Characterization Of PEG-Modified Paclitaxel

Wermeckes, Bernd; Heß, Michael; Dehne, Stefanie; Jo, Byung Ook W; Sohn, Jung-Sun

doi:10.1179/mri.2006.10.3.364

Cited by 3 publications

(1 citation statement)

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“…In some of these derivatives, paclitaxel is linked to macromolecules, such as poly(ethyleneglycol) [28,29,30,31,32,33,34,35,36,37,38,39,40,41,42], N -(2-hydroxypropyl)methacrylamide [39,43,44,45,46,47], carboxy-methyldextran [48], poly( l -glutamic acid) [49,50,51,52,53,54,55,56,57,58,59,60,61,62,63,64,65,66,67,68,69,70,71,72,73,74], peptides [75,76], proteins [77,78,79], dendrimers [37,42,80,81] and HA [82,83,84,85,86,87]. Joining a bioactive compound to a biocompatible polymer offers, in general, several advantages like better drug solubilization, stabili...…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis and Applications of Hyaluronic Acid-Paclitaxel Bioconjugates†

et al. 2008

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Paclitaxel (1a), a well known antitumor agent adopted mainly for the treatment of breast and ovarian cancer, suffers from significant disadvantages such as low solubility, certain toxicity and specific drug-resistance of some tumor cells. To overcome these problems extensive research has been carried out. Among the various proposed strategies, the conjugation of paclitaxel (1a) to a biocompatible polymer, such as hyaluronic acid (HA, 2), has also been considered. Coupling a bioactive compound to a biocompatible polymer offers, in general, many advantages such as better drug solubilization, better stabilization, specific localization and controlled release. Hereafter the design, synthesis and applications of hyaluronic acid-paclitaxel bioconjugates are reviewed. An overview of HA-paclitaxel combinations is also given.

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Section: Introductionmentioning

confidence: 99%

Design, Synthesis and Applications of Hyaluronic Acid-Paclitaxel Bioconjugates†

et al. 2008

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Biarmed Poly(ethylene glycol)-(pheophorbide a)₂ Conjugate as a Bioactivatable Delivery Carrier for Photodynamic Therapy

Kim

Cho

et al. 2014

Biomacromolecules

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In the study presented here, we developed a bioreducible biarmed methoxy poly(ethylene glycol)-(pheophorbide a)2 (mPEG-(ss-PhA)2) conjugate for cancer-cell-specific photodynamic therapy (PDT). PhA molecules were chemically conjugated with biarmed linkages at one end of the mPEG molecule via disulfide bonds. Under aqueous conditions, the amphiphilic mPEG-(ss-PhA)2 conjugate self-assembled to form core-shell-structured nanoparticles (NPs) with good colloidal stability. The mPEG-(ss-PhA)2 NPs exhibited intramolecular and intermolecular self-quenching effects that enabled the NPs to remain photoinactive in a physiological buffer. However, the dissociation of the NP structure was effectively induced by the cleavage of the disulfide bonds in response to intracellular reductive conditions, triggering the rapid release of PhA molecules in a photoactive form. In cell-culture systems, in addition to significant phototoxicity and intracellular uptake, we observed that the dequenching processes of PhA in the mPEG-(ss-PhA)2 NPs highly depended on the expression of intracellular thiols and that supplementation with glutathione monoethylester facilitated more rapid PhA release and enhanced the PhA phototoxicity. These findings suggest that the bioreducible activation mechanism of mPEG-(ss-PhA)2 NPs in cancer cells can maximize the cytosolic dose of active photosensitizers to achieve high cytotoxicity, thereby enhancing the treatment efficacy of photodynamic cancer treatment.

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Polymer prodrug approaches applied to paclitaxel

et al. 2010

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Paclitaxel possesses a unique mechanism of drug action as a new class of microtubule stabilizing agent which finally leads to disrupted mitosis and cell death. Recent findings have shown that paclitaxel initiates apoptosis through multiple mechanisms. However, the strong hydrophobicity of paclitaxel drastically limits its use in natural form. In addition, significant toxicity which is mainly ascribed to the non-specific, indiscriminate distribution among the tissues limited the application of paclitaxel in cancer therapy. Therefore, it remains of interest to improve their use by enhancing solubility, selectivity and in vivo delivery by preparing functional prodrugs selectively activable in tumour areas. This article summarizes results and information derived recently from paclitaxel prodrugs based mainly on macromolecular conjugates and their interactions with body fluids. We also explore the potential application of site-specific carriers in the development of tumor-targeting paclitaxel conjugates.

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Characterization Of PEG-Modified Paclitaxel

Cited by 3 publications

References 10 publications

Design, Synthesis and Applications of Hyaluronic Acid-Paclitaxel Bioconjugates†

Design, Synthesis and Applications of Hyaluronic Acid-Paclitaxel Bioconjugates†

Biarmed Poly(ethylene glycol)-(pheophorbide a)₂ Conjugate as a Bioactivatable Delivery Carrier for Photodynamic Therapy

Polymer prodrug approaches applied to paclitaxel

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Characterization Of PEG-Modified Paclitaxel

Cited by 3 publications

References 10 publications

Design, Synthesis and Applications of Hyaluronic Acid-Paclitaxel Bioconjugates†

Design, Synthesis and Applications of Hyaluronic Acid-Paclitaxel Bioconjugates†

Biarmed Poly(ethylene glycol)-(pheophorbide a)2 Conjugate as a Bioactivatable Delivery Carrier for Photodynamic Therapy

Polymer prodrug approaches applied to paclitaxel

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Biarmed Poly(ethylene glycol)-(pheophorbide a)₂ Conjugate as a Bioactivatable Delivery Carrier for Photodynamic Therapy