Hyperbranched Polyester Polyol Derivative as Drug Solubilizer

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This invention describes a composition and method involving a hyperbranched, sulfated polyester polyol derivative designed to effectively solubilize and deliver hydrophobic (poorly water-soluble) cancer drugs that contain at least one cyclic amine group. The system is specifically tailored to encapsulate such hydrophobic, heterocyclic tumor signal transduction inhibitors, increasing their aqueous solubility without the need for toxic organic solvents or traditional delivery systems like micelles or liposomes. The composition is primarily intended for use in anti-cancer therapies, facilitating improved oral or parenteral bioavailability of drugs that are normally very poorly soluble in water.

Use CasesContent extracted from patent full text and abstract with AI.

• Formulation of oral medications for hydrophobic cancer drugs containing cyclic amines to improve their absorption and effectiveness.
• Development of injectable (parenteral) anti-cancer drugs with higher solubility and stability, potentially reducing side effects and improving dosing consistency.
• Creation of fixed-dose combination drug products where multiple hydrophobic drugs with different physicochemical properties can be delivered together.
• Manufacturing of cancer drugs without the use of harmful organic solvents, enhancing patient safety and reducing formulation complexity.
• Potential use in other therapeutic or diagnostic applications requiring solubilization and delivery of poorly soluble compounds with cyclic amine groups.

BenefitsContent extracted from patent full text and abstract with AI.

• Significantly increases the aqueous solubility of hydrophobic, poorly soluble cancer drugs containing cyclic amines (up to 100-fold).
• Avoids the use of harmful organic solvents in drug formulations, increasing safety for patients and manufacturers.
• The encapsulating polymer is amphiphilic and can be made in a simple, scalable manner from readily available reagents.
• Allows for stable, freeze-dried storage of sensitive drug formulations, improving shelf-life and logistics.
• Enables tailored delivery for both oral and parenteral administration, potentially overcoming bioavailability limitations of current therapies.
• Reduces manufacturing complexity as the process can be performed entirely in water under mild conditions.
• May allow for combined delivery of multiple hydrophobic drugs with different properties, potentially simplifying therapy regimens and improving pharmacokinetic profiles.
• The system does not involve covalent modification of drugs, preserving their biological activity.

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Patent Abstract

The present invention relates to a composition comprising a hyperbranched polyester polyol derivative and a heterocyclic tumor signal transduction inhibitor comprising at least one cyclic amine. The hyperbranched polyester polyol derivative is obtainable by a method comprising the following steps: a) reacting only glycidol and ε-caprolactone at a temperature lying in a range of between 40 °C and 140 °C to obtain a hyperbranched polyester polyol derivative in which caprolactone residues and glycerol residues are randomly arranged; b) reacting the hyperbranched polyester polyol derivative of step a) with a sulfation reagent to obtain a sulfated hyperbranched polyester polyol as hyperbranched polyester polyol derivative.