Formulation, Optimization and In Vivo Evaluation of Fucoidan-Based Cream with Anti-Inflammatory Properties

Mar Drugs. 2021 Nov 17;19(11):643. doi: 10.3390/md19110643.

Abstract

Fucoidan is a polysaccharide found in brown alga with glorious potential for pharmacological activities, among which its anti-inflammatory properties have gained meaningful attention. Due to several advantages of formulations for topical application, this study aimed to develop and optimize a fucoidan-based cream formulation and to investigate its anti-inflammatory potential after topical application in vivo. Fucoidan from Fucus vesiculosus L. was used. The cream base consisting of olive oil and Kolliphor RH40 was optimized followed by in vitro agar diffusion and drug release studies. The fucoidan-based cream with 13% Kolliphor P 407, 1% Transcutol P, and 5% PEG400 showed good spreadability, washability, and colloidal stability, and it did not irritate the skin. The kinetics of fucoidan release from the optimized cream exhibited the best fit to the Korsmeyer-Peppas and Higuchi models with R2 > 0.99. Fucoidan release was controlled by drug diffusion and anomalous transport provided by the optimized cream base. The formulation was stable and provided high fucoidan release after storage for 1 year. Topical application of the fucoidan-based cream dose-dependently inhibited carrageenan-induced edema and ameliorated mechanical allodynia in rats. The efficacy of the fucoidan-based cream at a high dose was comparable with the efficacy of diclofenac gel. The fucoidan-based cream could be considered a promising anti-inflammatory formulation.

Keywords: anti-inflammatory; cream; drug release; formulation development; fucoidan; topical application.

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology*
  • Aquatic Organisms
  • Carrageenan
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Drug Compounding
  • Edema / chemically induced
  • Edema / drug therapy
  • Female
  • Phaeophyceae*
  • Polysaccharides / administration & dosage
  • Polysaccharides / chemistry
  • Polysaccharides / pharmacology*
  • Rats
  • Rats, Wistar

Substances

  • Anti-Inflammatory Agents
  • Polysaccharides
  • Carrageenan
  • fucoidan