Novel polyglycidol-lipid conjugates create a stabilizing hydrogen-bonded layer around cholesterol-containing dipalmitoyl phosphatidylcholine liposomes

Bakardzhiev, PavelInstitute of Polymers, Bulgarian Academy of Sciences, 103-A Acad. G. Bonchev St., 1113 Sofia, Bulgaria (författare)

Hybrid liposomes resulting from co-assembly of dipalmitoylphosphatidylcholine and polyglycidol-derivatized lipids were prepared. The latter were composed of a lipid-mimetic residue to which a linear polyglycidol chain (degree of polymerization, DP, in the 23â€“110 range) was conjugated. Formulations with varying copolymer type and content were prepared by film hydration technique followed by extrusion. The hybrid structures were studied by means of dynamic and electrophoretic light scattering, cryogenic transmission electron microscopy, and fluorescence spectroscopy. Cytotoxicity towards OPM-2 (multiple myeloma) and EJ (human urinary bladder carcinoma) cell lines was assessed as well. Predominantly unilamellar liposomes with mean hydrodynamic diameters in the 113â€“134Â nm range and neutral to slightly negative surface potential were prepared. The integrity of liposomes containing copolymers with DP of the polyglycidol chain 23 and 30 was preserved at copolymer contents up to 10Â mol%. Bilayer disks were observed at somewhat lower contents of the copolymers of the highest DP of the polyglycidol chain. The hybrid structures were less leaky than the plain liposomes, which was attributed to formation of a strongly hydrogen-bonded polyglycidol layer around the bilayer membrane. They exhibited low toxicological potential, favorable physicochemical characteristics, and ability to act as containers for sustained release.

Momekova, DenitsaDepartment of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, Medical University e Sofia, 2 Dunav St., 1000 Sofia, Bulgaria (författare)
Edwards, KatarinaUppsala universitet,Analytisk kemi(Swepub:uu)kataedwa (författare)
Konstantinov, SpiroDepartment of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University e Sofia, 2 Dunav St., 1000 Sofia, Bulgaria (författare)
Rangelov, StanislavInstitute of Polymers, Bulgarian Academy of Sciences, 103-A Acad. G. Bonchev St., 1113 Sofia, Bulgaria (författare)
Institute of Polymers, Bulgarian Academy of Sciences, 103-A Acad. G. Bonchev St., 1113 Sofia, BulgariaDepartment of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, Medical University e Sofia, 2 Dunav St., 1000 Sofia, Bulgaria (creator_code:org_t)

Ingår i:Journal of Drug Delivery Science and Technology: Elsevier29, s. 90-981773-2247

Av författaren/redakt...: Bakardzhiev, Pav ...; Momekova, Denits ...; Edwards, Katarin ...; Konstantinov, Sp ...; Rangelov, Stanis ...

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