Microencapsulated mTOR Inhibitor for Age-Related Disease Treatment

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Solution Overview

Problem

Current treatments for age-related diseases are inadequate in delaying aging and increasing lifespan, and there is a need for effective interventions that target the underlying mechanisms of age-related disorders.

Innovation Solution

Microcapsules encapsulating an inhibitor of the mammalian target of rapamycin (mTOR) are developed, which provide chronic inhibition of the mTOR pathway, using an enteric coating for delayed release in the intestinal tract, improving therapeutic efficacy and stability, and are administered to extend lifespan and treat age-related diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If mTOR inhibitor is administered without microencapsulation, then the treatment approach is simple, but therapeutic efficacy is reduced due to poor stability and premature release

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The mTOR inhibitor is nested within a microcapsule structure consisting of a core component containing the inhibitor and a coating layer providing enteric protection. This nested formulation ensures the inhibitor is protected from premature release in the stomach while being delivered to the intestine for optimal therapeutic effect, thereby improving reliability without excessive complexity.

Inventive Principle:
Principle #7Nested doll (Nesting)

Solution Approach 2:

The microcapsule is designed with an enteric coating that prevents premature release of the mTOR inhibitor in the acidic stomach environment. The coating acts in advance to protect the inhibitor until it reaches the intestinal tract, ensuring the drug is released at the optimal location for maximum therapeutic efficacy.

Inventive Principle:
Principle #10Preliminary action

2Stability of the object's composition

If mTOR inhibitor is released immediately in the stomach, then administration is simple, but the inhibitor suffers from poor stability and reduced effectiveness

Engineering Contradiction:
Improveinhibitor stabilityVSAvoidadministration complexity
Core Design Contradiction:
Stability of the object's compositionVSEase of operation

Solution Approach 1:

The enteric coating is applied in advance to the microcapsule core, creating a protective barrier before administration. This preliminary protective action ensures the inhibitor maintains its stability during gastric passage and is only released in the appropriate intestinal environment, without requiring complex administration procedures.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The enteric coating acts as an intermediary between the acidic stomach environment and the mTOR inhibitor. This intermediate layer protects the inhibitor from degradation in the stomach while allowing controlled release in the intestine, thereby improving stability without complicating administration.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If the coating releases the inhibitor immediately, then the release mechanism is simple, but therapeutic efficacy is compromised due to premature release

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidrelease timing control
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The enteric coating is designed with preliminary protective properties that prevent inhibitor release in the stomach. The coating's composition and structure are established in advance to ensure delayed release occurs only when the microcapsule reaches the intestinal tract, providing controlled timing for optimal therapeutic effect.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The coating is designed to respond to changes in environmental parameters, specifically pH differences between the stomach and intestine. The enteric coating remains intact in the acidic stomach environment (pH 1-3) but dissolves or becomes permeable in the more neutral intestinal environment (pH 6-7.4), thereby controlling release timing through parameter changes.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS20220023230A1Inhibition of mammalian target of rapamycin
Publication Date: 2022.01.27 BOARD OF RGT THE UNIV OF TEXAS SYST
  • US20220023230A1 patent drawing
  • US20220023230A1 patent drawing
  • US20220023230A1 patent drawing

AI summary

Disclosed are microcapsules that include an inhibitor of the mammalian target of rapamycin (mTOR) within the microcapsules, and pharmaceutical compositions and kits that include the microcapsules. Also disclosed are methods for treating or preventing an age-related disease, condition, or disorder in a subject that involve administering to a subject a pharmaceutically effective amount of microcapsules that includes an inhibitor of mTOR within the microcapsules.