Abstract
Silymarin (SM) is a plant extract obtained from Silybum marianum( milk thistle) . It is class II type drug according to Biopharmaceutics Classification System with low bioavailability due to its low solubility.
 Micro/nanonization during crystallization, surface modification and crystal structure modification may improve the dissolution rate of poorly water-soluble drugs.
 The aim of this study was to increase the water solubility and dissolution rate of SM by in-situ micronization using solvent change either by stirring or ultrasonic method. Stabilizers like Gelatin, PVP-K30, HPMC15, Pulullan were used to stabilize the prepared ultrafine crystals. Effect of type and concentration of hydrophilic polymer, solvent: antisolvent volume ratio and the effect of ultrasonic irradiation were studied. The prepared microcrystals were evaluated for their %yield, water solubility, crystals structure by XRD,DSC, and SEM. Particle size and dissolution rate were also tested . Silymarin microcrystals prepared by ultrasonic method and stabilized by 0.1%gelatin using 1:2 solvent: anti-solvent volume ratio showed the best results with particle size reduction from mean diameter of 1.5µm (untrated silymarin) to 0.43µm with uniform morphology and enhanced solubility and dissolution.
Highlights
Many new drugs are poorly water-soluble, with low dissolution and bioavailability [1]
Micro / nanonization during crystallization, surface modification and crystal structure modification may improve the dissolution rate of poorly water-soluble drugs
Resulting in low bioavailability [9].The aim of this study was to enhance the solubility of silymarin by preparing microcrystals by in- situ micronization technique using solvent change process in presence of protective hydrophilic polymers
Summary
Many new drugs are poorly water-soluble, with low dissolution and bioavailability [1]. One way for improving their dissolution rates is by decreasing the particle size. Decreasing the particle size increases the surface area, which results in an increase in the rate of dissolution of these drugs in aqueous media such as body fluids and enhance their absorption and bioavailability[2]. Micro / nanonization during crystallization, surface modification and crystal structure modification may improve the dissolution rate of poorly water-soluble drugs. Several studies have shown that modification of the crystalline form of the drug, by the inclusion of specific additives increases the rate of dissolution which can strongly affect the physicochemical and kinetic properties of the drug from the final product. Micro/nanoparticles can be produced by several techniques such as crystallization/precipitation and solvent evaporation and by spray drying methods[3]
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