In vitro intestinal membrane permeation enhancement of Thai anti-cancer recipe aqueous extracts loaded in thiolated-chitosan nanoparticles

Abstract

Chitosan and thiolated-chitosan nanoparticles loaded with the four aqueous extracts of anti-cancer Thai medicinal plant recipes were prepared by ionic interaction with tripolyphosphate (TPP) solution. The averages sizes, zeta-potentials and PDI of the chitosan and thiolated-chitosan nanoparticles loaded with the aqueous extracts were in range of 273.1±57.0 to 323±39.3 nm, +2.37±0.37 to +6.40±0.63 mV and 0.332 to 0.440; and 205.1±39.2 to 305.8±75.8 nm, +2.43±0.52 to +3.99±0.22 mV and 0.241 to 0.389, respectively, whereas 244.8±48.1 nm, +3.56±0.71 mV and 0.350; and 174.2±23.2 nm, +3.22±0.85 mV and 0.207 were observed in blank chitosan and thiolated-chitosan nanoparticles, respectively. The in vitro kinetic release and the intestinal membrane permeation by Ussing type chamber across the freshly excised rat intestinal mucosa of the markers (quinazoline and tryptamine) containing in the recipe extracts through the rat intestinal membrane were similar with the blank markers fitted to the zero order plot, and those loaded in the chitosan and thiolated-chitosan nanoparticles fitted to the Higuchi's equation. The thiolated-chitosan nanoparticles significantly improved the permeation of quinazoline and tryptamine with the highest transport enhancement ratio (R) of 4.13, and 4.11 (p <0.05) respectively. Thiolation significantly enhanced the permeation of the chitosan nanoparticles with the highest R of 1.44 for quinazoline, and 1.49 for tryptamine (p < 0.05). The permeation enhancing effect of the thiolated-chitosan was due to the increase of the drug release, which may be from the transient effect of chitosan on the paracellular transport processes by opening the tight-junctions. © 2012 American Scientific Publishers. All rights reserved.