Doxorubicin interacts with neutral lipid systems primarily through hydrophobic interactions, with cholesterol content influencing the structural changes in liposomes and monolayers.
Cholesterol content modulates doxorubicin-liposome interactions; hypothesis-generating for formulation optimization before any clinical consideration.
The action of doxorubicin, a cancer chemotherapeutic agent, on liposomes of dipalmitoylphosphatidylcholine obtained by extrusion, with or without cholesterol, and on monolayers of the same composition, was determined by photon correlation spectroscopy, penetration kinetics, and adsorption isotherms. Doxorubicin produced a wider vesicle distribution in both of liposomes, but liposomes containing cholesterol underwent an increase of mean diameter as well as polydispersity. In contrast, films containing cholesterol showed least interaction with the drug. Since both lipids are neutral, any interaction must be primarily hydrophobic.
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Hernández‐Borrell et al. (1991) studied this question.
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