title: Microparticles Containing Curcumin Solid Dispersion: Stability, Bioavailability and Anti-Inflammatory Activity.
abstract: This work aimed at improving the solubility of curcumin by the preparation of spray-dried ternary solid dispersions containing Gelucire®50/13-Aerosil® and quantifying the resulting in vivo oral bioavailability and anti-inflammatory activity. The solid dispersion containing 40% of curcumin was characterised by calorimetry, infrared spectroscopy and X-ray powder diffraction. The solubility and dissolution rate of curcumin in aqueous HCl or phosphate buffer improved up to 3600- and 7.3-fold, respectively. Accelerated stability test demonstrated that the solid dispersion was stable for 9 months. The pharmacokinetic study showed a 5.5-fold increase in curcumin in rat blood plasma when compared to unprocessed curcumin. The solid dispersion also provided enhanced anti-inflammatory activity in rat paw oedema. Finally, the solid dispersion proposed here is a promising way to enhance curcumin bioavailability at an industrial pharmaceutical perspective, since its preparation applies the spray drying, which is an easy to scale up technique. The findings herein stimulate further in vivo evaluations and clinical tests as a cancer and Alzheimer chemoprevention agent.
authors.affiliation: Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Via do Café, s/n, Campus USP, Ribeirão Preto, 14040-903, Brazil.
authors.forename: C C C
authors.initials: CC
authors.lastname: Teixeira
authors.affiliation: Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Via do Café, s/n, Campus USP, Ribeirão Preto, 14040-903, Brazil.
authors.forename: L M
authors.initials: LM
authors.lastname: Mendonça
authors.affiliation: Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Via do Café, s/n, Campus USP, Ribeirão Preto, 14040-903, Brazil.
authors.forename: M M
authors.initials: MM
authors.lastname: Bergamaschi
authors.affiliation: Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Via do Café, s/n, Campus USP, Ribeirão Preto, 14040-903, Brazil.
authors.forename: R H C
authors.initials: RH
authors.lastname: Queiroz
authors.affiliation: Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Via do Café, s/n, Campus USP, Ribeirão Preto, 14040-903, Brazil.
authors.forename: G E P
authors.initials: GE
authors.lastname: Souza
authors.affiliation: Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Via do Café, s/n, Campus USP, Ribeirão Preto, 14040-903, Brazil.
authors.forename: L M G
authors.initials: LM
authors.lastname: Antunes
authors.affiliation: Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Via do Café, s/n, Campus USP, Ribeirão Preto, 14040-903, Brazil. lapdfrei@usp.br.
authors.forename: L A P
authors.initials: LA
authors.lastname: Freitas
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000494:pharmacology; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003474:Curcumin / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000494:pharmacology; D004355:Drug Stability; D005223:Fats / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D008297:Male; D009821:Oils / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D012822:Silicon Dioxide / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods; D014961:X-Ray Diffraction / Q000379:methods
chemical_list: D000893:Anti-Inflammatory Agents; D005223:Fats; D009821:Oils; C071184:Gelucire 50-13; D012822:Silicon Dioxide; D003474:Curcumin
keywords: bioavailability; blood level; dissolution; rat paw oedema; solubility; spray drying; thermal analysis; turmeric