ABSTRACT
Aim To investigate the in vitro release be-havior of chitosan coated curcumin liposomes ( CMLP-CS ) and its pharmacokinetic characteristics in rats. Methods The cumulative release rate of CMLP-CS in pH 1. 2 hydrochloric acid solution and pH 6. 8 phos-phate buffer solution was investigated by dynamic dial-ysis method. The in vitro release curve was drawn. The release behavior was evaluated by similarity factor method. The drug concentration in blood was deter-mined by high performance liquid chromatography ( HPLC) . The pharmacokinetic data were analyzed by DAS 2.1.1 software. Results The cumulative release rate of CMLP-CS in pH 1. 2 hydrochloric acid solution and pH 6. 8 phosphate buffer solution was ( 70.48 ±0.50)％, (72.35 ± 1.04)％, respectively, and CM-LP-CS release in two release media was similar. AUC (0～72 h) , MRT (0～72 h) and Cmax were calculated to be 8.9, 3.7 and 1. 5 times of free curcumin, re-spectively. The relative bioavailability of CMLP-CS was 846. 5％. Conclusion CMLP-CS can improve the in vitro release behavior and significantly enhance the fraction of bioavailability of curcumin in rats.
ABSTRACT
Objective To investigate the in vivo pharmacokinetic characteristics of evodiamine-curcumin nanoparticles (ECNP), and to discuss the influence of curcumin (CUR) to the bioavailability of evodiamine (EVO). Methods ECNP were prepared by solvent evaporation method. Rats were orally given ECNP. After administration, blood samples were collected from the retinal venous plexus of SD rats at different time points. And the blood concentration of EVO was determined by HPLC. Results The AUC0-t of ECNP, mixture of evodiamine and curcumin (MEC) and free EVO were (3 197.74 ± 81.64) μg∙h/L, (1 387.73 ± 39.42) μg∙h/L, and (928.08 ± 54.84) μg∙h/L, respectively. The AUC0-t of MEC was 1.50 times as free EVO. The AUC0-t of ECNP was 3.45 and 2.30 times as EVO and MEC, respectively. Conclusion The absorption of EVO in rats was promoted with CUR, and nanoparticles can further improve the oral bioavailability of EVO in rats.