Degradation Behavior of Poly(ε-caprolactone)-<i>b</i>-poly(ethylene glycol)-<i>b</i>-poly(ε-caprolactone) Micelles in Aqueous Solution

Hu, Yong; Zhang, Leyang; Cao, Yiyi; Ge, Haixiong; Jiang, Xiqun; Yang, Changzheng

doi:10.1021/bm049845j

Cited by 126 publications

(92 citation statements)

References 25 publications

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“…Under all circumstances, DLS measurement showed a larger diameter than the TEM determination, probably because of dehydration of micelles and shrinkage of the PEG shell induced by water evaporation under the high vacuum before TEM observation. 28 The SEM photographs of the DTX-loaded PEG-PRL micelles further proved the spherical shape and showed a similar diameter to that of TEM, as shown in Figure 7.…”

Section: Preparation Of Dtx-loaded Micellessupporting

confidence: 58%

Polymeric micelles based on poly(ethylene glycol) block poly(racemic amino acids) hybrid polypeptides: conformation-facilitated drug-loading behavior and potential application as effective anticancer drug carriers

Gu¹,

Xu²,

Sui³

et al. 2012

IJN

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Abstract:In this work, racemic hybrid polypeptides poly(ethylene glycol) (PEG)-bpoly(racemic-leucine) (PRL) copolymers with different leucine residues have been synthesized and characterized. Using docetaxel as a model molecule, the high drug-loaded spherical micelles based on PEG-PRL were prepared successfully using dialysis, with a tunable particle size from 170 nm to 250 nm obtained by changing the length of the hydrophobic blocks. Facilitated drugloading behavior (higher drug-loading ability and easier drug-loading process) of PEG-PRL compared with their corresponding levo forms (PEG-b-poly[levo leucine]) was observed and clarified for the first time. With this facilitation, the highest drug-loading content and efficiency of PEG-PRL micelles can achieve 11.2% ± 0.4% and 67.2% ± 2.4%, respectively. All drugloaded PEG-PRL micelles exhibit a similar release behavior with a sustained release up to 72 hours. The PEG-PRL was shown to be nontoxic against MCF-7 and human umbilical vein endothelial cells up to a concentration of 100 μg/mL, displaying a good biocompatibility. Also, the docetaxel-loaded PEG-PRL micelles were more toxic than the free drug against MCF-7 human breast cancer cells -both dose and time dependent. Therefore, these high docetaxel-loaded micelles based on racemic hybrid polypeptides appear to be a novel promising nanomedicine for anticancer therapy.

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Section: Preparation Of Dtx-loaded Micellessupporting

confidence: 58%

Polymeric micelles based on poly(ethylene glycol) block poly(racemic amino acids) hybrid polypeptides: conformation-facilitated drug-loading behavior and potential application as effective anticancer drug carriers

Gu¹,

Xu²,

Sui³

et al. 2012

IJN

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“…Several studies have shown that hydrogels prepared by PLA segment combining with MPEG backbone had good amphiphilicity, thus making them dissolve well in both polar and non-polar solvents. Meanwhile, their biodegradation could also be enhanced (Hu et al, 2004). As a kind of unsaturated dicarboxylic acids, the structure of itaconic acid (IA) contains two carboxyl groups, which could significantly improve the pH-responsive ability of the obtained hydrogels synthesized by it (Milašinović et al, 2010).…”

Section: Introductionmentioning

confidence: 99%

Assessment of the drug loading, in vitro and in vivo release behavior of novel pH-sensitive hydrogel

