Self-microemulsifying drug delivery system for improving the bioavailability of huperzine A by lymphatic uptake.
10.1016/j.apsb.2017.02.002
- Author:
Fang LI
1
;
Rongfeng HU
1
;
Bin WANG
1
;
Yun GUI
1
;
Gang CHENG
1
;
Song GAO
1
;
Lei YE
1
;
Jihui TANG
2
Author Information
1. Anhui University of Chinese Medicine, Hefei 230038, China.
2. School of Pharmacy, Anhui Medical University, Hefei 230022, China.
- Publication Type:Journal Article
- Keywords:
Bioavailability;
Drug delivery systems;
Huperzine A;
Lymphatic transport;
SMEDDS;
Self-microemulsion;
Single-pass intestinal perfusion
- From:
Acta Pharmaceutica Sinica B
2017;7(3):353-360
- CountryChina
- Language:English
-
Abstract:
Huperzine A (Hup-A) is a poorly water-soluble drug with low oral bioavailability. A self-microemulsifying drug delivery system (SMEDDS) was used to enhance the oral bioavailability and lymphatic uptake and transport of Hup-A. A single-pass intestinal perfusion (SPIP) technique and a chylomicron flow-blocking approach were used to study its intestinal absorption, mesenteric lymph node distribution and intestinal lymphatic uptake. The value of the area under the plasma concentration-time curve (AUC) of Hup-A SMEDDS was significantly higher than that of a Hup-A suspension (<0.01). The absorption rate constant () and the apparent permeability coefficient () for Hup-A in different parts of the intestine suggested a passive transport mechanism, and the values ofandof Hup-A SMEDDS in the ileum were much higher than those in other intestinal segments. The determination of Hup-A concentration in mesenteric lymph nodes can be used to explain the intestinal lymphatic absorption of Hup-A SMEDDS. For Hup-A SMEDDS, the values of AUC and maximum plasma concentration () of the blocking model were significantly lower than those of the control model (<0.05). The proportion of lymphatic transport of Hup-A SMEDDS and Hup-A suspension were about 40% and 5%, respectively, suggesting that SMEDDS can significantly improve the intestinal lymphatic uptake and transport of Hup-A.
