← Back to Search
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
Download PDFAnalyze on Scholarcy
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
New perspectives on lipid and surfactant based drug delivery systems for oral delivery of poorly soluble drugs
A. Müllertz (2010)
Nanostructured lipid matrices for improved microencapsulation of drugs.
R. Mueller (2002)
Enhanced Intestinal Absorption of Cyclosporine in Rats Through the Reduction of Emulsion Droplet Size
B. Tarr (2004)
Nanosizing: a formulation approach for poorly-water-soluble compounds.
E. Merisko-Liversidge (2003)
Formulation of lipid-based delivery systems for oral administration: materials, methods and strategies.
C. Pouton (2008)
Oral bioavailability of cyclosporine: solid lipid nanoparticles (SLN) versus drug nanocrystals.
R. Mueller (2006)
Lipid--an emerging platform for oral delivery of drugs with poor bioavailability.
S. Chakraborty (2009)
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)
Lipid nanoparticles with a solid matrix (SLN, NLC, LDC) for oral drug delivery.
M. Muchow (2008)
Preparation and characterization of sterile and freeze-dried sub-200 nm nanoparticles.
Y. Konan (2002)
Fundamentals of Nuclear Pharmacy
G. Saha (1979)
Short- and long-term stability study of lyophilized solid lipid nanoparticles for gene therapy.
A. Del Pozo-Rodríguez (2009)
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)
Effects of lipophilic emulsifiers on the oral administration of lovastatin from nanostructured lipid carriers: physicochemical characterization and pharmacokinetics.
C. Chen (2010)
Lipid Nanoparticles with a Solid Matrix (SLN®, NLC®, LDC®) for Oral Drug Delivery
M. Muchow (2008)
Lipid-based delivery systems and intestinal lymphatic drug transport: A mechanistic update☆
Natalie L Trevaskis (2008)
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)
Transcytosis of nanoparticle and dendrimer delivery systems: evolving vistas.
A. Florence (2001)
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)
Nanosizing--oral formulation development and biopharmaceutical evaluation.
F. Kesisoglou (2007)
Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs
C. H. Porter (2007)
Drug Nanoparticles: Formulating Poorly Water-Soluble Compounds
E. Merisko-Liversidge (2008)
Lipid excipients and delivery systems for pharmaceutical development: a regulatory perspective.
M. Chen (2008)
Biodistribution and toxicity of nanodiamonds in mice after intratracheal instillation.
X. Zhang (2010)
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)
Lymphatic Transport of Drugs
W. Charman (1992)
Preparation and characterization of spironolactone-loaded nanocapsules for paediatric use.
I. Limayem Blouza (2006)
Nanosizing for oral and parenteral drug delivery: a perspective on formulating poorly-water soluble compounds using wet media milling technology.
E. Merisko-Liversidge (2011)
Pharmaceutical Technologies for Enhancing Oral Bioavailability of Poorly Soluble Drugs
Y. R. Krishnaiah (2010)
Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the lipid formulation classification system.
C. Pouton (2006)
Enhancing intestinal drug solubilisation using lipid-based delivery systems.
C. H. Porter (2008)
Biopharmaceutical challenges associated with drugs with low aqueous solubility--the potential impact of lipid-based formulations.
C. O'Driscoll (2008)
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)
Recent Advances in Lipid Nanoparticle Formulations with Solid Matrix for Oral Drug Delivery
S. Das (2010)
Solid lipid nanoparticles: production, characterization and applications.
W. Mehnert (2001)
Nanosuspension Formulations for Low-Soluble Drugs: Pharmacokinetic Evaluation Using Spironolactone as Model Compound
P. Langguth (2005)
Encapsulation of ascorbyl palmitate in nanostructured lipid carriers (NLC)--effects of formulation parameters on physicochemical stability.
Veerawat Teeranachaideekul (2007)
Understanding the lipid-digestion processes in the GI tract before designing lipid-based drug-delivery systems.
J. Bakala N'Goma (2012)
Freeze-drying of nanoparticles: formulation, process and storage considerations.
W. Abdelwahed (2006)
Rockville: Centre for Drug Evaluation and Research (CDER)
THE METABOLISM AND BIOPHARMACEUTICS OF SPIRONOLACTONE IN MAN
H. W. Overdiek (1987)
Approaches for the development of solid and semi-solid lipid-based formulations.
