Thermosensitive gel based on cellulose derivative for topical delivery of propolis in acne treatment

Pharm Dev Technol. 2022 Apr;27(4):490-501. doi: 10.1080/10837450.2022.2080221. Epub 2022 May 29.

Abstract

Thermosensitive bioadhesive formulations can display increased retention time, skin permeation, and improve the topical therapy of many drugs. Acne is an inflammatory process triggered by several factors like the proliferation of the bacteria Propionibacterium acnes. Aiming for a new alternative treatment with a natural source, propolis displays great potential due to its antibiotic, anti-inflammatory, and healing properties. This study describes the development of bioadhesive thermoresponsive platform with cellulose derivatives and poloxamer 407 for propolis skin delivery. Propolis ethanolic extract (PES) was added to the formulations with sodium carboxymethylcellulose (CMC) or hydroxypropyl methylcellulose (HPMC) and poloxamer 407 (Polox). The formulations were characterized as rheology, bioadhesion, and mechanical analysis. The selected formulations were investigated as in vitro propolis release, cytotoxicity, ex vivo skin permeation by Fourier Transform Infrared Photoacoustic Spectroscopy, and the activity against P. acnes. Formulations showed suitable sol-gel transition temperature, shear-thinning behavior, and texture profile. CMC presence decreased the cohesiveness and adhesiveness of formulations. Polox/HPMC/PES system displayed less cytotoxicity, modified propolis release governed by anomalous transport, skin permeation, and activity against P. acnes. These results indicate important advantages in the topical treatment of acne and suggest a potential formulation for clinical evaluation.

Keywords: Development; antibacterial activity; formulation; skin delivery; thermoresponsive systems.

MeSH terms

  • Acne Vulgaris* / drug therapy
  • Cellulose
  • Gels / chemistry
  • Humans
  • Hypromellose Derivatives
  • Poloxamer / chemistry
  • Propolis*

Substances

  • Gels
  • Poloxamer
  • Hypromellose Derivatives
  • Cellulose
  • Propolis