Thermosensitive Micelles Based on Folate‐Conjugated Poly(N‐vinylcaprolactam)‐block‐Poly(ethylene glycol) for Tumor‐Targeted Drug Delivery

Abstract

Thermosensitive PNVCL-b-PEG block copolymer coupled with folic acid was prepared as an anti-cancer drug carrier. This polymer self-assembled into stable micelles in aqueous solutions at above 33 degrees C. At 37 degrees C, the release profile of PNVCL-b-PEG-FA micelles showed a slower and more controlled release of the entrapped 5-FU than that at 25 degrees C. The blank and 5-FU-loaded PNVCL-b-PEG-FA micelles did not induce remarkable cytotoxicity against the EA.hy 926 human endothelial cell line; however, 5-FU-loaded PNVCL-b-PEG-FA micelles showed a cytotoxicity effect against 4T1 mouse mammary carcinoma cells due to the availability of loaded anti-cancer drugs delivered to the inside of the cancer cells by the folate-receptor-mediated endocytosis process.

Synthesis and characterization of “Living” star‐shaped poly(N‐vinylcaprolactam) with four arms and carboxylic acid end groups

“…[23][24][25] To date, no more than 16 articles have been reported on RAFT/MADIX polymerization of NVCL. 5,[23][24][25][26][27][28][29][30][31][32][33][34][35][36][37][38] Although some chain transfers agents (CTAs) have been successfully applied for the polymerization of NVCL, the control of polymerization was not demonstrated to be straightforward. For example, it has been reported that the use of dithioesters have not been effective in the polymerization of N-vinyl monomers 28 ; furthermore, only some selected dithiocarbamates, trithiocarbonates and xanthates have been reported to be effective for the controlled polymerization of PNVCL.…”

Stimuli-Responsive Polymeric Nanocarriers as Promising Drug and Gene Delivery Systems

“…In addition to PNIPAM, other thermo-responsive polymers such as PVCL, poly(2-hydroxyethyl methacrylate lactate) and poly(2-hydroxypropyl methacrylate lactate) (p(HPMA-Lac n ) have also been investigated as thermo-responsive core for block copolymer micelles (Prabaharan et al 2009;Rijcken et al 2007a). Hennink and co-workers developed thermo-responsive PEG-b-p(HPMA-Lac n ) block copolymer micelles and investigated as a carrier of PTX, photosensitizer and superparamagnetic iron oxide nanoparticles, for chemotherapy, photodynamic therapy, and magnetic resonance imaging, respectively (Soga et al 2005;Rijcken et al 2007b;Talelli et al 2009).…”

Síntese e caracterização de copolímeros em blocos biocompatíveis do tipo poli (N-vinilcaprolactama)-b-poli(etileno glicol) para encapsulação do cetoprofeno utilizando a técnica de secagem por atomização

“…Além disso, possui uma baixa taxa de deposição de material proteico, diminuindo sua ligação às proteínas plasmáticas, agregação de eritrócitos e impedindo o reconhecimento pelo sistema imunológico. Assim, o emprego de segmentos de PEG como bloco hidrofílico na elaboração de micelas poliméricas, pode impedir que o agente ativo sofra ataques indesejáveis em meios biológicos prolongando a sua circulação in vivo (PRABAHARAN et al, 2009).…”

“…Durante esse processo uma estrutura núcleo/casca (core/shell) pode se formar devido à fração de mPEG no copolímero, uma vez que seus segmentos são hidrofílicos independentemente da temperatura de ensaio. Sua presença na interface partícula-água fornece estabilidade coloidal ao sistema, formado assim, uma estrutura com núcleo constituído de PNVCL e a casca de mPEG, como reportado por Prabaharan et al (2009). Durante esse rearranjo estrutural, algumas moléculas de fármaco podem se desprender das partículas, sendo dissolvidas no meio de liberação, enquanto outras permanecem no núcleo.…”

“…As interações PNVCL/cetoprofeno podem reter as moléculas de fármaco por mais tempo, diminuindo, assim, a liberação do cetoprofeno para o meio de dissolução (PRABAHARAN et al, 2009). …”