QbD-based carbopol transgel formulation: characterization, pharmacokinetic assessment and therapeutic efficacy in diabetes

Drug Deliv. 2016;23(3):1057-66. doi: 10.3109/10717544.2014.936536. Epub 2014 Jul 17.

Abstract

In order to develop transdermal drug delivery system that facilitates the skin permeation of Pioglitazone (PZ) encapsulated in carbopol-based transgel system (proniosomes/niosome). The developed formulations were optimized using quality by design (QbD) approach and particle size, percentage entrapment and transdermal flux were determined. It was found to be more efficient delivery carriers with high encapsulation and enhanced flux value demonstrated that the permeation of PZ through skin was significantly increased with developed formulation. The transdermal enhancement from proniosome was 3.16 times higher than that of PZ from control formulation (ethanol buffer formulation, 3:7), which was further confirmed by confocal laser scanning microscopy. In vivo pharmacokinetic study of carbopol transgel showed a significant increase in bioavailability (2.26 times) compared with tablet formulation. It also showed better antidiabetic activity in comparison to marketed tablet, so our results suggest that carbopol-based transgel are an efficient carrier for delivery of pioglitazone through skin.

Keywords: Antidiabetic activity; Box–Behnken design; carbopol; pioglitazone; transgel.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylic Resins / administration & dosage
  • Acrylic Resins / chemistry*
  • Acrylic Resins / pharmacokinetics*
  • Administration, Cutaneous
  • Animals
  • Biological Availability
  • Chemistry, Pharmaceutical / methods
  • Diabetes Mellitus / drug therapy*
  • Drug Carriers / chemistry
  • Gels / administration & dosage
  • Gels / chemistry*
  • Gels / pharmacokinetics*
  • Hypoglycemic Agents / administration & dosage
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / pharmacokinetics
  • Liposomes / administration & dosage
  • Liposomes / chemistry
  • Liposomes / pharmacokinetics
  • Particle Size
  • Permeability
  • Rats
  • Rats, Wistar
  • Skin / metabolism*
  • Skin Absorption
  • Tablets / administration & dosage
  • Tablets / chemistry
  • Tablets / pharmacokinetics

Substances

  • Acrylic Resins
  • Drug Carriers
  • Gels
  • Hypoglycemic Agents
  • Liposomes
  • Tablets
  • carboxypolymethylene