Investigating the potential of employing bilosomes as a novel vesicular carrier for transdermal delivery of tenoxicam

Int J Pharm. 2015 May 15;485(1-2):329-40. doi: 10.1016/j.ijpharm.2015.03.033. Epub 2015 Mar 18.

Abstract

Bilosomes represent an evolving vesicular carrier that have been explored for oral vaccines delivery based on its ability to resist enzymes and bile salts in the gastrointestinal tract (GIT). Bilosomes vesicles are formed of bilayer membrane of non-ionic surfactant molecules encompassing bile salts. Although, bilosomes have not been proposed for transdermal drug delivery, this carrier seems to have promising potential in this regard. Accordingly, the aim of this investigation was to assess the capability and safety of utilizing bilosomes for transdermal delivery of tenoxicam (TX) as a model drug. A 3(1)2(2) full factorial design was adopted to study the effects of different formulation parameters on bilosomes properties and select the optimal formulation using Design-Expert(®) software. The selected formulation displayed nano-sized spherical vesicles (242.5 ± 6.43nm) with reasonable entrapment efficiency percent (68.33 ± 2.33%). Confocal laser scanning microscopy confirmed the capability of the flourolabeled bilosomes to penetrate deep within the skin. Both, ex vivo permeation and in vivo skin deposition studies confirmed the superiority of bilosomes over drug solution in delivering TX transdermally. In addition, in vivo histopathological study proved the safety of topically applied bilosomes. In summary, the highlighted results confirmed that bilosomes can be further adopted for delivering drugs transdermally.

Keywords: Bile salts; Bilosomes; Cholesterol (PubChem CID: 5997); Confocal laser scanning microscopy; Ex vivo permeation; Histopathology; In vivo skin deposition; Sodium deoxycholate (PubChem CID: 23668196); Span 40 (sorbitan monopalmitate) (PubChem CID: 23725021); Span 60 (sorbitan monostearate) (PubChem CID: 3793749); Span 80 (sorbitan monooleate) (PubChem CID: 5385498); Tenoxicam (PubChem CID: 54677971).

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage*
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / metabolism
  • Bile Acids and Salts / chemistry*
  • Calorimetry, Differential Scanning
  • Chemistry, Pharmaceutical
  • Drug Carriers*
  • Liposomes
  • Male
  • Microscopy, Confocal
  • Microscopy, Electron, Transmission
  • Models, Statistical
  • Nanoparticles
  • Nanotechnology
  • Particle Size
  • Permeability
  • Piroxicam / administration & dosage
  • Piroxicam / analogs & derivatives*
  • Piroxicam / chemistry
  • Piroxicam / metabolism
  • Rats, Wistar
  • Skin / metabolism*
  • Skin Absorption*
  • Surface Properties
  • Surface-Active Agents / chemistry*
  • Technology, Pharmaceutical / methods

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Bile Acids and Salts
  • Drug Carriers
  • Liposomes
  • Surface-Active Agents
  • Piroxicam
  • tenoxicam