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DEVELOPMENT AND EVALUATION OF ELASTIC LIPOSOME BASED TOPICAL GEL OF DIFLUNISAL FOR TREATMENT OF HYPERALGESIA IN MURINE MODEL
Author(s): ,
Kaur, A.*
Affiliations:
Panjab University, Department of Pharmaceutics- University Institute of Pharmaceutical Sciences, Chandigarh, India
Katare, D.O.P.
Affiliations:
Panjab University, Department of Pharmaceutics- University Institute of Pharmaceutical Sciences, Chandigarh, India
ESRA Academy. Kaur A. Sep 13, 2017; 196114; esra7-0434
Amanpreet Kaur
Amanpreet Kaur
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Abstract
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Background and Aims:

Diflunisal is a potent salicylic acid derivative, indicated for treatment of pain and inflammation associated with rheumatoid arthritis, osteoarthritis and post episiotomy pain. The oral administration leads to severe gastrointestinal side effects. The aim of the current proposal is to develop an elastic liposome based topical gel of diflunisal to improve its delivery and efficacy.

Methods:

Elastic liposomes of diflunisal were developed by thin film hydration method. The elastic liposomes were characterized for vesicle size, morphology, degree of elasticity, zeta potential, stability, rheology, texture etc. The ex vivo permeation across mice skin, histopathological investigations and in vivo therapeutic activity assessment for antihyperalgesia was studied using formalin induced hyperalgesia murine model. The protocol of study was duly approved (PU/IAEC/S/14/57) dated 29.10.2014.

Results:

The developed elastic liposomal vesicles were spherical and multilamellar in nature (Figure 1) with a particle size of 119.5 nm and PDI of 0.338. The percentage entrapment efficient of diflunisal was 81.45%. The ex vivo permeation across mice skin was 110.56 ± 3.45 µg/cm2. The effective skin penetration of rhodamine 123 labelled elastic liposomes was confirmed by confocal laser scanning microscopic studies(Figure 1). Histopathological study depicted the dermal safety of developed gel (Figure 1). Dermatokinetic studies across rat skin depicted effective concentration of diflunisal in skin as quantified by HPLC analysis.The antihyperalgesia was demonstrated by decrease in paw licking time and biting time in rats treated with diflunisal gel(Figure 2).


Figure 2
Figure 2

Conclusions:

The developed elastic liposome based topical gel was promising in effective pain relief in case of chronic inflammatory conditions.

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