Development of microparticles for oral administration of the non-conventional radical scavenger IAC and testing in an inflammatory rat model

Publication date: 15 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 1 Author(s): Nadia Passerini, Beatrice Albertini, Marcello Di Sabatino, Giuseppe Corace, Barbara Luppi, Donatella Canistro, Fabio Vivarelli, Silvia Cirillo, Antonio Soleti, Giulia Merizzi, Moreno Paolini The bis (1-hydroxy-2,2,6,6-tetramethyl-4-piperidinyl)-decandioate (IAC), is an innovative non- radical scavenger used with success in numerous disease models such as inflammation, neurological disorders, hepatitis and diabetes. The pharmacological treatments have been performed by the intraperitoneal route of administration, representing to date, the main limit for the drug use. The aim of this study was to develop a delivery system that allows the oral administration of IAC while maintaining its therapeutic efficacy. Solid Lipid Microparticles (SLMs) containing a theoretical 18% (w/w) of IAC have been produced by the spray congealing technology; three formulations have been tested (A, B and C) using different low melting point carriers (stearic acid, Compritol® HD5ATO and carnauba wax) alone or in combination. All IAC loaded SLMs exhibited a spherical shape, encapsulation efficiency higher than 94% and particle size suitable for the oral route. Administered per os at different dosages in an inflammation rat model, all SLMs demonstrated their efficacy in reducing oedema and alleviating pain, compared to the gold standards Indomethacin and Paracetamol. These results...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research