Improved Analgesic and Anti-Inflammatory Effect of Diclofenac Sodium by Topical Nanoemulgel: Formulation Development—In VitroandIn VivoStudies

Shadab Md,Zuhier Awan,Ponnurengam Malliappan Sivakumar,Sabna Kotta,Nabil A Alhakamy,Sohail Akhter,Md Shoaib Alam,Javed Ahmad,Mohammad A Khan,Hibah M Aldawsari

doi:10.1155/2020/4071818

Abstract

The present study aimed to develop diclofenac sodium nanoemulgel for managing pain and inflammation using the low-energy emulsification technique. Nanoemulsion of diclofenac was formulated using clove oil with adequate amount of surfactants and cosurfactants, and it was converted to hydrogel form using Carbopol 980 as the gelling agent. The droplet size of the oil globules in the nanoemulsion was found to be 64.07 ± 2.65 nm with a low polydispersity index (0.238 ± 0.02) along with high negative zeta potential (−39.06 mV). The developed nanoemulgel exhibited non-Newtonian and pseudoplastic behavior. Thein vitrorelease profile of the developed nanoemulgel was higher as compared to marketed and conventional gel. The carrageenan-induced paw edema test was performed in rats to evaluate the anti-inflammatory activity of developed nanoemulgel. The developed nanoemulgel showed significantly higher (p<0.01) effect in reducing pain and inflammation symptoms as compared to marketed as well as conventional gel of diclofenac. The overall findings of the study suggest that the developed nanoemulgel formulation of diclofenac can be used as a potential approach for the management of pain and inflammation.

Highlights

Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most commonly used drugs to reduce pain and inflammation associated with arthritic disorders [1]
An extra amount of diclofenac sodium was added to 2 ml of selected oil in Eppendorf tubes and thoroughly mixed in a vortex mixer, followed by shaking with an isothermal shaker kept at 25 ± 1°C for 72 h. e samples were subjected to centrifugation (Sigma Laborzentrifugen GmbH, Germany) at 3000 rpm for 15 min, and the obtained supernatant was passed through 0.22 μm filter syringe. e content of the drug was estimated with UV spectrophotometer at 254 nm after required dilution with methanol [18, 19]
Due to its higher concentration gradient, it will help in increasing the therapeutic efficacy by boosting the percutaneous drug permeation. e solubility of Diclofenac sodium (DFS) was found to be exceptionally high in clove oil (>500 mg/g)

Summary

Introduction

Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most commonly used drugs to reduce pain and inflammation associated with arthritic disorders [1]. Diclofenac sodium (DFS) is globally the most widely prescribed NSAID in management of pain and inflammation in various diseases including rheumatoid arthritis and osteoarthritis [2]. Topical delivery presents the advantage of avoiding the first-pass hepatic metabolism, thereby improving the bioavailability. When exploiting this route, there are some challenges related to drug absorption and permeation. A study shows that otic administration of DFS may lead to ototoxicity, which limits its topical usage in chronic otitis [11]. All these challenges show the need for the development of safe and effective topical formulation, which is economical

Methods

Results

Conclusion