Poly(HPMA)–chlorambucil conjugate nanoparticles: facile fabrication and in vitro anti-cancer activity
| Autor: | Xinhe Shi, Haining Li, Jia Zhang, Lu-Mei Pu, Guichen Li, Xu Weibing, Minzhi Zhao |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
medicine.diagnostic_test
Chlorambucil food and beverages macromolecular substances General Chemistry Catalysis In vitro Flow cytometry chemistry.chemical_compound chemistry Covalent bond Amphiphile polycyclic compounds Materials Chemistry medicine Biophysics Methacrylamide Cytotoxicity medicine.drug Conjugate |
| Zdroj: | New Journal of Chemistry. 45:18544-18551 |
| ISSN: | 1369-9261 1144-0546 |
| Popis: | Herein, the clinically approved nitrogen mustard, chlorambucil (Chl), is covalently embedded into a poly(N-(2-hydroxypropyl)methacrylamide, HPMA) vector via a hydrolysable ester bond to overcome the shortcomings of Chl as well as to achieve better efficacy. The well-defined poly-prodrug amphiphiles with Chl loading content >10 wt% can form uniform nanoparticles with an average diameter of 200 nm through a macromolecular self-assembly strategy. The detailed structure information and Chl release properties are carefully inspected. Cytotoxicity studies against the HepG2 and MCF-7 cell lines combined with flow cytometry reveal that the poly(HPMA)–Chl conjugate exhibits obvious targeting ability and markedly enhanced antitumor effect compared to the free Chl. After labelling with a fluorescent group, the cell uptake, lysosome escape and distribution in living organs of the poly-prodrug were also studied. |
| Databáze: | OpenAIRE |
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