Title:Crystalline Ethylene Oxide and Propylene Oxide Triblock Copolymer Solid Dispersion Enhance Solubility, Stability and Promoting Time- Controllable Release of Curcumin
VOLUME: 12 ISSUE: 1
Author(s):Thais F.R. Alves, Franciely C.C. das Neves Lopes, Marcia A. Rebelo, Juliana F. Souza, Katiusca da Silva Pontes, Carolina Santos, Patricia Severino, Jose M.O. Junior, Daniel Komatsu and Marco V. Chaud*
Affiliation:Laboratory of Biomaterials and Nanotechnology- UNISO. Sorocaba, SP, Laboratory of Biomaterials and Nanotechnology- UNISO. Sorocaba, SP, Laboratory of Biomaterials and Nanotechnology- UNISO. Sorocaba, SP, Laboratory of Biomaterials and Nanotechnology- UNISO. Sorocaba, SP, Laboratory of Biomaterials and Nanotechnology- UNISO. Sorocaba, SP, Laboratory of Biomaterials and Nanotechnology- UNISO. Sorocaba, SP, Institute of Technology and Research (ITP), University Tiradentes- UNIT. Aracaju, SE, Laboratory of Applicated Nuclear Physical-UNISO. Sorocaba, SP, Laboratory of Biomaterials - PUC-SP. Sorocaba, SP, Laboratory of Biomaterials and Nanotechnology- UNISO. Sorocaba, SP
Keywords:Curcumin, solid dispersion, solubility, stability, dissolution rate, permeability.
Abstract:Aims and Background: The design and development of an effective medicine are,
however, often faced with a number of challenges. One of them is the close relationship of drug's
bioavailability with solubility, dissolution rate and permeability. The use of curcumin's (CUR)
therapeutic potential is limited by its poor water solubility and low chemical stability. The purpose
was to evaluate the effect of polymer and solid dispersion (SD) preparation techniques to enhance the
aqueous solubility, dissolution rate and stability of the CUR. The recent patents on curcumin SD were
reported as (i) curcumin with polyvinylpyrrolidone (CN20071 32500 20071214, WO2006022012 and
CN20151414227 20150715), (ii) curcumin-zinc/polyvinylpyrrolidone (CN20151414227 20150715),
(iii) curcumin-poloxamer 188 (CN2008171177 20080605), (iv) curcumin SD prepared by melting
method (CN20161626746-20160801).
Materials and Methods: SD obtained by co-preciptation or microwave fusion and the physical
mixture of CUR with Poloxamer-407 (P-407), Hydroxypropylmetylcellulose-K4M (HPMC K4M) and
Polyvinylpyrrolidone-K30 (PVP-K30) were prepared at the ratios of 1:2; 1:1 and 2:1. The samples
were evaluated by solubility, stability, dissolution rate and characterized by SEM, PXRD, DSC and
FTIR.
Results: The solubility, stability (pH 7.0) and dissolution rate were significantly greater for SD
(CUR:P-407 1:2). The PXRD,SEM and DSC indicated a change in the crystalline state of CUR. The
enhancement of solubility was dependent on a combination of factors including the weight ratio,
preparation techniques and carrier properties. The drug release data fitted well with the Weibull equation,
indicating that the drug release was controlled by diffusion, polymer relaxation and erosion occurring
simultaneously.
Conclusion: Thus, these SDs, specifically CUR:P-407 1:2 w/w, can overcome the barriers of poor
bioavailability to reap many beneficial properties.
