Orally Delivered Curcumin-Loaded Microparticles Effectively Treat Mouse Model of Ulcerative Colitis

Microparticles (MPs) loaded with the efficient anti-inflammatory agent curcumin were found to effectively treat a mouse model of ulcerative colitis.

Ulcerative colitis is a chronic relapsing disease associated with uncontrolled inflammation in the gastrointestinal tract. It is a subtype of inflammatory bowel disease (IBD) and often affects the innermost mucosa of the intestine. The goal for ulcerative colitis therapy is to control inflammation, heal the mucosa, and reduce the need for surgery and hospitalization.

In the current study, investigators at Georgia State University (Atlanta, USA) used an emulsion-solvent evaporation method to fabricate MPs from pH-sensitive Evonik (Essen, Germany) Eudragit S100 and poly(lactide-co-glycolide) (PLGA). Eudragit S100 is composed of anionic copolymers based on methacrylic acid and methyl methacrylate that forms effective and stable enteric coatings with a fast dissolution in the upper bowel. PLGA is a copolymer used in a variety of [US] Food and Drug Administration approved therapeutic devices, owing to its biodegradability and biocompatibility. The MPs were loaded with curcumin (an efficient anti-inflammatory agent). As of June 2015, there were 116 clinical trials evaluating the possible anti-disease effect of curcumin in humans, as registered with the [US] National Institutes of Health, including studies on cancer, gastrointestinal diseases, cognitive disorders, and psychiatric conditions.

The spherical MPs that were produced had a desirable particle size ranging from 1.52 to 1.91 microns. Their loading efficiency could be regulated by changing the weight ratios of Eudragit S100 and PLGA, with some MPs exhibiting loading efficiencies over 80%. The fast release of curcumin from MPs in buffers (pH 1.2 and 6.8) could be significantly decreased by increasing the PLGA content. Eudragit 100/PLGA MPs with a weight ratio of 1:2 (MPs-4) were able to maintain sustained release of curcumin, releasing approximately 48% of the initial drug load at pH 7.2–7.4 during a 20 hour-incubation.

Results of in vivo experiments published in the August 1, 2015, online edition of the journal Colloids and Surfaces B: Biointerfaces revealed that orally administered MPs-4 had a superior therapeutic efficiency in alleviating colitis in an ulcerative colitis mouse model, compared to free curcumin.

"Orally administered microparticles may offer an efficient drug delivery system because they are characterized by a high drug loading capacity and may target colitis tissues based on abnormalities," said senior author Dr. Didier Merlin, professor of biomedical sciences at Georgia State University.

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Georgia State University
Evonik