Etodolac nanosuspension based gel for enhanced dermal delivery: in vitro and in vivo evaluation

Abstract

Aim

The objective of this study was to develop dermal nanosuspension (NS) based gel formulation of etodolac (ETD).

Methods

Etodolac nanosuspension (ETD-NS) was prepared by wet milling method and dispersed in hydroxypropyl methylcellulose (NS-HPMC) or hydroxyethyl cellulose (NS-HEC) gels. Rheologic and mechanical properties were investigated. In vitro and ex vivo permeability studies were performed. Topical anti-inflammatory and analgesic activity were evaluated in regard to carrageenan-induced inflammatory paw oedema and radiant heat tail-flick method, respectively.

Results

The ETD-NS with approximately 190 nm particle size (PS), 0.16 polydispersity index (PDI), and −15 mV zeta potential (ZP) values were obtained. The work of bioadhesion values of NS-HEC and NS-HPMC gels were 0.229 mJ/cm² for both gels. Dermal permeation of ETD from NS-HEC gel (7.18%) was found significantly higher than the NS-HPMC gel (4.56%). Enhanced anti-inflammatory and analgesic activity of NS-HEC gels were observed in comparison with micronised ETD.

Conclusions

ETD-NS based gel formulation is promising for topical delivery of ETD.

Keywords:

• Etodolac
• nanosuspension
• gel formulation
• dermal drug delivery
• permeation

Acknowledgements

This study was supported by a grant from The Scientific and Technological Research Council of Turkey (TUBITAK, 118S718). The correspondence author would like to thank especially Dr. Firat Nalbantoglu from Ashland, Dr. Abdullah Uslu from Nobel Pharmaceuticals and Timur Gucluer from Colorcon Inc. to support our study by providing Natrosol^® and Optiphen™ 300, micronised etodolac and HPMC, respectively.

Disclosure statement

The authors declare no interest the study reported in this article.

Additional information

Funding

This study was supported by a grant from The Scientific and Technological Research Council of Turkey [TUBITAK, 118S718].