SLN and NLC for topical delivery of ketoconazole
- 1 August 2005
- journal article
- Published by Informa UK Limited in Journal of Microencapsulation
- Vol. 22 (5), 501-510
- https://doi.org/10.1080/02652040500162436
Abstract
The clinical use of ketoconazole has been related to some adverse effects in healthy adults, specially local reactions, such as severe irritation, pruritus and stinging. The purpose of the present work is the assessment of ketoconazole stability in aqueous SLN and NLC dispersions, as well as the physicochemical stability of these lipid nanoparticles, which might be useful for targeting this drug into topical route, minimizing the adverse side effects and providing a controlled release. Lipid particles were prepared using Compritol 888 ATO as solid lipid. The natural antioxidant alpha-tocopherol was selected as liquid lipid compound for the preparation of NLC. Ketoconazole loading capacity was identical for both SLN and NLC systems (5% of particle mass). SLN were physically stable as suspensions during 3 months of storage, but the SLN matrix was not able to protect the chemically labile ketoconazole against degradation under light exposure. In contrast, the NLC were able to stabilize the drug, but the aqueous NLC dispersion showed size increase during storage. Potential topical formulations are light-protected packaged SLN or NLC physically stabilized in a gel formulation.Keywords
This publication has 18 references indexed in Scilit:
- Development of an intravenously injectable chemically stable aqueous omeprazole formulation using nanosuspension technologyEuropean Journal of Pharmaceutics and Biopharmaceutics, 2004
- Efficacy of a new ketoconazole bioadhesive vaginal tablet on Candida albicansIl Farmaco, 2004
- Scanning electron microscopy and atomic force microscopy imaging of solid lipid nanoparticles derived from amphiphilic cyclodextrinsEuropean Journal of Pharmaceutics and Biopharmaceutics, 2003
- Interfacial interactions between amphiphilic cyclodextrins and physiologically relevant cationsJournal of Colloid and Interface Science, 2003
- Nanostructured lipid matrices for improved microencapsulation of drugsInternational Journal of Pharmaceutics, 2002
- Preparation of solid lipid nanoparticles with clobetasol propionate by a novel solvent diffusion method in aqueous system and physicochemical characterizationInternational Journal of Pharmaceutics, 2002
- Solid lipid nanoparticles (SLN) for controlled drug delivery – a review of the state of the artEuropean Journal of Pharmaceutics and Biopharmaceutics, 2000
- Effect of Particle Size on Colloidal Solid TriglyceridesLangmuir, 2000
- Correlation between long-term stability of solid lipid nanoparticles (SLN™) and crystallinity of the lipid phaseEuropean Journal of Pharmaceutics and Biopharmaceutics, 1999
- Peptide-loaded solid lipid nanoparticles (SLN): Influence of production parametersInternational Journal of Pharmaceutics, 1997