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

Year: 2021

Journal: J. Microencapsul., Volume 38, MAY 19, page 218–232

Authors: Karakucuk, Alptug; Tort, Serdar; Han, Sevtap; Oktay, Ayse Nur; Celebi, Nevin

Organizations: Scientific and Technological Research Council of Turkey [TUBITAK] [118S718]

Keywords: Etodolac; nanosuspension; gel formulation; dermal drug delivery; permeation

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/cm(2) 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.