Morphology of the Micelles Formed by a Comb-Like PEG-Containing Copolymer Loaded with Antitumor Substances with Different Water Solubilities

Abstract

The controlled delivery of anticancer drugs is driven by their interaction with carrier molecules. By creating complicated micelle-like complexes, amphiphilic polymers provide an opportunity to load drugs of various kinds. In this work, the interaction of the comb-like PEG-containing polymer poly(VEP-co-GMA)-graft-PEG with the water-soluble antitumor antibiotic doxorubicin and new water-insoluble derivatives of thiozalidinone Les-3883 characterized by a high anticancer efficiency has been studied in aqueous solutions by means of the SAXS, DLS, TEM, and photoluminescence methods. The formation of polymer micelles and their complexes with drugs, as well as their structural changes, is observed. The obtained results give evidence that the mechanism of organization of supramolecular complexes depends on the drug solubility in water. A potential capability of poly(VEP-co-GMA)-graft-PEG to prolong the drug circulation lifetime is confirmed.

Covalent Conjugate of Ser-Pro-Cys Tripeptide with PEGylated Comb-Like Polymer as Novel Killer of Human Tumor Cells

“…Synthesis of the comb-like copolymer was conducted, as described earlier. − In Figure , a scheme of its conjugation with the SPC tripeptide is presented.…”

“…Procedures, described earlier, − were used to obtain a micelle-forming surface-active copolymer consisting of the backbone of the PEGylated comb-like polymer and the terminal fragment of the SPC tripeptide.…”

“…The composition of the P4 polymer was calculated from the results of elemental analysis. 8 The content of terminal CGE fragments in the P4 was determined from results of measurement of epoxide groups via back-titration of the residual HCl with KOH 10 1 H NMR spectra were recorded on a Bruker Avance DPX 300 spectrometer at 300.13 MHz. NMR spectra of the boule were recorded in a Bruker Avance DPX 300 at the working frequency of 300.13 MHz from a D 2 O solution.…”

“…Monomer conversion was controlled via dilatometric study . After polymerization was finished, the polymer was purified by precipitation and dried under vacuum until constant weight . A residual PEGMA was removed by dialysis using dialysis bags with pore sizes MWCO 6 kDa (Sigma-Aldrich, USA).…”

Antineoplastic Activity of Water-Soluble Form of Novel Kinase Inhibitor 1-(4-Chlorobenzyl)-3-chloro-4-(3-trifluoromethylphenylamino)-1H-pyrrole-2,5-dione immobilized on Polymeric Poly(PEGMA-co-DMM) Carrier

“…The polymer M5 and MI-1 solutions were mixed, added to 4.25 mL of Saline, and subjected to ultrasound (US) dispersion for 10 s. The solution of free polymer M5 was prepared by dilution of 45 mg of PC in 0.45 mL of DMSO. Next, it was added to the 4.0 mL of physiological solution and subjected to the ultrasound dispersion for 10 s [37], as a result, stable colloidal systems were formed (Figure 2). The size of M5 polymer micelles and drug-filled micellar structures of MI-1/M5 complex was determined by dynamic light scattering method (DLS) that was performed using a DynaPro NanoStar (Wyatt Technology, Santa Barbara, CA, USA).…”