Lipid‐DNAs as Solubilizers of mTHPC

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. Lipid‐DNA micellar drug‐delivery systems: Lipid‐DNA amphiphiles bearing different numbers of hyrophobic alkyl chains are prepared by using standard solid‐phase synthesis. Their self‐assembled micelles efficiently render the hydrophobic drug, meta‐tetra‐hydroxyphenyl‐chlorin (mTHPC) for photodynamic therapy (PDT) water‐soluble with high loading capacities, good biocompatibility and stability without irradiation and a high PDT efficacy upon irradiation in various cell lines.