Anhydrous mTOR Inhibitor Compositions for Topical Delivery

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Solution Overview

Problem

Current methods for delivering mTOR inhibitors topically are inefficient, leading to inadequate skin penetration and systemic absorption, which limits their effectiveness in treating skin disorders.

Innovation Solution

An anhydrous composition comprising an effective amount of one or more mTOR inhibitors, solvents, gelling agents, and antioxidants, specifically formulated to enhance topical delivery and minimize systemic absorption.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If topical delivery methods are used for mTOR inhibitors, then skin penetration is improved, but systemic absorption increases leading to side effects

Engineering Contradiction:
Improveskin penetration rateVSAvoidsystemic absorption and side effects
Core Design Contradiction:
SpeedVSObject-generated harmful factors

Solution Approach 1:

The patent changes the physical and chemical parameters of the delivery system by using anhydrous (water-free) formulations with specific solvent systems (e.g., glycols, esters, hydrocarbons) and controlling pH, viscosity, and molecular weight of components. These parameter changes optimize skin penetration while controlling systemic absorption through the unique anhydrous composition structure

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite material systems combining mTOR inhibitors with specific solvents (e.g., propylene glycol, ethylene glycol monoalkyl ethers), gelling agents, and antioxidants in anhydrous formulations. This composite approach creates a synergistic delivery system that enhances skin penetration while minimizing systemic side effects through the integrated composition design

Inventive Principle:
Principle #40Composite materials

2Ease of operation

If conventional topical formulations are used, then ease of application is maintained, but delivery efficiency is insufficient

Engineering Contradiction:
Improveease of topical applicationVSAvoiddelivery efficiency
Core Design Contradiction:
Ease of operationVSProductivity

Solution Approach 1:

The patent modifies formulation parameters including viscosity (through gelling agents), pH balance, and solvent composition to maintain ease of application. The anhydrous nature and specific rheological properties allow the formulation to remain spreadable and user-friendly while achieving superior delivery efficiency through enhanced skin penetration

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent applies local quality by creating formulations with specific regional properties - the anhydrous composition is designed to have optimal viscosity and spreadability at the application site while simultaneously providing targeted high-concentration delivery to the epidermis and dermis layers, achieving both ease of operation and high productivity

Inventive Principle:
Principle #3Local quality

3Reliability

If higher concentrations of mTOR inhibitors are used, then treatment effectiveness is improved, but systemic side effects increase

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidsystemic side effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent implements local quality by achieving high local concentration of mTOR inhibitors specifically in the skin layers (epidermis and dermis) through the anhydrous formulation design, while the overall systemic concentration remains low. This spatial differentiation allows effective treatment at the target site without proportionally increasing systemic side effects

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The anhydrous composition acts as an intermediary system that carries high concentrations of mTOR inhibitors to the skin target. The specific solvent system and gelling agents serve as mediators that facilitate localized high-dose delivery while controlling systemic absorption, decoupling local effectiveness from systemic exposure

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS12329748B2Anhydrous compositions of mTOR inhibitors and methods of use
Publication Date: 2025.06.17 PALVELLA THERAPEUTICS INC
  • US12329748B2 patent drawing
  • US12329748B2 patent drawing
  • US12329748B2 patent drawing

AI summary

Disclosed herein are compositions and methods for topical delivery of mTOR inhibitors. In one embodiment, an anhydrous composition includes one or more mTOR inhibitors, one or more solvents, one or more gelling agents, and one or more antioxidants. Also disclosed herein are methods to treat skin disorders using such compositions.