Abstract
The objective of the present investigation was to enhance the solubility of practically insoluble mirtazapine by preparing nanosuspension, prepared by using solvent anti solvent technology. Mirtazapine is practically insoluble in water which act as antidepressant .It was prepared as nano particles in order to improve its solubility and dissolution rate. Twenty formulas were prepared and different stabilizing agents were used with different concentrations such as poly vinyl pyrrolidone (PVPK-90), poly vinyl alcohol (PVA), poloxamer 188 and poloxamer 407. The ratios of drug to stabilizers used to prepare the nanoparticles were 1: 1 and 1:2. The prepared nanoparticles were evaluated for particle size, entrapment efficiency, dissolution study, Fourier transform infrared spectroscopy, differential scanning calorimetry, and atomic force microscopy. The percentage of drug entrapment efficiency of F1-F20 was ranged from 78.2% ± 1 to 95.9 % ± 1. The release rate and extent of mirtazapine nanoparticles were inversely proportional to the particle size of the drug i.e. it decreased when particle size increase. It is concluded that the nanoprecipitation have potential to formulate homogenous nanosuspensions with uniform-sized stable nanoparticles of mirtazapine. The prepared nanosuspension showed enhanced dissolution which may lead to enhanced solubility of mirtazapine.
Highlights
Solubility is of the most important parameterRapid addition of a drug solution to the anti-solvent to achieve the desired concentration of drug in leads to sudden super saturation of drug and systemic circulation for pharmacological response formation of ultrafine crystalline or amorphous drug to be shown
The particle size of F1-F4 at drug : stabilizer ratio 1:1 was ranged from 429 - 691 nm measured by particle size analyzer while for F11-F14 at drug : stabilizer ratio 1:2 the particle size ranged from 379 - 572 nm as in table [4] using poloxamer 188, poloxamer 407, PVP- K90 and poly vinyl alcohol (PVA) as primary stabilizers
Vinyl groups of PVA (Polyvinyl alcohol), due to their hydrophobic nature tend to adsorb onto the hydrophobic part of mirtazapine nanoparticles while –OH extend themselves outside into the aqueous environment and providing stabilization to the nanoparticles and preventing agglomeration. –OH bonds of PVA makes hydrogen bonding with water molecules and viscosity of it increases [19]
Summary
Solubility is of the most important parameter. Rapid addition of a drug solution to the anti-solvent to achieve the desired concentration of drug in leads to sudden super saturation of drug and systemic circulation for pharmacological response formation of ultrafine crystalline or amorphous drug to be shown. Water soluble drugs often solids[2]. Mirtazapine is an antidepressant drug used require high doses in order to reach therapeutic for the treatment of moderate to severe depression, plasma concentrations after oral administration. Low water solubility is the major problem bioavailability of 50 % due to first-pass metabolism, encountered with formulation development of new high protein binding (80 %) and very high half-life chemical entities[1]. The aim of this study is to formulate exist for the manufacturing of nanosuspension, and evaluate mirtazapine nanoparticles using precipitation has been applied to prepare submicron solvent anti solvent method
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Schedule a callMore From: Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512)
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