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Fate Of Nanostructured Lipid Carriers (NLCs) Following The Oral Route: Design, Pharmacokinetics And Biodistribution

A. Beloqui, M. A. Solinís, A. Delgado, C. Évora, A. Isla, A. Rodríguez-Gascón
Published 2014 · Materials Science, Medicine

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Abstract The aim of this study was to develop a nanostructured lipid carriers (NLC) formulation containing spironolactone (SPN-NLCs), and to investigate its potential for the oral delivery of poorly water-soluble compounds. SPN-NLCs were orally administered to rabbits and the pharmacokinetics of spironolactone and its metabolites was evaluated. As reference formulation, we administered syrup. Spironolactone was only detected in a few plasma samples; hence, metabolite levels were employed for the pharmacokinetic analysis. The absolute bioavailability of 7α-TMS was significantly higher with the syrup than those obtained with the SPN-NLCs (0.7 versus 0.4, p < 0.05). However, no significant differences were observed in the bioavailability of canrenone, revealing a different canrenone/7α-TMS ratio depending on the administered formulation. Orally administered 99mTc-radiolabeled SPN-NLCs were mainly detected in the small intestine. These results suggest the retention of the nanocarriers in the underlying epithelium and further uptake by the epithelial cells.
This paper references
10.1111/j.2042-7158.2010.01107.x
New perspectives on lipid and surfactant based drug delivery systems for oral delivery of poorly soluble drugs
A. Müllertz (2010)
10.1016/S0378-5173(02)00180-1
Nanostructured lipid matrices for improved microencapsulation of drugs.
R. Mueller (2002)
10.1023/A:1015843517762
Enhanced Intestinal Absorption of Cyclosporine in Rats Through the Reduction of Emulsion Droplet Size
B. Tarr (2004)
10.1016/S0928-0987(02)00251-8
Nanosizing: a formulation approach for poorly-water-soluble compounds.
E. Merisko-Liversidge (2003)
10.1016/J.ADDR.2007.10.010
Formulation of lipid-based delivery systems for oral administration: materials, methods and strategies.
C. Pouton (2008)
10.1016/J.IJPHARM.2006.02.045
Oral bioavailability of cyclosporine: solid lipid nanoparticles (SLN) versus drug nanocrystals.
R. Mueller (2006)
10.1016/j.ejpb.2009.06.001
Lipid--an emerging platform for oral delivery of drugs with poor bioavailability.
S. Chakraborty (2009)
10.1016/J.EJPB.2007.01.017
The effect of different lipid based formulations on the oral absorption of lipophilic drugs: the ability of in vitro lipolysis and consecutive ex vivo intestinal permeability data to predict in vivo bioavailability in rats.
A. Dahan (2007)
10.1080/03639040802130061
Lipid nanoparticles with a solid matrix (SLN, NLC, LDC) for oral drug delivery.
M. Muchow (2008)
10.1016/S0378-5173(01)00944-9
Preparation and characterization of sterile and freeze-dried sub-200 nm nanoparticles.
Y. Konan (2002)
10.1007/978-1-4757-4021-9
Fundamentals of Nuclear Pharmacy
G. Saha (1979)
10.1016/j.ejpb.2008.09.015
Short- and long-term stability study of lyophilized solid lipid nanoparticles for gene therapy.
A. Del Pozo-Rodríguez (2009)
10.1016/j.colsurfb.2012.01.001
Design and evaluation of polymer coated carvedilol loaded solid lipid nanoparticles to improve the oral bioavailability: a novel strategy to avoid intraduodenal administration.
Vinay Kumar Venishetty (2012)
10.1016/j.ejpb.2009.12.008
Effects of lipophilic emulsifiers on the oral administration of lovastatin from nanostructured lipid carriers: physicochemical characterization and pharmacokinetics.
C. Chen (2010)
10.1080/03639040802130061
Lipid Nanoparticles with a Solid Matrix (SLN®, NLC®, LDC®) for Oral Drug Delivery
M. Muchow (2008)
10.1016/j.addr.2007.09.007
Lipid-based delivery systems and intestinal lymphatic drug transport: A mechanistic update☆
Natalie L Trevaskis (2008)
10.5860/choice.34-3310
Guide for the Care and Use of Laboratory Animals
Division on Earth (1996)
Letter: Intestinal absorption of pertechnetate: calculation by the oral-intravenous plasma activity quotients and inverse convolution method.
J. Szymendera (1974)
10.1016/S0169-409X(01)00184-3
Transcytosis of nanoparticle and dendrimer delivery systems: evolving vistas.
A. Florence (2001)
10.1002/jps.23205
Toward the establishment of standardized in vitro tests for lipid-based formulations, part 1: method parameterization and comparison of in vitro digestion profiles across a range of representative formulations.
H. Williams (2012)
10.1016/J.ADDR.2007.05.003
Nanosizing--oral formulation development and biopharmaceutical evaluation.
