Enhancement of oral bioavailability of tripterine through lipid nanospheres: preparation, characterization, and absorption evaluation.
Oral delivery of anticancer drugs remains challenging because of limited water-solubility and/or poor permeability. Here, we aimed to enhance the oral bioavailability of tripterine (TRI, a plant-derived anticancer compound) using lipid nanospheres (LNs) and to determine the mechanisms of oral absorption. TRI-loaded LNs (TRI-LNs) were prepared by rapid dispersion of an ethanol mixture of TRI, lecithin, sodium oleate, and soybean oil into water. The obtained LNs were 150 nm in size with a high value of entrapment efficiency (99.95%). TRI-LNs were fairly stable and the drug release was negligible (<0.2%) in simulated physiological fluid. The pharmacokinetic results showed that LNs significantly enhanced the oral bioavailability of TRI with a relative bioavailability of 224.88% (TRI suspensions was used as a reference). The mechanistic studies demonstrated that improved intestinal permeability and post-enterocyte lymphatic transport were mainly responsible for the enhanced oral absorption. Our findings suggested that LNs may be a viable oral carrier for poorly bioavailable drugs.
College of Pharmacy, Jinan University, Guangzhou, China.
Xingwang
X
Zhang
Tianpeng
T
Zhang
Xiaotong
X
Zhou
Hongming
H
Liu
Hua
H
Sun
Zhiguo
Z
Ma
Baojian
B
Wu
D000284:Administration, Oral; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D002851:Chromatography, High Pressure Liquid; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles; D053978:Pentacyclic Triterpenes; D017550:Spectroscopy, Fourier Transform Infrared; D014315:Triterpenes / Q000493:pharmacokinetics*
D008055:Lipids; D053978:Pentacyclic Triterpenes; D014315:Triterpenes; C050414:celastrol
absorption potential; bioavailability; lipids; nanospheres; oral drug delivery; permeability; tripterine