Folate-conjugated methoxy poly(ethylene glycol)/poly(ɛ-caprolactone) amphiphilic block copolymeric micelles for tumor-targeted drug delivery

Park, Eun Kyoung; Kim, So Yeon; Lee, Sang Bong; Lee, Young Moo

doi:10.1016/j.jconrel.2005.09.039

Cited by 236 publications

(145 citation statements)

References 35 publications

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“…In tumor treatment the micelles system has proven effective in regression of tumor size while minimizing damage to the healthy tissues [4] and is being actively investigated in conjunction with hyperthermia [5], ultrasound [6], specific enzyme-induced cleavable bonds [7][8][9], and specific ligands or antibodies [10][11][12][13] for active targeting purposes.…”

Section: Introductionmentioning

confidence: 99%

Tumor pH-responsive flower-like micelles of poly(l-lactic acid)-b-poly(ethylene glycol)-b-poly(l-histidine)

Lee

Kim

et al. 2007

Journal of Controlled Release

421

267

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Polymeric micelles were constructed from poly(L-lactic acid) (PLA; M n 3K)-b-poly(ethylene glycol) (PEG; M n 2K)-b-poly(L-histidine) (polyHis; M n 5K) as a tumor pH-specific anticancer drug carrier. Micelles (particle diameter: ~ 80 nm; critical micelle concentration (CMC): 2 µg/ml) formed by dialysis of the polymer solution in dimethylsulfoxide (DMSO) against pH 8.0 aqueous solution, are assumed to have a flower-like assembly of PLA and polyHis blocks in the core and PEG block as the shell. The pH-sensitivity of the micelles originates from the deformation of the micellar core due to the ionization of polyHis at a slightly acidic pH. However, the co-presence of pH-insensitive lipophilic PLA block in the core prevented disintegration of the micelles and caused swelling/ aggregation. A fluorescence probe study showed that the polarity of pyrene retained in the micelles increased as pH was decreased from 7.4 to 6.6, indicating a change to a more hydrophilic environment in the micelles. Considering that the size increased up to 580 nm at pH 6.6 from 80 nm at pH 7.4 and that the transmittance of micellar solution increased with decreasing pH, the micelles were not dissociated but rather swollen/aggregated. Interestingly, the subsequent decline of pyrene polarity below pH 6.6 suggested re-self-assembly of the block copolymers, most likely forming a PLA block core while polyHis block relocation to the surface. Consequently, these pH-dependent physical changes of the PLA-b-PEG-b-polyHis micelles provide a mechanism for triggered drug release from the micelles triggered by the small change in pH (pH 7.2-6.5).

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Section: Introductionmentioning

confidence: 99%

Tumor pH-responsive flower-like micelles of poly(l-lactic acid)-b-poly(ethylene glycol)-b-poly(l-histidine)

Lee

Kim

et al. 2007

Journal of Controlled Release

421

267

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“…This differential expression has lead to the development of folate receptor-mediated diagnostic and therapeutic agents for the treatment of various cancers (Liu et al, 2005;Park et al, 2005). In this study, we have prepared and evaluated folate-conjugated micelles as a potential antitumor drug delivery system.…”

Section: Discussionmentioning

confidence: 99%

Isomeric Folate-Conjugated Polymeric Micelles Bind to Folate Receptors and Display Anticancer Effects

Dong¹,

Xie²,

Xie³

et al. 2014

Asian Pacific Journal of Cancer Prevention

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The present study aimed to prepare and evaluate polymeric micelles conjugated with folic acid through α-or γ-carboxyl groups for antitumor efficacy. The isomeric block copolymers, α-and γ-folate-polyethyleneglycoldistearoyl phosphatidylethanolamine (α-and γ-Fol-PEG-DSPE), were produced by solid phase peptide synthesis. Three types of doxorubicin (DOX)-loaded polymeric micelles (MPEG-DSPE-DOX and α-/ γ-Fol-PEG-DSPE-DOX micelles) were prepared via the film formation method. Compared with MPEG-DSPE-DOX micelles, the α-/ γ-Fol-PEG-DSPE-DOX micelles presented a higher cellular uptake behavior in the live cell study. Cell viability percentages were 81.8%, 57.3%, 56.6% at 2 hours for MPEG-DSPE-DOX, α-and γ-Fol-PEG-DSPE-DOX micelles, respectively (p<0.05). Using the KB xenograft tumor model, both α-and γ-folate-conjugated micelles were found to have better antitumor effects with lower toxicity in comparison with MPEG-DSPE-DOX micelles. No difference in in vivo antitumor efficacy was found between α-and γ-Fol-PEG-DSPE-DOX micelles. The folate-conjugated micelles might be a potentially useful strategy for tumor targeting of therapeutic agents, whether grafting with folic acid through α-or γ-carboxyl groups.

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“…Thus, folic acid has been used as a targeting ligand to deliver therapeutic agents to cancer cells due to its high binding affinity to folate receptors, low immunogenicity, ease of modification, small size and functional stability (Park et al, 2005). Several folate-drug conjugates have been reported in the literatures, such as folate-low molecular weight drugs , Aronov et al, 2003, Satyam, 2008, folate-liposomes (Gabizon et al, 2004, Shi et al, 2002, Wu et al, 2006, Xiang et al, 2008, folate-gene vectors (Kim et al, 2007, Liang et al, 2008, Yoshida et al, 2006, folate-nanoparticles (Pan andFeng, 2008, Chen et al, 2008), folate-micelles (Park et al, 2005, Alemdaroglu et al, 2008, Kim et al, 2008, Yang et al, 2008, Chu et al, 2009, folate-prodrugs (Henne et al, 2006, Suzuki et al, 2007, Cavallaro et al, 2006, folate-imaging agents (KE et al, 2004.…”

Section: Research Articlementioning

confidence: 99%

“…Therefore, targeting delivery of anticancer drugs has been widely investigated because it would not only improve therapeutic efficiency but also reduce the dose of drug that must be administered to achieve a therapeutic response, thus minimizing negative side effects (PARK et al, 2005). Recently, ligand-mediated targeting of anticancer drugs to tumor cells that express selectively or overexpress receptors has become a promising strategy for improving the therapeutic effect (SAPRA and ALLEN, 2003, MAJUMDAR et al, 2004, QIAN et al, 2002, DE et al, 2008.…”

Section: Introductionmentioning

confidence: 99%

Folate-conjugated methoxy poly (ethylene glycol)/poly (L-Alanine) amphiphilic block copolymeric micelles for targeted delivery of paclitaxel

2011

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Folate-conjugated methoxy poly(ethylene glycol)/poly(ɛ-caprolactone) amphiphilic block copolymeric micelles for tumor-targeted drug delivery

Cited by 236 publications

References 35 publications

Tumor pH-responsive flower-like micelles of poly(l-lactic acid)-b-poly(ethylene glycol)-b-poly(l-histidine)

Tumor pH-responsive flower-like micelles of poly(l-lactic acid)-b-poly(ethylene glycol)-b-poly(l-histidine)

Isomeric Folate-Conjugated Polymeric Micelles Bind to Folate Receptors and Display Anticancer Effects

Folate-conjugated methoxy poly (ethylene glycol)/poly (L-Alanine) amphiphilic block copolymeric micelles for targeted delivery of paclitaxel

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