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

Pharmacokinetics And Tissue Distribution Of Idarubicin-loaded Solid Lipid Nanoparticles After Duodenal Administration To Rats.

G. Zara, A. Bargoni, R. Cavalli, A. Fundaró, D. Vighetto, M. Gasco
Published 2002 · Medicine, Chemistry

Cite This
Download PDF
Analyze on Scholarcy
Share
Idarubicin-loaded solid lipid nanoparticles (IDA-SLN) and idarubicin in solution were prepared and the two formulations were administered to rats, either by the duodenal route or intravenously (iv). The aim of this research was to study whether the bioavailability of idarubicin can be improved by administering IDA-SLN duodenally to rats. Idarubicin and its main metabolite idarubicinol were determined in plasma and tissues by reversed-phase high-performance liquid chromatography. The pharmacokinetic parameters of idarubicin found after duodenal administration of the two formulations were different: area under the curve of concentration versus time (AUC) and elimination half-life were approximately 21 times and 30 times, respectively, higher after IDA-SLN administration than after the solution administration. Tissue distribution also differed: idarubicin and idarubicinol concentrations were lower in heart, lung, spleen, and kidneys after IDA-SLN administration than after solution administration. The drug and its metabolite were detected in the brain only after IDA-SLN administration, indicating that SLN were able to pass the blood-brain barrier. After iv IDA-SLN administration, the AUC of idarubicin was lower than after duodenal administration of the same formulation. Duodenal administration of IDA-SLN modifies the pharmacokinetics and tissue distribution of idarubicin. The IDA-SLN act as a prolonged release system for the drug.
This paper references
10.2165/00003495-198734010-00003
Pentoxifylline. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic efficacy.
A. Ward (1987)
10.1016/S0378-5173(00)00562-7
Cellular uptake and cytotoxicity of solid lipid nanospheres (SLN) incorporating doxorubicin or paclitaxel.
A. Miglietta (2000)
10.1016/S0169-409X(98)00041-6
Evaluation of nano- and microparticle uptake by the gastrointestinal tract.
Delie (1998)
10.1021/JM00187A010
Synthesis of daunorubicin analogues with novel 9-acyl substituents.
T. H. Smith (1979)
10.1016/S0939-6411(97)00107-0
NMR relaxometric investigations of solid lipid nanoparticles (SLN) containing gadolinium(III) complexes.
S. Morel (1998)
10.1006/PHRS.2000.0695
Non-stealth and stealth solid lipid nanoparticles (SLN) carrying doxorubicin: pharmacokinetics and tissue distribution after i.v. administration to rats.
A. Fundaró (2000)
10.1007/BF00172021
Idarubicin (4-demethoxydaunorubicin)
F. Ganzina (2004)
10.1056/NEJM199809243391307
Doxorubicin-induced cardiomyopathy.
P. Singal (1998)
10.1016/0378-5173(95)04388-8
Thymopentin in solid lipid nanoparticles
S. Morel (1996)
10.1211/0022357001774976
Biodistribution of Stealth and Non‐stealth Solid Lipid Nanospheres after Intravenous Administration to Rats
Valerio Podio (2000)
Idarubicin: a brief overview on pharmacology and clinical use.
P. Borchmann (1997)
10.1097/00007691-199810000-00024
P-glycoprotein-mediated efflux transport of anticancer drugs at the blood-brain barrier.
A. Tsuji (1998)
10.2165/00003088-199324040-00002
Clinical Pharmacokinetics of Idarubicin
J. Robert (1993)
10.1023/A:1011975120776
Solid Lipid Nanoparticles in Lymph and Plasma After Duodenal Administration to Rats
A. Bargoni (2004)
Antitumor activity of 4-demethoxydaunorubicin administered orally.
A. di Marco (1977)
10.5414/CPP38217
Induction of apoptosis by idarubicin: how important is the plasma peak?
F. Gieseler (2000)
10.1021/JS980084Y
Nanoparticle technology for delivery of drugs across the blood-brain barrier.
