卡莫氟固体脂质纳米粒的制备及工艺研究

Preparation and Its Technology of Solid Lipid Nanoparticles of Carmofur

目的:制备卡莫氟固体脂质纳米粒并考察其药剂性质。方法:采用高压均质法制备卡莫氟固体脂质纳米粒混悬液,以单因素考察和正交设计法筛选处方和工艺,并考察其形态、粒径、载药量及包封率。结果:优选出的较佳处方大豆卵磷脂、泊洛沙姆188、吐温-80和硬脂酸用量分别为8.0、12.0、1.0、7.5mg·mL-1;所制得的固体脂质纳米粒为圆整的实体粒子,表面光滑,平均粒径为78.7nm,载药量为23.47%,包封率为82.33%。结论:高压均质法可用于卡莫氟类脂溶性药物固体脂质纳米粒的制备。

OBJECTIVE： To prepare solid lipid nanoparticles（SLNs） of carmofur and to study the pharmaceutical property of it. METHODS： The SLNs of carmofur were prepared by the high pressure homogenization method; the formula and technology were optimized by the single factor exploration and orthogonal design, and the shape, particle size, loading capacity, and the encapsulation efficiency were investigated. RESULTS： The optimized preparation conditions for SLNs of carmofur were as follows： the amount of soybean lecithin, poloxamer 188, tween - 80 and stearic acid were 8.0, 12.0, 1.0, and 7.5mg · mL^-1 respectively; and the obtained solid lipid nanoparticles were round, smooth solid particles with particle size of 78.7 nm, loading capacity of 23.47% and encapsulation efficiency of 82.33%. CONCLUSION： The high pressure homogenization method is applicable for the preparation of SLNs of lipid soluble carmofur.