Enhancing both oral bioavailability and anti-ischemic stroke efficacy of ginkgolide B by preparing nanocrystals self-stabilized Pickering nano-emulsion

Abstract

Ginkgolide B (GB), which has been demonstrated as the most efficacious naturally occurring platelet-activating factor (PAF) antagonist, is extensively utilized for the management of cardiovascular and cerebrovascular ailments. Nevertheless, its limited oral bioavailability is hindered by its low solubility in gastric acid and inadequate stability in intestinal fluid, thereby constraining its practical application. This study aimed to develop GB nanocrystals (GB-NCs) and GB nanocrystals self-stabilized Pickering nano-emulsion (GB-NSSPNE) using a miniaturized wet bead milling method. Comparative evaluations were conducted in vivo and in vitro to assess their effectiveness. The findings revealed that GB-NSSPNE, with its intact nanoparticle slow release and absorption, was more effective in enhancing the oral bioavailability of GB compared to the rapid release and absorption of GB-NCs. This finding suggests a potential novel strategy for the oral delivery of GB.