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The efficacy of an oral-targeted drug delivery system (OTDDS) of oxymatrine (OMT) in UC treatment was investigated. Nanoparticles (OMT/SA-NPs) were prepared using OMT, pectin, Ca²⁺, chitosan (CS), and sialic acid (SA). The average particle size of OMT/SA-NPs was found to be 255.0 nm with a zeta potential value of −12.4 mV. The drug loading capacity and encapsulation efficiency were high at 14.65% and 84.83%, respectively. OMT/SA-NPs remained stable throughout the GIT and successfully targeted the delivery of OMT to the colon. OMT/SA-NPs showed excellent biocompatibility, anti-inflammatory activity, and dose- and time-dependent uptake by RAW 264.7 cells through SA-mediated endocytosisin vitro. OMT/SA-NPs also exhibited stronger anti-inflammatory and anti-colitis efficacy in vivo compared to free OMT due to (1) effective delivery of the drug to the colon and (2) site-specific targeting/internalization and prolonged retention mediated by SA (3) anti-inflammatory activity of both OMT and nanoparticles.
Fig. 2 Schematic illustration of using OMT/SA-NPs in the treatment of UC in mice. (Zhao C, et al. 2024)
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