Relieving PEGylation

Parrott, Matthew C.; DeSimone, Joseph M.

doi:10.1038/nchem.1230

Cited by 58 publications

(47 citation statements)

References 7 publications

(7 reference statements)

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“…For protein protection, PEG is the standard material to be conjugated to a protein, increasing protein stability (e.g. against heat, salts, and proteolysis), water solubility, and circulation time in the body [13,15,36]. The resulting PEGylated protein, however, often significantly loses its biological activity [31,[37][38][39][40].…”

Section: Introductionmentioning

confidence: 99%

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Super-hydrophilic zwitterionic poly(carboxybetaine) and amphiphilic non-ionic poly(ethylene glycol) for stealth nanoparticles

2012

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Section: Introductionmentioning

confidence: 99%

“…In addition to its hydrophilic property, PEG also has a hydrophobic character [13,34,35] although PEG is often considered as a hydrophilic polymer. Because of this amphiphilic feature, PEG is able to dissolve in many organic solvents in addition to water.…”

Section: Introductionmentioning

confidence: 99%

Super-hydrophilic zwitterionic poly(carboxybetaine) and amphiphilic non-ionic poly(ethylene glycol) for stealth nanoparticles

2012

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“…12,13 Recently, nanoparticle (NP)-based anticancer drug delivery systems, especially drug formulations with biodegradable polymeric NPs, have attracted considerable attention for their numerous advantages such as high cellular uptake, enhanced permeability and retention effect, and reduced cancer cell drug resistance. [14][15][16][17] Among the US Food and Drug Administration (FDA)-approved biodegradable polymers, poly(ε-caprolactone) (PCL) has gained considerable interest for drug delivery. However, its slow degradation rate and bad compatibility with soft tissues limit its application in nanomedicine.…”

Section: Introductionmentioning

confidence: 99%

Fabrication of genistein-loaded biodegradable TPGS-b-PCL nanoparticles for improved therapeutic effects in cervical cancer cells

Zhang¹,

Gan²,

Zeng³

et al. 2015

IJN

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Genistein is one of the most studied isoflavonoids with potential antitumor efficacy, but its poor water solubility limits its clinical application. Nanoparticles (NPs), especially biodegradable NPs, entrapping hydrophobic drugs have promising applications to improve the water solubility of hydrophobic drugs. In this work, TPGS- b -PCL copolymer was synthesized from ε-caprolactone initiated by d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) through ring-opening polymerization and characterized by Fourier transform infrared spectroscopy, proton nuclear magnetic resonance spectroscopy, gel permeation chromatography, and thermogravimetric analysis. The genistein-loaded NPs were prepared by a modified nanoprecipitation method and characterized in the aspects of particle size, surface charge, morphology, drug loading and encapsulation efficiency, in vitro drug release, and physical state of the entrapped drug. The TPGS- b -PCL NPs were found to have higher cellular uptake efficiency than PCL NPs. MTT and colony formation experiments indicated that genistein-loaded TPGS- b -PCL NPs achieved the highest level of cytotoxicity and tumor cell growth inhibition compared with pristine genistein and genistein-loaded PCL NPs. Furthermore, compared with pristine genistein and genistein-loaded PCL NPs, the genistein-loaded TPGS- b -PCL NPs at the same dose were more effective in inhibiting tumor growth in the subcutaneous HeLa xenograft tumor model in BALB/c nude mice. In conclusion, the results suggested that genistein-loaded biodegradable TPGS- b -PCL nanoparticles could enhance the anticancer effect of genistein both in vitro and in vivo, and may serve as a potential candidate in treating cervical cancer.

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“…It is encouraging that with the advancement of molecular science and nanotechnology, the nano-drug delivery system provides an effective platform for support. [44][45][46] It has provided an important approach for water-soluble preparation of hydrophobic drugs, targeting, and releasing slowly, which has become a research direction at home and abroad.…”

Section: Discussionmentioning

confidence: 99%

Enhancing the anti-ovarian cancer activity of quercetin using a self-assembling micelle and thermosensitive hydrogel drug delivery system

Wang

et al. 2018

RSC Adv.

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Ovarian cancer, as one of the killers that threaten women's health, has been studied extensively. As a natural bioflavonoid with prospective effects, quercetin is highly recognized for its anti-cancer applications.However, one of the major challenges that quercetin faces is its poor water solubility, instability in physiological media, and subsequent poor bioavailability. Thus, optimizing the ideal drug delivery options is necessary to facilitate the harnessing of the maximum benefits from quercetin. In this study, a quercetin-loaded thermosensitive injectable hydrogel system (Qu-M-hydrogel composites) was constructed based on nanotechnology. Quercetin was encapsulated into MPEG-PCL (with a high drug loading of 7% and minor particle size of 32 nm) and then added into the blank thermosensitive hydrogel Pluronic F-127. The Qu-M-hydrogel composites showed a much slower release than Qu-M in vivo.Moreover, the cytotoxicity, apoptosis induction, and anti-tumor effects of the Qu-M-hydrogel composites on the abdominal SKOV-3 ovarian cancer mouse models were investigated in vivo. Compared with other groups, the Qu-M-hydrogel composites exhibited improved apoptosis induction and cell growth inhibition effects and in vivo trials showed a better balance between the anti-tumor efficacy in the Qu-M-hydrogel composite group than in other groups at an equal drug dose. In conclusion, the prepared Qu-M-hydrogel composites enhanced the anti-tumor activity by providing a high local quercetin concentration, sustained and stable drug release, extended drug retention inside the tumor, and low toxicity to normal tissues. The Qu-M-hydrogel composites might have great potential for clinical application in anti-ovarian cancer activity.

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Relieving PEGylation

Abstract: A new type of protein–polymer conjugate provides improved stability without detrimentally affecting bioactivity, and thus offers great potential for the development of new peptide-based drugs.

Cited by 58 publications

References 7 publications

Super-hydrophilic zwitterionic poly(carboxybetaine) and amphiphilic non-ionic poly(ethylene glycol) for stealth nanoparticles

Super-hydrophilic zwitterionic poly(carboxybetaine) and amphiphilic non-ionic poly(ethylene glycol) for stealth nanoparticles

Fabrication of genistein-loaded biodegradable TPGS-b-PCL nanoparticles for improved therapeutic effects in cervical cancer cells

Enhancing the anti-ovarian cancer activity of quercetin using a self-assembling micelle and thermosensitive hydrogel drug delivery system

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