醋酸地塞米松固体脂质纳米粒的制备与处方优化

Preparation and optimization of dexamethasone acetate solid lipid nanoparticles by orthogonal design

目的:制备醋酸地塞米松(dexamethasone acetate,DA)固体脂质纳米粒(solid lipid nanoparticles,SLN)并优化其处方组成。方法:采用乳化蒸发法制备醋酸地塞米松固体脂质纳米粒(DA-SLN)。以包封率、载药量及粒径为考察指标,运用正交试验设计优化处方。结果:DA-SLN的最优处方组成为A2B2C2D2,即药脂比1∶10,泊洛沙姆质量分数为2.0%,乳化温度为70℃,乳剂与分散相体积比为1∶6。优化处方的各指标值依次为粒径(180.8±3.3)nm,载药量(3.21±0.01)%,包封率(78.7±0.5)%。结论:乳化蒸发法适于制备DA-SLN,经优选后得到的处方合理、可行,可用于DA新型局部给药制剂的研究。

OBJECTIVE To prepare and optimize the composition of dexamethasone acetate solid lipid nanoparticles （DA- SLN）. METHODS Solvent emulsification/evaporation method was used to prepare dexamethasone acetate solid lipid nanoparticles. The best formulation of the solid lipid nanoparticles of dexamethasone acetate was optimized by orthogonal design, the entrapment efficiency, drug loading and diameter were taken as criteria. RESULTS The optimum formula of DA SLN was A2B2C2 （DA; Precirol ATO5 1 ：10; the concentration of Poloxamer was 2. 0%; the temperature of emulsification was 71℃; emulsion： dispersed part 1：6）. The mean diameter of the optimum formula was （180. 8 ±3.3）nm. the drug loading was （3. 21 ± 0. 01 ） % and the entrapment efficiency was （78.7± 0. 5） %. CONCLUSION .Solvent emulsification/evaporation method is suitable to prepare DA-SLN. The optimum formula of DA-SLN is reasonable and feasible in prescription. It may be used in a research about the novel topical preparation of DA.