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Light crosslinkable small molecular micelles with enediyne units are designed for developing efficient drug delivery systems. Gemcitabine (GEM) is chosen as a model hydrophilic drug and is tethered with a maleimide-based enediyne (EDY) as a hydrophobic tail in the preparation of amphiphilic EDY-GEM. The stable micellar particles are obtained by crosslinking the enediyne moieties via photo-induced Bergman cyclization polymerization in aqueous media. The light-crosslinked spherical micelles with a size of 80 nm are characterized with dynamic light scattering (DLS) and electron microscopy, showing robust micellar stability, bright fluorescent emission due to their intrinsic conjugated structure, and potential passive tumor-targeting ability through the enhanced permeability and retention (EPR) effect. The drug-loaded micelles, as an example of light crosslinked small-molecule micelle based drug delivery system, exhibit high drug loading contents (50%) and greatly improved cytotoxicity towards A549 cells (decreasing the IC50 value of Gemcitabine by 10 times) thanks to the greatly increased cellular uptake of the drug-loaded micelles as confirmed by confocal laser scanning microscopy (CLSM). The light crosslinkable enediyne based small-molecular micellar system therefore provides a simple yet efficient drug-delivery platform for cancer chemotherapy.
This article was published in the following journal.
Name: ACS applied materials & interfaces
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Part of a MESSENGER RNA molecule that undergoes a conformation change upon binding a specific metabolite or other small molecule thereby regulating the messenger RNA's transcription, post-transcriptional processing, transport, translation, or stability in response to varying levels of the metabolite or other small molecule.
Removal of a drug from the market due to the identification of an intrinsic property of the drug that results in a serious risk to public health.
Small containers or pellets of a solid drug implanted in the body to achieve sustained release of the drug.
Chemical analysis based on the phenomenon whereby light, passing through a medium with dispersed particles of a different refractive index from that of the medium, is attenuated in intensity by scattering. In turbidimetry, the intensity of light transmitted through the medium, the unscattered light, is measured. In nephelometry, the intensity of the scattered light is measured, usually, but not necessarily, at right angles to the incident light beam.
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
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