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  • The accumulation of drugs within large unilamellar vesicles exhibiting a proton gradient: a survey.

The accumulation of drugs within large unilamellar vesicles exhibiting a proton gradient: a survey.

Chemistry and physics of lipids (1990-03-01)
T D Madden, P R Harrigan, L C Tai, M B Bally, L D Mayer, T E Redelmeier, H C Loughrey, C P Tilcock, L W Reinish, P R Cullis
ABSTRACT

We have shown previously that transmembrane proton gradients can be used to efficiently accumulate biogenic amines [M.B. Bally et al. (1988) Chem. Phys. Lipids 47, 97-107] and doxorubicin [L.D. Mayer, M.B. Bally and P.R. Cullis (1986) Biochim. Biophys. Acta 857, 123-126] to high concentrations within liposomes. To determine the generality of this loading procedure, representative drugs from a variety of different classes (antineoplastics, local anaesthetics, antihistamines, etc.) were examined as to their ability to redistribute in response to a proton gradient. While the majority of drugs examined, all of which are weak bases, were accumulated by large unilamellar vesicles exhibiting a pH gradient (interior acid) the extent of uptake varied considerably between different pharmaceuticals. These differences are discussed in the context of various factors which will likely influence drug accumulation including its membrane/water partition coefficient and its solubility in the intravesicular medium.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
NanoFabTX-DOTAP Lipid Mix, for synthesis of cationic (DOTAP) liposomes
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NanoFabTx - PEG Lipid Mix, for synthesis of PEGylated liposomes
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NanoFabTx- COOH Lipid Mix, for synthesis of carboxyl functionalized liposomes
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NanoFabTx-DC-Chol Lipid Mix, for synthesis of cationic (DC-cholesterol) liposomes
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NanoFabTX- NH2 Lipid Mix, for synthesis of amine functionalized liposomes