Document Detail

Lectin-functionalized liposomes for pulmonary drug delivery: effect of nebulization on stability and bioadhesion.
MedLine Citation:
PMID:  11457648     Owner:  NLM     Status:  MEDLINE    
The generation of respirable aerosols of a functionalized colloidal carrier has been investigated in this study. Lectin-functionalized liposomes, which proved to show improved cell association (using A549 cell line and primary human alveolar cells) even in the presence of a commercial lung surfactant preparation, have been developed. The stability of non-functionalized liposomes during nebulization using a jet nebulizer (Pari II provocation nebulizer, operated using an air flow of 30 l/min) was firstly investigated, and the experimental and formulation conditions were optimized and applied for the preparation of lectin-functionalized liposomes. The incorporation of cholesterol enhanced the stability of the liposomes during nebulization (from 15-20% leakage of a hydrophilic marker to 8% upon cholesterol incorporation) and upon incubation with lung surfactant preparation. Nebulization of the functionalized liposomes did not significantly influence their physical stability. Their enhanced cell binding capability (compared to non-functionalized liposomes) was also maintained. A drop in cell association compared to fresh functionalized liposomes was detected after nebulization, nevertheless, the binding was still significantly higher than that of the non-functionalized liposomes. The deposition of the liposomal preparation in lung periphery, proved by the deposition of the liposomal preparation on the lower stages of an ASTRA type cascade impinger and a mean median aerodynamic diameter (MMAD) of 2.85 microm, makes it a potential candidate as a macromolecule-drug carrier for local and/or systemic administration.
R Abu-Dahab; U F Schäfer; C M Lehr
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences     Volume:  14     ISSN:  0928-0987     ISO Abbreviation:  Eur J Pharm Sci     Publication Date:  2001 Aug 
Date Detail:
Created Date:  2001-07-17     Completed Date:  2001-10-18     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  9317982     Medline TA:  Eur J Pharm Sci     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  37-46     Citation Subset:  IM    
Department of Biopharmaceutics and Pharmaceutical Technology, Saarland University, P.O. Box 15 11 50, D-66041, Saarbrücken, Germany.
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MeSH Terms
Cells, Cultured
Chemistry, Physical
Cholesterol / chemistry
Drug Carriers
Drug Delivery Systems*
Drug Stability
Lung / metabolism*
Nebulizers and Vaporizers
Physicochemical Phenomena
Pulmonary Alveoli / cytology,  drug effects
Pulmonary Surfactants / pharmacology
Reg. No./Substance:
0/Drug Carriers; 0/Lectins; 0/Liposomes; 0/Pulmonary Surfactants; 2644-64-6/1,2-Dipalmitoylphosphatidylcholine; 57-88-5/Cholesterol

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