Loading efficiency of doxorubicin into the micelle-like structures formed by function-spacer-lipid constructs self-assembly depends on constructs’ functional part

Abstract

Supramolecular self-assemble systems based on neoglycolipids: Galili-Ad-CMG2-Ad-DOPE, A(type2)-Ad-CMG2-Ad-DOPE are studied here and compared with the well-studied Biotin-CMG2-Ad-DOPE, as well as with their combinations with NH2-CMG2-Ad-DOPE. They are function-spacer-lipid constructs with unique structure that allows them to form micelle-like supramers and be stable, what makes them a potential drug nanocarriers. The structural properties of the obtained supramolecular systems are studied depending on their functional part, and the loading efficiency of doxorubicin into the supramers is determined to reveal the influence of the functional part. The resulting supramers were separated from the unbound molecules by dialysis, the nanoparticles morphology were studied by atomic force microscopy, and the loading efficiency was calculated based on spectrophotometry data. The encapsulation of doxorubicin was confirmed based on changes in the size and shape of the supramers, as well as a decrease in the ratio of unbound molecules. According to the loading efficiency calculations, it was estimated that supramers formed by A(type2)-Ad-CMG2-Ad-DOPE are the most efficient nanocarriers with loading efficiency of 82 %. Supramers formed by NH2-CMG2-Ad-DOPE (no functional part) showed 1.5 times less efficiency. Finally, the least efficient carriers are supramers formed by Biotin-CMG2-Ad-DOPE (14%).