Bio-based topical system for enhanced salicylic acid delivery: preparation and performance of gels

J Pharm Pharmacol. 2016 Aug;68(8):999-1009. doi: 10.1111/jphp.12582. Epub 2016 Jun 12.

Abstract

Objectives: New salicylic acid (SA)-loaded gels were developed using excipients made from renewable materials, and our goal was to improve drug permeation in the topical treatment of acne vulgaris.

Methods: We studied the preparation parameters to obtain suitable gel formulations. Only naturally occurring polymers were used as gelling agents. Two hydrogels and three lipogels were selected and characterized in terms of drug loading, pH, viability cells, rheology, mechanical properties and in vitro permeation; these hydrogels and lipogels were compared with the traditional ointment. We also evaluated skin parameters before and after gel application.

Key findings: The formulations that we studied are non-Newtonian fluids; they have high drug loading and suitable mechanical properties. Lipogels exhibit a slower and more linear in vitro permeation profile compared with hydrogels. The different vehicles that we used affected drug permeation and improve patient compliance. Cytotoxicity studies suggest that all of the formulations are non-toxic.

Conclusions: Lipogels demonstrate appropriate technological features and improved performance compared with the traditional ointment with regard to their composition. Lipogels may represent a new bio-based topical system for SA delivery. The use of 'green' excipients leads to 'skin-friendly' formulations that are able to satisfy environmental safety.

Keywords: gel; green formulation; renewable resources; skin permeation; topical delivery.

MeSH terms

  • Acne Vulgaris / drug therapy
  • Administration, Cutaneous
  • Administration, Topical
  • Adult
  • Chemistry, Pharmaceutical
  • Drug Carriers
  • Drug Delivery Systems*
  • Excipients
  • Gels / chemistry
  • Humans
  • Particle Size
  • Permeability
  • Rheology
  • Salicylic Acid / administration & dosage*
  • Salicylic Acid / metabolism
  • Salicylic Acid / therapeutic use
  • Skin / metabolism*
  • Skin Absorption*
  • Viscosity
  • Young Adult

Substances

  • Drug Carriers
  • Excipients
  • Gels
  • Salicylic Acid