F. Kesisoglou (2007)
10.1038/nrd2197
Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs
C. H. Porter (2007)
10.1177/0192623307310946
Drug Nanoparticles: Formulating Poorly Water-Soluble Compounds
E. Merisko-Liversidge (2008)
10.1016/J.ADDR.2007.09.010
Lipid excipients and delivery systems for pharmaceutical development: a regulatory perspective.
M. Chen (2008)
10.1016/j.toxlet.2010.07.001
Biodistribution and toxicity of nanodiamonds in mice after intratracheal instillation.
X. Zhang (2010)
10.1016/j.jconrel.2008.03.021
Rationalizing the selection of oral lipid based drug delivery systems by an in vitro dynamic lipolysis model for improved oral bioavailability of poorly water soluble drugs.
A. Dahan (2008)
10.1201/9780203748572
Lymphatic Transport of Drugs
W. Charman (1992)
10.1016/J.IJPHARM.2006.06.022
Preparation and characterization of spironolactone-loaded nanocapsules for paediatric use.
I. Limayem Blouza (2006)
10.1016/j.addr.2010.12.007
Nanosizing for oral and parenteral drug delivery: a perspective on formulating poorly-water soluble compounds using wet media milling technology.
E. Merisko-Liversidge (2011)
10.4172/JBB.1000027
Pharmaceutical Technologies for Enhancing Oral Bioavailability of Poorly Soluble Drugs
Y. R. Krishnaiah (2010)
10.1016/J.EJPS.2006.04.016
Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the lipid formulation classification system.
C. Pouton (2006)
10.1016/J.ADDR.2007.10.014
Enhancing intestinal drug solubilisation using lipid-based delivery systems.
C. H. Porter (2008)
10.1016/J.ADDR.2007.10.012
Biopharmaceutical challenges associated with drugs with low aqueous solubility--the potential impact of lipid-based formulations.
C. O'Driscoll (2008)
10.1016/S0939-6411(00)00087-4
Solid lipid nanoparticles (SLN) for controlled drug delivery - a review of the state of the art.
R. Mueller (2000)
Dissolution test for solid dosage forms
European Pharmacopeia. (2007)
Fundamentals of Nuclear Pharmacy. 6th edn
G B Saha (2010)
10.1208/s12249-010-9563-0
Recent Advances in Lipid Nanoparticle Formulations with Solid Matrix for Oral Drug Delivery
S. Das (2010)
10.1016/S0169-409X(01)00105-3
Solid lipid nanoparticles: production, characterization and applications.
W. Mehnert (2001)
10.1081/DDC-52182
Nanosuspension Formulations for Low-Soluble Drugs: Pharmacokinetic Evaluation Using Spironolactone as Model Compound
P. Langguth (2005)
10.1016/J.IJPHARM.2007.03.022
Encapsulation of ascorbyl palmitate in nanostructured lipid carriers (NLC)--effects of formulation parameters on physicochemical stability.
Veerawat Teeranachaideekul (2007)
10.4155/TDE.11.138
Understanding the lipid-digestion processes in the GI tract before designing lipid-based drug-delivery systems.
J. Bakala N'Goma (2012)
10.1016/J.ADDR.2006.09.017
Freeze-drying of nanoparticles: formulation, process and storage considerations.
W. Abdelwahed (2006)
Rockville: Centre for Drug Evaluation and Research (CDER)
(2001)
10.1515/DMDI.1987.5.4.273
THE METABOLISM AND BIOPHARMACEUTICS OF SPIRONOLACTONE IN MAN
H. W. Overdiek (1987)
10.1016/J.ADDR.2007.09.006
Approaches for the development of solid and semi-solid lipid-based formulations.
V. Jannin (2008)
10.1093/ilar/ilw049
The Guide for the Care and Use of Laboratory Animals.
L. Michael (2016)
10.1016/J.ADDR.2007.05.006
Oral lipid-based formulations.
D. Hauss (2007)
10.1016/j.ddtec.2005.05.019
Nanoparticle uptake by the oral route: Fulfilling its potential?
A. Florence (2005)



This paper is referenced by
10.1016/j.ijpharm.2016.06.131
Ethyl oleate-containing nanostructured lipid carriers improve oral bioavailability of trans-ferulic acid ascompared with conventional solid lipid nanoparticles.
Yongtai Zhang (2016)
10.1080/17425255.2019.1621289
Solid lipid matrix mediated nanoarchitectonics for improved oral bioavailability of drugs
S. Banerjee (2019)
10.1039/c7nr07736j
The stimulation of GLP-1 secretion and delivery of GLP-1 agonists via nanostructured lipid carriers.
