Novel lipid based oral formulation of curcumin: development and optimization by design of experiments approach

Int J Pharm. 2012 Oct 15;436(1-2):617-23. doi: 10.1016/j.ijpharm.2012.07.031. Epub 2012 Jul 27.

Abstract

The clinical utility of curcumin (CRM) is limited due to its poor oral bioavailability. Lipid based oral formulations (LBOFs) are emerging as useful oral drug delivery systems for 'difficult to deliver' molecules like CRM. In present study, we report novel Type IV LBOF for CRM using Gelucire 44/14, Labrasol, Vit. E TPGS and PEG 400 with superior CRM loading and enhanced oral bioavailability. The optimization of LBOF for CRM loading and post dilution droplet size was carried out by design of experiments (DoE) approach with Box-Behnken design. Oral bioavailability of optimized LBOF (O-LBOF) was evaluated in male Sprague-Dawley (SD) rats at a dose of 250 mg/kg. Raw CRM (control) showed C(max) and AUC(0-∞) of 32.29 ng/ml and 38.07 ng h/ml, respectively. O-LBOF improved C(max) and AUC(0-∞) by 11.6 and 35.8 folds respectively over control.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacokinetics
  • Biological Availability
  • Curcumin / administration & dosage
  • Curcumin / chemistry*
  • Curcumin / pharmacokinetics
  • Drug Carriers / administration & dosage
  • Drug Carriers / chemistry*
  • Drug Carriers / pharmacokinetics
  • Excipients / administration & dosage
  • Excipients / chemistry
  • Excipients / pharmacokinetics
  • Glycerides
  • Male
  • Organic Chemicals / administration & dosage
  • Organic Chemicals / chemistry
  • Organic Chemicals / pharmacokinetics
  • Polyethylene Glycols / administration & dosage
  • Polyethylene Glycols / chemistry
  • Polyethylene Glycols / pharmacokinetics
  • Rats
  • Rats, Sprague-Dawley
  • Solubility
  • Surface-Active Agents / administration & dosage
  • Surface-Active Agents / chemistry
  • Surface-Active Agents / pharmacokinetics
  • Vitamin E / administration & dosage
  • Vitamin E / analogs & derivatives
  • Vitamin E / chemistry
  • Vitamin E / pharmacokinetics

Substances

  • Antineoplastic Agents
  • Drug Carriers
  • Excipients
  • Glycerides
  • Organic Chemicals
  • Surface-Active Agents
  • Labrasol
  • gelucire 44-14
  • Vitamin E
  • Polyethylene Glycols
  • Curcumin
  • tocophersolan