Solid state mechanochemical simultaneous activation of the constituents of the Silybum marianum phytocomplex with crosslinked polymers**This paper is dedicated to Professor Fulvio Rubessa, who recently retired from his position as full professor at the Faculty of Pharmacy, University of Trieste, after more than 40 years of distinguished academic career.

Voinovich, Dario; Perissutti, Beatrice; Magarotto, Lorenzo; Ceschia, D.; Guiotto, P.; Bilia, Anna Rita

doi:10.1002/jps.21417

Cited by 18 publications

(3 citation statements)

References 24 publications

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“…In the context of mechanochemical activation of pharmaceutically relevant solids, the first study performed in our group dates back in 2008, and consisted on milling the Silybum Marianum phytocomplex in the presence of two crosslinked polymers [50], namely crosslinked polyvinylpyrrolidone and carboxymethylcellulose sodium that had the function of carrier and stabilizing agents for the activated extract. The 1:1 weight/weight (w/w) and 1:3 w/w extract:carrier mixtures were processed for 60 min using a planetary mill and the resulting solid products were characterized using different solid state techniques.…”

Section: Mechanochemical Activation/mechanochemistrymentioning

confidence: 99%

Better and greener: sustainable pharmaceutical manufacturing technologies for highly bioavailable solid dosage forms

Bertoni

Hasa

Albertini

et al. 2022

Drug Deliv. and Transl. Res.

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Section: Mechanochemical Activation/mechanochemistrymentioning

confidence: 99%

Better and greener: sustainable pharmaceutical manufacturing technologies for highly bioavailable solid dosage forms

Bertoni

Hasa

Albertini

et al. 2022

Drug Deliv. and Transl. Res.

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“…This revealed the formation of H-bond between the drug and -OH group of HPMC E 15LV in dispersion (14). The characteristic peaks at 1600-1300 and below 1300 cm -1 were found to change their intensity in the following order: co-precipitated < spray-dried < kneaded solid dispersion, but the H-bond interaction which occurred in solid disperions resulted in lower peak intensity (7,15). The IR spectra also demonstrate disruption of the crystal lattice (8).…”

Section: Solubility Of Silymarinmentioning

confidence: 99%

Silymarin-solid dispersions: Characterization and influence of preparation methods on dissolution

Sonali¹,

Tejal²,

Thakkar³

et al. 2010

Acta Pharmaceutica

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Seeds of milk thistle (Silybum marianum L. Gaertn, Asteraceae) have been used in medicine for over 2,000 years. Silymarin (SLM), an antihepatotoxic phytocomplex, is a mixture of flavonolignans which has been widely used as a therapeutic agent for a variety of acute and chronic liver diseases. Silymarin is practically insoluble in water; therefore, upon oral administration, its absorption rate in the gastrointestinal tract is low, providing only about 20 to 40 % bioavailability (1).Several approaches have been attempted to improve oral bioavailability of silymarin, complexation with a phospholipid (2), formation of an inclusion complex with b-cyclodextrin and hydroxypropyl-b-cyclodextrin (3), solid dispersion with a hydrophilic polymer such as PEG 6000 (4), selfmicroemulsifying systems (5), co-precipitates (6) and a complex with crosslinked polymers (7). The influence of preparation methodology of silymarin solid dispersions using a hydrophilic polymer on the dissolution performance of silymarin was investigated. Silymarin solid dispersions were prepared using HPMC E 15LV by kneading, spray drying and co-precipitation methods and characterized by FTIR, DSC, XRPD and SEM. Dissolution profiles were compared by statistical and model independent methods. The FTIR and DSC studies revealed weak hydrogen bond formation between the drug and polymer, while XRPD and SEM confirmed the amorphous nature of the drug in co-precipitated solid dispersion. Enhanced dissolution compared to pure drug was found in the following order: co-precipitation > spray drying > kneading methodology (p < 0.05). All preparation methods enhanced silymarin dissolution from solid dispersions of different characteristics. The co-precipitation method proved to be best and provided a stable amorphous solid dispersion with 2.5 improved dissolution compared to the pure drug.

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“…To improve the bioabsorption and bioavailability of silymarin, several strategies have been investigated to modify the physicochemical nature of silymarin; there are solid dispersion, 9 liposome, 10 selfmicroemulsifying drug delivery system, 11 and mechanical activation with hydrophilic polymers. 12 However, report on formulating silymarin in nanoscale remains limited. Nanotechnology is a powerful tool for use in the development of novel drug delivery system.…”

Section: Introductionmentioning

confidence: 99%

Characteristics and Antioxidant Activities of Silymarin Nanoparticles

Hsu

et al. 2012

j nanosci nanotechnol

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Silymarin, a well known hepatoprotective drug, has been routinely used in treating liver disorders. However, its bioavailability and therapeutic efficiency are limited by the poor aqueous solubility. In this study, we used the nanoprecipitation technique to develop a nanoparticles system to improve the solubility of silymarin. The newly developed silymarin nanoparticles were characterized for mean particle size, morphology, intermolecular interaction, crystalline features and dissolution property, as well as assessing for antioxidant activities. Results indicated that a drastic change in the physiochemical properties of silymarin was noted in the form of nanoparticles, as displayed by the extremely small particle size (46.1 +/- 1.73 nm), the formation of intermolecular hydrogen bonding between silymarin and matrix of nanoparticles, and the rendering of amorphous state. These phenomena have contributed to the enhanced dissolution property of silymarin nanoparticles, as well as a greater potency in DPPH radical scavenging, anti-superoxide anion formation, and superoxide anion scavenging activities than the crude silymarin. The present study concludes that silymarin nanoparticles have an improved physicochemical property as demonstrated by an increased solubility and enhanced antioxidant activities.

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Cited by 18 publications

References 24 publications

Better and greener: sustainable pharmaceutical manufacturing technologies for highly bioavailable solid dosage forms

Better and greener: sustainable pharmaceutical manufacturing technologies for highly bioavailable solid dosage forms

Silymarin-solid dispersions: Characterization and influence of preparation methods on dissolution

Characteristics and Antioxidant Activities of Silymarin Nanoparticles

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