Curcumin nanoparticles containing poloxamer or soluplus tailored by high pressure homogenization using antisolvent crystallization

Int J Pharm. 2019 May 1:562:124-134. doi: 10.1016/j.ijpharm.2019.03.038. Epub 2019 Mar 18.

Abstract

Curcumin is a natural active constituent of Curcuma longa from Zingiberaceae family that shows many different pharmacological effects such as anticancer, antioxidant, anti-inflammatory, antimicrobial and antiviral effect. However, its bioavailability is profoundly limited by its poor water solubility. In this study antisolvent crystallization followed by freeze drying was used for the preparation of curcumin nanoparticles. The presence of different ratios of hydrophilic polymers (poloxamer 188 & soluplus) on physicochemical properties of curcumin nanoparticles was also investigated. In addition, the effect of high pressure homogenization (HPH) on solubility and dissolution properties of curcumin was investigated. All nanoparticle formulations were examined to determine their particle size distribution, saturation solubility, morphology (SEM), solid state (DSC, XRPD and FT-IR) and dissolution behavior. It was observed that curcumin crystallized in the presence of polymers exhibited better solubility and dissolution rate in comparison with original curcumin. The results showed that the concentration of the stabilizer and the method used to prepare nanoparticles can control the dissolution of curcumin. The crystallized nanoparticles showed polymorph 2 curcumin with lower crystallinity and higher dissolution rate. Curcumin nanoparticles containing 50% soluplus prepared via HPH method presented 16-fold higher solubility than its original form. In conclusion, samples crystalized and proceed with HPH technique showed smaller particle size, better re-dispersibility, higher solubility and dissolution rate in water compared with a sample prepared using a simple antisolvent crystallization process.

Keywords: Antisolvent crystallization; Curcumin; Dissolution rate; High pressure homogenization.

MeSH terms

  • Crystallization
  • Curcumin / chemistry*
  • Drug Carriers / chemistry*
  • Drug Compounding / methods*
  • Freeze Drying
  • Nanoparticles / chemistry*
  • Poloxamer / chemistry*
  • Polyethylene Glycols / chemistry*
  • Polyvinyls / chemistry*
  • Pressure
  • Solubility

Substances

  • Drug Carriers
  • Polyvinyls
  • polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer
  • Poloxamer
  • Polyethylene Glycols
  • Curcumin