In vitro release and in situ gastrointestinal absorption of evodiamine butyryl derivative-loaded solid lipid nanoparticles
10.3969/j.issn.1001-1978.2018.05.026
- VernacularTitle:吴茱萸碱丁酰基衍生物固体脂质纳米粒的体外释放及在体胃肠吸收研究
- Author:
Lan YANG
1
;
Kun WAN
;
Jian-Bo YANG
;
Sheng-Lei YAN
;
Qi-Rao ZHANG
;
Jing-Qing ZHANG
;
Xue-Yuan HU
Author Information
1. 重庆医科大学药学院重庆高校药物工程研究中心
- Keywords:
evodiamine;
evodiamine butyryl deriva-tive;
solid lipid nanoparticles;
in vitro release;
in situ gastrointestinal absorption;
absorption rate constant;
apparent permeability coefficient
- From:
Chinese Pharmacological Bulletin
2018;34(5):724-728
- CountryChina
- Language:Chinese
-
Abstract:
Aim To prepare evodiamine butyryl deriva-tive (EBD) and evodiamine butyryl derivative-loaded solid lipid nanoparticles (EBDLN), and study its re-lease in vitro,and to investigate its in situ gastrointesti-nal absorption. Methods EBD was prepared by a one-step synthetized method, and then EBDLN was prepared by a film dispersion method. Dynamic dialy-sis was used to evaluate drug release in vitro,and sin-gle-pass gastrointestinal perfusion was employed to study the gastrointestinal absorption of EDM,EBD and EBDLN. Results In identical release media, there were identical drug release tendencies of EBD and EB-DLN, but the release rate of EBDLN was faster than EBD. Compared with EDM and EBD, the Kavalues and Pappvalues of EBDLN in every perfusion segment increased significantly. The Kaof EBDLN in stomach, duodenum, jejunum, ileum and colon was 110.14-fold,56.70-fold,51.23-fold,45.70-fold and 127.23-fold of free EDM respectively. The Pappvalue of EB-DLN was 9.74-fold, 4.48-fold, 3.82-fold and 11.3-fold of that of free EDM. Conclusion EBDLN has sustained effect and can enhance the gastrointestinal absorption of EDM and EBD.
