scholarly journals Phosphatidylinositol Stabilizes Fluid-Phase Liposomes Loaded with a Melphalan Lipophilic Prodrug

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 473
Author(s):  
Daria Tretiakova ◽  
Irina Le-Deigen ◽  
Natalia Onishchenko ◽  
Judith Kuntsche ◽  
Elena Kudryashova ◽  
...  

Previously, a liposomal formulation of a chemotherapeutic agent melphalan (Mlph) incorporated in a fluid lipid bilayer of natural phospholipids in the form of dioleoylglyceride ester (MlphDG) was developed and the antitumor effect was confirmed in mouse models. The formulation composed of egg phosphatidylcholine (ePC), soybean phosphatidylinositol (PI), and MlphDG (8:1:1, by mol) showed stability in human serum for at least 4–5 h. On the contrary, replacing PI with pegylation of the liposomes, promoted fast dissociation of the components from the bilayer. In this work, interactions of MlphDG-liposomes with the most abundant plasma protein—albumin—in function of the presence of PI in the formulation were explored using Fourier transform infrared spectroscopy. The release of MlphDG from the liposomes was studied by asymmetrical flow field-flow fractionation (AF4) using micelles formed by a polyethylene glycol conjugate with phosphatidylethanolamine to mimic the physiological lipid sink like lipoproteins. Our results show that PI actually protects the membrane of MlphDG-liposomes from the protein penetration, presumably due to pairing between the positively charged MlphDG and negatively charged PI, which compensates for the heterogeneity of the lipid bilayer. The AF4 technique also evidences high stability of the formulation as a drug carrier.

2018 ◽  
Vol 28 (2) ◽  
pp. 429-432
Author(s):  
Dilyana Zvezdova

Chitosan, a hydrophilic biopolymer industrially obtained by N-deacetylation of chitin, can be applied as an antimicrobial agent. It highlights the applications of chitosan as an antimicrobial agent against fungi, bacteria, and viruses and as an elicitor of plant defense mechanisms. A series of novel chitosan-sulfathiazole nanocomposite (CSFZ) films were prepared by using solvent casting method for wound healing application. Fourier transform infrared spectroscopy (FTIR) was employed to ascertain the interaction between negatively charged sulfathiazole and positively charged chitosan. Moreover, the antibacterial activity of the films was investigated against gram positive and gram negative microorganisms. It was found that all CSFZ films showed good inhibitory activity against all the tested bacteria as compared to control. The above analysis suggested that the CSFZ films could be used as potential candidates for wound healing application.


Nanoscale ◽  
2018 ◽  
Vol 10 (22) ◽  
pp. 10609-10619 ◽  
Author(s):  
Stephen C. L. Hall ◽  
Cecilia Tognoloni ◽  
Jack Charlton ◽  
Éilís C. Bragginton ◽  
Alice J. Rothnie ◽  
...  

Positively charged poly(styrene-co-maleimide) extracts functional membrane proteins into nanodiscs, overcoming some limitations of current nanodisc technology.


2000 ◽  
Vol 55 (9-10) ◽  
pp. 758-763 ◽  
Author(s):  
Janina Gabrielska ◽  
Teresa Kral ◽  
Marek Langner ◽  
Stanislaw Przestalski

Abstract Phenyltins are chemicals widely used in industry, hence their occurrence in the human environment is frequent and widespread. Such compounds include hydrophobic phenyl rings bonded to positively charged tin. This molecular structure makes them capable of adsorbing onto and penetrating through biological membranes, hence they are potentially hazardous. Two such compounds, diphenyltin and triphenyltin, show different steric constraints when interacting with the lipid bilayer. It has been demonstrated that these compounds are positioned at different locations within model lipid bilayers, causing dissimilarity in their ability to affect membrane properties. In this paper we present a study regarding the ability of these two phenyltins to facilitate the transport of S2O4-2 ions across the lipid bilayer, evaluated by a fluorescence quenching assay. In concentration range of up-to 60 μm those compounds do not affect lipid bilayer topology, when evaluated by vesicle size distribution. Both phenyltins facilitate the transfer of S2O4-2 across the model lipid bilayer, but the dependence of dithionite transport on phenyltin concentration is different for both. In principle, above 20 μm triphenyltin is more efficient in transfering ions across the lipid bilayer than diphenyltin.


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