TPGS-g-PLGA/Pluronic F68 mixed micelles for tanshinone IIA delivery in cancer therapy

Zhang, Jinming; Li, Yingbo; Fang, Xiefan; Zhou, Demin; Wang, Ying; Chen, Meiwan

doi:10.1016/j.ijpharm.2014.09.017

Cited by 76 publications

(46 citation statements)

References 55 publications

(51 reference statements)

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“…CMC) and then the sizes of micelles as well as their distribution were determined by dynamic light scattering (DLS) at given time intervals. 23 …”

Section: Comparison Of Micellar Stabilitymentioning

confidence: 99%

Effects of X-shaped reduction-sensitive amphiphilic block copolymer on drug delivery

Xiao¹,

Wang²

2015

IJN

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To study the effects of X-shaped amphiphilic block copolymers on delivery of docetaxel (DTX) and the reduction-sensitive property on drug release, a novel reduction-sensitive amphiphilic copolymer, (PLGA) 2 -SS-4-arm-PEG 2000 with a Gemini-like X-shape, was successfully synthesized. The formation of nanomicelles was proved with respect to the blue shift of the emission fluorescence as well as the fluorescent intensity increase of coumarin 6-loaded particles. The X-shaped polymers exhibited a smaller critical micelle concentration value and possessed higher micellar stability in comparison with those of linear ones. The size of X-shaped (PLGA) 2 -SS-4-arm-PEG 2000 polymer nanomicelles (XNMs) was much smaller than that of nanomicelles prepared with linear polymers. The reduction sensitivity of polymers was confirmed by the increase of micellar sizes as well as the in vitro drug release profile of DTX-loaded XNMs (DTX/XNMs). Cytotoxicity assays in vitro revealed that the blank XNMs were nontoxic against A2780 cells up to a concentration of 50 µg/mL, displaying good biocompatibility. DTX/XNMs were more toxic against A2780 cells than other formulations in both dose- and time-dependent manners. Cellular uptake assay displayed a higher intracellular drug delivery efficiency of XNMs than that of nanomicelles prepared with linear polymers. Besides, the promotion of tubulin polymerization induced by DTX was visualized by immunofluorescence analysis, and the acceleration of apoptotic process against A2780 cells was also imaged using a fluorescent staining method. Therefore, this X-shaped reduction-sensitive (PLGA) 2 -SS-4-arm-PEG 2000 copolymer could effectively improve the micellar stability and significantly enhance the therapeutic efficacy of DTX by increasing the cellular uptake and selectively accelerating the drug release inside cancer cells.

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“…CMC) and then the sizes of micelles as well as their distribution were determined by dynamic light scattering (DLS) at given time intervals. 23 …”

Section: Comparison Of Micellar Stabilitymentioning

confidence: 99%

Effects of X-shaped reduction-sensitive amphiphilic block copolymer on drug delivery

Xiao¹,

Wang²

2015

IJN

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“…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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“…27 According to various reports, the low absolute value of zeta potential was associated with insufficient electric repulsion among particles, which would lead to aggregation. 15,28 In this study, a high absolute zeta potential of −32.67±0.87 mV for the F68-VES/ MIT micelles ( Figure 4B) was observed, which might indicate the uniform distribution of the particles.…”

Section: Characterization Of F68-ves/mit Micellesmentioning

confidence: 48%

“…9,[12][13][14] According to published reports, hydrophobic drugs could be incorporated into F68-based micelles, which were used to deliver drugs to enhance their anticancer effect. [14][15][16] For example, cholesterolcoupled F68 micelles could enhance the anticancer activity of cabazitaxel compared to a Tween 80-based drug solution. 14 However, F68 has a high critical micelle concentration (CMC) and a low drug loading (DL) capacity, resulting in poor dilution stability of the micelles.…”

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confidence: 99%

Vitamin E succinate-conjugated F68 micelles for mitoxantrone delivery in enhancing anticancer activity

Liu¹,

Xu²,

Wu³

et al. 2016

IJN

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Mitoxantrone (MIT) is a chemotherapeutic agent with promising anticancer efficacy. In this study, Pluronic F68-vitamine E succinate (F68-VES) amphiphilic polymer micelles were developed for delivering MIT and enhancing its anticancer activity. MIT-loaded F68–VES (F68–VES/MIT) micelles were prepared via the solvent evaporation method with self-assembly under aqueous conditions. F68–VES/MIT micelles were found to be of optimal particle size with the narrow size distribution. Transmission electron microscopy images of F68–VES/MIT micelles showed homogeneous spherical shapes and smooth surfaces. F68–VES micelles had a low critical micelle concentration value of 3.311 mg/L, as well as high encapsulation efficiency and drug loading. Moreover, F68–VES/MIT micelles were stable in the presence of fetal bovine serum for 24 hours and maintained sustained drug release in vitro. Remarkably, the half maximal inhibitory concentration (IC 50 ) value of F68–VES/MIT micelles was lower than that of free MIT in both MDA-MB-231 and MCF-7 cells (two human breast cancer cell lines). In addition, compared with free MIT, there was an increased trend of apoptosis and cellular uptake of F68–VES/MIT micelles in MDA-MB-231 cells. Taken together, these results indicated that F68–VES polymer micelles were able to effectively deliver MIT and largely improve its potency in cancer therapy.

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TPGS-g-PLGA/Pluronic F68 mixed micelles for tanshinone IIA delivery in cancer therapy

Cited by 76 publications

References 55 publications

Effects of X-shaped reduction-sensitive amphiphilic block copolymer on drug delivery

Effects of X-shaped reduction-sensitive amphiphilic block copolymer on drug delivery

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

Vitamin E succinate-conjugated F68 micelles for mitoxantrone delivery in enhancing anticancer activity

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