Convex Microparticle Ballistic Delivery for Corneal Drug Bioavailability

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Solution Overview

Problem

The delivery of drugs to the eye, particularly to the cornea, is challenging due to its biophysical properties, including layered heterogeneity, which complicates the uptake and controlled administration of drug species through traditional methods, leading to low bioavailability and short duration of action.

Innovation Solution

A method and system for controlled ballistic delivery of biologically active cargo to the cornea using convex microparticles with specific dimensions and densities, propelled at high velocities to target regions within the corneal tissue, ensuring precise placement and sustained action without the need for surgery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If traditional topical administration methods are used to deliver drugs to the cornea, then the administration process is simple and non-invasive, but the bioavailability is low and the duration of action is short due to the layered heterogeneity of corneal tissue

Engineering Contradiction:
ImprovebioavailabilityVSAvoiddelivery method complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent replaces traditional mechanical/topical administration methods with a ballistic delivery system that uses controlled impact forces to penetrate corneal layers. Microparticles are accelerated to specific velocities (10-500 m/s) to overcome the cornea's layered heterogeneity and achieve reliable drug delivery to target depths, resolving the contradiction between simple administration and reliable bioavailability.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

Solution Approach 2:

The invention changes key parameters of the delivery system including microparticle density (1-20 g/cc), velocity (10-500 m/s), and size (1-50 μm) to optimize penetration depth and bioavailability. By adjusting these parameters, the system achieves controlled delivery through the cornea's heterogeneous layers, transforming a simple but ineffective method into a reliable delivery system.

Inventive Principle:
Principle #35Parameter changes

2Duration of action of moving object

If traditional topical administration is used, then no surgical intervention is needed, but the duration of action is short and requires frequent re-administration

Engineering Contradiction:
Improveduration of drug actionVSAvoidadministration ease
Core Design Contradiction:
Duration of action of moving objectVSEase of operation

Solution Approach 1:

The ballistic delivery system performs preliminary action by embedding microparticles containing drug cargo directly into the corneal tissue at the desired depth during a single administration event. This preliminary placement ensures sustained release over extended periods, eliminating the need for frequent re-administration while maintaining ease of operation through a single non-surgical procedure.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The invention uses nested structures where microparticles containing drug cargo are embedded within the corneal tissue matrix. The microparticles act as nested delivery vehicles that release drugs gradually from within the tissue, extending the duration of action while requiring only a single initial administration.

Inventive Principle:
Principle #7Nested doll (Nesting)

3Reliability

If high velocity ballistic delivery is used to overcome corneal barriers, then bioavailability increases, but tissue damage and safety concerns increase

Engineering Contradiction:
Improvedrug delivery reliabilityVSAvoidtissue damage
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by using microparticles with specific density and size properties tailored for different target depths within the cornea. Low-density particles (1-2.5 g/cc) are used for superficial epithelial delivery, medium-density particles (2.5-7.8 g/cc) for stromal delivery, and high-density particles (7.8-20 g/cc) for deep interface delivery. This localized optimization achieves reliable delivery to specific regions while minimizing unnecessary tissue damage.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The invention employs beforehand cushioning by using biocompatible carrier materials and controlled particle velocities to mitigate potential tissue damage. The microparticles are designed with appropriate density and surface properties that reduce mechanical trauma during penetration, while the controlled velocity range (10-500 m/s) prevents excessive force that could cause harm, thus cushioning against harmful effects while maintaining delivery reliability.

Inventive Principle:
Principle #11Beforehand cushioning (Prior cushioning)

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 overcomes the biological barrier to mass-transfer, achieving higher bioavailability and sustained action of drugs, even in populations with difficulty adhering to topical administration schedules, such as children and the elderly, by embedding microparticles in the corneal tissue for prolonged release.

Implementation Method 1

contacting the epithelium of the cornea with a convex microparticle comprising the cargo optionally in combination with a carrier material, the convex microparticle having an average dimension from 5 to 30 μm and an average density ρp from 1 g/cc up to less than 20 g/cc, the contacting performed at particle velocity of at least 100 m/s and preferably from 200 to 500 m/s, to ballistically delivering the convex microparticle to a target region of the cornea

Methodology Applied
Scientific EffectBallistic delivery: Impact Force

Data Source

PatentUS20220015943A1Ballistic delivery and related particles, compositions, methods and systems
Publication Date: 2022.01.20 CALIFORNIA INST OF TECH
  • US20220015943A1 patent drawing
  • US20220015943A1 patent drawing
  • US20220015943A1 patent drawing

AI summary

Methods and systems and related particles and compositions that can be used to deliver a biologically active cargo such as a drug to a cornea of an individual, the delivery performed in a rapid, nonsurgical, and/or controllable fashion are described. Particularly, a method is described for controlled ballistic delivery of a cargo in a microparticle to the cornea of an individual, including a biologically active cargo.