Fluidized Bed Hot-Melt Granulation as a Tool to Improve Curcuminoid Solubility

Autor(es)

Teixeira, Cristiane C. C. ^[1] ; de Paiva Junior, Elias ^[1] ; Pedro de Freitas, Luis Alexandre ^[1]

Afiliação do(s) autor(es)

^[1] Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, Inst Nacl Ciencia & Tecnol INCT Nanotecnol Farmac, Via Cafe S-N, Campus USP, BR-14040903 Ribeirao Preto, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: AAPS PHARMSCITECH; v. 19, n. 3, p. 1061-1071, APR 2018.
• Citações Web of Science: 3

Resumo

Curcumin is the main bioactive component of Curcuma longa L. and has recently aroused growing interest from the scientific community. Unfortunately, the medicinal properties attributed to curcuminoids are impaired by their low oral bioavailability or low solubility in aqueous solutions. Many strategies have been studied to improve curcumin solubility; however, the preparation of granules using hydrophilic materials has never been attempted. The aim of this work was to develop curcumin granules by fluidized bed hot-melt granulation using the hydrophilic carrier GelucireA (R) 50:13. A two-level factorial design was used to verify the influence of GelucireA (R) 50:13 and lactose contents found in the granules on their size, morphology, bulk and tapped densities, flow, moisture content, and water activity. The granules obtained were also evaluated by differential scanning calorimetry, thermogravimetric analysis, X-ray powder diffraction, and infrared spectrometry. The curcumin solubility and dissolution rates in water were determined by liquid chromatography. The best formulation provides an increase of curcumin solubility of 4642-fold and 3.8-fold compared to the physical mixture. The dissolution tests showed a maximum drug release from granules after 45 min of 70% at pH 1.2 and 80% at pH 5.8 and 7.4, while for non-granulated curcumin, the release was below 20% in all pH. The solid-state characterization and solubility measurement showed good stability of granules over 9 months. The results attest that the fluidized bed hot-melt granulation with hydrophilic binders is an attractive and promising alternative to obtain solid forms of curcumin with enhanced bioavailability. (AU)

• Processo FAPESP: 15/25128-5 - Desenvolvimento de extratos de endopleura uchi microencapsulados em dispersões sólidas para fins fitoterápicos
• Beneficiário: Luis Alexandre Pedro de Freitas
• Modalidade de apoio: Auxílio à Pesquisa - Regular
• Processo FAPESP: 13/23327-5 - DESENVOLVIMENTO E APLICAÇÃO DA TÉCNICA DE NEBULIZAÇÃO-LIOFILIZAÇÃO (Spray freeze drying) PARA OBTENÇAO DE EXTRATO SECO DE Baccharis dracunculifolia De Candole
• Beneficiário: Cristiane Cardoso Correia Teixeira
• Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado