STUDY OF AMPHIPHILIC PROPERTIES OF COPOLYESTERS WITH CHROMOPHORE GROUPS IN THE WATER-OCTANOL SYSTEM

2018;
: 145-151
1
Lviv Polytechnic National University
2
Lviv Polytechnic National University
3
Lviv Polytechnic National University
4
Lviv Polytechnic National University
5
Lviv Polytechnic National University

In recent years, nanoscale forms, except targeted drug delivery to the pathological sites for therapy, can  be functionalized with drugs as well as fluorescent substances therefore their diagnostics and therapeutic potential is enormous. Such nanoscale forms usually are formed due to the self-assembly of biocompatible amphiphilic block copolymers in an aqueous medium. In this case lipophilic fragments of polymer macromolecules form nanocarrier core which can be loaded with molecules of lipophilic drugs. At the same time hydrophilic fragments of macromolecules form the hydration shell of the nanocontainers, which ensures their stability.

This work describes the synthesis of aminofunctional соpolyesters based on the dibasic α-amino acids and polyetherdiols of different nature with simultaneous use as a comonomer of a fluorescent dye of the xanthine series - fluorescein and an investigation of their lyophilicity coefficient, which characterizes the affinity of the molecule to the lipid phase as compared to water. The amphiphilic nature of the obtaining  polymers was provided by the use of monomers of different nature for their synthesis: lipophilic N-derivatives of glutamic acid (GluL, GluSt) and hydrophilic polyether diols.

It was determined the effect of elementary chain structure of macromolecules of new aminofunctional copolyesters with chromophore groups on the partition coefficient thereof in water-octanol system and the experimental and calculated characteristics of the hydrophilic-lipophilic balance (HLB) of macromolecules.

Most of the investigated copolyester have low logarithms of the distribution coefficient LogP = -0.5 ÷ 0.5, and therefore can equally be distributed between the water and lipid phases, which is one of the determining factors in the development of drug delivery systems.

These results suggest that obtained aminofunctional copolyestries with chromophore groups can penetrate into living cells and thereby increase the concentration of drugs in target tissues.

The ability of the engineered nanoparticles to interact with cells and tissues at a molecular level provides them with a distinct advantage over other polymeric or macromolecular substances.

All these are expected to facilitate the development of novel fluorescein-containing diagnostic and therapeutic nanoscale forms for early diagnosis and therapy.

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