Polymorphic behaviour of Compritol (R) 888 ATO as bulk lipid and as SLN and NLC

• Type: Article in International Scientific Journal
• Date: 2006

Authors

Souto, EB (Author) Other; Mehnert, W (Author) Other; Mueller, RH (Author) Other

Journal

Title: Journal of Microencapsulation

Vol. 23

Pages: 417-433

ISSN: 0265-2048

Publisher: Taylor & Francis

Indexing

ISI Web of Knowledge - 102 Citations

Scopus - 137 Citations

Other information

Authenticus ID: P-00F-SBT

DOI: 10.1080/02652040600612439

Abstract (EN): Compritol((R))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 (similar to 70 degrees 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((R))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 (alpha-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((R))888 ATO is composed of very small amounts of the unstable alpha 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.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 17