Online citations, reference lists, and bibliographies.
← Back to Search

Self-assembled Micelles Of Novel Amphiphilic Copolymer Cholesterol-coupled F68 Containing Cabazitaxel As A Drug Delivery System

Yanzhi Song, Qingjing Tian, Zhenjun Huang, D. Fan, Zhennan She, Xinrong Liu, Xiaobo Cheng, B. Yu, Yihui Deng
Published 2014 · Chemistry, Medicine

Save to my Library
Download PDF
Analyze on Scholarcy
Share
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 IC50 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.
This paper references
10.1016/0378-5173(95)04386-1
Development of amphiphilic diblock copolymers as micellar carriers of taxol
X. Zhang (1996)
10.2147/IJN.S38221
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
Liangcen Chen (2013)
10.2147/DDDT.S13029
Cabazitaxel: a novel second-line treatment for metastatic castration-resistant prostate cancer
C. Paller (2011)
10.1002/1097-0142(19940115)73:2<253::AID-CNCR2820730204>3.0.CO;2-F
Cholesterol content in tumor tissues is inversely associated with high‐density lipoprotein cholesterol in serum in patients with gastrointestinal cancer
S. Dessi (1994)
10.1200/JCO.2006.24.18_SUPPL.4080
SP1049C as first-line therapy in advanced (inoperable or metastatic) adenocarcinoma of the oesophagus: A phase II window study.
A. Armstrong (2006)
10.1016/J.SEMCANCER.2005.07.008
Immune suppression in cancer: effects on immune cells, mechanisms and future therapeutic intervention.
T. Whiteside (2006)
10.2147/ijn
科技期刊稿件处理的精细化管理——《International Journal of Nanomedicine〉〉投稿体会
鲁翠涛 (2014)
10.1186/1556-276X-6-354
Development of Polysorbate 80/Phospholipid mixed micellar formation for docetaxel and assessment of its in vivo distribution in animal models
H. Song (2011)
10.1002/jcb.10724
Cholesterol and prostate cancer
M. Freeman (2004)
10.1007/s10637-010-9399-1
A phase 2 study of SP1049C, doxorubicin in P-glycoprotein-targeting pluronics, in patients with advanced adenocarcinoma of the esophagus and gastroesophageal junction
J. Valle (2010)
10.1016/j.colsurfb.2011.03.013
Preparation and characterization of thermosensitive pluronic F127-b-poly(ɛ-caprolactone) mixed micelles.
Q. Zhou (2011)
10.1016/J.JCONREL.2003.10.018
Micellar formulations for drug delivery based on mixtures of hydrophobic and hydrophilic Pluronic block copolymers.
K. Oh (2004)
10.1083/jcb.200910104
Targeting of drugs and nanoparticles to tumors
E. Ruoslahti (2010)
10.1002/mabi.201000332
Synergistic anticancer effects achieved by co-delivery of TRAIL and paclitaxel using cationic polymeric micelles.
Ashlynn L. Z. Lee (2011)
10.1016/j.colsurfb.2010.06.017
Effect of porous silica on sustained release behaviors of pH sensitive pluronic F127/poly(acrylic acid) hydrogels containing tulobuterol.
K. Kim (2010)
Fluorescence Probes for Critical Micelle Concentration
K. Ananthapadmanabhan (2001)
10.1016/j.ijpharm.2009.04.030
Paclitaxel-loaded Pluronic P123/F127 mixed polymeric micelles: formulation, optimization and in vitro characterization.
Z. Wei (2009)
10.1016/S0168-3659(02)00009-3
Pluronic block copolymers as novel polymer therapeutics for drug and gene delivery.
A. Kabanov (2002)
10.1177/0885328209357110
Encapsulation of Curcumin in Pluronic Block Copolymer Micelles for Drug Delivery Applications
A. Sahu (2011)
10.1016/J.EJPS.2005.07.002
Permeabilisation and solubilisation of soybean phosphatidylcholine bilayer vesicles, as membrane models, by polysorbate, Tween 80.
S. Simões (2005)
A multicenter phase II study of XRP6258 administered as a 1-h iv infusion every 3 weeks in taxaneresistant metastatic breast cancer patients
X Pivot (2008)
10.1016/j.jconrel.2012.03.003
Ligands located within a cholesterol domain enhance gene delivery to the target tissue.
L. Xu (2012)
10.1002/JPS.10190
Distribution, metabolism, and excretion of a novel surface-active agent, purified poloxamer 188, in rats, dogs, and humans.
J. M. Grindel (2002)
10.1016/j.biomaterials.2011.11.032
The use of cholesterol-containing biodegradable block copolymers to exploit hydrophobic interactions for the delivery of anticancer drugs.
Ashlynn L. Z. Lee (2012)
10.2217/fon.11.23
TROPIC: Phase III trial of cabazitaxel for the treatment of metastatic castration-resistant prostate cancer.
