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Polymorphic Behaviour Of Compritol®888 ATO As Bulk Lipid And As SLN And NLC

E. Souto, W. Mehnert, R. Mueller
Published 2006 · Chemistry, Medicine

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Compritol®888 ATO (glycerol behenate) is widely used as a pharmaceutical excipient in the field of solid dosage forms due to its lubricating properties. It is an amphiphilic material with a high melting point (∼70°C) and, therefore, it can also be used to prepare aqueous colloidal dispersions. The aim of this paper is to study the suitability of Compritol®888 ATO for the production of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) for the entrapment of a lipophilic model drug. This study assesses the crystalline structure of the bulk lipid, as well as the changes that occur in its crystal lattice with the addition of ‘impurities’, such as oil (α-tocopherol) and drug (ketoconazole), using DSC and X-ray diffraction analysis before and after thermal stress. Aqueous SLN and NLC dispersions were produced using an appropriate surfactant/co-surfactant system and their physicochemical stability was assessed by PCS, LD, DSC and by WAXS. It was found that the crystalline lattice of Compritol®888 ATO is composed of very small amounts of the unstable α polymorphic form characteristic of triacylglycerols, which disappears after thermal stress of bulk lipid. Mixing oils and drug molecules which are soluble in this lipid decreased its lattice organization and, thus, was revealed to be suitable for production of lipid nanoparticles containing ketoconazole. However, particle growth could not be avoided during shelf life.
This paper references
10.1080/02652040500162436
SLN and NLC for topical delivery of ketoconazole
E. Souto (2005)
10.1023/A:1016270724413
Preparation and Physicochemical Characterization of Aqueous Dispersions of Coenzyme Q10 Nanoparticles
B. Siekmann (2004)
Submicronized parenteral carrier systems based on solid lipids
B Siekmann (1992)
10.1107/S0108768198009392
Structure of mono-acid even-numbered β-triacylglycerols
A. J. V. Langevelde (1999)
Feste Lipidnanopartikel (SLN ) als kolloidaler Arzneistoffträger für die orale Applikation von Ciclosporin A
S. Runge (1998)
Feste Lipid-Nanopartikel mit prolongierter Wirkstoffliberation: Herstellung, Langzeitsabilität, Charakterisierung, Freisetzungsverhalten und Mechanismen
A Mü Hlen (1996)
Melt-homogenized solid lipid nanoparticles stabilized by the nonionic surfactant tyloxapol
B Siekmann (1994)
10.1016/0378-5173(93)90177-H
Investigations on the physical state of lipid nanoparticles by synchrotron radiation X-ray diffraction
K. Westesen (1993)
Fat crystal structure in cream and butter
D. Precht (1988)
10.1016/S0378-5173(00)00378-1
Characterisation of a novel solid lipid nanoparticle carrier system based on binary mixtures of liquid and solid lipids.
V. Jenning (2000)
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)
Thermal behaviour and polymorphism of acylglycerides
Hagemann JW. (1988)
10.1016/S0163-7827(98)00019-8
Molecular interactions and kinetic properties of fats.
K. Sato (1999)
Effects of surfactants on crystallization and polymorphic transformation of fats and fatty acids
N. Garti (1988)
Crystallization and polymorphism of fats and fatty acids
N. Garti (1988)
Melt-homogenized solid lipid nanoparticles stabilized by the nonionic surfactant tyloxapol. I. Preparation and particle size determination
B Siekmann (1994)
Röntgendiffraktometrischer Nachweis der Polymorphie
K Thoma (1983)
Investigation of the factors influencing the incorporation of clotrimazole-loaded lipid nanoparticles prepared by hot high-pressure homogenization
EB Souto (2006)
10.1021/LA990856L
Effect of Particle Size on Colloidal Solid Triglycerides
H. Bunjes (2000)
10.1201/9780849359033-56
Solid Lipid Nanoparticles (SLN) and Nanostructured Lipid Carriers (NLC) for Dermal Delivery
R. Mu¨ller (2005)
Effect of particle size on colloidal size solid triglycerides
H Bunjes (2000)
Comparison of parenteral lipid emulsions and solid lipid nanoparticles
K Westesen (1994)
Structure of mono-acid even-numbered beta-triacylglycerols.
van Langevelde A (1999)
Fest-flüssig (halbfeste) Lipidpartikel und Verfahren zur Herstellung hochkonzentrierter Lipidpartikeldispersionen
RH Müller (1998)
Untersuchungen zur Herstellung und zum Rekristallisationsverhalten schmelzemulgierter intravenös applizierbarer Glyceridnanopartikel
B. Siekmann (1995)
10.1016/J.BBALIP.2003.09.003
Micelle formation of sodium chenodeoxycholate and solubilization into the micelles: comparison with other unconjugated bile salts.
Ryoko Ninomiya (2003)
10.1080/02652040500435295
Investigation of the factors influencing the incorporation of clotrimazole in SLN and NLC prepared by hot high-pressure homogenization
E. Souto (2006)
10.1016/S0378-5173(97)04890-4
Investigation of the gel formation of phospholipid-stabilized solid lipid nanoparticles
K. Westesen (1997)
Feste Lipidnanopartikel (SLN Õ ) als kolloidaler Arzneistoffträger fü r die orale Applikation von Ciclosporin A
S Runge (1998)
Feste Lipid Nanopartikel (SLN): Mechanismen der physikalischen Destabilisierung und Stabilisierung
C. Freitas (1998)
10.1016/S0939-6411(98)00074-5
Correlation between long-term stability of solid lipid nanoparticles (SLN) and crystallinity of the lipid phase.
C. Freitas (1999)
10.17169/REFUBIUM-12273
SLN and NLC for topical delivery of antifungals
E. Souto (2005)



