A novel solid dispersion system for natural product-loaded medicine: silymarin-loaded solid dispersion with enhanced oral bioavailability and hepatoprotective activity

Abstract

A surface-attached silymarin-loaded solid dispersion with improved dissolution profile and enhanced oral bioavailability was formulated using silymarin, polyvinylpyrrolidone (PVP) and Tween 80 in water. In this solid dispersion, hydrophilic PVP was adhered onto the surface of crystalline drug rendering silymarin hydrophilic without changing its crystallinity. The drug solubility from the optimised solid dispersion prepared with silymarin/PVP/Tween 80 at the weight ratio of 5/2.5/2.5 increased by almost 650-fold compared to drug powder. The drug was physically and chemically stable in the solid dispersion for at least 6 months. Moreover, the solid dispersion enhanced the oral bioavailability of the drug in rats by almost 3-fold compared to the commercial product. The silymarin-loaded solid dispersion also exhibited advanced hepatoprotective bioactivity against CCl4-induced liver damage compared to silymarin or the commercial product. Thus, this silymarin-loaded solid dispersion would be useful for the enhancement of oral bioavailability and hepatoprotective activity of poorly water-soluble silymarin.

Formulation development and systematic optimization of stabilized ziprasidone hydrochloride capsules devoid of any food effect

“…On coming in contact with the aqueous medium, the polymer helps the drug to attain sufficient wettability and consequently enhanced solubility. The results are in accordance with published literature where improved solubility profiles of low soluble drugs have been attained with solid dispersions [29][30][31][32][33] .…”

Preparation, characterizations and anti-pollutant activity of 7,3′,4′-trihydroxyisoflavone nanoparticles in particulate matter-induced HaCaT keratinocytes

“…32 Previous studies have indicated that PVP K30 serves as a good solubilizing agent to overcome the poor aqueous solubility of drugs such as curcumin 33 and silymarin. 34 Our results also demonstrated that PVP K30 is an appropriate excipient to reduce the particle size and increase the aqueous solubility of raw 734THI using planetary BMT. Moreover, Khutoryanskiy reported that polymers formulated with poorly soluble drugs may improve their aqueous solubility by forming intra-and intermolecular hydrogen bonds.…”

The preparation and physicochemical characterization of eprosartan mesylate-laden polymeric ternary solid dispersions for enhanced solubility and dissolution rate of the drug

“…Solid dispersion − the dispersal of a hydrophobic drug in a hydrophilic polymer with or without the addition of a surfactant − is an excellent strategy to enhance the solubility and dissolution of water-insoluble drugs. [9][10][11][12][13][14][15][16][17][18][19] A solid dispersion prepared with the addition of a surfactant (a ternary solid dispersion) results in greater improvement of the solubility and dissolution of BCS class 2 drugs as compared to solid dispersions prepared without a surfactant (binary solid dispersions). 20 Solid dispersions can be prepared conventionally by the melting method, 21 the kneading method, 22 the solvent evaporation method, 9 or the lyophilization technique.…”