CelLuminate™ VPS (Vesicle-forming Polymer System)
Researchers now have the opportunity to deliver bioactive molecules of their choice into live cells using CelLuminate VPS (Vesicle-forming Polymer System).
Initially developed as a revolution in live cell imaging and tracking, CelLuminate has many and varied applications in life science research. CelLuminate VPS has been shown to be delivered efficiently in a broad range of primary cells and cell lines, both animal and human, with minimal cytotoxic effect. A range of biological molecules have been delivered to date, ranging from small molecules such as cell stains, to larger species such as RNA, DNA and proteins.
pH-controlled vesicle formation
poly (2-methacryloyloxyethyl phosphorylcholine)-co-(diisopropylaminoethyl methacrylate) (PMPC-PDPA)
Du et al. J. Am. Chem. Soc. 2005, 127, 17982
CelLuminate VPS is a proprietary biomimetic PMPC-PDPA copolymer formulation for the encapsulation and delivery of bioactive agents to animal or mammalian cells with minimal effect on cell toxicity and metabolism.1,2 Based on the phospholipid chemistry of cell membranes, the polymer vesicles can be formed by self-assembly of the pH-sensitive AB diblock copolymer poly (2-methacryloyloxyethyl phosphorylcholine)-co-(diisopropylamino)ethyl methacrylate).
The PMPC block is highly biocompatible, whilst the PDPA imparts pH sensitivity. At physiological pH, the copolymer forms colloidally stable nanometre-sized vesicles, whereas below the pKa of the PDPA block (~6.4), rapid dissociation of the vesicles occurs as the tertiary amine on the PDPA becomes protonated. This pH switch can be exploited to control the formation of vesicles in the presence of other bioactive molecules and hence afford encapsulation and protection of these species. This may be within the hydrophobic membrane or the aqueous core of the vesicle, depending upon the properties of the species being encapsulated. Particularly facile encapsulation is possible with large biomacromolecules such as DNA and proteins.
The biomimetic surface chemistry of the polymer vesicles ensures extremely efficient uptake by cells that undergo endocytosis. The rate and amount of vesicles endocytosed is orders of magnitude higher than conventional liposomal systems. The pH drop in the endosome is utilised to deliver the desired payload into the cell cytosol.
Endosome escape
- Surface chemistry ensures extremely rapid cellular uptake
- Size dependency allows tailored uptake kinetics
Rapid, size-dependent cellular uptake
- Orders of magnitude: More vesicles/cell than standard lipsomes or targeted systems
Cellular uptake comparisons
CelLuminate™ VPS has been shown to be delivered efficiently in a broad range of primary cells and cell lines, both animal and human, within minimal cytotoxic effects.
A range of biological molecules have been delivered to date ranging from small molecules such as cell stains, to larger species such as RNA, DNA and proteins.
Example molecule types
- Rhodamine B octadecyl ester perchlorate
- BODIPY® TR ceramide
- Fluoresceine DHPE
- NBD cholesterol
- Propidium iodide
- FITC-Antibodies
- Cy3-Nucleic acid
- Quantum dots
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