Low Molecular Weight Polymer Enhances Drug Bioavailability
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Solution Overview
Problem
Existing pharmaceutical drug carriers, particularly polymers, face challenges in bioavailability due to non-degradability, accumulation in the body leading to toxicity, and inability to cross biological barriers.
Innovation Solution
A polymer consisting of a succession of monomers with specific chemical properties, including a mean pKa between 6.0 and 7.0 and a charge density at pH 7.0 between 20 and 50%, is developed to enhance the bioavailability of pharmaceutical components by improving solubility and epithelial permeability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If synthetic polymers are used as carriers to improve bioavailability, then solubility and membrane permeability are improved, but accumulation in the body occurs causing potential inflammation and immune reactions
Solution Approach 1:
The patent applies parameter changes by carefully controlling the molecular weight of the polymer carrier to be below 10 kDa, which enables renal elimination and prevents accumulation-induced toxicity while maintaining effective bioavailability enhancement. This specific parameter threshold resolves the contradiction between improving drug delivery and avoiding harmful accumulation effects.
Solution Approach 2:
The patent employs biodegradable polymer carriers that are designed to be transient and eliminable from the body through renal excretion. These short-lived carriers perform their function of improving bioavailability and then naturally degrade and eliminate, preventing long-term accumulation and associated toxicity issues.
2Reliability
If synthetic polymers are used as carriers, then bioavailability is improved, but diffusion ability across biological barriers is lost
Solution Approach 1:
The patent applies parameter changes by optimizing the polymer's molecular weight, charge density, and hydrophilicity parameters. These parameter adjustments enable the polymer to achieve both improved bioavailability and sufficient diffusion ability across biological barriers, resolving the contradiction between these two properties.
3Quantity of substance
If polymer molecular weight is increased to improve carrier capacity, then drug loading is improved, but renal elimination is prevented causing accumulation
Solution Approach 1:
The patent applies parameter changes by precisely controlling the polymer molecular weight to remain below the 10 kDa threshold. This parameter optimization allows the carrier to maintain adequate drug loading capacity while remaining small enough for renal filtration and elimination, preventing accumulation and associated toxicity.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The polymer effectively increases the bioavailability and intracellular delivery of pharmaceutical components, including poorly soluble drugs and nucleic acids, while maintaining a low toxicity profile and allowing for various administration modes.
Implementation Method 1
wherein the said polymer has a mean pKa between 6.0 and less than 7.0 and a charge density at pH 7.0 between 20 and 50% (number of the positively charged monomers:total number of monomers)
Data Source
AI summary
A polymer substantially consisting of a succession of monomers according to the formula I for use in increasing the bioavailability of pharmaceutical component to a mammalian patient, a process for formulating the polymer and the pharmaceutical component.