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

Bioavailability Enhancement Of Paclitaxel Via A Novel Oral Drug Delivery System: Paclitaxel-Loaded Glycyrrhizic Acid Micelles

F. Yang, Q. Zhang, Qian-ying Liang, S. Wang, Bo-xin Zhao, Ya-tian Wang, Yun Cai, Guo-feng Li
Published 2015 · Chemistry, Medicine

Cite This
Download PDF
Analyze on Scholarcy
Share
Paclitaxel (PTX, taxol), a classical antitumor drug against a wide range of tumors, shows poor oral bioavailability. In order to improve the oral bioavailability of PTX, glycyrrhizic acid (GA) was used as the carrier in this study. This was the first report on the preparation, characterization and the pharmacokinetic study in rats of PTX-loaded GA micelles The PTX-loaded micelles, prepared with ultrasonic dispersion method, displayed small particle sizes and spherical shapes. Differential scanning calorimeter (DSC) thermograms indicated that PTX was entrapped in the GA micelles and existed as an amorphous state. The encapsulation efficiency was about 90%, and the drug loading rate could reach up to 7.90%. PTX-loaded GA micelles displayed a delayed drug release compared to Taxol in the in vitro release experiment. In pharmacokinetic study via oral administration, the area under the plasma concentration-time curve (AUC0→24 h) of PTX-loaded GA micelles was about six times higher than that of Taxol (p < 0.05). The significant oral absorption enhancement of PTX from PTX-loaded GA micelles could be largely due to the increased absorption in jejunum and colon intestine. All these results suggested that GA would be a promising carrier for the oral delivery of PTX.
This paper references
10.1016/J.EJPB.2007.09.018
Cellular uptake and cytotoxicity of shell crosslinked stearic acid-grafted chitosan oligosaccharide micelles encapsulating doxorubicin.
F. Hu (2008)
10.1016/S0378-5173(99)00134-9
Drug-surfactant-propellant interactions in HFA-formulations.
C. Vervaet (1999)
10.1016/j.ejps.2012.05.015
Enhanced oral bioavailability of paclitaxel in pluronic/LHR mixed polymeric micelles: preparation, in vitro and in vivo evaluation.
Fatima Zohra Dahmani (2012)
10.1016/j.fct.2014.03.013
Systemic toxicity induced by paclitaxel in vivo is associated with the solvent cremophor EL through oxidative stress-driven mechanisms.
F. C. Campos (2014)
[Effects of 18 alpha-glycyrrhizic acid on rat liver cytochrome P450 isoenzymes and phase II transferase].
J. Yang (2001)
10.1016/j.ijpharm.2012.06.030
Stabilized micelles as delivery vehicles for paclitaxel.
K. Yoncheva (2012)
10.1248/YAKUSHI1947.120.10_849
A drug over the millennia: pharmacognosy, chemistry, and pharmacology of licorice.
S. Shibata (2000)
10.1016/S0142-9612(00)00292-1
Taxol-loaded block copolymer nanospheres composed of methoxy poly(ethylene glycol) and poly(epsilon-caprolactone) as novel anticancer drug carriers.
S. Kim (2001)
10.1016/j.biomaterials.2010.09.036
Development and in vivo evaluation of an oral drug delivery system for paclitaxel.
J. Iqbal (2011)
10.1016/j.ejpb.2010.06.007
Polymeric micelles for oral drug delivery.
G. Gaucher (2010)
10.1016/j.ijpharm.2011.04.066
Development of a liposomal formulation of the natural flavonoid fisetin.
N. Mignet (2012)
10.1002/jps.22241
Hydrotropic solubilization of poorly water-soluble drugs.
J. Kim (2010)
10.1134/S1607672913010092
β-casein micelle formation in water-ethanol solutions
T. A. Konnova (2013)
10.1080/10611860410001693760
Use of Targeting Agents to Increase Uptake and Localization of Drugs to the Intestinal Epithelium
G. J. Russell-Jones (2004)
10.1073/PNAS.94.5.2031
Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine.
A. Sparreboom (1997)
10.1016/S0378-5173(01)00986-3
Paclitaxel and its formulations.
