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Drug Nanocarriers For Cancer Chemotherapy Based On Microemulsions: The Case Of Vemurafenib Analog PLX4720.

I. Theochari, M. Goulielmaki, D. Danino, V. Papadimitriou, A. Pintzas, A. Xenakis
Published 2017 · Chemistry, Medicine

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Oil-in-water (O/W) microemulsions based on Tween 80 as the emulsifier and triacetin as the dispersed oil phase were formulated to be used as delivery vehicles of Vemurafenib analog PLX4720. PLX4720 is a lipophilic antitumor drug against various cancer types correlated with the BRAFV600E mutation. The limits of the single-phase region corresponding to O/W microemulsions as described by ternary phase diagrams were examined. Droplet size measurements determined by dynamic light scattering (DLS) showed mean droplet diameters equal to 10±0.1nm both in the presence and in absence of the drug. Cryogenic-transmission electron microscopy (Cryo-TEM) images of the microemulsions showed the existence of small structures with uniform size distribution having also average diameters of approximately 10nm. Electron paramagnetic resonance (EPR) spectroscopy applying the spin probing technique confirmed PLX4720 location in the oil cores excluding its participation in the surfactants monolayer. Furthermore, cell viability assays on colon cancer cell lines Colo-205 and HT29 showed that microemulsions did not exhibit any cytotoxicity when added in ratios between 0.005% v/v and 0.2% v/v. When the cells were treated with encapsulated PLX4720 at two different concentrations (0.063 and 0.12μΜ) the same response as when dissolved in classic DMSO was observed.
This paper references
10.1016/S0169-409X(00)00103-4
Microemulsion-based media as novel drug delivery systems
M. J. Lawrence (2000)
10.1016/J.CIS.2006.11.016
Microemulsions as carriers for drugs and nutraceuticals.
Aviram Spernath (2006)
10.1016/J.JCONREL.2007.02.014
Phosphatidylcholine embedded microemulsions: physical properties and improved Caco-2 cell permeability.
Aviram Spernath (2007)
10.1073/pnas.1011614107
Triton X-100 concentration effects on membrane permeability of a single HeLa cell by scanning electrochemical microscopy (SECM)
Dipankar Koley (2010)
10.1016/j.ejpb.2010.07.002
Microemulsions for oral delivery of insulin: design, development and evaluation in streptozotocin induced diabetic rats.
G. Sharma (2010)
10.1002/9780470571224.PSE349
Liquid Dosage Forms
Maria V. Rubio-Bonilla (2010)
10.1021/jf902761h
Stability of citral in oil-in-water emulsions prepared with medium-chain triacylglycerols and triacetin.
Seung Jun Choi (2009)
10.1201/9781498710565
Colloidal Drug Delivery Systems
J. Kreuter (1994)
10.1021/acs.langmuir.5b01397
Celecoxib Encapsulation in β-Casein Micelles: Structure, Interactions, and Conformation.
Tanya Turovsky (2015)
10.1007/b11625
Lecithin organogels as model carriers of pharmaceuticals
M. Zoumpanioti (2004)
10.1016/j.ejps.2012.07.005
Evaluation of cytotoxicity of surfactants used in self-micro emulsifying drug delivery systems and their effects on paracellular transport in Caco-2 cell monolayer.
Z. Ujhelyi (2012)
10.1073/pnas.0711741105
Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity
J. Tsai (2008)
10.3109/10717544.2010.522613
Preparation and evaluation of ibuprofen-loaded microemulsion for improvement of oral bioavailability
L. Hu (2011)
10.1016/B978-0-12-092350-2.50008-4
3 – Theory of Slow Tumbling ESR Spectra for Nitroxides
J. Freed (1976)
10.1016/j.colsurfb.2008.12.038
Determining the cytotoxicity of catanionic surfactant mixtures on HeLa cells.
N. Vlachy (2009)
10.1158/0008-5472.CAN-14-0247
Say no to DMSO: dimethylsulfoxide inactivates cisplatin, carboplatin, and other platinum complexes.
M. Hall (2014)
10.1038/nrd1494
Nanosuspensions in drug delivery
Barrett E. Rabinow (2004)
10.1002/JPS.20995
Microemulsions--modern colloidal carrier for dermal and transdermal drug delivery.
Sandra Heuschkel (2008)
10.1016/J.COCIS.2012.06.001
Microemulsions as delivery systems
M. Fanun (2012)
10.1016/j.jcis.2015.02.011
Water-dilutable microemulsions for transepithelial ocular delivery of riboflavin phosphate.
N. Lidich (2016)
10.1016/S0168-3659(00)00343-6
Preparation and evaluation of biphenyl dimethyl dicarboxylate microemulsions for oral delivery.
C. K. Kim (2001)
10.1016/J.COCIS.2012.10.003
Cryo-TEM of soft molecular assemblies
D. Danino (2012)
10.2147/IJN.S18821
Enhanced effect and mechanism of water-in-oil microemulsion as an oral delivery system of hydroxysafflor yellow A
J. Qi (2011)
Cell Viability Assays
T. Riss (2016)
10.1021/la501789z
Making sense of Brownian motion: colloid characterization by dynamic light scattering.
P. Hassan (2015)
10.1002/JPS.10221
Light-scattering studies of testosterone enanthate containing soybean oil/C18:1E10/water oil-in-water microemulsions.
C. Malcolmson (2002)
10.1038/nrd3847
Vemurafenib: the first drug approved for BRAF-mutant cancer
G. Bollag (2012)
10.1016/J.IJPHARM.2007.08.057
Stable drug encapsulation in micelles and microemulsions.
A. Narang (2007)
10.1016/J.JMR.2005.08.013
EasySpin, a comprehensive software package for spectral simulation and analysis in EPR.
S. Stoll (2006)
10.1016/0166-6622(81)80064-9
The definition of microemulsion
Ingvar Danielsson (1981)
10.1038/nature00766
Mutations of the BRAF gene in human cancer
Helen Davies (2002)
10.1201/9781420089608.CH11
Places of Microemulsion and Emulsion in Cancer Therapy: In Vitro and In Vivo Evaluation
E. Karasulu (2008)
10.2174/187221108786241679
Microemulsions: a novel approach to enhanced drug delivery.
S. Talegaonkar (2008)
10.1248/CPB.53.1246
Synthesis of ibuprofen eugenol ester and its microemulsion formulation for parenteral delivery.
X. Zhao (2005)
10.1038/nprot.2006.179
Sulforhodamine B colorimetric assay for cytotoxicity screening
V. Vichai (2006)
10.1049/iet-nbt.2014.0010
In vitro cytotoxic activity of chitosan-bullfrog oil microemulsion against melanoma cells.
Cínthia C Bonatto (2015)
10.1007/978-1-4613-0743-3_1
Calculating Slow Motional Magnetic Resonance Spectra
D. Schneider (1989)
10.1517/17425247.2013.749234
Topical delivery of aceclofenac as nanoemulsion comprising excipients having optimum emulsification capabilities: preparation, characterization and in vivo evaluation
S. Dasgupta (2013)



