Oral administration of pH-sensitive curcumin-loaded microparticles for ulcerative colitis therapy.
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.
Institute for Clean Energy and Advanced Materials, Faculty for Materials and Energy, Southwest University, Chongqing 400715, PR China; Center for Diagnostics and Therapeutics, Institute for Biomedical Sciences, Georgia State University, Atlanta 30302, USA. Electronic address: bxiao@gsu.edu.
Bo
B
Xiao
Institute for Clean Energy and Advanced Materials, Faculty for Materials and Energy, Southwest University, Chongqing 400715, PR China.
Xiaoying
X
Si
Center for Diagnostics and Therapeutics, Institute for Biomedical Sciences, Georgia State University, Atlanta 30302, USA.
Mingzhen
M
Zhang
Center for Diagnostics and Therapeutics, Institute for Biomedical Sciences, Georgia State University, Atlanta 30302, USA; Atlanta Veterans Affairs Medical Center, Decatur 30033, USA.
Didier
D
Merlin
D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000627:therapeutic use*; D003093:Colitis, Ulcerative / Q000139:chemically induced / Q000188:drug therapy* / Q000473:pathology; D003474:Curcumin / Q000008:administration & dosage* / Q000627:therapeutic use*; D003692:Delayed-Action Preparations; D016264:Dextran Sulfate; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D005260:Female; D006863:Hydrogen-Ion Concentration; D019344:Lactic Acid; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry*; D009929:Organ Size / Q000187:drug effects; D010316:Particle Size; D009195:Peroxidase / Q000378:metabolism; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011109:Polymethacrylic Acids
D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D011109:Polymethacrylic Acids; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; C038300:methylmethacrylate-methacrylic acid copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D016264:Dextran Sulfate; D009195:Peroxidase; D003474:Curcumin
Curcumin; Microparticle; Oral administration; Ulcerative colitis; pH Sensitivity