Phospholipid-detergent systems: effects of polysorbates on the release of liposomal caffeine

It is well known that surfactants are capable of interacting with phospholipid vesicles leading to different aggregated structures and finally to mixed micellar systems. By means of diffusion experiments with Valia-Chien cells the effect of different vesicular structures (MLV and SUV) and that of th...

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Published inFarmaco (Società chimica italiana : 1989) Vol. 53; no. 10; pp. 650 - 654
Main Authors Fadda, Anna Maria, Baroli, Bianca Maria, Maccioni, Anna Maria, Sinico, Chiara, Valenti, Donatella, Alhaique, Franco
Format Journal Article
LanguageEnglish
Published Lausanne Elsevier SAS 01.11.1998
Elsevier Science
Subjects
Biological and medical sciences
Diffusion
General pharmacology
Liposomes
Medical sciences
Mixed micelles
MLV
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Sustained release
SUV
Mixed micelles
Sustained release
Liposomes
Diffusion
SUV
MLV
Multilayer
Controlled release form
Liposome
Mixed micelle
Phospholipid
Lipophily
Polymer
Drug adjuvant
Surfactant
Complex lipid
Lamellar structure
Concentration effect
Dosage form
Polysorbate
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Summary:It is well known that surfactants are capable of interacting with phospholipid vesicles leading to different aggregated structures and finally to mixed micellar systems. By means of diffusion experiments with Valia-Chien cells the effect of different vesicular structures (MLV and SUV) and that of three polysorbates on the release of a model drug (caffeine) from various vesicle formulations was studied. Obtained results indicate that a remarkable delayed/sustained caffeine release is obtained only with the MLV preparations and that the presence of increasing surfactant concentrations initially leads to a further decrease of drug delivery rate and then to a faster release that reaches a maximum when only mixed micelles are present. The variation of the observed effects with the different tested surfactants, in relation to their lipophilicity (HLB values), is also discussed.
ISSN:0014-827X
1879-0569
DOI:10.1016/S0014-827X(98)00081-0