Sustained release of sodium deoxycholate from PLGA-PEG-PLGA thermosensitive polymer

Artif Cells Nanomed Biotechnol. 2018;46(sup2):1170-1177. doi: 10.1080/21691401.2018.1481861. Epub 2018 Jul 10.

Abstract

Delivery of the drugs to the target tissue and reducing their side effects on surrounding tissues is still a significant challenge for pharmaceutical scientists. The aim of this study was to investigate the suitability of PLGA-PEG-PLGA triblock copolymer as a matrix material for a sustained-release system of sodium deoxycholate (NaDC). The copolymer was synthesized by ring-opening polymerization reaction, using microwave irradiation and characterized by different techniques. It was shown that the introduction of NaDC to the PLGA-PEG-PLGA copolymer did not influence its inherent sol-gel transition behaviour, but increased the sol-gel transition. The results showed the appropriate NaDC/polymer interaction and the formation of NaDC/polymer-mixed micelle. The sustained release of NaDC from the copolymer lasted for 2 days. This release can be attributed to the formation of NaDC/polymer-mixed micelles and trapping NaDC in the copolymer matrix. The cytolytic efficacy of NaDC-loaded copolymer and sustained release of NaDC were investigated on human adipocytes. Overall a sustained-release formulation for NaDC can be used to study localized fat dissolution.

Keywords: PLGA–PEG–PLGA copolymer; localized fat; sodium deoxycholate; thermosensitive.

MeSH terms

  • Adipocytes / cytology
  • Adipocytes / drug effects
  • Cell Survival / drug effects
  • Delayed-Action Preparations
  • Deoxycholic Acid / chemistry*
  • Drug Carriers / chemistry*
  • Drug Carriers / pharmacology
  • Humans
  • Polyesters / chemistry*
  • Polyesters / pharmacology
  • Polyethylene Glycols / chemistry*
  • Polyethylene Glycols / pharmacology
  • Temperature*

Substances

  • Delayed-Action Preparations
  • Drug Carriers
  • Polyesters
  • poly(lactide-co-glycolide)-block-poly(ethylene glycol)-block-poly(lactide-co-glycolide)
  • Deoxycholic Acid
  • Polyethylene Glycols