Oral administration of pH-sensitive curcumin-loaded microparticles for ulcerative colitis therapy

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-stepfabricated 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.

Biodistribution and targeting potential assessment of mucoadhesive chitosan nanoparticles designed for ulcerative colitis via scintigraphy

“…19,20 To overcome these limitations, various novel sustained delivery systems have been reported for specifying curcumin availability directly to colitis tissues, such as tablets, liposomes, microspheres, nanostructured lipid carriers, self-emulsifying drug delivery system (SEDDS) and pellets. 10,[21][22][23] However, these suffer from wellknown limitations, including unintentional release throughout the GIT, long term stability and lower penetration through the mucus layer. Such obstacles can be overcome by nanoparticles (NPs).…”

Modern drug delivery strategies applied to natural active compounds

“…reasons, it was possible to reduce the oral administration dose of more than 80% to attain the same therapeutic effect. PLGA was used also in presence of pH-sensitive Eudragit S100 (ERS100), anionic copolymers based on methacrylic acic and methyl methacrylate that dissolved in aqueous media of pH 6-7, to obtain curcumin drug delivery microparticles (MPs) as anti-inflammatory agent in colitis tissues [82]. Due to its characteristic, when the pH shifts to neutral colon medium, an increase in the ERS100 content was associated with a considerable increase in the burst release and permeability of curcumin, increasing its diffusion-based loss.…”

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“…CUR-loaded chitosan microspheres were initially formulated by emulsion cross-linking method and then coated with Eudragit S-100. The pharmacodynamics of the prepared formulation was analysed in mice by acetic acid induced colitis model 32 . The prepared microspheres were of uniform spherical shape with good entrapment efficiency (73.88% to 82.50%).…”