Cyclic Macromolecule Nanoparticles for Sustained HDACi Delivery
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Solution Overview
Problem
Current drug delivery systems face limitations such as poor stability, limited drug loading capacities, limited abilities for sustained release and distribution, and inefficient fabrication methods, particularly for Histone Deacetylase inhibitors (HDACi) which experience rapid clearance and poor tissue distribution when delivered in free form.
Innovation Solution
Development of a cross-linked network of cyclic macromolecules, such as β-cyclodextrin-poly (β-amino ester) nanoparticles, that utilize covalent and non-covalent interactions to encapsulate active agents like HDACi, enabling high loading and sustained release through a generalizable strategy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If free drugs are administered, then simple administration is achieved, but solubility and pharmacokinetics are limited
Solution Approach 1:
The patent uses cyclic macromolecules (cyclodextrins) as intermediary carriers to encapsulate hydrophobic drugs, forming inclusion complexes that improve solubility and pharmacokinetics while maintaining simple administration routes. The cyclic macromolecules act as mediators between the drug and biological environment.
Solution Approach 2:
The patent modifies the physical and chemical parameters of drugs by encapsulating them in cyclic macromolecule carriers, transforming poorly soluble drugs into soluble nanoparticle formulations that maintain therapeutic efficacy while improving pharmacokinetic properties.
2Productivity
If current drug delivery agents are used, then drug delivery is achieved, but stability is poor
Solution Approach 1:
The patent creates composite nanoparticle systems combining cyclic macromolecules (cyclodextrins) with cross-linking agents and functional polymers to achieve both effective drug delivery and enhanced formulation stability. The composite structure provides mechanical stability while maintaining drug release capability.
Solution Approach 2:
The patent divides the drug delivery system into functional segments: cyclic macromolecule cores for drug encapsulation, cross-linking agents for structural stability, and surface-functionalized polymers for stability and targeting, allowing each component to optimize its specific function.
3Productivity
If current drug delivery agents are used, then drug delivery is achieved, but drug loading capacities are limited
Solution Approach 1:
The patent develops universal cyclic macromolecule-based nanoparticle platforms that can encapsulate various hydrophobic drugs with high loading capacities through inclusion complex formation, allowing a single carrier system to serve multiple drug delivery applications with enhanced capacity.
4Productivity
If current drug delivery agents are used, then drug delivery is achieved, but sustained release ability is limited
Solution Approach 1:
The patent creates dynamic nanoparticle systems where the cross-linked cyclic macromolecule network provides controlled porosity and degradation rates, enabling sustained drug release over extended periods while maintaining the ability to respond to physiological conditions for controlled release kinetics.
5Productivity
If current fabrication methods are used, then drug delivery systems are produced, but fabrication efficiency is inefficient
Solution Approach 1:
The patent employs preliminary self-assembly of cyclic macromolecules into nanoparticle cores before drug encapsulation and cross-linking, streamlining the fabrication process by pre-forming the carrier structure with appropriate size and stability characteristics before final drug loading.
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 nanoparticles achieve high drug loading (up to 30% w/w) and sustained release (up to 21 days) of HDACi, demonstrating improved bioavailability and tissue distribution, including delivery to the brain and spinal cord.
Implementation Method 1
the cyclic macromolecules are covalently cross-linked to one another by a plurality of cross-linking agents
Implementation Method 2
the cross-linking agents and the functional groups form a polymer matrix
Data Source
AI summary
In an embodiment, the present disclosure pertains to a composition. In some embodiments, the composition includes a cross-linked network of cyclic macromolecules. In some embodiments, the cyclic macromolecules are covalently cross-linked to one another by a plurality of cross-linking agents. In some embodiments, at least some of the cross-linking agents are covalently functionalized with a plurality of functional groups. In some embodiments, the plurality of functional groups include a chain of at least three atoms that protrude out of the cross-linking agents. In some embodiments, the cross-linking agents and the functional groups form a polymer matrix, such as poly (β-amino ester). In some embodiments, the composition is in the form of particles. In another embodiment, the present disclosure pertains to a method of administering an active agent to a subject. In some embodiments, the method includes administering a composition of the present disclosure to the subject.