Formulation and Evaluation of Silymarin Microcrystals by In- Situ Micronization Technique

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 mo...

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Bibliographic Details
Main Authors: Ala'a Dheia Noor (Author), Eman B.H. Al-Khedairy (Author)
Format: Book
Published: College of Pharmacy University of Baghdad, 2019-06-01T00:00:00Z.
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Summary: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.
Item Description:10.31351/vol28iss1pp1-16
2521-3512
1683-3597