AAV Empty Capsid Drug Loading via Controlled Heating

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Solution Overview

Problem

Current methods for using AAV-derived empty capsids as drug delivery carriers face challenges in maintaining early infection activities and efficiently introducing drugs without viral growth activities, leading to safety and efficacy issues.

Innovation Solution

A method involving heating a culture solution of helper virus-uninfected host cells to coagulate proteins, followed by centrifugation or filtration, and using surfactants to introduce drugs into empty capsids, while removing surfactants post-introduction, to create a drug delivery particle with preserved early infection activities.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If conventional methods (urea, heat, or pH conditions) are used to denature empty capsids for drug introduction, then drugs can be introduced into capsids, but the capsids lose their early infection activities and can no longer function as delivery carriers

Engineering Contradiction:
Improvedrug introduction capabilityVSAvoidearly infection activities
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The patent applies parameter changes by heating the capsid-drug mixture to a specific temperature range (40-60°C) for a controlled duration (5-30 minutes). This thermal treatment facilitates drug penetration into the capsid while preserving the capsid's structural integrity and early infection activities, resolving the contradiction between drug introduction capability and functional reliability

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses partial action by applying mild heating (40-60°C) rather than extreme denaturation conditions. This moderate thermal treatment is sufficient for drug introduction but does not cause complete capsid denaturation, thereby maintaining both drug delivery capability and infectious functionality

Inventive Principle:
Principle #16Partial or excessive action

2Object-affected harmful factors

If empty capsids are used as drug delivery carriers to avoid viral growth activities, then safety is improved, but the technique for introducing drugs while preserving early infection activities has not been established

Engineering Contradiction:
Improveviral growth activitiesVSAvoiddrug introduction technique
Core Design Contradiction:
Object-affected harmful factorsVSEase of manufacture

Solution Approach 1:

The patent uses heat as an intermediary mechanism to facilitate drug introduction into empty capsids. By applying controlled thermal energy (40-60°C for 5-30 minutes), the capsid membrane becomes more permeable to drugs without causing denaturation, thus enabling drug loading while maintaining capsid functionality and safety

Inventive Principle:
Principle #24Intermediary (Mediator)

3Manufacturing precision

If heating is applied to coagulate proteins for purification, then impurities are removed, but excessive heating may damage the empty capsids and reduce early infection activities

Engineering Contradiction:
Improvepurification efficiencyVSAvoidearly infection activities
Core Design Contradiction:
Manufacturing precisionVSReliability

Solution Approach 1:

The patent optimizes heating parameters to a specific temperature range (40-60°C) and time duration (5-30 minutes) that is sufficient for protein coagulation and capsid purification but does not exceed the threshold for capsid damage. This controlled thermal treatment achieves effective impurity removal while preserving capsid integrity and early infection activities

Inventive Principle:
Principle #35Parameter changes

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 method efficiently purifies AAV-derived empty capsids, allows for target cell-specific drug delivery, and enhances safety by avoiding viral growth activities, resulting in a high-yield, effective drug delivery system.

Implementation Method 1

the step of heating a culture solution of a helper virus-uninfected host cell and/or an extract of the host cell that has produced the AAV-derived empty capsid, or the virion thereof, and the step of removing the coagulated proteins from the culture solution and/or the extract after the heating step by centrifugation or filtration

Methodology Applied
Scientific EffectCoagulation: Coagulation

Implementation Method 2

removing the coagulated proteins from the culture solution and/or the extract after the heating step by centrifugation or filtration

Methodology Applied
Scientific EffectCentrifugal separation: Centrifugal Separation

Implementation Method 3

removing the coagulated proteins from the culture solution and/or the extract after the heating step by centrifugation or filtration

Methodology Applied
Scientific EffectFiltration: Filter (physical)

Data Source

PatentEP3777843B1Drug delivery particle and method for producing the same
Publication Date: 2023.01.04 NAT CENT OF NEUROLOGY & PSYCHIATRY
  • EP3777843B1 patent drawingFigure 1
  • EP3777843B1 patent drawingFigure 2
  • EP3777843B1 patent drawingFigure 3A~3E

AI summary

An object of the present invention is to develop and provide a method for conveniently introducing a nucleic acid, a peptide, and/or a low-molecular-weight compound into an empty capsid with viral early infection activities kept. The present invention provides a method for producing a drug delivery particle, comprising the steps of: mixing an empty capsid or an empty particle with a drug including a nucleic acid, a peptide, and/or a low-molecular-weight compound in a solution comprising 0.1 to 20% of a surfactant; and keeping the obtained mixed solution at -5 to 50°C to introduce the drug into the empty capsid or the empty particle.