Online citations, reference lists, and bibliographies.
Please confirm you are human
(Sign Up for free to never see this)
← Back to Search

Cyclosporine-loaded Solid Lipid Nanoparticles (SLN): Drug-lipid Physicochemical Interactions And Characterization Of Drug Incorporation.

R. Mueller, S. Runge, V. Ravelli, A. Thünemann, W. Mehnert, E. Souto
Published 2008 · Chemistry, Medicine

Save to my Library
Download PDF
Analyze on Scholarcy
Solid lipid nanoparticles (SLN) were produced loaded with cyclosporine A in order to develop an improved oral formulation. In this study, the particles were characterized with regard to the structure of the lipid particle matrix, being a determining factor for mode of drug incorporation and drug release. Differential scanning calorimetry (DSC) and wide-angle X-ray scattering (WAXS) measurements were employed for the analysis of the polymorphic modifications and mode of drug incorporation. Particles were produced using Imwitor 900 as lipid matrix (the suspension consisted of 10% particles, 8% Imwitor 900, 2% cyclosporine A), 2.5% Tagat S, 0.5% sodium cholate and 87% water. DSC and WAXS were used to analyse bulk lipid, bulk drug, drug incorporated in the bulk and unloaded and drug-loaded SLN dispersions. The processing of the bulk lipid into nanoparticles was accompanied by a polymorphic transformation from the beta to the alpha-modification. After production, the drug-free SLN dispersions converted back to beta-modification, while the drug-loaded SLN stayed primarily in alpha-modification. After incorporation of cyclosporine A into SLN, the peptide lost its crystalline character. Based on WAXS data, it could be concluded that cyclosporine is molecularly dispersed in between the fatty acid chains of the liquid-crystalline alpha-modification fraction of the loaded SLN.
This paper references
Analytical profiles of drug substances
K. Florey (1972)
Solid lipid nanoparticles (SLN) for controlled drug delivery--drug release and release mechanism.
A. Zur Mühlen (1998)
Preparation of submicron drug particles in lecithin-stabilized o/w emulsions I. Model studies of the precipitation of cholesteryl acetate
B. Sjoestroem (1992)
Solid lipid nanoparticles (SLN) for controlled drug delivery. II. Drug incorporation and physicochemical characterization.
C. Schwarz (1999)
Cytotoxicity of magnetite-loaded polylactide, polylactide/glycolide particles and solid lipid nanoparticles
R. Mueller (1996)
A study of the freeze-drying conditions of calixarene based solid lipid nanoparticles.
P. Shahgaldian (2003)
Properties and stability of a liquid crystal form of cyclosporine-the first reported naturally occurring peptide that exists as a thermotropic liquid crystal.
D. Lechuga-Ballesteros (2003)
Handbook of Pharmaceutical Controlled Release Technology
D. Wise (2000)
Solid Lipid Nanoparticles (SLN) and Nanostructured Lipid Carriers (NLC) for Dermal Delivery
R. Mu¨ller (2005)
Crystallization tendency and polymorphic transitions in triglyceride nanoparticles
H. Bunjes (1996)
Preparation of solid lipid nanoparticles by a solvent emulsification-diffusion technique.
M. Trotta (2003)
Solid lipid nanoparticles (SLN) for controlled drug delivery - a review of the state of the art.
R. Mueller (2000)
Solid lipid nanoparticles: production, characterization and applications.
W. Mehnert (2001)
Differential interaction of human renal P-glycoprotein with various metabolites and analogues of cyclosporin A.
J. Charuk (1995)
Physicochemical investigations on the structure of drug-free and drug-loaded solid lipid nanoparticles (SLN) by means of DSC and 1H NMR.
E. Zimmermann (2005)
Solid lipid nanoparticles (SLN) : an alternative colloidal carrier system for controlled drug delivery
R. Mueller (1995)
Novel lipid-based colloidal dispersions as potential drug administration systems – expectations and reality
K. Westesen (2000)
Physicochemical characterization of lipid nanoparticles and evaluation of their drug loading capacity and sustained release potential
K. Westesen (1997)
Solubility and Mass and Nuclear Magnetic Resonance Spectroscopic Studies on Interaction of Cyclosporin A with Dimethyl‐α‐ and ‐β‐Cyclodextrins in Aqueous Solution
K. Miyake (1999)
Solvent injection as a new approach for manufacturing lipid nanoparticles--evaluation of the method and process parameters.
M. Schubert (2003)
Large-Scale Production of Solid Lipid Nanoparticles (SLN) and Nanosuspensions (DissoCubes)
Donald L. Wise (2000)
Oral bioavailability of cyclosporine: solid lipid nanoparticles (SLN) versus drug nanocrystals.
R. Mueller (2006)
Medium scale production of solid lipid nanoparticles (SLN) by high pressure homogenization
V. Jenning (2002)
Lipid Nanoparticles (Solid Lipid Nanoparticles and Nanostructured Lipid Carriers) for Cosmetic, Dermal, and Transdermal Applications
E. Souto (2007)
Solid lipid nanoparticles (SLN) for controlled drug delivery
R. Mueller (1996)
The Kelvin equation and solubility of small particles.
Kenneth G. Nelson (1972)
Pellets as carriers of solid lipid nanoparticles (SLN) for oral administration of drugs
J. F. Pinto (1999)
Crystallization and polymorphism of fats and fatty acids
N. Garti (1988)
Investigations on the physical state of lipid nanoparticles by synchrotron radiation X-ray diffraction
K. Westesen (1993)
Preparation of submicron drug particles in lecithin-stabilized o/w emulsions. II. Characterization of cholesteryl acetate particles
B. Sjoestroem (1993)
The triglyceride lipases of the pancreas Published, JLR Papers in Press, October 1, 2002. DOI 10.1194/jlr.R200012-JLR200
M. Lowe (2002)
Production of solid lipid nanoparticles (SLN): scaling up feasibilities
A. Dingler (2002)

