Synthesis and characterization of novel thermo-responsive F68 block copolymers with cell-adhesive RGD peptide

Hwa, Myoung; Choi, Jiyeon; Choi, Bo Gyu; Kim, Ik Hwan; Jeong, Byeongmoon; Han, Dong Keun

doi:10.1016/j.jcis.2011.04.041

Cited by 35 publications

(28 citation statements)

References 39 publications

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“…Nevertheless, due to its high PEO/PPO ratio, the drug encapsulation efficiency (EE) and stability of single F68 micelles are poor. 19 Some strategies have been explored to enhance the kinetic stability of F68 micelles in the blood stream upon dilution and to reduce the critical micelle concentration (CMC), including generating mixed micelles with different Pluronic copolymers, 20 F68-drug conjugates, 21 and F68 complexed with other amphiphilic copolymers. 22 However, both the copolymer complexes and chemical conjugation prodrug approaches require excess amounts of polymers, resulting in reduced drug loading (DL) efficiency.…”

Section: Introductionmentioning

confidence: 99%

Redox-sensitive micelles composed of disulfide-linked Pluronic-linoleic acid for enhanced anticancer efficiency of brusatol

Zhang¹,

Fang²,

Li³

et al. 2018

IJN

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Brusatol (Bru) exhibits promising anticancer effects, with both proliferation inhibition and chemoresistance amelioration activity. However, the poor solubility and insufficient intracellular delivery of Bru greatly restrict its application. Herein, to simultaneously utilize the advantages of Pluronics as drug carriers and tumor microenvironment-responsive drug release profiles, a flexible amphiphilic copolymer with a polymer skeleton, that is, Pluronic ® F68 grafting with linoleic acid moieties by redox-reducible disulfide bonds (F68-SS-LA), was synthesized. After characterization by 1 H-nuclear magnetic resonance and Fourier transform infrared spectroscopy, the redox-sensitive F68-SS-LA micelles were self-assembled in a much lower critical micelle concentration than that of the unmodified F68 copolymer. Bru was loaded in micelles (Bru/SS-M) with high loading efficiency, narrow size distribution, and excellent storage stability. The redox-sensitive Bru/SS-M exhibited rapid particle dissociation and drug release in response to a redox environment. Based on the enhanced cellular internalization, Bru/SS-M achieved higher cytotoxicity in both Bel-7402 and MCF-7 cells compared with free Bru and nonreducible micelles. The improved anticancer effect was attributed to the remarkably decreased mitochondrial membrane potential and increased reactive oxygen species level as well as apoptotic rate. These results demonstrated that F68-SS-LA micelles possess great potential as an efficient delivery vehicle for Bru to promote its anticancer efficiency via an oxidation pathway.

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Section: Introductionmentioning

confidence: 99%

Redox-sensitive micelles composed of disulfide-linked Pluronic-linoleic acid for enhanced anticancer efficiency of brusatol

Zhang¹,

Fang²,

Li³

et al. 2018

IJN

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“…To overcome the instability of F68 micelles, several stabilization approaches have been investigated, including mixed micelles and chemical modifications. 12,13 Cholesterol, an essential membrane component in animal cells, is produced by the liver. Boyd et al found that cancer cells obtained a large amount of cholesterol from serum to support their rapid growth, which led to a metabolic disorder of cholesterol and hypocholesterolemia.…”

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confidence: 99%

Self-assembled micelles of novel amphiphilic copolymer cholesterol-coupled F68 containing cabazitaxel as a drug delivery system

