Self-micellizing solid dispersions enhance the properties and therapeutic potential of fenofibrate: Advantages, profiles and mechanisms

Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Nian-Qiu Shi, Yong Zhang, Yan Li, Hong-Wei Lai, Xiao Xiao, Bo Feng, Xian-Rong Qi The goal of this work was to compare fenofibrate (FEN)-containing self-micellizing solid dispersion (SmSD) and non-self-micellizing solid dispersion (NsSD) systems. Exploration of underlying mechanisms to improve FEN dissolution/solubility profiles was conducted to understand the enhanced therapeutic potential. SmSD and NsSD of FEN systems (SmSD/FEN and NsSD/FEN) were fabricated using a fuse-quench cooling method. The self-micellizing Soluplus® cloud point was then determined experimentally and FEN phase solubility was measured in solutions containing self-micellizing Soluplus® or non-self-micellizing polymers. Physicochemical characteristics of SmSD/FEN and NsSD/FEN were evaluated using microscopic morphology, amorphous state, thermal performance, dissolution and solubility profiles. FEN exhibited an amorphous state in SmSD/FEN but was not completely amorphous in NsSD/FEN. The dissolution and solubility profile of SmSD/FEN achieved about 1.2- to 2-fold improvement over that of NsSD/FEN. Consequently, relatively enhanced hypolipidemic efficacy in vivo was observed in SmSD/FEN vs NsSD/FEN, as measured by serum levels of total cholesterol (TC), total triglycerides (TG), low-density lipoprotein (LDL) and high-density lipoprotein (HDL). Compared with non-self-micellizing polym...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research