U. Schroeder (1998)
10.1111/j.2042-7158.1995.tb06714.x
The Transfer of Polystyrene Microspheres from the Gastrointestinal Tract to the Circulation after Oral Administration in the Rat
J. Eyles (1995)
10.1023/A:1018888927852
Body Distribution of Camptothecin Solid Lipid Nanoparticles After Oral Administration
Shicheng Yang (2004)
10.1016/S0145-2126(99)00041-7
Idarubicin overcomes P-glycoprotein-related multidrug resistance: comparison with doxorubicin and daunorubicin in human multiple myeloma cell lines.
D. J. Roovers (1999)
10.1006/PHRS.2000.0737
Transmucosal transport of tobramycin incorporated in SLN after duodenal administration to rats. Part I--a pharmacokinetic study.
R. Cavalli (2000)
10.1016/0378-5173(93)90313-5
Solid lipospheres of doxorubicin and idarubicin
R. Cavalli (1993)
10.1007/BF00296245
Aspects of cytotoxic drug penetration, with particular reference to anthracyclines
D. Kerr (2004)
10.3109/10611869509015936
Factors affecting the oral uptake and translocation of polystyrene nanoparticles: histological and analytical evidence.
A. Florence (1995)
Plasma pharmacokinetics and cerebrospinal fluid concentrations of idarubicin and idarubicinol in pediatric leukemia patients: a Childrens Cancer Study Group report.
J. Reid (1990)
10.1007/BF00306743
Clinical pharmacology of 4-demethoxydaunorubicin (DMDR)
K. Lu (2004)
10.1063/1.1678153
Analysis of Macromolecular Polydispersity in Intensity Correlation Spectroscopy: The Method of Cumulants
D. Koppel (1972)
10.1016/S0169-409X(00)00122-8
Nanoparticulate systems for brain delivery of drugs.
J. Kreuter (2001)
10.1007/BF00175378
Phase I trial of 4-demethoxydaunorubicin (idarubicin) with single oral doses
S. Kaplan (2004)
10.1016/0378-4347(88)80049-5
High-performance liquid chromatographic determination of doxorubicin and its metabolites in plasma and tissue.
L. Rose (1988)
10.2337/diab.37.2.246
New Approach for Oral Administration of Insulin With Polyalkylcyanoacrylate Nanocapsules as Drug Carrier
C. Damgé (1988)
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)
10.2165/00002512-199711010-00006
Oral Idarubicin
M. Buckley (1997)
Improved peroral delivery of avarol with polybutylcyanoacrylate nanoparticles
P. Beck (1994)
10.1248/CPB.36.3503
Analysis of 4-demethoxydaunorubicin and metabolites in plasma and urine.
J. Beijnen (1988)
10.1016/0006-8993(95)00023-J
Passage of peptides through the blood-brain barrier with colloidal polymer particles (nanoparticles)
J. Kreuter (1995)
10.1038/clpt.1986.239
Plasma and human leukemic cell pharmacokinetics of oral and intravenous 4‐demethoxydaunomycin
Paul A J Speth (1986)



This paper is referenced by
10.1201/9780849374555.CH10
Brain Delivery by Nanoparticles
S. Gelperina (2006)
10.1016/j.nano.2008.08.003
Effect of lipid core material on characteristics of solid lipid nanoparticles designed for oral lymphatic delivery.
Rishi Paliwal (2009)
10.4155/TDE.10.7
Effect of lipid matrix on repaglinide-loaded solid lipid nanoparticles for oral delivery.
M. K. Rawat (2010)
10.1007/978-1-4939-1399-2_4
Diagnosing Biopharmaceutical Limitations
S. Jenkins (2015)
Development, characterization and evaluation of solid lipid nanoparticles as a potential anticancer drug delivery system
M. Patel (2012)
Optimising nanomedicine pharmacokinetics using PBPK modelling
D. Moss (2017)
10.1201/9781420008449.CH13
Pharmaceutical Applications of Nanoparticulate Drug-Delivery Systems
Y. Pathak (2007)
10.3390/molecules13020230
Cholesterylbutyrate Solid Lipid Nanoparticles as a Butyric Acid Prodrug
A. Brioschi (2008)
10.1007/978-1-4614-9434-8_20
Delivery Systems for Lymphatic Targeting
I. Singh (2013)
10.1016/j.ijpharm.2008.04.027
Pharmacokinetics and pharmacodynamics of chlorambucil delivered in parenteral emulsion.
