Formulation, optimization and characterization of gemfibrozil nanocrystals prepared by wet milling technique

Abstract

Today, nanotechnology has a variety of application areas. Pharmacy is one of the most important application fields of
nanotechnology. Preparation of nanoparticular drug delivery systems such as nanocrystals could improve the solubility and
bioavailability of poorly water soluble drugs. Gemfibrozil (GEM) is a low water soluble drug biopharmaceutical classification system II and used as a lipid regulating agent. In this study, a rapid and simple wet milling method was used for preparation of GEM nanosuspension (GEM NS). The use of sonication after wet milling process reduced the milling time significantly. Different concentrations of stabilizers (polyvinyl pyrrolidone K30 [PVP K30] and Tween 80) were tested for preparation of GEM NSs. The finest GEM NS was obtained by 0.5% w/v GEM, 1% w/v PVP K30 and 2% w/v Tween 80. The size and zeta potential of finest GEM NS were 238.2 ± 2.5 nm and - 19.6 ± 0.1 mV, respectively.The morphology of dried GEM NS was observed using atomic force microscopy. Differential scanning calorimetry of GEM and GEM NS confirmed that there was no interaction between GEM and stabilizers. Compared with GEM, the solubility of GEM NS increased significantly.

Key words: Gmefibrozil, nanocrystal, poorly soluble drugs, wet milling