S. Oudard (2011)
10.1158/0008-5472.CAN-05-3627
Contributions of human tumor xenografts to anticancer drug development.
E. Sausville (2006)
Novel cabazitaxel drug delivery system
10.1016/j.colsurfb.2012.04.017
Curcumin loaded mixed micelles composed of Pluronic P123 and F68: preparation, optimization and in vitro characterization.
L. Zhao (2012)
10.1016/J.JCONREL.2004.09.021
Controlled and targeted tumor chemotherapy by micellar-encapsulated drug and ultrasound.
Z. Gao (2005)
10.1158/1078-0432.CCR-08-0596
Phase I and Pharmacokinetic Study of XRP6258 (RPR 116258A), a Novel Taxane, Administered as a 1-Hour Infusion Every 3 Weeks in Patients with Advanced Solid Tumors
A. Mita (2009)
10.1002/JPS.10397
Amphiphilic block copolymers for drug delivery.
M. Adams (2003)
10.1371/journal.pone.0072238
Effect of Doxorubicin/Pluronic SP1049C on Tumorigenicity, Aggressiveness, DNA Methylation and Stem Cell Markers in Murine Leukemia
Daria Y. Alakhova (2013)
10.1016/J.JCONREL.2004.03.026
Novel pH-sensitive supramolecular assemblies for oral delivery of poorly water soluble drugs: preparation and characterization.
V. Sant (2004)
10.1093/annonc/mdn171
A multicenter phase II study of XRP6258 administered as a 1-h i.v. infusion every 3 weeks in taxane-resistant metastatic breast cancer patients.
X. Pivot (2008)
Plasma lipids, lipoproteins, and familial breast cancer.
N. Boyd (1995)
10.1016/j.ejpb.2008.11.010
Polymeric drugs for efficient tumor-targeted drug delivery based on EPR-effect.
H. Maeda (2009)
10.1016/j.jcis.2011.04.041
Synthesis and characterization of novel thermo-responsive F68 block copolymers with cell-adhesive RGD peptide.
Myoung-Hwa Cha (2011)
10.1016/S0168-3659(01)00492-8
Process design for efficient and controlled drug incorporation into polymeric micelle carrier systems.
F. Kohori (2002)
10.1021/mp100097b
Effect of cholesterol nanodomains on the targeting of lipid-based gene delivery in cultured cells.
L. Xu (2010)
10.1016/j.jconrel.2008.05.009
Esterase-catalyzed dePEGylation of pH-sensitive vesicles modified with cleavable PEG-lipid derivatives.
Huan Xu (2008)
10.1021/la00063a015
Fluorescence probes for critical micelle concentration determination.
E. Goddard (1985)
10.1002/JPS.21076
In vivo comparative study of lipid/DNA complexes with different in vitro serum stability: effects on biodistribution and tumor accumulation.
Y. Zhang (2008)
10.1016/j.coph.2012.07.009
Cholesterol and breast cancer development.
C. Danilo (2012)
10.1016/j.colsurfb.2011.02.038
Nanostructured lipid carriers as novel carrier for parenteral delivery of docetaxel.
D. Liu (2011)
10.1016/j.biomaterials.2013.02.071
pH-triggered intracellular release from actively targeting polymer micelles.
X. Guo (2013)
For personal use only



This paper is referenced by
10.1021/acs.bioconjchem.6b00155
Redox-Sensitive Citronellol-Cabazitaxel Conjugate: Maintained in Vitro Cytotoxicity and Self-Assembled as Multifunctional Nanomedicine.
P. Xue (2016)
10.1007/s13346-017-0403-6
The antitumor efficacy of docetaxel is enhanced by encapsulation in novel amphiphilic polymer cholesterol-coupled tocopheryl polyethylene glycol 1000 succinate micelles
Qingjing Tian (2017)
10.2147/IJN.S125041
Enhancing the oral bioavailability of biochanin A by encapsulation in mixed micelles containing Pluronic F127 and Plasdone S630
X. Wu (2017)
10.3109/10717544.2015.1037970
Synthesis, characterization and anti-cancer activity of Pluronic F68–curcumin conjugate micelles
Yuee Cai (2016)
10.1007/s10637-017-0533-1
Antitumor activity of raloxifene-targeted poly(styrene maleic acid)-poly (amide-ether-ester-imide) co-polymeric nanomicelles loaded with docetaxel in breast cancer-bearing mice
Saeede Enteshari (2017)
10.3390/polym12112620
Polymeric Drug Delivery Systems Bearing Cholesterol Moieties: A Review
Paweł Misiak (2020)
10.1080/03639045.2020.1820037
Development and evaluation of polymeric micelle containing tablet formulation for poorly water-soluble drug: tamoxifen citrate
Kıvılcım Öztürk-Atar (2020)
10.1039/C6RA01779G
Targeted nanoparticles from xyloglucan–doxorubicin conjugate loaded with doxorubicin against drug resistance
X. Xie (2016)
10.1016/j.jconrel.2017.11.046
Epithelia transmembrane transport of orally administered ultrafine drug particles evidenced by environment sensitive fluorophores in cellular and animal studies
Yike Xie (2018)
10.1080/03639045.2016.1185438
Anti prostate cancer using PEGylated bombesin containing, cabazitaxel loading nano-sized drug delivery system
W. Chen (2016)
10.1080/1061186X.2016.1233975
Cabazitaxel and indocyanine green co-delivery tumor-targeting nanoparticle for improved antitumor efficacy and minimized drug toxicity
Xiaowei Tai (2017)
10.3390/polym10101060
Synthesis and Properties of Low-Molecular-Weight PEI-Based Lipopolymers for Delivery of DNA
Miao-Miao Xun (2018)
10.1016/j.actbio.2014.12.018
Folate-decorated hydrophilic three-arm star-block terpolymer as a novel nanovehicle for targeted co-delivery of doxorubicin and Bcl-2 siRNA in breast cancer therapy.
