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Lipid-DNAs as Solubilizers of mTHPC.
Liu, Yun ; de Vries, Jan Willem ; Liu, Qing ; Hartman, Alwin M ; Wieland, Gerhard D ; Wieczorek, Sebastian ; Börner, Hans G ; Wiehe, Arno ; Buhler, Eric ; Stuart, Marc C A ... show 3 more
Liu, Yun
de Vries, Jan Willem
Liu, Qing
Hartman, Alwin M
Wieland, Gerhard D
Wieczorek, Sebastian
Börner, Hans G
Wiehe, Arno
Buhler, Eric
Stuart, Marc C A
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2018-01-19
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Abstract
Hydrophobic drug candidates require innovative formulation agents. We designed and synthesized lipid-DNA polymers containing varying numbers of hydrophobic alkyl chains. The hydrophobicity of these amphiphiles is easily tunable by introducing a defined number of alkyl chain-modified nucleotides during standard solid-phase synthesis of DNA using an automated DNA synthesizer. We observed that the resulting self-assembled micelles solubilize the poorly water-soluble drug, meta-tetra-hydroxyphenyl-chlorin (mTHPC) used in photodynamic therapy (PDT) with high loading concentrations and loading capacities. A cell viability study showed that mTHPC-loaded micelles exhibit good biocompatibility without irradiation, and high PDT efficacy upon irradiation. Lipid-DNAs provide a novel class of drug-delivery vehicle, and hybridization of DNA offers a potentially facile route for further functionalization of the drug-delivery system with, for instance, targeting or imaging moieties.
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1521-3765
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Attribution-NonCommercial-ShareAlike 3.0 United States
