The preparation of silybin–phospholipid complex and the study on its pharmacokinetics in rats

Xiao, Yanyu; Song, Yunmei; Chen, Zhipeng; Ping, Qineng

doi:10.1016/j.ijpharm.2005.10.001

Cited by 304 publications

(125 citation statements)

References 7 publications

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“…Derivatives of silybin with improved solubility may surmount these pharmacologic limitations [15,16]. The silybin phytosome complex (silybin plus phosphatidylcholine) has been coformulated with vitamin E (Realsil (RA); Istituto Biochimico Italiano, Lorenzini S.p.a., Italy).…”

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confidence: 99%

Silybin combined with phosphatidylcholine and vitamin E in patients with nonalcoholic fatty liver disease: A randomized controlled trial

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Andreone

Brisc

et al. 2012

Free Radical Biology and Medicine

219

147

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The only currently recommended treatment for nonalcoholic fatty liver disease (NAFLD) is lifestyle modification. Preliminary studies of silybin showed beneficial effects on liver function. Realsil (RA) comprises the silybin phytosome complex (silybin plus phosphatidylcholine) coformulated with vitamin E. We report on a multicenter, phase III, double-blind clinical trial to assess RA in patients with histologically documented NAFLD. Patients were randomized 1:1 to RA or placebo (P) orally twice daily for 12 months. Prespecified primary outcomes were improvement over time in clinical condition, normalization of liver enzyme plasma levels, and improvement of ultrasonographic liver steatosis, homeostatic model assessment (HOMA), and quality of life. Secondary outcomes were improvement in liver histologic score and/or decrease in NAFLD score without worsening of fibrosis and plasma changes in cytokines, ferritin, and liver fibrosis markers. We treated 179 patients with NAFLD; 36 were also HCV positive. Forty-one patients were prematurely withdrawn and 138 patients analyzed per protocol (69 per group). Baseline patient characteristics were generally well balanced between groups, except for steatosis, portal infiltration, and fibrosis. Adverse events (AEs) were generally transient and included diarrhea, dysgeusia, and pruritus; no serious AEs were recorded. Patients receiving RA but not P showed significant improvements in liver enzyme plasma levels, HOMA, and liver histology. Body mass index normalized in 15% of RA patients (2.1% with P). HCV-positive patients in the RA but not the P group showed improvements in fibrogenesis markers. This is the first study to systematically assess silybin in NAFLD patients. Treatment with RA but not P for 12 months was associated with Free

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mentioning

confidence: 99%

Silybin combined with phosphatidylcholine and vitamin E in patients with nonalcoholic fatty liver disease: A randomized controlled trial

Loguercio

Andreone

Brisc

et al. 2012

Free Radical Biology and Medicine

219

147

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“…Owing to its high resolution, selectivity, and convenience, highperformance liquid chromatography (HPLC) is an important analytical tool in the study of food, herbal medicines, and other natural extracts. [16][17][18][19] Chemical fingerprints based on chromatographic profiles have been recommended as a method for assessing natural products. 20 Similarity evaluation or pattern recognition algorithms can be applied to such chromatographic fingerprints to identify the chemical richness or novelty of complex mixtures, and many studies on chromatographic fingerprint methods have now been reported.…”

Section: Introductionmentioning

confidence: 99%

Chromatographic Fingerprint-Bioactivity Relationships of the Antitumor Properties of Bufo bufo gargarizans Skin Extracts

et al. 2016

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Statistical analyses of high-performance liquid chromatography (HPLC)-based chemical fingerprints of Bufo bufo gargarizans toad skin extracts were integrated with antitumor evaluations as a means to more effectively identify bioactive constituents. Specifically, chemical fingerprints of Bufo bufo gargarizans skin extract samples obtained from ten different regions in China were generated by HPLC, and then subjected to similarity analysis and principal component analysis (PCA). Concurrently, a MCF-7 breast cancer cell model was adopted to obtain the antitumor activity of different toad skin extracts. The chromatographic fingerprint-bioactivity relationships of the Bufo bufo gargarizans extracts were then evaluated by Pearson correlation analysis. The results demonstrated that all skin extract samples inhibited the proliferation of MCF-7 cells to some extent, and that there was a correlation between the chemical fingerprints and the anti-proliferative activity. Bufotalin, bufalin, and cinobufagin, three known components of Bufo bufo gargarizans that were identified in the chemical fingerprints, were highlighted as constituents responsible for the observed bioactivity. The activity of cinobufagin was confirmed by cell viability and colony formation assays using MCF-7 cells. The approach documented here provides a more effective means to associate chemical information on medicinal extracts with the principle components responsible for their bioactivity, and to therefore expedite drug discovery.

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“…The recent developments were to improve the therapeutic performance of the conventional drug by formulating them as new drug delivery system, which could maximize the properties of these molecules (Yanyu et al, 2006;Sharma et al, 2010). Phyto-medicines complexes are chemical mixtures, prepared from herbal drugs, showed a high percentage of drug loading, which makes the delivery of drug clinically feasible (Semalty et al, 2010).…”

Section: Discussionmentioning

confidence: 99%

Development, characterization and toxicological evaluations of phospholipids complexes of curcumin for effective drug delivery in cancer chemotherapy

et al. 2014

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The purpose of this study was to prepare and characterize the complexes between curcumin (CU) phosphatidylcholine (PC) and hydrogenated soya phosphatidylcholine (HSPC) and to evaluate their anticancer activity. These CU-PC and CU-HSPC complexes (CU-PC-C and CU-HSPC-C) were evaluated for various physical parameters like Fourier transform infrared spectroscopy, melting point, solubility, scanning electron microscopy and the in vitro drug release study. These data confirmed the formation of phospholipids complexes. The in vitro hemolysis study showed that the complex was non-hemolytic. The anti-cancer potential of the complexes was demonstrated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay in MCF-7 cell line. This increase may be due to the amphiphilic nature of the complexes, which significantly enhances the water and lipid solubility of the CU. Unlike the free CU (which showed a total of only 90% drug release at the end of 8 h), complex showed around 40-60% release at the end of 8 h in dissolution studies. It showed that (when given in equimolar doses) complexes have significantly decreased the amount of CU available for absorption as compared with CU-free drug. Both CU-PC-C and CU-HSPC-C were found to be non-toxic at the dose equivalent to 2000 mg/kg of body weight of CU in the toxicity study. Acute and subacute toxicity studies confirmed the oral safety of the formulation. A series of genotoxicity studies was conducted, which revealed the non-genotoxicity potential of the developed complexes. Thus, it can be concluded that the phospholipid complexes of CU may be a promising candidate in cancer therapy.

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The preparation of silybin–phospholipid complex and the study on its pharmacokinetics in rats

Cited by 304 publications

References 7 publications

Silybin combined with phosphatidylcholine and vitamin E in patients with nonalcoholic fatty liver disease: A randomized controlled trial

Silybin combined with phosphatidylcholine and vitamin E in patients with nonalcoholic fatty liver disease: A randomized controlled trial

Chromatographic Fingerprint-Bioactivity Relationships of the Antitumor Properties of Bufo bufo gargarizans Skin Extracts

Development, characterization and toxicological evaluations of phospholipids complexes of curcumin for effective drug delivery in cancer chemotherapy

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