A. K. Singla (2002)
10.1021/JP0739770
Effect of glycyrrhizic acid on lappaconitine phototransformation.
V. S. Kornievskaya (2007)
10.2147/IJN.S54040
Development of PLGA-based itraconazole injectable nanospheres for sustained release
Xiaomei Bian (2013)
Bioanalysis, pharmacokinetics, and pharmacodynamics of the novel anticancer drug paclitaxel (Taxol).
J. Beijnen (1994)
10.1021/JA052188Y
Loading of hydrophobic materials into polymer particles: implications for fluorescent nanosensors and drug delivery.
Huiguang Zhu (2005)
Nitric oxide donors can enhance the intestinal transport and absorption of insulin and
G Fetih (2005)
10.1248/BPB.19.1596
Pharmacokinetic study of taxol-loaded poly(lactic-co-glycolic acid) microspheres containing isopropyl myristate after targeted delivery to the lung in mice.
H. Sato (1996)
alpha-Tocopherol succinate-modified chitosan as a micellar delivery system for paclitaxel: Preparation, characterization and in vitro/in vivo
N. Liang (2012)
Sample Availability: Samples of the compounds of PTX and GA are available from the authors. © 2015 by the authors; licensee MDPI
10.1080/02652040110081406
The effect of oral absorption enhancers on the in vivo performance of insulin-loaded poly(ethylcyanoacrylate) nanospheres in diabetic rats
M. A. Radwan (2002)
10.1016/J.JCONREL.2005.05.017
Nitric oxide donors can enhance the intestinal transport and absorption of insulin and [Asu(1,7)]-eel calcitonin in rats.
G. Fetih (2005)
10.1002/JPS.2600520506
Phase solubility of solid species formed by magnesium aluminate from aqueous solutions containing sulfate ions.
T. Higuchi (1963)
10.1016/j.biomaterials.2010.12.039
Multifunctional Pluronic P123/F127 mixed polymeric micelles loaded with paclitaxel for the treatment of multidrug resistant tumors.
Wei Zhang (2011)
Polymeric micelles for oral drug
G. Gaucher (2010)
10.1038/SJ.JID.5700485
Nanoemulsions as versatile formulations for paclitaxel delivery: peroral and dermal delivery studies in rats.
S. Khandavilli (2007)
10.1016/j.jphotobiol.2012.03.006
Study on the interaction of glycyrrhizin and glycyrrhetinic acid with RNA.
Shohreh Nafisi (2012)
10.1016/j.ejps.2009.09.010
Combined hydroxypropyl-beta-cyclodextrin and poly(anhydride) nanoparticles improve the oral permeability of paclitaxel.
M. Agüeros (2009)
10.1016/S0928-0987(00)00081-6
Preparation and characterization of solid lipid nanospheres containing paclitaxel.
R. Cavalli (2000)
10.1016/J.FCT.2006.07.003
Inhibition of P-glycoprotein-mediated transport by terpenoids contained in herbal medicines and natural products.
N. Yoshida (2006)
10.1016/j.biomaterials.2013.10.063
A review of polypeptide-based polymersomes.
Lanxia Zhao (2014)
10.3390/md8041305
Chitosan Based Polyelectrolyte Complexes as Potential Carrier Materials in Drug Delivery Systems
J. Hamman (2010)
10.1002/chem.201102795
β-Cyclodextrin/glycyrrhizic acid functionalised quantum dots selectively enter hepatic cells and induce apoptosis.
M. Zhao (2012)
This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons
10.1016/j.ijpharm.2011.12.004
α-Tocopherol succinate-modified chitosan as a micellar delivery system for paclitaxel: preparation, characterization and in vitro/in vivo evaluations.
N. Liang (2012)
10.1016/j.jep.2005.04.015
A history of the therapeutic use of liquorice in Europe
C. Fiore (2005)
10.1016/j.ejpb.2008.08.015
Oral microemulsions of paclitaxel: in situ and pharmacokinetic studies.
Adwoa O. Nornoo (2009)
10.1016/j.foodchem.2014.04.022
Dynamic light scattering-based method to determine primary particle size of iron oxide nanoparticles in simulated gastrointestinal fluid.