V. Jannin (2008)
The Guide for the Care and Use of Laboratory Animals.
L. Michael (2016)
Oral lipid-based formulations.
D. Hauss (2007)
Nanoparticle uptake by the oral route: Fulfilling its potential?
A. Florence (2005)
This paper is referenced by
Ethyl oleate-containing nanostructured lipid carriers improve oral bioavailability of trans-ferulic acid ascompared with conventional solid lipid nanoparticles.
Yongtai Zhang (2016)
Solid lipid matrix mediated nanoarchitectonics for improved oral bioavailability of drugs
S. Banerjee (2019)
The stimulation of GLP-1 secretion and delivery of GLP-1 agonists via nanostructured lipid carriers.
N. Shrestha (2018)
Nanostructured lipid carriers: versatile oral delivery vehicle
Neelam Poonia (2016)
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)
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)
A Mechanistic Study on Nanoparticle-Mediated Glucagon-Like Peptide-1 (GLP-1) Secretion from Enteroendocrine L Cells.
A. Beloqui (2016)
Combined Treatment of Tyrosine Kinase Inhibitor-Labeled Gold Nanorod Encapsulated Albumin With Laser Thermal Ablation in a Renal Cell Carcinoma Model.
C. Callaghan (2016)
Nanostructured lipid carriers as oral delivery systems for poorly soluble drugs
Ana Beloqui (2017)
Lipid nanoparticles to counteract gastric infection without affecting gut microbiota
C. L. Seabra (2018)
Development of liposome-encapsulated ketoconazole: formulation, characterisation and evaluation of pharmacological therapeutic efficacy
Sarbani Ashe (2015)
Bridging the Gap between the Bench and the Clinic : Inflammatory Bowel Disease
Susan Z. Hua (2017)
Nanocolloidal lipidic carriers of olmesartan medoxomil surface-tailored with Concavalin-A for lectin receptor targeting.
S. Beg (2018)
Nanostructured lipid carriers: Promising drug delivery systems for future clinics.
A. Beloqui (2016)
Solid lipid nanoparticles and nanostructured lipid carriers as novel drug delivery systems: applications, advantages and disadvantages
Parisa Ghasemiyeh (2018)
Nanostructured lipid carriers (NLC) system: A novel drug targeting carrier
Vedanti R. Salvi (2019)
Lipid Nanoparticles as Carriers for RNAi against Viral Infections: Current Status and Future Perspectives
J. Torrecilla (2014)
Development, optimization and evaluation of long chain nanolipid carrier for hepatic delivery of silymarin through lymphatic transport pathway.
Shilpa Chaudhary (2015)
Dextran-protamine coated nanostructured lipid carriers as mucus-penetrating nanoparticles for lipophilic drugs.
A. Beloqui (2014)
Lipid-based Nanoplatforms in Cancer Therapy: Recent Advances and Applications.
Kuldeep Rajpoot (2020)
Candesartan cilexetil loaded nanodelivery systems for improved oral bioavailability.
N. Dudhipala (2017)
Nanodrugs in Medicine and Healthcare: Oral Delivery
A. Sosnik (2016)
Optimization of nanostructured lipid carriers: understanding the types, designs, and parameters in the process of formulations
B. Subramaniam (2020)
Nanostructured lipid (NLCs) carriers as a bioavailability enhancement tool for oral administration
Bharti Gaba (2015)
A comparative study of curcumin-loaded lipid-based nanocarriers in the treatment of inflammatory bowel disease.
A. Beloqui (2016)
Nanostructured lipid carriers: A potential use for skin drug delivery systems.
A. Czajkowska-Kośnik (2019)
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)
Spironolactone nanocrystals for oral administration: Different pharmacokinetic performances induced by stabilizers.
Simeng Mu (2016)
Herbal and polymeric approaches for liver-targeting drug delivery: novel strategies and their significance
R. Rohilla (2016)
Nanostructured lipid carriers versus microemulsions for delivery of the poorly water-soluble drug luteolin.
Ying Liu (2014)
Novel nanoemulsion based lipid nanosystems for favorable in vitro and in vivo characteristics of curcumin.
Kun Wan (2016)