Objective: To construct baicalin chitosan microparticles and compare the in vitro transdermal diffusion of baicalin in microparticles and cream.
Methods: Baicalin chitosan microparticles were constructed by using neutralization method and optimized by orthogonal test; The in vitro transdermal diffusion of baicalin in microparticles and cream was compared by using Franz cell.
Results: When the drug:stuff ratio was 1:3, concentration of chitosan was 2 mg/mL, mixed duration was 10 min, both the entrapment efficiency and drug loading efficiency of baicalin chitosan microparticles were over 60%; After 36 h, the cumulative release percentage of baicalin in microparticles and cream in vitro transdermal diffusion was 4.04% and 30%, respectively. The content of drug in microparticles and cream in the skin was 0.11% and 0.14%, respectively. And there was no significant difference (w = 7, P = 0.127) between the content of drug in microparticles and cream in the skin.
Conclusion: The optimal procedure is simple and convenient with high entrapment efficiency and drug loading efficiency. The drug in the microparticles could be released slower and form local drug reservoir in the skin.