Stability of the Metastable α-Polymorph in Solid Triglyceride Drug-Carrier Nanoparticles

Colloidal dispersions of crystalline nonpolar lipids are under intensive investigation as carrier systems in pharmaceutics and nutrition. In this context, the controlled preparation of particles in a metastable polymorphic state is of some interest for the delivery of active substances. In the prese...

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Veröffentlicht in:Langmuir : the ACS journal of surfaces and colloids. - 1992. - 31(2015), 24 vom: 23. Juni, Seite 6663-74
1. Verfasser: Joseph, Sonja (VerfasserIn)
Weitere Verfasser: Rappolt, Michael, Schoenitz, Martin, Huzhalska, Vera, Augustin, Wolfgang, Scholl, Stephan, Bunjes, Heike
Format: Online-Aufsatz
Sprache:English
Veröffentlicht: 2015
Zugriff auf das übergeordnete Werk:Langmuir : the ACS journal of surfaces and colloids
Schlagworte:Journal Article Research Support, Non-U.S. Gov't Drug Carriers Phospholipids Triglycerides Polyvinyl Alcohol 9002-89-5 Glycocholic Acid G59NX3I3RT
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245 1 0 |a Stability of the Metastable α-Polymorph in Solid Triglyceride Drug-Carrier Nanoparticles 
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520 |a Colloidal dispersions of crystalline nonpolar lipids are under intensive investigation as carrier systems in pharmaceutics and nutrition. In this context, the controlled preparation of particles in a metastable polymorphic state is of some interest for the delivery of active substances. In the present study, tristearin particles stabilized with three α-polymorph-preserving emulsifier regimes ((I) sodium glycocholate/saturated long-chain phospholipids, (II) sodium glycocholate, and (III) poly(vinyl alcohol) (PVA)) were investigated concerning the stability of the metastable α-polymorph after controlled crystallization of the particles from the melt. Upon long-term storage, the α-polymorph was preserved best in PVA-stabilized dispersions, followed by those stabilized with the glycocholate/phospholipid mixture and finally those stabilized solely with the bile salt. In particular for rapidly crystallized nanoparticles, the formation of an α-polymorph with highly reduced lamellarity was observed. According to time-/temperature-resolved synchrotron X-ray diffraction analysis with simultaneous DSC (differential scanning calorimetry) studies, this less-ordered α-polymorph transformed into the common, lamellar α-form upon heating. Although the presence of the less-ordered form is probably related to the extraordinarily high stability of the metastable α-polymorph observed in some of the dispersions, it could not completely prevent the transition into the stable β-polymorph. The higher the transition temperature of the less-ordered α-form to the ordered one, the slower was the polymorphic transition to the stable β-polymorph. To estimate the polymorphic stability of the differently stabilized particles upon isothermal long-term storage, standard DSC measurements on samples stored at 23 °C for 4 weeks seem to be of predictive value 
650 4 |a Journal Article 
650 4 |a Research Support, Non-U.S. Gov't 
650 7 |a Drug Carriers  |2 NLM 
650 7 |a Phospholipids  |2 NLM 
650 7 |a Triglycerides  |2 NLM 
650 7 |a Polyvinyl Alcohol  |2 NLM 
650 7 |a 9002-89-5  |2 NLM 
650 7 |a Glycocholic Acid  |2 NLM 
650 7 |a G59NX3I3RT  |2 NLM 
700 1 |a Rappolt, Michael  |e verfasserin  |4 aut 
700 1 |a Schoenitz, Martin  |e verfasserin  |4 aut 
700 1 |a Huzhalska, Vera  |e verfasserin  |4 aut 
700 1 |a Augustin, Wolfgang  |e verfasserin  |4 aut 
700 1 |a Scholl, Stephan  |e verfasserin  |4 aut 
700 1 |a Bunjes, Heike  |e verfasserin  |4 aut 
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