Graft copolymers with tunable amphiphilicity tailored for efficient dual drug delivery via encapsulation and pH-sensitive drug conjugation

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61389013%3A_____%2F20%3A00525612" target="_blank" >RIV/61389013:_____/20:00525612 - isvavai.cz</a>

Výsledek na webu

<a href="https://pubs.rsc.org/en/content/articlelanding/2020/PY/D0PY00609B#!divAbstract" target="_blank" >https://pubs.rsc.org/en/content/articlelanding/2020/PY/D0PY00609B#!divAbstract</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1039/D0PY00609B" target="_blank" >10.1039/D0PY00609B</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Graft copolymers with tunable amphiphilicity tailored for efficient dual drug delivery via encapsulation and pH-sensitive drug conjugation

Popis výsledku v původním jazyce

Polymer-based drug delivery systems may significantly improve cancer therapy. We developed amphiphilic poly(ε-caprolactone)-graft-(poly-N-(2-hydroxypropyl) methacrylamide) copolymers (PCL-graft-pHPMA) with tunable amphiphilicity intended for efficient dual delivery via simultaneous encapsulation of hydrophobic drug, Bcl-2 inhibitor ABT-199, and pH-sensitive conjugation of other chemotherapeutics, doxorubicin, to desired sites, e.g. tumors. Using controlled RAFT polymerization and click chemistry well-defined PCL-graft-pHPMA of diverse Mw and physical properties were prepared. By simple dissolution they self-assembled into highly stable micelles with Dh approximately 25 nm and low critical micelle concentration (around 5 μg mL−1). The total drug payload reached 17 wt% while maintaining system solubility. The micelles exhibited long-term stability in buffers, while they were cleaved in the presence of lipase, thus proving degradation and drug release after uptake to lysosomes of cancer cells with minimal drug leakage during blood circulation. PCL-graft-pHPMA micelles may serve as a long-circulating drug depo for effective dual therapy of diverse malignancies.

Název v anglickém jazyce

Graft copolymers with tunable amphiphilicity tailored for efficient dual drug delivery via encapsulation and pH-sensitive drug conjugation

Popis výsledku anglicky

Polymer-based drug delivery systems may significantly improve cancer therapy. We developed amphiphilic poly(ε-caprolactone)-graft-(poly-N-(2-hydroxypropyl) methacrylamide) copolymers (PCL-graft-pHPMA) with tunable amphiphilicity intended for efficient dual delivery via simultaneous encapsulation of hydrophobic drug, Bcl-2 inhibitor ABT-199, and pH-sensitive conjugation of other chemotherapeutics, doxorubicin, to desired sites, e.g. tumors. Using controlled RAFT polymerization and click chemistry well-defined PCL-graft-pHPMA of diverse Mw and physical properties were prepared. By simple dissolution they self-assembled into highly stable micelles with Dh approximately 25 nm and low critical micelle concentration (around 5 μg mL−1). The total drug payload reached 17 wt% while maintaining system solubility. The micelles exhibited long-term stability in buffers, while they were cleaved in the presence of lipase, thus proving degradation and drug release after uptake to lysosomes of cancer cells with minimal drug leakage during blood circulation. PCL-graft-pHPMA micelles may serve as a long-circulating drug depo for effective dual therapy of diverse malignancies.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

10404 - Polymer science

Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2020

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Polymer Chemistry

ISSN

1759-9954

e-ISSN

—

Svazek periodika

11

Číslo periodika v rámci svazku

27

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

16

Strana od-do

4438-4453

Kód UT WoS článku

000548629600005

EID výsledku v databázi Scopus

2-s2.0-85088905155