Bicelles can form in a mixture composed of long- and short- lipids with an appropiate molar ratio (i.e., long-to-short) ranged from 2 and 6, and they are able to encapsulate lipophilic molecules in the hydrophobic region. It has been proved that at low lipid concentration bicelles undergo an irreversible disc-to-vesicle transition with increased temperature. Previously, enhanced cellular uptake was found for the discoidal bicelles compared to the vesicles of the identical chemical composition. In this presentation, we will show Nile red and meta-tetra(hydroxyphenyl)chlorin (a photodynamic therapeutic agent) can be entrapped in the bicelles. Moreover, a PEGylated lipid with folate functional group can anchor in the surface of bicelles providing targeting effect to KB cancer cells. A consistent trend is found for the in vitro and in vivo efficacy: folate-discs &gt; folate-vesicles &gt; non-folate-discs &gt; non-folate-vesicles. The advantages of bicelles as nanocarriers including highly biocompatibility, well-defined size, robust formation, easy encapsulation of hydrophobic molecules (therapeutics and/or diagnostics) and scalable one-pot synthesis. Therefore, they can serve as a generalized in vivo multi-modal delivery platform.

Design efficacious targeting lipid nanoparticles

2019 Spring National Meeting

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