Dong

You

et al. 2014

Drug Delivery

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, then mixing them together to prepare hydrogel through the heat-initiated free radical polymerization method. Differential scanning calorimetry and X-ray diffraction methods were used to verify whether dexamethasone was loaded into hydrogels. In vitro drug release behavior and in vivo pharmacokinetic study were also investigated in detail.Results: Dexamethasone was successfully loaded into hydrogel, and its loading capacity was improved (5 mg/g). Both the in vitro release study and the in vivo pharmacokinetic study showed the good colon-targeting character of the pH-sensitive P(LE-IA-MEG) hydrogel (T max ¼ 1.0 h, C max ¼ 2.16 mg/ml of dexamethasone; T max ¼ 3.9 h, C max ¼ 0.43 mg/ml of dexamethasone hydrogel). Discussion: Dexamethasone could be targeted to the colon site by P(LE-IA-MEG) hydrogel, thereby improving its therapeutic effect and reduce its side effects. Conclusion: P(LE-IA-MEG) hydrogel might have great potential application in colon-targeted drug delivery systems. KeywordsDexamethasone, drug-loading, in vitro drug release study, in vivo pharmacokinetic study, pH-sensitive History

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“…PEG is hydrophilic, nontoxic, and nonimmunogenic. 18,19 Therefore, the MPEG-PCL copolymer is biodegradable and biocompatible. The MPEG-PCL micelle is nontoxic, easy to produce, monodispersed and appropriately small.…”

Section: Introductionmentioning

confidence: 99%

Preparation, characterization and application of star-shaped PCL/PEG micelles for the delivery of doxorubicin in the treatment of colon cancer

Gao¹,

Wang²,

Wei³

et al. 2013

IJN

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Star-shaped polymer micelles have good stability against dilution with water, showing promising application in drug delivery. In this work, biodegradable micelles made from star-shaped poly(ε-caprolactone)/poly(ethylene glycol) (PCL/PEG) copolymer were prepared and used to deliver doxorubicin (Dox) in vitro and in vivo. First, an acrylated monomethoxy poly (ethylene glycol)-poly(ε-caprolactone) (MPEG-PCL) diblock copolymer was synthesized, which then self-assembled into micelles, with a core-shell structure, in water. Then, the double bonds at the end of the PCL blocks were conjugated together by radical polymerization, forming star-shaped MPEG-PCL (SSMPEG-PCL) micelles. These SSMPEG-PCL micelles were monodispersed (polydispersity index = 0.11), with mean diameter of ≈25 nm, in water. Blank SSMPEG-PCL micelles had little cytotoxicity and did not induce obvious hemolysis in vitro. The critical micelle concentration of the SSMPEG-PCL micelles was five times lower than that of the MPEG-PCL micelles. Dox was directly loaded into SSMPEG-PCL micelles by a pH-induced self-assembly method. Dox loading did not significantly affect the particle size of SSMPEG-PCL micelles. Dox-loaded SSMPEG-PCL (Dox/SSMPEG-PCL) micelles slowly released Dox in vitro, and the Dox release at pH 5.5 was faster than that at pH 7.0. Also, encapsulation of Dox in SSMPEG-PCL micelles enhanced the anticancer activity of Dox in vitro. Furthermore, the therapeutic efficiency of Dox/SSMPEG-PCL on colon cancer mouse model was evaluated. Dox/SSMPEG-PCL caused a more significant inhibitory effect on tumor growth than did free Dox or controls (P , 0.05), which indicated that Dox/SSMPEG-PCL had enhanced anticolon cancer activity in vivo. Analysis with terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) showed that Dox/SSMPEG-PCL induced more tumor cell apoptosis than free Dox or controls. These results suggested that SSMPEG-PCL micelles have promising application in doxorubicin delivery for the enhancement of anticancer effect.

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Degradation Behavior of Poly(ε-caprolactone)-b-poly(ethylene glycol)-b-poly(ε-caprolactone) Micelles in Aqueous Solution

Cited by 126 publications

References 25 publications

Polymeric micelles based on poly(ethylene glycol) block poly(racemic amino acids) hybrid polypeptides: conformation-facilitated drug-loading behavior and potential application as effective anticancer drug carriers

Polymeric micelles based on poly(ethylene glycol) block poly(racemic amino acids) hybrid polypeptides: conformation-facilitated drug-loading behavior and potential application as effective anticancer drug carriers

Assessment of the drug loading, in vitro and in vivo release behavior of novel pH-sensitive hydrogel

Preparation, characterization and application of star-shaped PCL/PEG micelles for the delivery of doxorubicin in the treatment of colon cancer

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