphere-like shape under transmission electron microscopy with an average diameter of 250.6 nm and the zeta potential of CUR-NS was -27.92 mV. Solubility and dissolution rate of CUR in the form of CUR-NS were significantly increased due to the small particle size and the crystalline state of CUR was preserved to increase its stability against degradation. Superior cytotoxicity in Hela and MCF-7 cells was obtained for CUR-NS compared with CUR solution. The safety evaluation showed that, compared with the CUR solution, CUR-NS provided less local irritation and phlebitis risks, lower rate of erythrocyte hemolysis. These findings suggest that CUR-NS may represent a promising new drug formulation for intravenous administration in the treatment of certain cancers.</.
引用
收藏
页码:131 / 142
页数:12
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