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

Author(s)

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

Affiliation

^[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

• Document type: Journal article
• Source: AAPS PHARMSCITECH; v. 19, n. 3, p. 1061-1071, APR 2018.
• Web of Science Citations: 3

Abstract

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)

• FAPESP's process: 15/25128-5 - DEVELOPMENT OF SOLID DISPERSIONS CONTAINING ENDOPLEURA UCHI EXTRACTS FOR PHYTOPHARMACEUTICAL PURPOSES
• Grantee: Luis Alexandre Pedro de Freitas
• Support Opportunities: Regular Research Grants
• FAPESP's process: 13/23327-5 - DEVELOPMENT AND APPLICATION OF THE SPRAY FREEZE DRYING TECHNIQUE TO OBTAIN DRIED EXTRACTS OF Baccharis dracunculifolia De Candole
• Grantee: Cristiane Cardoso Correia Teixeira
• Support Opportunities: Scholarships in Brazil - Post-Doctoral