Seungchul Yang (2014)
10.1007/s11095-012-0958-3
Effects of Particle Size and Surface Modification on Cellular Uptake and Biodistribution of Polymeric Nanoparticles for Drug Delivery
S. Kulkarni (2012)
10.1111/j.2042-7158.1962.tb11122.x
THE SOLUBILISING PROPERTIES OF LIQUORICE
K. James (1962)
10.2174/138955709789878123
The complexes of drugs with carbohydrate-containing plant metabolites as pharmacologically promising agents.
T. G. Tolstikova (2009)
Effects of particle size and surface modification on cellular uptake and biodistribution of polymeric nanoparticles for drug
S. A. Kulkarni (2013)
10.3109/00498250903271997
Effects of diammonium glycyrrhizinate on the pharmacokinetics of aconitine in rats and the potential mechanism
L. Chen (2009)
10.2147/IJN.S30721
Liposomes and nanotechnology in drug development: focus on neurological targets
P. Ramos-Cabrer (2013)
10.3109/10717541003777233
Enhanced oral paclitaxel bioavailability after administration of paclitaxel-loaded nanosponges
S. Torne (2010)
Sample Availability: Samples of the compounds of PTX and GA are available from the authors
10.1002/jps.21895
Evidence of carrier-mediated transport in the penetration of donepezil into the rat brain.
Mi-Hwa Kim (2010)
10.3109/10717544.2014.919544
Influence of glycyrrhizin on permeability and elasticity of cell membrane: perspectives for drugs delivery
O. Selyutina (2016)
10.1016/S0142-9612(03)00419-8
Preparation and characterization of poly(lactic acid)-poly(ethylene glycol)-poly(lactic acid) (PLA-PEG-PLA) microspheres for controlled release of paclitaxel.
G. Ruan (2003)
[Preparation of paclitaxel-loaded polybutylcyanoacrylate nanoparticles].
R. Chen (2010)



This paper is referenced by
10.18535/IJMSCI/V3I4.03
Pragmatic Approach To Drug Discovery Through Biophysical Perspective
Amit Alok (2016)
10.4172/pharmaceutical-sciences.1000500
Enhancing Solubility of Candesartan Cilexetil by Co-milling; Preparation of Candesartan Cilexetil-glycyrrhizic Acid Composite
L. J. (2019)
10.1016/J.JDDST.2019.101201
Pharmaceutical perspective on the translational hurdles of phytoconstituents and strategies to overcome
N. Sayed (2019)
10.1007/s13346-018-0565-x
Atorvastatin calcium inclusion complexation with polysaccharide arabinogalactan and saponin disodium glycyrrhizate for increasing of solubility and bioavailability
Ruiping Kong (2018)
10.1016/j.biopha.2017.08.123
Glycyrrhizic acid: A promising carrier material for anticancer therapy.
Xitong Su (2017)
10.5451/unibas-006618381
Stimuli-responsive amphiphilic peptides for biomedical applications
Severin J. Sigg (2016)
10.1016/J.IJPHARM.2020.119483
Optimization of solid self-dispersing micelle for enhancing dissolution and oral bioavailability of valsartan using Box-Behnken design.
Yoon Tae Goo (2020)
10.5530/IJPER.51.4S.84
Enhancement of Paclitaxel Oral Bioavailability in Swiss Mice by Four Consecutive Days of Pre-Treatment with Curcumin
A. Sharma (2017)
10.3390/ma12071058
Amphiphilic Copolymer of Polyhedral Oligomeric Silsesquioxane (POSS) Methacrylate for Solid Dispersion of Paclitaxel
S. Chatterjee (2019)
10.1016/j.ijpharm.2018.07.046
Drug metabolites and their effects on the development of adverse reactions: Revisiting Lipinski’s Rule of Five
C. M. Chagas (2018)
10.2147/IJN.S110251
Styrene maleic acid-encapsulated paclitaxel micelles: antitumor activity and toxicity studies following oral administration in a murine orthotopic colon cancer model
N. Parayath (2016)
10.1016/j.ijpharm.2017.10.011
Enhanced solubility and bioavailability of simvastatin by mechanochemically obtained complexes.
