Preparation and Quality Evaluation of Chloramphenicol Solid Lipid Nanoparticles

OBJECTIVE:To prepare Chloramphenicol solid lipid nanoparticles(CAP-SLN) and to study the quality of it.METHODS:The preparation technilogy of CAP-SLN was optimized by orthogonal test with the entrapment efficiency and drug loading amount as index and with proportion of CAP to Precirol ATO 5(drug-to-lipid ratio),amount of poloxamer,emulsifying temperature,volume ratio of emulsion-disperse phase as factors.CAP-SLN was prepared by emulsification evaporation-low temperature solidification technique.The quality of preparation was evaluated with particle size,Zeta potential,drug-loading amount,stability and in vitro drug release rate as index.RESULTS:The optimal formulation was as follows:drug-to-lipid ratio of 1:10,the weight of poloxamer of 2%,emulsifying temperature of 70 ℃,drug-to-lipid of 1:7.The mean diameter of CAP-SLN was 227 nm.The zeta potential was-30.5 mV.The entrapment efficacy was 65.9%.The average drug-loading amount was 6.59%.CAP-SLN could keep stable at 4 ℃ at least for one month.The entrapment efficacy of CAP-SLN at 25 ℃ decreased significantly while particle size increased.The burst release of CAP-SLN was found during the former 4 h.The drug release rate of it was 58.86% at 4 h and reached 85.09% at 48 h.The in vitro drug release behavior was in line with Weibull equation.CONCLUSION:The preparation technique and formulation are practicable.CAP-SLN is up to quality standard and can achieve sustained-release effects.