Polymeric Nano-Delivery System™
Our Polymeric Nano-Delivery System™ (PNDS) technologies are an excellent complement to Contramid because they allow optimized delivery of water-insoluble drugs with poor bioavailability or safety profiles.
What Are They?
PNDS are a library of block copolymers designed to address the unmet needs of insoluble drug delivery. Comprising hydrophobic and hydrophilic GRAS (generally recognized as safe) subunits fused as novel molecular entities, PNDS can be simply manufactured to form stable nano-vehicles or micelles that entrap insoluble drugs, making them available for oral or parenteral administration in safe and convenient forms.
How Do They Work?
The hydrophobic block of the copolymers complex with the insoluble drug mass then associate to form the stable micellar core; the hydrophilic segments form a corona that bonds with water molecules rendering the drug bioavailable. Post oral or intravenous administration, drug-bearing micelles release their payloads directly to intestinal absorption surfaces, safely maximizing bioavailability (oral platform), or into the blood-stream to accumulate in the desired site of action (intravenous platform).
What Are Their Advantages?
PNDS are simple to manufacture, solvent free delivery systems offering:
Oral Platform
- Oral delivery of insoluble small and macromolecules currently only available as parenteral formulations;
- Optimized bioavailability via, massive surface absorption area, muco-adhesion to absorption surfaces, and pH- targeted site-specific delivery;
- Convenient and flexible out-patient administration of drugs currently requiring prolonged hospital-based drug infusions;
- Increased drug-exposure to minimize side-effects via, for example, metronomic dosing.
Intravenous Platform
- Intravenous (and subcutaneous) delivery of insoluble drugs and macromolecules;
- Lipid, solvent free formulation;
- Targeted delivery via the enhanced permeability and retention effect (oncology products);
- Increase dosing without dose limiting side-effects.
What Have We Accomplished With PNDS?
Oral Platform: In pre-clinical models we have increased the rate of oral absorption and extent of oral bioavailability of fenofibrate to more than 80%, using a safe, capsule-based formulation. We have also successfully identified stable, high-loading concentration formulations of a series of cytotoxic agents in rodent models, and demonstrated double-digit oral bioavailability with a highly insoluble oncology drug with applications in colon and lung cancer.
Intravenous Platform: We have developed an improved, clear, lipid and preservative-free, formulation of propofol that, in animal models, has been shown to display comparable pharmacokinetics and pharmacodynamics to current market leaders. We have also identified a series of stable, solvent-free cytoxic drug formulations with very high maximum tolerated doses compared to current products. In animal models, these formulations displayed similar effectiveness to current products on a dose to dose basis but, due to their greater tolerability, could be safely dosed more highly and therefore more effectively than current formulations.