Ruiping Kong (2017)
Nanotechnology in Drug Delivery 52 3 Nanotechnology systems for oral drug delivery : challenges and opportunities
Alberto Berardi (2016)
10.1016/j.pharmthera.2020.107618
Glycyrrhizin: An alternative drug for the treatment of COVID-19 infection and the associated respiratory syndrome?
C. Bailly (2020)
10.1002/bmc.3960
Development and qualification of an LC-MS/MS method for investigating the biological implications of micelle entrapped paclitaxel in cell culture and rats.
A. Kaddoumi (2017)
10.1016/j.ijpharm.2020.119101
Enhanced penetration and anti-psoriatic efficacy of curcumin by improved smartPearls technology with the addition of glycyrrhizic acid.
N. Jin (2020)
10.1111/cbdd.13524
Design of diffusion‐controlled drug delivery devices for controlled release of Paclitaxel
Anurag Pramanik (2019)
10.2174/1567201816666190313155117
Molecular Dynamics Simulations of Glycyrrhizic Acid Aggregates as Drug-Carriers for Paclitaxel.
M. Hussain (2019)
10.1080/10717544.2016.1189625
Curcumin-carboxymethyl chitosan (CNC) conjugate and CNC/LHR mixed polymeric micelles as new approaches to improve the oral absorption of P-gp substrate drugs
J. Ni (2016)
10.1016/j.ijpharm.2019.01.047
Glycyrrhizic acid as a multifunctional drug carrier – From physicochemical properties to biomedical applications: A modern insight on the ancient drug
O.Yu. Selyutina (2019)
10.1007/s00232-020-00132-3
Effect of Glycyrrhizic Acid and Arabinogalactan on the Membrane Potential of Rat Thymocytes Studied by Potential-Sensitive Fluorescent Probe
Yuri I Glazachev (2020)
10.3109/10717544.2015.1135489
Formulation and evaluation of novel glycyrrhizic acid micelles for transdermal delivery of podophyllotoxin
Yatian Wang (2016)
10.3390/molecules23081904
Permeability of Ciprofloxacin-Loaded Polymeric Micelles Including Ginsenoside as P-glycoprotein Inhibitor through a Caco-2 Cells Monolayer as an Intestinal Absorption Model
Behzad Sharif Makhmal Zadeh (2018)
10.1016/J.JDDST.2019.01.014
Disodium salt of glycyrrhizic acid – A novel supramolecular delivery system for anthelmintic drug praziquantel
Elizaveta S. Meteleva (2019)
10.1080/10717544.2016.1228715
Oral administration of amphotericin B nanoparticles: antifungal activity, bioavailability and toxicity in rats
M. A. Radwan (2017)
10.1371/journal.pone.0217578
Using glycyrrhizic acid to target sumoylation processes during Epstein-Barr virus latency
G. L. Bentz (2019)
10.1016/j.yrtph.2017.10.023
Safety against nephrotoxicity in paclitaxel treatment: Oral nanocarrier as an effective tool in preclinical evaluation with marked in vivo antitumor activity
H. Choudhury (2017)
10.1016/B978-0-323-47720-8.00002-X
A novel approach to the oral delivery of bionanostructures for systemic disease
R. M. P. Gutiérrez (2017)
10.18632/oncotarget.8019
β-casein nanovehicles for oral delivery of chemotherapeutic drug combinations overcoming P-glycoprotein-mediated multidrug resistance in human gastric cancer cells
Maya Bar-Zeev (2016)
LOADING OF CLARITHROMYCIN AND PACLITAXEL ON SYNTHESIZED CdS/NiO NANOPARTICLES AS PROMISING NANOCARRIERS
Mustafa R. Abdulbaqi (2016)
10.3390/molecules24213947
Supramolecular Carotenoid Complexes of Enhanced Solubility and Stability—The Way of Bioavailability Improvement
A. L. Focsan (2019)
10.1016/j.ijpharm.2019.118693
Formulation of injectable glycyrrhizic acid-hydroxycamptothecin micelles as new generation of DNA topoisomerase I inhibitor for enhanced antitumor activity.
J. Cai (2019)
See more
Semantic Scholar Logo Some data provided by SemanticScholar