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载有阿霉素的固体脂质纳米粒的制备与表征

Preparation and characterization of solid lipid nanoparticles loaded with doxorubicin.

作者信息

Subedi Robhash Kusam, Kang Keon Wook, Choi Hoo-Kyun

机构信息

BK21 Project Team, College of Pharmacy, Chosun University, 375 Seosuk-dong, Dong-gu, Gwangju 501-759, South Korea.

出版信息

Eur J Pharm Sci. 2009 Jun 28;37(3-4):508-13. doi: 10.1016/j.ejps.2009.04.008. Epub 2009 May 3.

Abstract

Solid lipid nanoparticles (SLN) loaded with doxorubicin were prepared by solvent emulsification-diffusion method. Glyceryl caprate (Capmul)MCM C10) was used as lipid core, and curdlan as the shell material. Dimethyl sulfoxide (DMSO) was used to dissolve both lipid and drug. Polyethylene glycol 660 hydroxystearate (Solutol)HS15) was employed as surfactant. Major formulation parameters were optimized to obtain high quality nanoparticles. The mean particle size measured by photon correlation spectroscopy (PCS) was 199nm. The entrapment efficiency (EE) and drug loading capacity (DL), determined with fluorescence spectroscopy, were 67.5+/-2.4% and 2.8+/-0.1%, respectively. The drug release behavior was studied by in vitro method. Cell viability assay showed that properties of SLN remain unchanged during the process of freeze-drying. Stability study revealed that lyophilized SLN were equally effective (p<0.05) after 1 year of storage at 4 degrees C. In conclusion, SLN with small particle size, high EE, and relatively high DL for doxorubicin can be obtained by this method.

摘要

采用溶剂乳化扩散法制备了载有多柔比星的固体脂质纳米粒(SLN)。癸酸甘油酯(Capmul MCM C10)用作脂质核心,可得然胶用作壳材料。二甲基亚砜(DMSO)用于溶解脂质和药物。聚乙二醇660羟基硬脂酸酯(Solutol HS15)用作表面活性剂。对主要配方参数进行了优化以获得高质量的纳米粒。通过光子相关光谱法(PCS)测得的平均粒径为199nm。用荧光光谱法测定的包封率(EE)和载药量(DL)分别为67.5±2.4%和2.8±0.1%。采用体外方法研究了药物释放行为。细胞活力测定表明,SLN的性质在冻干过程中保持不变。稳定性研究表明,冻干的SLN在4℃储存1年后同样有效(p<0.05)。总之,通过该方法可获得粒径小、EE高且对多柔比星载药量相对较高的SLN。

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