Propranolol hydrochloride-loaded liposomal gel for transdermal delivery: Characterization and in vivo evaluation

Int J Pharm. 2015 Jun 20;487(1-2):135-41. doi: 10.1016/j.ijpharm.2015.04.023. Epub 2015 Apr 13.

Abstract

This study was to develop propranolol hydrochloride (PRO)-loaded liposomal gel as a topical drug delivery system. Scanning electron microscope (SEM) revealed that the liposomes were spherical and scattered in the surface of the gel. Pseudoplastic flows of PRO liposomal gel were showed after stored at three different temperatures. Besides, PRO liposomal gel showed non-irritating to the skin of rabbit. Skin deposition studies in vivo demonstrated that PRO liposomal gel can apparently increase drug content in skin compared with PRO gel. Histopathology examination showed that PRO liposomal gel could obviously weaken the barrier function of stratum corneum (SC) by comparison with PRO gel. What is more, the plasma pharmacokinetic showed the maximum concentration in plasma was 0.41 μg/mL and 1.17 μg/mL after topical and oral administration respectively. However, tissue distribution study showed PRO liposomal gel obviously changed drug distribution in tissues, significantly increased drug concentration in skin with about 74 folds compared with PRO gel. In conclusion, liposomes-based gel could be a promising vehicle as a transdermal delivery system of PRO.

Keywords: Liposomal gel; Pharmacokinetic; Propranolol hydrochloride; Tissue distribution; Transdermal delivery.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Cutaneous
  • Adrenergic beta-Antagonists / administration & dosage*
  • Adrenergic beta-Antagonists / adverse effects
  • Adrenergic beta-Antagonists / pharmacokinetics
  • Animals
  • Dermatitis, Irritant / pathology
  • Drug Delivery Systems
  • Gels
  • Irritants
  • Liposomes / chemistry*
  • Particle Size
  • Propranolol / administration & dosage*
  • Propranolol / adverse effects
  • Propranolol / pharmacokinetics
  • Rabbits
  • Rheology
  • Skin / drug effects
  • Skin / pathology

Substances

  • Adrenergic beta-Antagonists
  • Gels
  • Irritants
  • Liposomes
  • Propranolol