Glycerosomes: Use of hydrogenated soy phosphatidylcholine mixture and its effect on vesicle features and diclofenac skin penetration

Int J Pharm. 2016 Sep 10;511(1):198-204. doi: 10.1016/j.ijpharm.2016.07.009. Epub 2016 Jul 12.

Abstract

In this work, diclofenac was encapsulated, as sodium salt, in glycerosomes containing 10, 20 or 30% of glycerol in the water phase with the aim to ameliorate its topical efficacy. Taking into account previous findings, glycerosome formulation was modified, in terms of economic suitability, using a cheap and commercially available mixture of hydrogenated soy phosphatidylcholine (P90H). P90H glycerosomes were spherical and multilamellar; photon correlation spectroscopy showed that obtained vesicles were ∼131nm, slightly larger and more polydispersed than those made with dipalmitoylphosphatidylcholine (DPPC) but, surprisingly, they were able to ameliorate the local delivery of diclofenac, which was improved with respect to previous findings, in particular using glycerosomes containing high amount of glycerol (20 and 30%). Finally, this drug delivery system showed a high in vitro biocompatibility toward human keratinocytes.

Keywords: (trans)Dermal drug delivery; DSC; Hydrogenated phospholipid vesicles; Keratinocytes; Pig skin; Rheology.

MeSH terms

  • Animals
  • Cells, Cultured
  • Diclofenac / administration & dosage
  • Diclofenac / metabolism*
  • Drug Delivery Systems / methods
  • Glycerol / administration & dosage
  • Glycerol / metabolism*
  • Glycine max / metabolism
  • Humans
  • Hydrogenation
  • Keratinocytes / drug effects
  • Keratinocytes / metabolism
  • Organ Culture Techniques
  • Phosphatidylcholines / administration & dosage
  • Phosphatidylcholines / metabolism*
  • Skin Absorption / drug effects*
  • Skin Absorption / physiology
  • Swine

Substances

  • Phosphatidylcholines
  • phospholipon 90G
  • Diclofenac
  • Glycerol