Preparation of silymarin proliposome: A new way to increase oral bioavailability of silymarin in beagle dogs

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

doi:10.1016/j.ijpharm.2006.03.037

Cited by 120 publications

(49 citation statements)

References 20 publications

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“…It is reported that the plasma concentrations of total metabolites ranged from 0 to 4 µmol/L with an intake of 50 mg aglycone equivalents depending on the flavonoids [38]. Therefore, researchers made many efforts to enhance the oral bioavailability of flavonoids, such as prodrugs of scutellarin [39], phospholipid complex of silybin [40], and proliposome of silymarin [41]. Our results demonstrate that hyperoside could induce osteoblastic differentiation of osteosarcoma cells without cytotoxicity, thus hyperoside could serve as a naturally derived tumour differentiation agent.…”

Section: Discussionmentioning

confidence: 99%

Hyperoside, a Flavonoid Compound, Inhibits Proliferation and Stimulates Osteogenic Differentiation of Human Osteosarcoma Cells

Zhang

Ying

et al. 2014

PLoS ONE

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Osteosarcoma, one of the most common malignant bone tumours, is generally considered a differentiation disease caused by genetic and epigenetic disruptions in the terminal differentiation of osteoblasts. Novel therapies based on the non-cytotoxic induction of cell differentiation-responsive pathways could represent a significant advance in treating osteosarcoma; however, effective pharmaceuticals to induce differentiation are lacking. In the present study, we investigated the effect of hyperoside, a flavonoid compound, on the osteoblastic differentiation of U2OS and MG63 osteosarcoma cells in vitro. Our results demonstrated that hyperoside inhibits the proliferation of osteosarcoma cells by inducing G0/G1 arrest in the cell cycle, without causing obvious cell death. Cell migration assay further suggested that hyperoside could inhibit the invasion potential of osteosarcoma cells. Additionally, osteopontin and runt-related transcription factor 2 protein levels and osteocalcin activation were upregulated dramatically in hyperoside-treated osteosarcoma cells, suggesting that hyperoside may stimulates osteoblastic differentiation in osteosarcoma cells. This differentiation was accompanied by the activation of transforming growth factor (TGF)-β and bone morphogenetic protein-2, suggesting that the hyperoside-induced differentiation involves the TGF-β signalling pathway. To our knowledge, this study is the first to evaluate the differentiation effect of hyperoside in osteosarcoma cells and assess the possible potential for hyperoside treatment as a future therapeutic approach for osteosarcoma differentiation therapy.

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Section: Discussionmentioning

confidence: 99%

Hyperoside, a Flavonoid Compound, Inhibits Proliferation and Stimulates Osteogenic Differentiation of Human Osteosarcoma Cells

Zhang

Ying

et al. 2014

PLoS ONE

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“…, 2006). The SPC used in the present study was produced with phosphatidylcholine by a method that forms a ‘phytosome’ that has properties distinct from liposomes or proliposomes (Yan‐Yu et al. , 2006; Yanyu et al.…”

Section: Discussionmentioning

confidence: 99%

Bioavailability of a silybin–phosphatidylcholine complex in dogs

Filburn

Kettenacker

Griffin

2007

Vet Pharm & Therapeutics

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Liver dysfunction often is associated with an imbalance in the production and removal of free radicals derived from oxygen and nitrogen and has been managed clinically with antioxidant supplements, including silymarin extract derived from milk thistle. The potential for enhanced bioavailability of a phytosome complex containing phosphatidylcholine and silybin, the primary active flavonolignan in silymarin extract, was tested in dogs. A group of eight beagles (four males, four females) were dosed orally with a silybin-phosphatidylcholine complex (SPC) and a commercially available standardized silymarin extract containing equivalent levels of silybin. Dosing with the SPC resulted in Cmax, Tmax, and AUC0-24 h values (mean+/-SD) for total silybin of 1310+/-880 ng/mL, 2.87+/-2.23 h, and 11,200+/-6520 ng.h/mL, respectively; corresponding values for a standardized silymarin extract were 472+/-383 ng/mL, 4.75+/-2.82 h, and 3720+/-4970 ng.h/mL. A second, separate group of beagles were also dosed with the extract alone, yielding values of 449+/-402 ng/mL, 6.87+/-7.43 h, and 2520+/-2976 ng.h/mL. These data show that a phytosome complex of phosphatidylcholine and silybin markedly enhances bioavailability in dogs.

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“…The proliposome was prepared according to the method reported by Xiao et al 21. the film-deposition on the carrier method with minor modification.…”

Section: Methodsmentioning

confidence: 99%

Formulation development andin vitrocharacterization of proliposomes for topical Delivery of aceclofenac

2008

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Non-steroidal antiinflammatory drugs are routinely prescribed for the patients with rheumatic disease and such patients are at increased risk of serious gastrointestinal complications, when non-steroidal antiinflammatory drugs administered by oral route. The aim of the present study was to develop and characterized a vesicular drug carrier system (proliposome) for topical delivery of aceclofenac to overcome the problems related with oral route. Aceclofenac proliposome were prepared by the film-deposition on carriers method and characterized for size and surface morphology, drug content in both proliposomes and liposomal system, percent yield, in vitro drug release studies and drug permeation studies. The prepared system was also characterized for drug-excipients interaction by Fourier transform infrared spectrophotometer and stability studies. The size and surface morphology were studied using optical microscopy, scanning electron microscopy and transmission electron microscopy. A spherical shape of reconstituted aceclofenac liposome with an average vesicular size of about 500 nm was observed in photomicrographs. The maximum entrapment efficiency of reconstituted liposomes was 80.31% whereas the drug content in proliposomes was found to be more than 90%. In vitro release of drug was significantly retarded indicating sustained release of aceclofenac from proliposomes. Stability study was performed at various temperatures indicating that aceclofenac proliposomes are stable at lower temperature.

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Preparation of silymarin proliposome: A new way to increase oral bioavailability of silymarin in beagle dogs

Cited by 120 publications

References 20 publications

Hyperoside, a Flavonoid Compound, Inhibits Proliferation and Stimulates Osteogenic Differentiation of Human Osteosarcoma Cells

Hyperoside, a Flavonoid Compound, Inhibits Proliferation and Stimulates Osteogenic Differentiation of Human Osteosarcoma Cells

Bioavailability of a silybin–phosphatidylcholine complex in dogs

Formulation development andin vitrocharacterization of proliposomes for topical Delivery of aceclofenac

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