Active loading of doxorubicin into polymeric vesicles

COLL 250

Amira Choucair, Patrick Lim Soo, and Adi Eisenberg. Department of Chemistry, McGill University, 801 Sherbrooke Str. W, Montreal, QC H3A 2K6, Canada
Polystyrene-b-poly (acrylic acid) block copolymers can self-assemble in solution to form aggregates of different morphologies, including vesicles. Vesicles, which are spherical bilayers with a hydrophobic wall and a hydrophilic interior, have several applications in areas such as cosmetics, pollution control, and drug delivery. The ability to incorporate doxorubicin (DOX), an anticancer drug, in the internal cavity of PS310-b-PAA36 vesicles is examined. Two different incorporation methods are compared. In the first, DOX is simply mixed with the polymeric vesicles (i.e. passive loading). The second method involves creating a pH gradient between the internal cavity of the vesicles, and the external aqueous solution in which the vesicles are suspended, and then adding DOX (i.e. active loading). The extent of incorporation, using both methods, is also tested as a function of the softness (permeability) of the vesicle wall. The results show that in the absence of a pH gradient (i.e. with passive loading), the extent of incorporation is modest and remains constant regardless of the softness of the vesicle wall. However, by applying a pH gradient, the loading of DOX is enhanced, especially as the permeability of the vesicle wall increases.