Multivalent Prodrug Carrier Sustained Release
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Solution Overview
Problem
Current drug delivery systems face challenges in achieving sustained release of biologically active agents with high relative ratios of parent drugs, often requiring frequent dosing and suffering from irregular release patterns and cumbersome formulations.
Innovation Solution
The development of prodrugs with multiple parent drug molecules attached to carrier moieties, which undergo spontaneous or enzyme-assisted cleavage in physiological conditions to provide sustained release, reducing dosing frequency and improving bioavailability by extending the duration of action per dose.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of stationary object
If microencapsulation technologies are used to achieve sustained release, then stability and time-release properties are improved, but the amount of parent drug delivered is low relative to formulation weight
Solution Approach 1:
The patent employs a multivalent carrier molecule that serves as a central core with multiple drug molecules attached to its arms, creating a nested structure where the carrier encapsulates and presents multiple drug molecules simultaneously. This increases the drug payload density while maintaining sustained release properties through the carrier's controlled degradation or dissociation.
Solution Approach 2:
The invention creates a composite prodrug structure combining a carrier molecule (such as a peptide, protein, or synthetic polymer) with multiple drug molecules linked through labile bonds. This composite architecture enables both the stability and sustained release characteristics of the carrier and the high therapeutic payload of multiple drug molecules, resolving the contradiction between formulation weight and active drug amount.
2Stability of the object's composition
If frequent dosing is required to maintain therapeutic levels, then blood level stability is improved, but patient compliance deteriorates
Solution Approach 1:
The multivalent prodrug structure enables continuous drug release over an extended period through the gradual degradation or dissociation of the carrier molecule and its attached drug molecules. This sustained release maintains therapeutic blood levels continuously, eliminating the need for frequent dosing and thereby improving patient compliance while preserving blood level stability.
3Quantity of substance
If prodrugs require large amounts of drug/excipient/prodrug mixtures for administration, then dosing coverage is improved, but bioavailability efficiency deteriorates
Solution Approach 1:
The patent merges multiple drug molecules with a single carrier molecule to create a multivalent prodrug complex. This combining approach increases the effective drug payload per administration while the carrier's design ensures efficient release and bioavailability of all attached drug molecules, thereby improving both dosing coverage and bioavailability efficiency simultaneously.
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
This approach allows for a longer duration of action per dose, reduces the daily dosing requirement, and achieves controlled and sustained release of parent drugs with higher relative ratios in formulations, enhancing patient compliance and therapeutic efficacy.
Implementation Method 1
prodrugs with multiple parent drug molecules attached to carrier moieties, which undergo spontaneous or enzyme-assisted cleavage in physiological conditions to provide sustained release
Data Source
AI summary
The present invention accomplishes this by having multiple molecules of parent drugs attached to carrier moieties and by extending the period during which the parent drug is released and absorbed after administration to the patient and providing a longer duration of action per dose than the parent drug itself. Prodrug conjugates are suitable for sustained delivery of heteroaryl, lactam-amide-, imide-, sulfonamide-, carbamate-, urea-, benzamide-, acylaniline-, cyclic amide- and tertiary amine-containing parent drugs that are substituted at the amide nitrogen or oxygen atom with labile aldehyde-linked prodrug moieties. The carrier groups of the prodrugs can be hydrophobic to reduce the polarity and solubility of the parent drug under physiological conditions.