* Zobrazit nápovědu

16 záznamů v Medvik Filtry

Článek

In Vitro and in Vivo Behavior of Liposomes Decorated with PEGs with Different Chemical Features

Mastrotto, Francesca
Autor Mastrotto, Francesca Department of Pharmaceutical and Pharmacological Sciences , University of Padova , via F. Marzolo 5 , 35131 Padova , Italy
Brazzale, Chiara
Autor Brazzale, Chiara Department of Pharmaceutical and Pharmacological Sciences , University of Padova , via F. Marzolo 5 , 35131 Padova , Italy
Bellato, Federica
Autor Bellato, Federica Department of Pharmaceutical and Pharmacological Sciences , University of Padova , via F. Marzolo 5 , 35131 Padova , Italy
De Martin, Sara
Autor De Martin, Sara Department of Pharmaceutical and Pharmacological Sciences , University of Padova , via F. Marzolo 5 , 35131 Padova , Italy
Grange, Guillaume
Autor Grange, Guillaume Drug Research Program, Faculty of Pharmacy , University of Helsinki , 00014 Helsinki , Finland
Mahmoudzadeh, Mohamad
Autor Mahmoudzadeh, Mohamad Drug Research Program, Faculty of Pharmacy , University of Helsinki , 00014 Helsinki , Finland
Magarkar, Aniket
Autor Magarkar, Aniket Institute of Organic Chemistry and Biochemistry , Academy of the Sciences of the Czech Republic , 166 10 Prague , Czech Republic
Bunker, Alex
Autor Bunker, Alex Drug Research Program, Faculty of Pharmacy , University of Helsinki , 00014 Helsinki , Finland
Salmaso, Stefano
Autor Salmaso, Stefano Department of Pharmaceutical and Pharmacological Sciences , University of Padova , via F. Marzolo 5 , 35131 Padova , Italy
Caliceti, Paolo
Autor Caliceti, Paolo Department of Pharmaceutical and Pharmacological Sciences , University of Padova , via F. Marzolo 5 , 35131 Padova , Italy

Molecular pharmaceutics. 2020 ; 17 (2) : 472-487. [pub] 20200122

Mol Pharm
ISSN 1543-8392
Medvik
Zdroj

The colloidal stability, in vitro toxicity, cell association, and in vivo pharmacokinetic behavior of liposomes decorated with monomethoxy-poly(ethylene glycol)-lipids (mPEG-lipids) with different chemical features were comparatively investigated. Structural differences of the mPEG-lipids used in the study included: (a) surface-anchoring moiety [1,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE), cholesterol (Chol), and cholane (Chln)]; (b) mPEG molecular weight (2 kDa mPEG45 and 5 kDa mPEG114); and (c) mPEG shape (linear and branched PEG). In vitro results demonstrated that branched (mPEG114)2-DSPE confers the highest stealth properties to liposomes (∼31-fold lower cell association than naked liposomes) with respect to all PEGylating agents tested. However, the pharmacokinetic studies showed that the use of cholesterol as anchoring group yields PEGylated liposomes with longer permeance in the circulation and higher systemic bioavailability among the tested formulations. Liposomes decorated with mPEG114-Chol had 3.2- and ∼2.1-fold higher area under curve (AUC) than naked liposomes and branched (mPEG114)2-DSPE-coated liposomes, respectively, which reflects the high stability of this coating agent. By comparing the PEGylating agents with same size, namely, linear 5 kDa PEG derivatives, linear mPEG114-DSPE yielded coated liposomes with the best in vitro stealth performance. Nevertheless, the in vivo AUC of liposomes decorated with linear mPEG114-DSPE was lower than that obtained with liposomes decorated with linear mPEG114-Chol. Computational molecular dynamics modeling provided additional insights that complement the experimental results.

MeSH
biologická dostupnost MeSH
cholany aplikace a dávkování chemie farmakokinetika MeSH
cholesterol aplikace a dávkování chemie farmakokinetika MeSH
fosfatidylethanolaminy aplikace a dávkování chemie farmakokinetika MeSH
HeLa buňky MeSH
lidé MeSH
lipidy MeSH
liposomy MeSH
molekulová hmotnost MeSH
myši inbrední BALB C MeSH
myši MeSH
nosiče léků farmakokinetika MeSH
polyethylenglykoly aplikace a dávkování chemie farmakokinetika MeSH
povrchové vlastnosti MeSH
příprava léků metody MeSH
simulace molekulární dynamiky MeSH
stabilita léku MeSH
zvířata MeSH
Check Tag
lidé MeSH
myši MeSH
zvířata MeSH
Publikační typ
časopisecké články MeSH

Článek online

Consumption of pistachio nuts beneficially affected blood lipids and total antioxidant activity in rats fed a high-cholesterol diet

Folia biologica (Praha). 2009 ; 55 (4) : 132-136.

ISSN 0015-5500
Medvik
Zdroj

Although nuts are typically high in dietary fat, novel studies have shown that regular consumption of these heart-healthy foods might confer a beneficial effect on cardiovascular disease risk. In the present study, we aimed to analyse the effects of pistachio consumption on blood lipids, antioxidant activity, oxidative stress and sialic acid levels in high-fat-fed rats for 8 weeks. The oxidant-antioxidant status was evaluated by the determination of lipid peroxidation (thiobarbituric acid-reactive substances), total antioxidant activity, reduced glutathione content, activity of superoxide dismutase and total thiol levels. Furthermore, tissue damage was evaluated by total sialic acid levels in serum. Total cholesterol, triglycerides, sialic acid and thiobarbituric acid-reactive substances significantly increased whereas total antioxidant activity, reduced glutathione, total thiol levels significantly decreased in the hyperlipidaemic group compared to the control group. Pistachio consumption significantly decreased triglycerides and thiobarbituric acid-reactive substance levels and significantly increased total antioxidant activity in the hyperlipidaemic group. In conclusion, pistachio supplementation may improve blood lipids and ameliorate oxidative stress in experimental hyperlipidaemia, which may have beneficial applications in the prevention of cardiovascular diseases. However, its antioxidant mechanisms remain to be investigated.