Nanosuspension: An Emerging Trend for Bioavailability Enhancement of Etodolac

Abstract

Etodolac (ET) (poorly soluble drug) nanosuspensions were prepared by both pH shift method and antisolvent techniques in order to increase its dissolution rate. Various stabilizers were used, namely, Tween 20 and 80, HPMC, PVP K44, PVA, PEG 400, NaCMC, and -cyclodextrin. The prepared nanosuspensions were characterized by Fourier transform infrared spectroscopy (FTIR) and scanning electron microscope (SEM) and evaluated for their particle size, particle size distribution, and in vitro dissolution rate. In general, it was found that the antisolvent method for the preparation of ET nanosuspensions reduced the drug particle size to a higher extent compared to the pH shift method. The dissolution rate of ET in distilled water was markedly enhanced in the nanosized system, as more than 65% of drug dissolved in 10 min from all the nanosuspension formulations except F5 (stabilized with PVP K44) and F8 (stabilized with Tween 20), as compared to less than 20% of crude drug. Nanoparticles prepared by antisolvent method using Tween 80 as a stabilizer were selected for further in vivo study. The in vivo test demonstrated that nanoparticles of ET were well absorbed with a percentage drug absorption value 2.7 times more than that of micrometric size of crude ET.

Experimental and molecular modeling approach to optimize suitable polymers for fabrication of stable fluticasone nanoparticles with enhanced dissolution and antimicrobial activity

“…It has been reported that a higher temperature can cause instability of the nanosuspensions, because the Brownian motion and kinetic energies of the suspended particles increase at an elevated temperature, which results in the aggregation and agglomeration of the particles. 64 Furthermore, at higher temperature, viscosity is decreased 80 and solubility of the suspended particles increases, which potentially leads to increase in interparticulate interaction, when particle growth can occur. For maximum stability of the nanosuspensions, Freitas and Müller 81 recommended storing the nanosuspensions at a temperature range of 2°C–8°C.…”

Enhanced Solubility and Dissolution Rate of Clopidogrel by Nanosuspension: Formulation via High Pressure Homogenization Technique and Optimization Using Box Behnken Design Response Surface Methodology

“…According to Figure 18, the increase of number of remaining homogenization cycle under 1500 bar also able to reduce the particle size proportionally. However, the particle size became slightly bigger with the increase of stabilizer:drug mass ratio instead of giving reduction effect which may due excessive envelop of stabilizer surround the drug particles (Afifi et al, 2015). In Figure 4, it shows that the increase of both homogenization pressure in first 10 cycles and number of remaining homogenization cycle under 1500 bar gave combination effect in the particle size reduction.…”

Preparation and Characterization of Oral Nanosuspension Loaded With Curcumin

“…CUR NS was prepared by the precipitation-high speed homogenization (HSH Ultraturrax T-25 IKA) method ( fig. 1) [6,7]. Briefly, a solution of the drug in the solvent was slowly introduced into antisolvent phase containing a surfactant, at 1:15 solvent: antisolvent ratio at homogenization speed of 10,000 rpm for 10 min.…”

“…Top-down technology involves the disintegration of larger particles into nanoparticles, examples of which are high-pressure homogenization and milling methods [6]. NS enhance solubility of drugs that are poorly water-soluble and poorly lipid soluble by increase in surface area following particle size reduction, increase in saturation solubility, increase in the time available for dissolution because of inherent adherence characteristics of nanoparticles to the gastrointestinal wall (high specific surface area being indicative of a high interactive potential with biological surfaces) [7].…”