[en] The purpose of this research was to investigate the effects of processing conditions on the characteristics of solid lipid microparticles (SLM) with a potential application as carriers for pulmonary administration. Compritol ( 5.0% wt/ wt) SLM dispersions were prepared by rotor-stator homogenization, at different surfactant concentrations and emulsification times. The SLM were characterized, in terms of morphology and size, after lyophilization and sterilization by autoclaving process. In vivo assessment was carried out in rats by intratracheal instillation of either placebo or SLM dispersion, and by bronchoalveolar lavage for cytological analysis. Mean particle size of 4 to 5 mum was achieved using 0.3% and 0.4% ( wt/ wt) of emulsifier ( Poloxamer 188) and emulsification times of 2 and 5 minutes. The particles showed spherical shape and smooth surface. The morphology of microparticles, the size, and the size distribution were not substantially modified after lyophilization and sterilization. Total cell counts showed no significant differences between placebo and SLM 0.5% or 2.5% groups. Regarding cytology, percentage of polymorphonuclear neutrophils and macrophages did not significantly differ between groups. These results suggest that a single intratracheal administration of the SLMs does not induce a significant inflammatory airway response in rats and that the SLMs might be a potential carrier for encapsulated drug via the pulmonary route.
Disciplines :
Pharmacy, pharmacology & toxicology
Author, co-author :
Sanna, V.; Université de Sassari Italie
Kirschvink, Nathalie; Université de Liège - ULiège
Gustin, Pascal ; Université de Liège - ULiège > Département de sciences fonctionnelles > Pharmacologie, pharmacothérapie et toxicologie
Gavini, E.; Université de Sassari Italie
Roland, Isabelle ; Centre Hospitalier Universitaire de Liège - CHU > Pharmacie
Delattre, Luc ; Université de Liège - ULiège > Département de pharmacie > Département de pharmacie
Evrard, Brigitte ; Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique
Language :
English
Title :
Preparation and in vivo toxicity study of solid lipid microparticles as carrier for pulmonary administration
Publication date :
2004
Journal title :
AAPS PharmSci
ISSN :
1530-9932
eISSN :
1522-1059
Publisher :
Amer Assoc Pharmaceutical Scientists, Alexandria, United States - Virginia
Volume :
5
Issue :
2
Pages :
Article 27
Peer reviewed :
Peer Reviewed verified by ORBi
Funders :
Ministère de la Région wallonne (Economie, PME, de la Recherche et des Technologies nouvelles)
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