Preparation and characterization of Nelfinavir Mesylate nanocrystals by ball milling

Abstract

The objective of the present study was to formulate Nelfinavir mesylate nanocrystals by ball milling to improve its pharmacokinetic behavior in turn bioavailability. Nanocrystals were prepared by dispersing the drug in Poloxamer 407 solution and subjected for size reduction by ball milling. The nanocrystals were lyophilized using mannitol ascryoprotectant. The free flowing powder forms of nanocrystals powder was evaluated for its particle size, zeta potential, solubility, in vitro dissolution. Solid-state characteristics were studied by Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC) and Fourier Transform Infra-Red Spectroscopy. The particle size and zeta potential of optimized formulation was found to be 740.12 ± 79.21 nm and 23.31 ± 1.10 mV respectively with PDI of 0.20 ± 0.07. DSC analysis and SEM revealed that there was slight decrease in crystallinity in the nanocrystals compared to raw crystals. Increased dissolution velocity was observed along with increased saturation solubility. Thus it can be concluded that increase in solubility and dissolution velocity of Nelfinavirmesylate was observed by formulating it as nanocrystals.