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Kurzfassung

Releasable on demand PEGylated drug-nanocarriers.

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Hintergrund

Technology Surface coating of drug-loaded nanocarriers (i.e. liposomes, micelles, etc.) with polyethylene glycol ('PEGylation') enables prolonged blood circulation and hence an effective accumulation in target organs (e.g. solid cancer tissues) but might also hold some disadvantages: hindrance of active targeting approaches, inhibition of cellular uptake and endosomal escape. 'PEG release on demand' can combine beneficial attributes: longevity (PEGylation), stimuli sensitivity (de-PEGylation on demand) and targetability (passive and active) and adds the potential of increased drug specificity, reduced drug-related side effects and reduced adverse body reactions against PEGylated particles (shortened circulation). All current switchable on demand systems, however, typically apply quiet weak triggers and/ or show other severe disadvantages, i.e. effective cleavage hindered by PEG shell (e.g. proteases), not easy to administrate in deep-tissue regions (e.g. light, temperature, ultrasound), might also dissolve carriers (e.g. temperature, ultrasound).

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Lösung

In the technology presented, nanocarriers are PEGylated via linker and ligand (see Fig. 1), allowing stable, PEGylated nanocarriers to (passively or actively) accumulate in target tissue. Only upon systemic administration of an excess of free ligand (remote trigger) nanocarriers are de-PEGylated and the cargo is more easily released and/ or an (targeted or passive) interaction with surrounding (target-) tissue is enabled.

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Vorteile

• Active targeting ligands also - alternatively or in addition - could be coupled to PEG-shell, recognizing e.g. overexpressed receptors in target cells.
• Active targeting approaches might apply one or combinations of targeting or internalization strategies or even strategies addressing drug bioavailability at the (sub-)cell level.
• Most of the conventional chemotherapeutic agents have poor pharmacokinetics profiles and are distributed nonspecifically in the body leading to systemic toxicity associated with serious side effects.
•  Preferential cargo
  
  • small molecule anticancer drugs (individual or in combination)
  • therapeutic antibody, with or without antibody drug conjugates
  • siRNA or pDNA

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Anwendungsbereiche

Drug Delivery Systems