Abstract

Aim: The main objective of the current research work was to formulate and evaluate Diacerein-loaded transferosomal topical gel to overcome the drawbacks associated with oral administration of Diacerein in Osteo arthritis treatment.
 Study Design: Transferosomal topical gel
 Methodology: Transferosomes were developed using different ratios of Phospholipid® 90G as phospholipid and Span-60 as surfactant and cholesterol as fluidity buffer. The selected best formulation of transferosomes was further optimized as a topical gel using different rate controlling polymers such as hydroxylethyl cellulose (HEC), hydroxyl propyl methylcellulose (HPMC) and, carbopol. Transcutol P was used as a penetration enhancer. In vitro diffusion studies of developed formulations were carried out using Franz diffusion cell apparatus.
 Results: The formulations prepared with Hydroxy ethyl cellulose (TBG1, TBG2, TBG3), HPMC (TBG4, TBG5, TBG6) was shown rapid drug release when compared to formulations prepared with carbopol (TBG7, TBG8, TBG9) are showing controlled drug release.Where the formulation prepared with carbopol with 0.75% concentration has shown acceptable extended drug release for 12 hours with acceptable other physico-chemical properties.
 Conclusion: It can be concluded that Diacerein-loaded transferosomal gel can be administered topically for the treatment of osteoarthritis with reduced oral side effects.

Highlights

  • Osteoarthritis (OA) is the most commonly occurring rheumatologic problem and type of arthritis with the prevalence of 22%- 39% in India

  • Cholesterol (CH), Span 60, hydroxylethyl cellulose (HEC), hydroxyl propyl methylcellulose (HPMC), Carbopol, and Transcutol P were purchased from Signet India

  • From the results of in vitro physico chemical properties and diffusion studies of transferosomal gel formulations, it can be concluded that the topical formulation of Diacerein can be successfully formulated with transferomal gel approach using Phospholipon G and cholesterol as lipid layer, span 60 as edge activator, Transcutol P as permeation enhancer and carbopol as gelling agent and optimized formulation has met the all the predetermined 5

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Summary

Introduction

Osteoarthritis (OA) is the most commonly occurring rheumatologic problem and type of arthritis with the prevalence of 22%- 39% in India. OA is most commonly affects the joints in the knees, hands, hips, feet and spine. As per the WHO, worldwide 9.6% of men and 18.0% of women over 60 years of age have symptomatic OA [1,2,3,4,5,6,7]. Diacerein is an anthraquinone moiety used to treat OA, works by blocking the actions of interleukin-1 beta a protein involved in the inflammation and destruction of cartilage. Diacerein is 4,5- diacetyloxy-9,10dioxo-anthracene-2-carboxylic acid [8,9,10,11]

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