The Fluorosome™ technique for investigating membrane on‐ and off‐loading of drugs by β‐CD and sonicated SUV

FEBS Letters

Melchior, Donald L¹  Fix, Marina¹ 

[1] Department of Biochemistry and Molecular Pharmacology, University of Massachusetts Medical School, NRB, 364 Plantation Street, Worcester, MA 01605-2324, USA

关键词: Fluorosome;    Nitrobenzoxa-1;    3-diazolyl fluorophore;    Diphenylhexatrienyl propanoyl fluorophore;    Drug delivery system;    Cyclodextrin;    Sonicated small unilamellar vesicle;    β-CD;    β-cyclodextrin;    β-DPH-HPC;    2-(3-(diphenylhexatrienyl)propanoyl)-1-hexadecanoyl-sn-glycero-3-phosphocholine;    DMSO;    dimethyl sulfoxide;    egg PC;    egg phosphatidylcholine;    MLV;    multilamellar vesicles;    NBD-C6-HPC;    2-(6-(7-nitrobenz-2-oxa-1;    3-diazol-4-yl)amino)hexanoyl-1-hexadecanoyl-sn-glycero-3-phosphocholine;    sSUV;    sonicated small unilamellar vesicles;    Tris;    tris(hydroxymethyl)aminomethane;   

DOI  :  10.1016/S0014-5793(02)02512-7

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

The application of the Fluorosome technique to test drug delivery systems is described. Fluorosomes, egg phosphatidylcholine liposomes with bilayer embedded fluorophores, were employed to investigate the ability of sonicated small unilamellar vesicles (sSUV) and β-cyclodextrins (β-CD) to deliver drugs into or extract drugs from the fluorosome's phospholipid bilayer. The addition of phloretin to a fluorosome suspension resulted in fluorescence reduction reflecting phloretin entering the bilayer and quenching fluorophore fluorescence. Subsequent addition of sSUV to phloretin pretreated fluorosomes showed an increase in fluorescence reflecting phloretin extraction from the fluorosome membrane. Sequential additions of β-estradiol loaded β-CD to fluorosomes as well as the addition of β-estradiol alone resulted in fluorescence reduction due to β-estradiol insertion into the membrane. Further addition of pure β-CD resulted in a fluorescence increase indicating β-estradiol extraction from the fluorosome membrane.

【 授权许可】

Unknown