This paper is referenced by
Lipid Nanoparticulate Drug Delivery And Nanomedicine
H. M. Mansour (2012)
Pharmacokinetics and biodistribution of the nanoparticles
K. Raza (2017)
Cellular uptake of coumarin-6 as a model drug loaded in solid lipid nanoparticles.
I. Rivolta (2011)
Lipid nanoparticles for the delivery of poorly water‐soluble drugs
H. Bunjes (2010)
Lopinavir loaded solid lipid nanoparticles (SLN) for intestinal lymphatic targeting.
M. R. Aji Alex (2011)
Nanostructured Lipid Carriers
Jingyuan Wen (2018)
Lipid-drug conjugates: a potential nanocarrier system for oral drug delivery applications
S. Banerjee (2018)
Thermal characterization of solid lipid nanoparticles containing praziquantel
Adélia Emília de Almeida (2011)
Formulation development and in vitro evaluation of didanosine-loaded nanostructured lipid carriers for the potential treatment of AIDS dementia complex
Kasongo Wa Kasongo (2011)
Oral apomorphine delivery from solid lipid nanoparticles with different monostearate emulsifiers: pharmacokinetic and behavioral evaluations.
Ming-Jun Tsai (2011)
Solid self-nanoemulsifying cyclosporin A pellets prepared by fluid-bed coating: preparation, characterization and in vitro redispersibility
Y. Lei (2011)
Lipid-based colloidal systems (nanoparticles, microemulsions) for drug delivery to the skin: materials and end-product formulations
E. Souto (2011)
Preparation and in vitro and in vivo characterization of cyclosporin A-loaded, PEGylated chitosan-modified, lipid-based nanoparticles
L. Zhang (2013)
Porous Magnesium Aluminometasilicate Tablets as Carrier of a Cyclosporine Self-Emulsifying Formulation
C. Sander (2009)
Solid Lipid Nanoparticles and Nanostructured Lipid Carriers: A Review of the Effect of Physicochemical Formulation Factors in the Optimization Process, Different Preparation Technique, Characterization, and Toxicity
G. Poovi (2019)
Development, optimization and evaluation of long chain nanolipid carrier for hepatic delivery of silymarin through lymphatic transport pathway.
Shilpa Chaudhary (2015)
Nanostructured lipid carriers: An emerging platform for improving oral bioavailability of lipophilic drugs
S. Khan (2015)
Nanopartí­culas hí­bridas polimérico-lipí­dicas para veiculação de siRNA na terapia antisense de doenças cutâneas
M. M. Araújo (2017)
Preparation, characterization, and evaluation of gatifloxacin loaded solid lipid nanoparticles as colloidal ocular drug delivery system
M. A. Kalam (2010)
Binary lipids-based nanostructured lipid carriers for improved oral bioavailability of silymarin
Mingzhu Shangguan (2014)
Surface-modified solid lipid nanoparticles for oral delivery of docetaxel: enhanced intestinal absorption and lymphatic uptake
H. Cho (2014)
Nanostructured lipid carriers for improved oral delivery and prolonged antihyperlipidemic effect of simvastatin.
Heba A Fathi (2018)
Improved delivery of voriconazole to Aspergillus fumigatus through solid lipid nanoparticles as an effective carrier
H. R. Kelidari (2018)
Nanoparticules lipidiques de type Janus à compartiment superparamagnétique : du procédé de mise en oeuvre aux applications théranostiques
E. Millart (2017)
Investigating the correlation between in vivo absorption and in vitro release of fenofibrate from lipid matrix particles in biorelevant medium.
Nrupa Borkar (2014)
Novel Self-Assembled Polycaprolactone–Lipid Hybrid Nanoparticles Enhance the Antibacterial Activity of Ciprofloxacin
M. E. Omer (2020)
Cyclosporin A-loaded poly(ethylene glycol)-b-poly(d,l-lactic acid) micelles: preparation, in vitro and in vivo characterization and transport mechanism across the intestinal barrier.
Y. Zhang (2010)
Development, Optimization, and Evaluation of Carvedilol-Loaded Solid Lipid Nanoparticles for Intranasal Drug Delivery
Heba M. Aboud (2015)
Sustained-release solid dispersions of ibuprofen prepared by microwave irradiation
M. Moneghini (2008)
Transport features and structural optimization of solid lipid nanoparticles crossing the intestinal epithelium
Guihong Chai (2016)
Formulation and evaluation of prazosin hydrochloride loaded solid lipid nanoparticles
Sandip A. Bandgar (2018)
Overcoming poor oral bioavailability using nanoparticle formulations - opportunities and limitations.
Preshita P Desai (2012)
See more
Semantic Scholar Logo Some data provided by SemanticScholar