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.
Highlights
Marine-derived compounds demonstrate promising biological activities, and they are truly biodegradable and biocompatible, encouraging the development of novel formulations with specific pharmacological features of interest for the pharmaceutical industry.In particular, interest in the development of formulations with fucoidan has rapidly increased in the past few decades [1–4]
Taking together the results of Higuchi’s and Korsmeyer–Peppas models, we suggest that fucoidan release was due to both diffusions of the drug and anomalous transport provided by the optimized cream base
The cream base consisting of olive oil and Kolliphor RH40 was optimized, followed by in vitro agar diffusion and drug release studies
Summary
Interest in the development of formulations with fucoidan has rapidly increased in the past few decades [1–4]. Fucoidan is a polysaccharide with glorious potential for pharmacological activities [5–7]. The anti-inflammatory properties of fucoidan have gained meaningful attention [8,9]. Due to the complexity of inflammation processes, there is an urgent need for the development of new and safe anti-inflammatory agents with multiple mechanisms of action. Anti-inflammatory mechanisms described for fucoidan include scavenging of free radicals [11,12], suppression of the production of nitric oxide, tumor necrosis factor-alpha (TNF-α), prostaglandin E2, interleukin-1 beta, and interleukin-6 [13,14], selective inhibition of cyclooxygenase-2 [12], and downregulation of the expression of mitogen-activated protein kinase p38, Akt, extracellular signal-regulated kinase (ENK), and c-Jun N-terminal kinase (JNK) [15,16]
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