Srinivas Ganta (2008)
10.1016/j.ejpb.2014.05.004
Solid lipid nanoparticles as vehicles of drugs to the brain: current state of the art.
L. Gastaldi (2014)
10.1016/J.JCONREL.2004.01.005
Preparation, characterization and in vitro release kinetics of clozapine solid lipid nanoparticles.
V. Venkateswarlu (2004)
10.1016/j.pneurobio.2008.12.002
Delivery of peptide and protein drugs over the blood–brain barrier
I. Brasnjevic (2009)
10.1007/978-0-387-76554-9_2
Multifunctional Polymeric Nanosystems for Tumor-Targeted Delivery
P. Magadala (2008)
10.17169/REFUBIUM-15652
Nanostructured Lipid Carriers (NLC) in dermal and personal care formulations
A. Hommoss (2009)
Engineering lipid nanocapsule systems for intracellular delivery of anticancer drugs
P. Moreno (2014)
DRUG DELIVERY SYSTEMS PROVIDE BETTER OPTION FOR MANAGEMENT OF TUBERCLULOSIS
M. Raja (2002)
10.1016/S0079-6123(08)80011-8
Solid lipid nanoparticles for brain tumors therapy
A. Brioschi (2009)
10.1016/j.jconrel.2017.01.039
ApoE‐modified solid lipid nanoparticles: A feasible strategy to cross the blood‐brain barrier
R. Dal Magro (2017)
Solid lipid nanoparticles :A promising tool for drug delivery system
B. Basu (2010)
10.1007/978-3-662-47862-2_11
Nanostructured Lipid Carriers (NLC): The Second Generation of Solid Lipid Nanoparticles
R. Mueller (2016)
10.1016/S0079-6123(08)80011-8
Chapter 11 - Solid lipid nanoparticles for brain tumors therapy: State of the art and novel challenges.
A. Brioschi (2009)
NANOSTRUCTURE LIPID CARRIERS (NLC) FOR TOPICAL APPLICATION: A REVIEW
Gajanan Y. Shinde (2013)
10.1166/JBN.2009.1021
Development of idarubicin and doxorubicin solid lipid nanoparticles to overcome Pgp-mediated multiple drug resistance in leukemia.
P. Ma (2009)
10.1016/J.IJPHARM.2004.12.030
New surface-modified lipid nanoparticles as delivery vehicles for salmon calcitonin.
M. Garcia-Fuentes (2005)
Mikrosfery lipidowe jako nowa postać leku pozajelitowego : opracowanie metody sporządzania i próba inkorporacji substancji leczniczych
J. Pietkiewicz (2005)
10.1016/j.ijpharm.2011.11.035
Lipomer of doxorubicin hydrochloride for enhanced oral bioavailability.
Derajram M Benival (2012)
10.1016/J.JCONREL.2005.06.006
Pharmacokinetics, tissue distribution and bioavailability of clozapine solid lipid nanoparticles after intravenous and intraduodenal administration.
K. Manjunath (2005)
10.1002/jps.22435
Studies on binary lipid matrix based solid lipid nanoparticles of repaglinide: in vitro and in vivo evaluation.
M. K. Rawat (2011)
10.1016/j.jconrel.2011.10.027
Polypeptide conjugates of D-penicillamine and idarubicin for anticancer therapy.
S. Wadhwa (2012)
10.5772/54781
Solid Lipid Nanoparticles: Tuneable Anti-Cancer Gene/Drug Delivery Systems
Tranum Kaur (2013)
10.1016/j.cis.2019.102033
Nanoparticles fabricated from bulk solid lipids: Preparation, properties, and potential food applications.
Q. Zhong (2019)
See more
Semantic Scholar Logo Some data provided by SemanticScholar