J. Qian (2015)
10.3390/pharmaceutics11030141
Cabazitaxel-Loaded Nanocarriers for Cancer Therapy with Reduced Side Effects
N. Kommineni (2019)
10.1016/j.canlet.2016.01.050
Development of highly efficient nanocarrier-mediated delivery approaches for cancer therapy.
K. Jeong (2016)
10.1016/J.POLYMER.2017.11.034
Effect of Fe 3 O 4 NPs on micellization and release behavior of CBABC-type pentablock copolymer
A. Pal (2017)
10.1038/srep28373
Dual Drug Loaded Biodegradable Nanofibrous Microsphere for Improving Anti-Colon Cancer Activity
Rangrang Fan (2016)
Drug Delivery Using Nanoparticles
Nicomp® DLS (2019)
10.1039/C5RA10341J
Self-organized nanoparticle drug delivery systems from a folate-targeted dextran–doxorubicin conjugate loaded with doxorubicin against multidrug resistance
Yuannian Zhang (2015)
10.1039/c9ra07250k
Glycyrrhetinic acid modified and pH-sensitive mixed micelles improve the anticancer effect of curcumin in hepatoma carcinoma cells
J. Song (2019)
10.1039/C8RA03787F
Co-delivery of doxorubicin and itraconazole by Pluronic® P123 coated liposomes to enhance the anticancer effect in breast cancers
Yi Lin (2018)
10.1080/09205063.2018.1483616
Synthesis, characterization, and in vitro evaluation of TRAIL-modified, cabazitaxel -loaded polymeric micelles for achieving synergistic anticancer therapy
Caochuan Feng (2018)
10.1016/j.msec.2019.03.002
Comparison of paclitaxel solid dispersion and polymeric micelles for improved oral bioavailability and in vitro anti-cancer effects.
J. Choi (2019)
10.1007/s10965-020-02392-y
Amphiphilic copolymers modified with oleic acid and cholesterol by combining ring opening polymerization and click chemistry with improved amphotericin B loading capacity
Angie V. Angarita-Villamizar (2021)
10.2147/IJN.S278688
Bilosomes as Promising Nanovesicular Carriers for Improved Transdermal Delivery: Construction, in vitro Optimization, ex vivo Permeation and in vivo Evaluation
Sadek Ahmed (2020)
10.1016/j.msec.2017.05.126
Peptide functionalized poly ethylene glycol-poly caprolactone nanomicelles for specific cabazitaxel delivery to metastatic breast cancer cells.
P. Mahdaviani (2017)
10.1016/j.seppur.2020.117829
Optimal synthesis of high fouling-resistant PVC-based ultrafiltration membranes with tunable surface pore size distribution and ultralow water contact angle for the treatment of oily wastewater
Tausif Ahmad (2021)
10.1007/s12274-018-2171-0
Current taxane formulations and emerging cabazitaxel delivery systems
B. Sun (2018)
10.1016/j.ejps.2017.03.017
A novel nanosuspension of andrographolide: Preparation, characterization and passive liver target evaluation in rats
Ligang Guo (2017)
10.1016/j.canlet.2017.09.029
Cabazitaxel-conjugated nanoparticles for docetaxel-resistant and bone metastatic prostate cancer.
Bryan Hoang (2017)
10.15407/POLYMERJ.37.03.299
Synthesis of surface-active cholesterylcontaining copolymers based on poly(maleic anhydride-co-ethyltrioxyethylene methacrylate)
Zoriana Demchuk (2015)
10.1080/03639045.2017.1349784
Polysialic acid and pluronic F127 mixed polymeric micelles of docetaxel as new approach for enhanced antitumor efficacy
T. Zhang (2017)
See more
Semantic Scholar Logo Some data provided by SemanticScholar