Development of Etofenamate-Loaded Semisolid SLN Dispersions and Evaluation of Anti-Inflammatory Activity for Topical Application

作者：Badilli Ulya; Sengel Turk C Tuba^*; Onay Besikci Arzu; Tarimci Nilufer

来源：Current Drug Delivery, 2015, 12(2): 200-209.

DOI：10.2174/1567201811666140613112721

• Anti-inflammatory activity
• Compritol 888 ATO
• Etofenamate
• Precirol ATO 5
• Semisolid SLN
• Topical drug delivery system

Dermal application of various active substances is widely preferred for topical or systemic delivery. SLNs consist of biocompatible and non-toxic lipids and have a great potential for topical application in drugs. In this study, semisolid SLN formulations were successfully prepared by a novel one-step production method as a topical delivery system of etofenamate, an anti-inflammatory drug. Compritol 888 ATO and Precirol ATO 5 were chosen as lipid materials for the fabrication of the formulations. In-vitro evaluation of the formulations was performed in terms of encapsulation efficiency, particle size, surface charge, thermal behavior, rheological characteristics, in vitro drug release profile, kinetics, mechanisms, stability, and anti-inflammatory activity. The colloidal size and spherical shape of the particles were proved. According to the results of the rheological analysis, it was demonstrated that the semisolid SLN formulations have a gel-like structure. Stability studies showed that semisolid SLNs were stable at 4 degrees C for a six month period. Zero order release was obtained with Precirol ATO 5, while Compritol 888 ATO followed the square root of time (Higuchi's pattern) dependent release. Semisolid SLNs showed higher inhibitory activity of COX in comparison with pure etofenamate. In conclusion, etofenamate-loaded semisolid SLN formulations can be successfully prepared in a novel one-step production method and useful for topical application.

• 出版日期2015