Abstract

Objective: The current work was aimed to prepare a topical gel containing curcumin (CUR) for the treatment of microbial infections on skin.
 Methods: CUR was complexed with the β-cyclodextrin (β-CD) using kneading method in 1:1, 1:2, and 1:3 molar ratios and characterized. The inclusion complex with high aqueous solubility was loaded in the topical gel containing (2% CUR) which was prepared using carbopol, sodium CMC, and guar gum and evaluated for viscosity, spreadability, extrudability, pH, drug content, and in vitro diffusion studies. The in vitro anti-inflammatory activity of the gel was performed by albumin protein denaturation technique, the statistical analysis was done using ANOVA followed Dunnett’s t-test. The antimicrobial activity of CUR was evaluated using standard strains of Candida albicans and Escherichia coli by agar well diffusion method.
 Results: The complexation of CUR had an increased solubility up to 103.09 times for 1:3 molar ratio with in vitro dissolution 90.64% for 60 min. The optimized formulation F9 had viscosity of 6500.3 cps and 97.5% in vitro drug diffusion for 8 h which follows zero-order release kinetics. In vitro anti-inflammatory activity studied showed that the CUR gel has a good potency for renaturation and was as effective as standard diclofenac with 76.9% inhibition (p=0.0507). CUR showed approx. 3 mm diameter of zone of inhibition against C. albicans and E. coli.
 Conclusion: A stable topical gel of CUR using β-CD and carbopol was successfully prepared which showed better in vitro diffusion with promising anti-inflammatory and antifungal action.

Highlights

  • Herbal medicines are still the mainstay of about 75–80% of the world’s population, majorly in developing countries due to better cultural acceptability, better compatibility with the human body, complete cure, and lesser side effects

  • Materials CUR was purchased from Sisco Research Laboratories (SRL, Mumbai, India), CAS Number: [458-37-7]. β-Cyclodextrin (β-CD), carbopol, sodium CMC, guar gum, and menthol were obtained from SD FineChem Limited, Chennai, India

  • Determination of partition coefficient Partition coefficient is an important parameter as it is a measure of drugs lipophilicity and an indication of its ability to cross the cell membrane

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Summary

Introduction

Herbal medicines are still the mainstay of about 75–80% of the world’s population, majorly in developing countries due to better cultural acceptability, better compatibility with the human body, complete cure, and lesser side effects. Low potency, and instability are inherent problems of several herbal medicines. CUR [1,7-Bis-(4-hydroxy-3methoxyphenyl)-hepta-1,6-diene-3,5-dione] is an oil-soluble pigment, practically insoluble in water at acidic and neutral pH, soluble in alkali, and highly susceptible for pH change having molecular weight 368.38 g/mole and a melting point of 175–180°C [2]. Following oral administration (up to 8 g/day), it is poorly absorbed and only the traces of compound appear in blood. It undergoes extensive first-pass metabolism and is a suitable candidate for topical gel formulation [2,3]

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