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Abstract
Oral colon-specific drug delivery is of great interest for ulcerative colitis (UC)
therapy. Here, an emulsion-solvent evaporation method was used to fabricate microparticles
(MPs) with pH-sensitive Eudragit S100 (ERS100) and poly(lactide-co-glycolide) (PLGA),
and the MPs were loaded with curcumin (an efficient anti-inflammatory agent). The
resultant spherical MPs had a desirable particle size ranging from 1.52 to 1.91 μm.
Their loading efficiency could be regulated by changing the weight ratios of ERS100
and PLGA, with some MPs exhibiting loading efficiencies over 80%. It was observed
that the fast release of curcumin from MPs in buffers (pH 1.2 and 6.8) could be significantly
decreased by increasing the PLGA content. ERS100/PLGA MPs with a weight ratio of 1:2
(MPs-4) were able to maintain sustained release of curcumin, releasing ∼ 48% of the
initial drug load at pH 7.2-7.4 during a 20 h-incubation. Most importantly, in vivo
experiments revealed that orally administered MPs-4 had a superior therapeutic efficiency
in alleviating colitis in a UC mouse model, compared to curcumin. Collectively, our
one-step-fabricated curcumin-loaded MPs have the properties of pH-sensitivity, controlled
drug release and colon targeting, and thus, may hold promise as a readily scalable
drug carrier for the efficient clinical treatment of UC.