Influence of Chitosan Nanoparticles as the Absorption Enhancers on Salvianolic acid B In vitro and In vivo Evaluation.

BACKGROUND: Salvianolic acid B (SalB) represents the most abundant and bio-active phenolic constituent among the water-soluble compounds of Salvia miltiorrhiza. But the therapeutic potential of SalB has been significantly restricted by its poor absorption.

METHODS: In this study, chitosans (CS) and CS nanoparticles (NPs) with different molecular weights (MWs), which have influence on the absorption of SalB, was also investigated.

RESULTS: As a preliminary study, water-soluble CS with various MWs (3, 30, 50, and 100 kDa) was chosen. We investigated the MW-dependent Caco-2 cell layer transport phenomena in vitro of CS and NPs at concentrations (4 μg/ml, w/v). SalB, in presence CS or NPs has no significant toxic effect on Caco-2 cell. As the MW increases, the absorption enhancing effect of CS increases. However, as the MW decreases, the absorption enhancing effect of NPs increases. The AUC0-∞ of the SalB-100 kDa CS was 4.25 times greater than that of free SalB. And the AUC0-∞ of the SalB-3 kDa NPs was 16.03 times greater than that of free SalB.

CONCLUSION: CS and NPs with different MWs as the absorption enhancers can promote the absorption of SalB. And the effect on NPs is better than CS.

SUMMARY: Formation mechanism for NPs.