CA4固体脂质纳米粒的制备及体外释药特性的考察

Preparation and in vitro release of CA4-loaded solid lipid nanoparticles

目的制备CA4固体脂质纳米粒(CA4-SLNs),并考察其理化性质及体外释药特性。方法通过乳化蒸发-低温固化法制备CA4-SLNs,用透射电镜观察形态,激光粒度仪测定粒径和ξ电位,HPLC法测定包封率与载药量,透析法考察其体外释药特性。结果 CA4-SLNs在透射电镜下呈球形或类球形,分布均匀,平均粒径为73.23nm,PDI为0.238,Zeta电位为-30.5mV;测得3批CA4-SLNs样品的平均包封率为98.62%,载药量为3.89%;体外释药符合Weibull模型:lnln[1/(1-Q)]=0.6123lnt-0.736(r=0.9917)。结论乳化蒸发-低温固化法适用于CA4-SLNs的制备,所制纳米粒的包封率较高,释药初期稍有突释,后即出现缓释。

OBJECTIVE To prepare the CA4-loaded solid lipid nanoparticles（CA4-SLNs） and investigate its physicochemical properties and in vitro release profile.METHODS CA4-SLNs were prepared by the method of emulsification evaporation-solidification at low temperature.The morphology was examined by transmission electron microscope.The particle size and ξ potential were determined by laser granularity equipment.The unencapsulated CA4 and solid lipid nanoparticles were separated by centrifugation and the encapsulation efficiency and drug-loading efficiency were detected by HPLC.The in vitro release profile of CA4-SLNs was studied using dialysis technology.RESULTS The obtained SLNs were spherical.The mean particle size was 73.23 nm.The PDI was 0.238,and the ξ potential was-30.5 mV.The average encapsulation efficiency and drug loading of the optimized SLN were 98.62% and 3.89%.The release in vitro accorded to the Weibull order model：lnln[1 /（1-Q）]= 0.6123lnt-0.736（r = 0.9917）.CONCLUSION The method of emulsification-evaporation was appropriate for the preparation of CA4-loaded solid lipid nanoparticles and the drug encapsulation efficiency was high.The in vitro release test showed that the drug could sustained-release from SLN after a burst release in initial phase.