Formulation and evaluation of novel controlled release of topical pluronic lecithin organogel of mefenamic acid

Abstract

In the present study, pluronic lecithin based organogels (PLO gels) were formulated as topical carrier for controlled delivery of mefenamic acid. Ten organogel formulations were prepared by a method employing lecithin as lipophilic phase and pluronic F-127 as hydrophilic phase in varying concentrations to study various parameters using in vitro diffusion study and in vivo studies. All formulations were found to be off-white, homogenous, and reluctant to be washed easily and have pH value within the range of 5.56-5.80 which is nonirritant. Polymer concentration increased in formulations of F1 to F5 (lecithin) and F6 to F10 (pluronic) resulted in decrease of the gelation temperature, increase of viscosity and reduction of spreadability of gels having polymer tendency to form rigid 3D network. Organogels with higher viscosity were found to be more stable and retard the drug release from the gel. The formulations of F2 and F3 were selected for kinetic studies and stability studies, as they found to have all physical parameters within acceptable limits, highest percent drug content and exhibited highest drug release in eight hours. The order of drug release from various formulations was found to be F24F34F104F44F14F94F84F54F74F6. The optimized formulation F2 was found to follow zero order rate kinetics showing controlled release of the drug from the formulations. In vivo anti-inflammatory activity of optimized mefenamic acid organogel (F2) against a standard marketed preparation (Volini gel) was found satisfactory and significant. KeywordsIn vitro anti-inflammatory activity, in vitro release, mefenamic acid, pluronic lecithin organogels History

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“…Formulations were tested for organoleptic properties such as odor, color, texture, phase separation, and greasiness. [22] Homogeneity test…”

“…About 100 mg of gel was pressed between the thumb and the index finger to notice the consistency of gel that any particles being attached or detached on the finger. [22] Washability Gels were rubbed on backside skin of the hand. After drying, the layer was washed with tap water and observed whether it is washable or not.…”

“…After drying, the layer was washed with tap water and observed whether it is washable or not. [22] pH determination…”

Gellan Gum-Based Hydrogel for the Transdermal Delivery of Nebivolol: Optimization and Evaluation

“…In this context, gel formulations like hydrogels could be more appropriate for nebivolol transdermal therapy because of its low dose. Literature signifies that gel formulations like hydrogels, organogels, and emulgels have consistently been studied for delivering pharmaceutical actives through the skin [16,17,18]. Hydrogel, a versatile drug delivery system, has emerged as an attractive delivery mode for transdermal therapy of drugs because of the physicochemical and biological characteristics it possesses, which includes controlled drug release, good stability, higher percutaneous absorption, and nontoxic nature.…”

Anti-Inflammatory Drug-Loaded Biopolymeric Spongious Matrices With Therapeutic Perspectives in Burns Treatment

“…Mefenamic acid (MA), a non-steroidal anti-inflammatory drug (2-[(2,3-dimethylphenyl)amino]benzoic acid), belongs to Biopharmaceutics Classification System class II (low solubility and high permeability) [26,34]. MA, available on market in different forms as tablets, capsules, suspensions, is used to reduce pain and the first phase of post-traumatic inflammation by inhibition of cyclooxygenase-2 and prostaglandin synthesis [2,33,34], proving also its efficiency in various topical designed formulations [17,18]. Due to its short elimination half-life (2 hours) [34] and side effects specific to the NSAIDs, using the MA for the topical route of administration is a viable option.…”