Methoxy poly(ethylene glycol) and ϵ-caprolactone amphiphilic block copolymeric micelle containing indomethacin.

Kim, So Yeon; Shin, Il Gyun; Lee, Young Moo; Cho, Chong Su; Sung, Yong Kiel

doi:10.1016/s0168-3659(97)00124-7

Cited by 306 publications

(196 citation statements)

References 31 publications

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“…The similar phenomenon was also observed by other researchers. 25,26 For an example, the long hydrophobic chain length of amphiphilic block copolymers poly(ethyl-2-cyanoacrylate) (PECA) derived from trimethylene carbonate, lactide, and mPEG was reported to slow down the release of 9-nitro-20(S)-camptothecin. 19 The release of drug from polymeric micelles is influenced by several factors including polymer hydrophobic core length and structure, physical state of the core, amount and properties of incorporated drugs, strength of the interaction between drug and hydrophobic core, and location of the drug loading.…”

Section: Discussionmentioning

confidence: 99%

Poly(ethylene glycol)-Block-Poly(2-methyl-2-benzoxycarbonyl-propylene Carbonate) Micelles for Rapamycin Delivery: In Vitro Characterization and Biodistribution

Mahato

2011

Journal of Pharmaceutical Sciences

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Our objective was to synthesize an amphiphilic diblock copolymer for micellar delivery of rapamycin. Poly(ethylene glycol)-block-poly(2-methyl-2-benzoxycarbonyl-propylene carbonate) (PEG-b-PBC) with different hydrophobic core lengths were synthesized from methoxy poly(ethylene glycol) and 2-methyl-2-benzoxycarbonyl-propylene carbonate through ring-opening polymerization using 1,8-diazabicycloundec-7-ene as a catalyst. The critical micelle concentration of PEG-b-PBC was around 10 −8 M and depends on the hydrophobic core length. Rapamycin was effectively incorporated into micelles and drug loading increased with increasing hydrophobic core length, with maximal drug loading of 10% (w/w, drug/polymer), drug loading efficiency of about 85%, and mean particle size of around 70 nm. The drug release profile was also dependent on the hydrophobic core length and the drug release from PEG 114 -b-PBC 30 micelles was the slowest. We also determined the toxicity of rapamycin micelles on insulinoma (INS-1E) $-cells and human islets. Encapsulation of rapamycin into PEG-b-PBC micelles reduced its toxicity. Biodistribution of rapamycin-loaded PEG-b-PBC micelles was determined after systemic administration into mice. Rapamycin-loaded PEG-b-PBC micelles showed little difference in pharmacokinetics and biodistribution characteristics in mice compared with rapamycin carrying nanosuspension. In conclusion, rapamycin formulated with PEG-b-PBC micelles showed significantly reduced toxicity on INS-1E $-cells and human islets, but had similar biodistribution profiles as those of nanosuspensions.

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Section: Discussionmentioning

confidence: 99%

Poly(ethylene glycol)-Block-Poly(2-methyl-2-benzoxycarbonyl-propylene Carbonate) Micelles for Rapamycin Delivery: In Vitro Characterization and Biodistribution

Mahato

2011

Journal of Pharmaceutical Sciences

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“…24 Nearly 100% of the DTX in Taxotere injections and approximately 60% of the DTX in mixed micelles was released after being immersed for 12 hours, indicating that DTX released much slower from micelles than from Taxotere. Normally, it is assumed that a drug is released by several processes, 25 including diffusion through the polymer matrix, release by polymer degradation and solubilization, or diffusion through microchannels that exist in the polymer matrix. DTX is physically entrapped in the hydrophobic core of the Pluronics, which restricted its release.…”

Section: In Vitro Release Profilementioning

confidence: 99%

Pluronic P105/F127 mixed micelles for the delivery of docetaxel against Taxol-resistant non-small cell lung cancer: optimization and in vitro, in vivo evaluation

