Improvement of Ferulic Acid Antioxidant Activity by Multiple Emulsions: In Vitro and In Vivo Evaluation

Ferulic acid is a derivative of cinnamic acid showing efficacious anti-oxidant activity. It catalyzes the stable phenoxy radical formation, upon absorption of ultraviolet light, giving the strength to ferulic acid for terminating free radical chain reactions. Ultraviolet rays are one of the most dangerous factors that daily assault the skin, causing excessive generation of reactive oxygen species (ROS), which are regarded to be important contributors to a variety of cutaneous alterations. The skin possesses endogenous antioxidant defense systems, but the excess of ROS leads to an oxidant–antioxidant imbalance. Although ferulic acid is daily introduced in human organism with the diet, its bioavailability after oral administration is poor, particularly in the skin. The aim of this investigation was to evaluate three types of emulsions (W/O/W multiple emulsions and two simple emulsions) as suitable formulations for topical application of the active compound. In vitro studies were performed to investigate the stability and release profiles of these systems. Multiple emulsions showed great stability and the best ability to carry and release ferulic acid. In vivo evaluations highlighted their best capability to treat UV-B-induced erythema. These findings suggested multiple emulsions as an innovative and more efficient vehicle for topical application of ferulic acid.

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Nanomiemgel - A Novel Drug Delivery System for Topical Application - In Vitro and In Vivo Evaluation

PLoS ONE ◽

10.1371/journal.pone.0115952 ◽

2014 ◽

Vol 9 (12) ◽

pp. e115952 ◽

Cited By ~ 23

Author(s):

Jaganmohan Somagoni ◽

Cedar H. A. Boakye ◽

Chandraiah Godugu ◽

Apurva R. Patel ◽

Henrique Antonio Mendonca Faria ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Topical Application ◽

In Vivo Evaluation ◽

Novel Drug Delivery System ◽

Novel Drug

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

Marine Drugs ◽

10.3390/md19110643 ◽

2021 ◽

Vol 19 (11) ◽

pp. 643

Author(s):

Ekaterina D. Obluchinskaya ◽

Olga N. Pozharitskaya ◽

Elena V. Flisyuk ◽

Alexander N. Shikov

Keyword(s):

Topical Application ◽

Colloidal Stability ◽

High Dose ◽

In Vivo Evaluation ◽

Release Studies ◽

Anti Inflammatory ◽

Kinetics Of ◽

Best Fit

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.

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Formulation of meloxicam gel for topical application: In vitro and in vivo evaluation

Acta Pharmaceutica ◽

10.2478/v10007-010-0020-0 ◽

2010 ◽

Vol 60 (2) ◽

pp. 153-163 ◽

Cited By ~ 15

Author(s):

Yogeshwar Bachhav ◽

Vandana Patravale

Keyword(s):

Topical Application ◽

Skin Irritation ◽

Inflammatory Activity ◽

Rat Skin ◽

In Vivo Evaluation ◽

Topical Gel ◽

Skin Delivery ◽

Anti Inflammatory

Formulation of meloxicam gel for topical application: In vitro and in vivo evaluation Skin delivery of NSAIDs offers several advantages over the oral route associated with potential side effects. In the present investigation, topical gel of meloxicam (MLX) was formulated using N-methyl pyrrolidone (NMP) as a solubilizer and Carbopol Ultrez 10® as a gelling polymer. MLX gel was evaluated with respect to different physicochemical parameters such as pH, viscosity and spreadability. Irritation potential of MLX gel was studied on rabbits. Permeation of MLX gel was studied using freshly excised rat skin as a membrane. Anti-inflammatory activity of MLX gel was studied in rats and compared with the commercial formulation of piroxicam (Pirox® gel, 0.5% m/m). Accelerated stability studies were carried out for MLX gel for 6 months according to ICH guidelines. MLX gel was devoid of any skin irritation in rabbits. After 12 h, cumulative permeation of MLX through excised rat skin was 3.0 ± 1.2 mg cm-2 with the corresponding flux value of 0.24 ± 0.09 mg cm-2 h-1. MLX gel exhibited significantly higher anti-inflammatory activity in rats compared to Pirox® gel. Physicochemically stable and non-irritant MLX gel was formulated which could deliver significant amounts of active substance across the skin in vitro and in vivo to elicit the anti-inflammatory activity.

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