Song¹,

Tian²,

Huang³

et al. 2014

IJN

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Despite being one of the most promising amphiphilic block copolymers, use of Pluronic F68 in drug delivery is limited due to its high critical micelle concentration (CMC). In this study, we developed a novel F68 derivative, cholesterol-coupled F68 (F68-CHMC). This new derivative has a CMC of 10 μg/mL, which is 400-fold lower than that of F68. The drug-loading capacity of F68-CHMC was investigated by encapsulating cabazitaxel, a novel antitumor drug. Drug-loaded micelles were fabricated by a self-assembly method with simple dilution. The optimum particle size of the micelles was 17.5±2.1 nm, with an entrapment efficiency of 98.1% and a drug loading efficiency of 3.16%. In vitro release studies demonstrated that cabazitaxel-loaded F68-CHMC micelles had delayed and sustained-release properties. A cytotoxicity assay of S180 cells showed that blank F68-CHMC was noncytotoxic with a cell viability of nearly 100%, even at a concentration of 1,000 μg/mL. The IC 50 revealed that cabazitaxel-loaded F68-CHMC micelles were more cytotoxic than Tween 80-based cabazitaxel solution and free cabazitaxel. In vivo antitumor activity against S180 cells also indicated better tumor inhibition by the micelles (79.2%) than by Tween 80 solution (56.2%, P <0.05). Based on these results, we conclude that the F68-CHMC copolymer may be a potential nanocarrier to improve the solubility and biological activity of cabazitaxel and other hydrophobic drugs.

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“…Pluronic block copolymer is one of the most widely used materials to construct micelles. Pluronic block copolymers are benign and some of them have been approved by FDA as pharmaceutical excipients (Cha et al, 2011). These macromolecules are surface active and self-assemble into micelles above critical micelle concentrations (CMCs) and certain temperatures.…”

Section: Introductionmentioning

confidence: 99%

Preparation of sodium cholate-based micelles through non-covalent ıbonding interaction and application as oral delivery systems for paclitaxel

Zhao

2015

Drug Delivery

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In present study, two types of micelles based on sodium cholate (NaC) were prepared through non-covalent bonding interaction and the potential of micelles as oral drug delivery systems for paclitaxel (PTX) was evaluated. Pluronic-chitosan (F127-CS) and Pluronic-poly (acrylic acid) (F127-PAA) copolymers were synthesized. Electrostatic interaction and hydrogen bond were used to prepare F127-CS/NaC micelles and F127-PAA/NaC micelles, respectively. The physicochemical characteristics of micelles were determined. An average diameter of 67.5 nm and unimodal pattern of size distribution were observed for F127-CS/NaC micelles. While for F127-PAA/NaC micelles, an average diameter of 85.89 nm and non-unimodal pattern of size distribution were observed. The results revealed that F127-CS/NaC micelles were more integrated than F127-PAA/NaC micelles. Further experiments showed that the F127-CS/NaC micelles had a higher drug-loading content of 12.8% and a lower critical micelle concentration (CMC) of 2.5 Â 10 À3 mol/L compared with F127-PAA/NaC micelles. In vitro cytotoxicity analysis demonstrated that the PTX-loaded F127-CS/NaC micelles were of great efficiency in inhibiting the growth of drug-resistant breast cancer MCF-7 cells (MCF-7/Adr). The intragastric administration of the PTX-loaded F127-CS/NaC micelles in rats provided a 4.33-fold higher absolute bioavailability compared to commercial Taxol Õ , indicating an efficient oral absorption of PTX delivered by micelles. These findings signify that F127-CS/NaC micelle may be a promising carrier for the delivery of PTX.

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Synthesis and characterization of novel thermo-responsive F68 block copolymers with cell-adhesive RGD peptide

Cited by 35 publications

References 39 publications

Redox-sensitive micelles composed of disulfide-linked Pluronic-linoleic acid for enhanced anticancer efficiency of brusatol

Redox-sensitive micelles composed of disulfide-linked Pluronic-linoleic acid for enhanced anticancer efficiency of brusatol

Self-assembled micelles of novel amphiphilic copolymer cholesterol-coupled F68 containing cabazitaxel as a drug delivery system

Preparation of sodium cholate-based micelles through non-covalent ıbonding interaction and application as oral delivery systems for paclitaxel

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