Nobex issued PEG-based polymer patents
its 'PEGylation' technology of small polyethylene glycols (PEG) for
modifying molecules for improved drug performance.
As more peptide hormones are identified as potential drugs, particularly those for chronic diseases of metabolism and the cardiovascular system, oral delivery in tablet form is the ideal method to achieve patient convenience and compliance as well as provide new medical benefits in some cases.
The two new patents detail a method of oral delivery of both peptide-based and small organic molecules as well as other routes of administration including injection, pulmonary and transdermal delivery. Essentially they will enable the conversion of injectable-only drugs into oral drugs
One of the patents, entitled: "Substantially monodispersed mixtures of polymers having polyethylene glycol moieties," covers small molecular-weight (up to several hundred Daltons) PEG polymers in which most of the PEG molecules have the same molecular weight.
The patent covers monodispersed PEG polymers such as individual compositions of matter, as well as in combination with other components such as the alkyl and fatty acid compounds that are used in proprietary micro-alkylPEGylation technology for drug modification.
The other patent, entitled "Methods of synthesizing substantially monodispersed mixtures of polymers having polyethylene glycol moieties," covers synthetic methods for producing the monodispersed PEG and micro-alkylPEG ("oligomer") compositions.
"The technology enables the synthesis of small, pure molecular weight polymers and polymer-drug molecules simplifying manufacturing and chemical analyses extending the patent lives of covered compounds," said Christopher Price, president of Nobex.
"We believe the technology will be of licensing interest to other companies using PEG-based polymers to modify their therapeutic molecules. We have observed that even a single ethylene glycol unit difference in a pure polymer-modified drug can yield significantly different biological performance."
Micro-alkylPEG polymers soluble, ionic and nonionic surfactant properties will find value in pharmaceutical formulations, prepared foods and skin products. Its small, monodispersed molecular structure and chemical properties may also be useful in areas such as nanotechnology.
Modification of peptide drugs for oral delivery is achieved by chemically coupling the small, pure oligomers covered by the new patents to the peptide at one or more selected sites, creating a new, pure single molecular entity.
The oligomers balance of water and lipid solubility provided by the different polymers changes the chemical and biological properties of the drug. The results are improvements in characteristics such as increased shelf stability, resistance to enzymes, absorption into the body from the GI tract, and lengthened circulation time in the blood.
PEG polymers are well established in the biopharmaceutical industry for modifying the pharmacology of large protein drug molecules that are administered by injection. Large molecular weight (several 1,000 Daltons) PEG polymers are attached to the protein drug in random fashion and at variable numbers of sites on each molecule.
This approach provides well-documented benefits to the pharmacokinetics and bioactivity of the PEG-modified drug administered by injection. However, PEG-modified proteins are not suited for delivery by the oral route of administration due to their very large size.
