Topical Formulations with Nanomicelles for Ocular Stability

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Solution Overview

Problem

Current ophthalmic formulations lack stability at high temperatures and effective ocular tissue distribution, particularly for anterior and posterior eye delivery, and often include pharmaceutically active agents that have not received regulatory approval for ocular conditions.

Innovation Solution

Development of topical formulations incorporating polyoxyl lipids or fatty acids, such as HCO-40, HCO-60, and HCO-80, and polyalkoxylated alcohols like octoxynol-40, which form nanomicelles, providing stability and improved ocular tissue distribution without the need for approved active agents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If current ophthalmic formulations are used, then ocular tissue distribution can be achieved, but stability at high temperatures deteriorates

Engineering Contradiction:
Improveformulation stabilityVSAvoidhigh temperature stability
Core Design Contradiction:
Stability of the object's compositionVSTemperature

Solution Approach 1:

The patent changes the physical-chemical parameters of the formulation by incorporating nanomicelles with specific polyoxyl lipids (HCO-40, HCO-60, HCO-80) and fatty acids. These parameter changes in molecular structure and aggregation state enable the formulation to maintain stability at high temperatures while improving ocular tissue distribution.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite nanomicellar system combining multiple components: polyoxyl lipids, fatty acids, and surfactants. This composite structure leverages the synergistic properties of each component to achieve both high temperature stability and effective ocular tissue distribution, resolving the technical contradiction between stability and temperature resistance.

Inventive Principle:
Principle #40Composite materials

2Reliability

If nanomicelles are incorporated to improve ocular tissue distribution, then delivery effectiveness improves, but formulation complexity increases

Engineering Contradiction:
Improveocular tissue distributionVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent segments the formulation into distinct functional components: nanomicelles for targeted delivery, polyoxyl lipids for stability, and surfactants for solubility. This segmentation allows each component to perform its specific function efficiently, improving ocular tissue distribution while managing overall formulation complexity through modular design.

Inventive Principle:
Principle #1Segmentation

3Object-affected harmful factors

If approved active agents are excluded from the formulation, then safety profile improves, but therapeutic efficacy may be limited

Engineering Contradiction:
Improvesafety profileVSAvoidtherapeutic efficacy
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent uses nanomicelles as intermediary carriers that can deliver therapeutic agents to ocular tissues without requiring the active agent itself to be in the formulation. This intermediary approach improves the safety profile by excluding approved active agents while maintaining potential therapeutic efficacy through the delivery capability of the nanomicellar system.

Inventive Principle:
Principle #24Intermediary (Mediator)

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 formulations demonstrate enhanced stability at high temperatures and improved ocular tissue distribution, making them suitable for anterior and posterior eye delivery without the inclusion of pharmaceutically active agents that have received regulatory approval for ocular conditions.

Implementation Method 1

the formulations include nanomicelles

Methodology Applied
Scientific EffectNanomicelle formation: Self-Assembly

Implementation Method 2

a polyoxyl lipid or fatty acid and a polyalkoxylated alcohol

Methodology Applied
Scientific EffectSurfactant action: Surfactant

Data Source

PatentUS20240358840A1Topical formulations and uses thereof
Publication Date: 2024.10.31 SUN PHARMACEUTICAL INDUSTRIES LTD
  • US20240358840A1 patent drawing
  • US20240358840A1 patent drawing
  • US20240358840A1 patent drawing

AI summary

Provided herein include formulations for topical administration, such as ophthalmic formulations, and methods of using such formulations. In some aspects and embodiments the formulations may include a polyoxyl lipid or fatty acid, and/or a polyalkoxylated alcohol and may include nanomicelles. Also include methods of treating or preventing diseases or conditions, such as ocular diseases or conditions.