N. Shrestha (2018)
10.4155/fsoa-2016-0030
Nanostructured lipid carriers: versatile oral delivery vehicle
Neelam Poonia (2016)
10.1007/s00289-020-03293-2
Synthesis and evaluation of the efficiency of antibacterial hydrogel beads based on the sodium alginate–ferula gum for delayed release of quercetin
M. S. Seyed Dorraji (2020)
10.1016/j.nano.2015.02.018
Advances in oral nano-delivery systems for colon targeted drug delivery in inflammatory bowel disease: selective targeting to diseased versus healthy tissue.
Susan Hua (2015)
10.1021/ACS.MOLPHARMACEUT.6B00871
A Mechanistic Study on Nanoparticle-Mediated Glucagon-Like Peptide-1 (GLP-1) Secretion from Enteroendocrine L Cells.
A. Beloqui (2016)
10.1016/j.xphs.2015.11.017
Combined Treatment of Tyrosine Kinase Inhibitor-Labeled Gold Nanorod Encapsulated Albumin With Laser Thermal Ablation in a Renal Cell Carcinoma Model.
C. Callaghan (2016)
10.1016/J.JDDST.2017.06.013
Nanostructured lipid carriers as oral delivery systems for poorly soluble drugs
Ana Beloqui (2017)
10.1016/j.ejpb.2018.02.030
Lipid nanoparticles to counteract gastric infection without affecting gut microbiota
C. L. Seabra (2018)
10.1049/MNL.2014.0198
Development of liposome-encapsulated ketoconazole: formulation, characterisation and evaluation of pharmacological therapeutic efficacy
Sarbani Ashe (2015)
10.1201/9781315152356-9
Bridging the Gap between the Bench and the Clinic : Inflammatory Bowel Disease
Susan Z. Hua (2017)
10.2217/nnm-2018-0188
Nanocolloidal lipidic carriers of olmesartan medoxomil surface-tailored with Concavalin-A for lectin receptor targeting.
S. Beg (2018)
10.1016/j.nano.2015.09.004
Nanostructured lipid carriers: Promising drug delivery systems for future clinics.
A. Beloqui (2016)
10.4103/1735-5362.235156
Solid lipid nanoparticles and nanostructured lipid carriers as novel drug delivery systems: applications, advantages and disadvantages
Parisa Ghasemiyeh (2018)
10.1016/J.JDDST.2019.02.017
Nanostructured lipid carriers (NLC) system: A novel drug targeting carrier
Vedanti R. Salvi (2019)
10.1155/2014/161794
Lipid Nanoparticles as Carriers for RNAi against Viral Infections: Current Status and Future Perspectives
J. Torrecilla (2014)
10.1016/j.ijpharm.2015.02.070
Development, optimization and evaluation of long chain nanolipid carrier for hepatic delivery of silymarin through lymphatic transport pathway.
Shilpa Chaudhary (2015)
10.1016/j.ijpharm.2014.04.027
Dextran-protamine coated nanostructured lipid carriers as mucus-penetrating nanoparticles for lipophilic drugs.
A. Beloqui (2014)
10.2174/1568009620666200115160805
Lipid-based Nanoplatforms in Cancer Therapy: Recent Advances and Applications.
Kuldeep Rajpoot (2020)
10.4155/tde-2016-0063
Candesartan cilexetil loaded nanodelivery systems for improved oral bioavailability.
N. Dudhipala (2017)
10.1002/9783527800681.CH24
Nanodrugs in Medicine and Healthcare: Oral Delivery
A. Sosnik (2016)
10.1007/s11051-020-04848-0
Optimization of nanostructured lipid carriers: understanding the types, designs, and parameters in the process of formulations
B. Subramaniam (2020)
10.3109/10717544.2014.898110
Nanostructured lipid (NLCs) carriers as a bioavailability enhancement tool for oral administration
Bharti Gaba (2015)
10.1016/j.colsurfb.2016.03.038
A comparative study of curcumin-loaded lipid-based nanocarriers in the treatment of inflammatory bowel disease.
A. Beloqui (2016)
10.1016/j.pharep.2018.10.008
Nanostructured lipid carriers: A potential use for skin drug delivery systems.
A. Czajkowska-Kośnik (2019)
10.1186/s12951-014-0039-3
The role of lipid-based nano delivery systems on oral bioavailability enhancement of fenofibrate, a BCS II drug: comparison with fast-release formulations
Tengfei Weng (2014)
10.1016/j.colsurfb.2016.07.051
Spironolactone nanocrystals for oral administration: Different pharmacokinetic performances induced by stabilizers.
Simeng Mu (2016)
10.3109/10717544.2014.945018
Herbal and polymeric approaches for liver-targeting drug delivery: novel strategies and their significance
R. Rohilla (2016)
10.1016/j.ijpharm.2014.09.052
Nanostructured lipid carriers versus microemulsions for delivery of the poorly water-soluble drug luteolin.
Ying Liu (2014)
10.1016/j.ijpharm.2016.03.055
Novel nanoemulsion based lipid nanosystems for favorable in vitro and in vivo characteristics of curcumin.
Kun Wan (2016)
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