This paper is referenced by
10.2478/acph-2018-0025
Enhancement of ketoconazole dissolution rate by the liquisolid technique
M. Molaei (2018)
10.1007/s13346-020-00757-w
3,5,4′-Trimethoxy-trans-stilbene loaded microemulsion for cutaneous melanoma therapy by transdermal drug delivery
Junyong Wu (2020)
10.1016/j.cis.2018.11.004
Basic principles of drug delivery systems - the case of paclitaxel.
S. Ezrahi (2019)
10.1016/J.MOLLIQ.2018.07.109
Development of food grade O/W nanoemulsions as carriers of vitamin D for the fortification of emulsion based food matrices: A structural and activity study
Ioanna Golfomitsou (2018)
10.1016/j.jddst.2020.102008
A review on developments and prospects of anti-inflammatory in microemulsions
Larissa Pereira Alves (2020)
10.3390/biomimetics3020013
Oil-In-Water Microemulsions as Hosts for Benzothiophene-Based Cytotoxic Compounds: An Effective Combination
I. Theochari (2018)
10.1134/S0036024418120312
Solubilization of Biologically Active Heterocyclic Compounds by Biocompatible Microemulsions
A. B. Mirgorodskaya (2018)
10.1016/j.ejmech.2018.09.005
Recent advances of RAF (rapidly accelerated fibrosarcoma) inhibitors as anti-cancer agents.
Usama M. Ammar (2018)
10.1016/j.colsurfb.2019.110366
Encapsulation of vitamin B12 into nanoengineered capsules and soft matter nanosystems for targeted delivery.
L. A. Maiorova (2019)
10.1016/j.molliq.2020.112479
Curcumin-loaded low-energy nanoemulsions: Linking EPR spectroscopy-analysed microstructure and antioxidant potential with in vitro evaluated biological activity
I. Nikolic (2020)
10.1016/j.colsurfb.2020.110974
Development of a microemulsion for encapsulation and delivery of gallic acid. The role of chitosan.
Evgenia Mitsou (2020)
10.1021/acs.langmuir.7b00213
Reverse Micelles As Antioxidant Carriers: An Experimental and Molecular Dynamics Study.
Maria D. Chatzidaki (2017)
10.1016/j.colsurfb.2018.09.063
Potentiality of microemulsion systems in treatment of ophthalmic disorders: Keratoconus and dry eye syndrome - In vivo study.
N. Lidich (2019)
10.1016/j.colsurfb.2019.110482
Hydroxytyrosol encapsulated in biocompatible water-in-oil microemulsions: How the structure affects in vitro absorption.
Evgenia Mitsou (2019)
10.1208/s12249-018-1093-1
Getting the Jump on the Development of Bullfrog Oil Microemulsions: a Nanocarrier for Amphotericin B Intended for Antifungal Treatment
Wógenes N. Oliveira (2018)
10.1007/s00396-020-04603-w
Structural dynamics of tween-based microemulsions for antimuscarinic drug mirabegron
M. Nazar (2020)
10.1016/j.colsurfa.2018.09.079
Encapsulation of oils and fragrances by core-in-shell structures from silica particles, polymers and surfactants: The brick-and-mortar concept
G. M. Radulova (2018)
10.1016/j.canlet.2019.02.050
Adefovir dipivoxil sensitizes colon cancer cells to vemurafenib by disrupting the KCTD12-CDK1 interaction.
Jingqing Yang (2019)
10.3390/ma13051048
Self-Assembly of Organic Nanomaterials and Biomaterials: The Bottom-Up Approach for Functional Nanostructures Formation and Advanced Applications
D. Lombardo (2020)
10.1016/j.mencom.2019.05.027
Formulation, drug release features and in vitro cytotoxic evaluation of nonionic mixed surfactant stabilized water-in-oil microemulsion loaded with doxorubicin
N. Sedyakina (2019)
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