Chen¹,

Sha²,

Jiang³

et al. 2013

IJN

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Abstract:The aim of this work was to establish a novel polymeric mixed micelle composed of Pluronic P105 and F127 copolymers loaded with the poorly soluble antitumor drug docetaxel (DTX) against Taxol-resistant non-small cell lung cancer. A central composite design was utilized to optimize the preparation process, helping to improve drug solubilization efficiency and micelle stability. Prepared by a thin-film hydration method, the average size of the optimized mixed micelle was 23 nm, with a 92.40% encapsulation ratio and a 1.81% drug-loading efficiency. The optimized formulation showed high storage stability in lyophilized form, with 95.7% of the drug content remaining after 6 months' storage at 4°C. The in vitro cytotoxicity assay showed that the IC50 values for Taxotere ® and mixed micelles were similar for A549, while on A549/Taxol cell lines, DTX-loaded P105/F127 mixed micelles showed a superior hypersensitizing effect; their IC50 value (0.059 µg/mL) was greatly reduced compared to those of Taxotere injections (0.593 µg/mL). The in vivo pharmacokinetic study showed that the mixed-micelle formulation achieved a 1.85-fold longer mean residence time in circulation and a 3.82-fold larger area under the plasma concentration-time curve than Taxotere. In addition, therapeutic improvement of mixed micelles in vivo against A549/Taxol was obtained. The tumor inhibition rate of the micelles was 69.05%, versus 34.43% for Taxotere (P , 0.01). Therefore, it could be concluded from the results that DTX-loaded P105/F127 mixed micelles might serve as a potential antitumor drug delivery system to overcome multidrug resistance in lung cancer.

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“…Using mPEG2000-DSPE, the T 50% values for F5 (1:5), F6 (1:10), and F7 (1:5:10) varied from 10.95 to 12.83 h (p>0.05), while using mPEG5000-DSPE, the T 50% values for F11 (1:5), F12 (1:10), and F13 (1:5:10) varied from 11.74 to 13.63 h (p>0.05). Kim et al (31) reported that as the amount of drug loading in the nanoparticles increased, the drug release rate decreased. They concluded that the level of drug release seemed to depend on the amount of drug entrapped inside the micelle.…”

Section: In Vitro Drug Releasementioning

confidence: 99%

Rehydrated Lyophilized Rifampicin-Loaded mPEG–DSPE Formulations for Nebulization

2010

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Abstract. Rifampicin-loaded nanoparticles were prepared using two different molecular weights of poly-(ethylene oxide)-block-distearoyl phosphatidyl-ethanolamine (mPEG2000-DSPE and mPEG5000-DSPE) polymers. Particle sizes of all formulations studied were in the range of 162-395 nm. The entrapment efficiency (EE) was not affected by the copolymer's molecular weight, and the highest EE (100%) was obtained with drug to copolymer ratio of 1:5. The differential scanning calorimetry (DSC) thermograms showed Tg of rifampicin-loaded PEG-DSPE nanoparticles that shifted to a lower value, indicating entrapment of rifampicin in polymer matrix. The Fourier transformed infrared spectra revealed no chemical interactions between the drug and both copolymers. The in vitro drug release from the formulations occurred over 3 days and followed first-order release kinetic and Higuchi diffusion model. The nebulization of rehydrated lyophilized rifampicin mPEG-DSPE formulations had mass median aerodynamic diameter of 2.6 µm and fine particle fraction of 42%. The aerodynamic characteristic of the preparations was not influenced by the molecular weight of the copolymers. Therefore, it is suggested that both mPEG-DSPE are promising candidates as rifampicin carrier for pulmonary delivery.

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Methoxy poly(ethylene glycol) and ϵ-caprolactone amphiphilic block copolymeric micelle containing indomethacin.

Cited by 306 publications

References 31 publications

Poly(ethylene glycol)-Block-Poly(2-methyl-2-benzoxycarbonyl-propylene Carbonate) Micelles for Rapamycin Delivery: In Vitro Characterization and Biodistribution

Poly(ethylene glycol)-Block-Poly(2-methyl-2-benzoxycarbonyl-propylene Carbonate) Micelles for Rapamycin Delivery: In Vitro Characterization and Biodistribution

Pluronic P105/F127 mixed micelles for the delivery of docetaxel against Taxol-resistant non-small cell lung cancer: optimization and in vitro, in vivo evaluation

Rehydrated Lyophilized Rifampicin-Loaded mPEG–DSPE Formulations for Nebulization

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