This paper is referenced by
10.3109/03639045.2015.1118490
Controlled release tablet formulation containing natural Δ9-tetrahydrocannabinol
Nagendra Punyamurthula (2016)
Drug Delivery and Pharmacokinetics 3 . 1 Drug Delivery
(2017)
10.1007/978-1-4939-1289-6_12
Development of Pilosebaceous Unit-Targeted Drug Products
G. W. Lu (2014)
10.1007/s13346-020-00733-4
Atorvastatin-loaded solid lipid nanoparticles as eye drops: proposed treatment option for age-related macular degeneration (AMD)
Monika Yadav (2020)
10.1080/03639045.2017.1395459
QbD-driven development and evaluation of nanostructured lipid carriers (NLCs) of Olmesartan medoxomil employing multivariate statistical techniques
S. Beg (2018)
10.3109/1061186X.2010.523787
Brain targeting of risperidone-loaded solid lipid nanoparticles by intranasal route
S. Patel (2011)
10.1002/med.20201
Nanoparticulate devices for brain drug delivery
C. Celia (2011)
10.1002/9783527610419.NTLS0257
Solid Lipid Nanoparticles to Improve Brain Drug Delivery
P. Blasi (2012)
10.1016/j.ejpb.2014.04.015
Impact of lipid dynamic behavior on physical stability, in vitro release and skin permeation of genistein-loaded lipid nanoparticles.
L. M. Andrade (2014)
10.1021/acs.molpharmaceut.5b00015
Determination of solid state characteristics of spray-congealed Ibuprofen solid lipid microparticles and their impact on sustaining drug release.
Priscilla Chui Hong Wong (2015)
10.1016/j.chemphyslip.2014.07.005
Polymorphism of glyceryl behenates: from the individual compounds to the pharmaceutical excipient.
Perrine Pivette (2014)
10.1016/j.colsurfb.2010.02.003
Molecular interaction and localization of tocotrienol-rich fraction (TRF) within the matrices of lipid nanoparticles: evidence studies by Differential Scanning Calorimetry (DSC) and Proton Nuclear Magnetic Resonance spectroscopy ((1)H NMR).
Hazem Ali (2010)
10.1080/03639040802130061
Lipid Nanoparticles with a Solid Matrix (SLN®, NLC®, LDC®) for Oral Drug Delivery
M. Muchow (2008)
10.1016/J.JDDST.2018.10.032
In vitro and in vivo evaluation of MHY908-loaded nanostructured lipid carriers for the topical treatment of hyperpigmentation
Hasanul Banna (2018)
10.1016/j.jconrel.2008.12.018
Polymeric nanoparticulate system: a potential approach for ocular drug delivery.
R. C. Nagarwal (2009)
10.3109/10717544.2013.834412
Evaluation of the cytotoxic effect of camptothecin solid lipid nanoparticles on MCF7 cells
C. Y. Acevedo-Morantes (2013)
10.1016/j.ejps.2017.12.006
Mannose‐functionalized solid lipid nanoparticles are effective in targeting alveolar macrophages
A. Costa (2018)
10.3390/molecules25030685
Sucupira Oil-Loaded Nanostructured Lipid Carriers (NLC): Lipid Screening, Factorial Design, Release Profile, and Cytotoxicity
R. Vieira (2020)
10.1002/jps.22784
Improved and safe transcorneal delivery of flurbiprofen by NLC and NLC-based hydrogels.
E. González-Mira (2012)
10.1007/s40005-013-0087-y
Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs): recent advances in drug delivery
G. Yoon (2013)
10.1007/s13346-019-00632-3
Formulation of topical ibuprofen solid lipid nanoparticle (SLN) gel using hot melt extrusion technique (HME) and determining its anti-inflammatory strength
A. Bagde (2019)
Studies on the Synthesis and Characterization of Encapsulated Organogels for Controlled Drug Delivery Applications
S. S. Sagiri (2014)
10.1016/J.COFS.2019.02.005
Opportunities and challenges in developing orally administered cannabis edibles
P. Chen (2019)
10.3109/10717544.2010.483257
Solid lipid nanoparticles for ocular drug delivery
A. Seyfoddin (2010)
10.1016/j.nano.2009.02.003
Nanomedicines for ocular NSAIDs: safety on drug delivery.
J. Araújo (2009)
Application of Supercritical Fluid Technology for Preparation of Drug Loaded Solid Lipid Nanoparticles
Z. Akbari (2020)
10.1016/S1773-2247(11)50005-X
Lipid-based colloidal systems (nanoparticles, microemulsions) for drug delivery to the skin: materials and end-product formulations
E. Souto (2011)
10.1016/J.JDDST.2018.12.023
Polyphenols-enriched Hibiscus sabdariffa extract-loaded nanostructured lipid carriers (NLC): Optimization by multi-response surface methodology
S. Pimentel-Moral (2019)
10.1016/j.ejps.2020.105278
Evolution of the microstructure and the drug release upon annealing the drug loaded lipid-surfactant microspheres.
V. Kushwah (2020)
Chapter V Nanoformulations for Overcoming Poor Solubility
(2017)
10.1007/s10973-012-2709-4
Characterization of silver sulfadiazine-loaded solid lipid nanoparticles by thermal analysis
Catenacci Laura (2012)
10.1016/j.colsurfb.2015.03.049
Sodium alginate-cross-linked polymyxin B sulphate-loaded solid lipid nanoparticles: Antibiotic resistance tests and HaCat and NIH/3T3 cell viability studies.
P. Severino (2015)
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