Topical Delivery System with Chemical Drivers and Depot
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Solution Overview
Problem
Current topical formulations face challenges in controlling the release of therapeutic agents, leading to rapid absorption into the bloodstream, causing systemic side effects and undesirable drug spikes.
Innovation Solution
A topical delivery system comprising a pharmaceutical composition with a therapeutic agent, chemical drivers like amino benzoate local anesthetics, ethoxydiglycol, and methylsulfonylmethane, combined with a depot component such as liposomes or polymersomes to maintain the agent in the skin and facilitate controlled release, reducing systemic distribution.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional topical formulations are used to deliver therapeutic agents, then the agent can be applied to the skin, but rapid absorption into the bloodstream occurs causing system side effects and undesirable drug spikes
Solution Approach 1:
The patent introduces chemical drivers as intermediary substances that mediate between the therapeutic agent and the skin barrier. These chemical drivers (such as amino benzoate local anesthetics, ethoxydiglycol, and methylsulfonylmethane) facilitate controlled penetration of the therapeutic agent through the stratum corneum while preventing rapid systemic absorption, thus resolving the contradiction between delivering the agent and avoiding harmful systemic effects
Solution Approach 2:
The patent modifies the physical and chemical parameters of the formulation by incorporating specific chemical drivers and depot components. These parameter changes alter the permeability, diffusion rate, and retention characteristics of the therapeutic agent in the skin, enabling controlled release profiles that prevent both insufficient local effect and excessive systemic absorption
2Productivity
If conventional topical formulations are used, then therapeutic agents can be applied to the skin, but rapid release occurs causing undesirable drug spikes
Solution Approach 1:
The patent implements periodic or controlled release action through the use of depot components that release the therapeutic agent in a controlled manner over time. This periodic release mechanism prevents the rapid initial spike followed by abrupt cessation, instead providing a sustained, controlled release profile that maintains therapeutic levels without causing harmful peaks
Solution Approach 2:
The patent ensures continuity of useful action by using depot components that maintain the therapeutic agent in the skin over extended periods. This continuous presence with controlled release prevents the discontinuous pattern of rapid absorption followed by rapid elimination, thereby eliminating drug spikes while maintaining therapeutic effectiveness
3Reliability
If chemical drivers are added to enhance penetration, then therapeutic agent delivery is improved, but formulation complexity increases
Solution Approach 1:
The patent merges multiple functional components (therapeutic agent, chemical drivers, and depot components) into a single integrated topical formulation. This combining approach achieves enhanced penetration and controlled release through synergistic interactions between the components, while presenting a unified product that manages formulation complexity through cohesive design rather than separate elements
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 system effectively delivers therapeutic agents locally within the skin, minimizing systemic absorption and side effects, allowing for sustained biological activity at the target tissue.
Implementation Method 1
chemical drivers comprising an amino benzoate local anesthetic, ethoxydiglycol and methylsulfonylmethane, wherein the chemical drivers are effective at acting synergistically to deliver the therapeutic agent
Implementation Method 2
the chemical drivers are effective at acting synergistically to deliver the therapeutic agent
Implementation Method 3
a depot component that is effective to keep the active agent locally in the skin; reduce distribution of the active agent to the blood stream; to encapsulate the pharmaceutical composition
Implementation Method 4
depot component that is effective to keep the active agent locally in the skin
Implementation Method 5
facilitate controlled or delayed type release of the active therapeutic agent
Implementation Method 6
facilitate controlled or delayed type release of the active therapeutic agent
Data Source
AI summary
The described invention provides a topical delivery system comprising a pharmaceutical composition for application directly to a skin of a subject in need thereof comprising (a) an effective therapeutic amount of an active therapeutic agent; (b) chemical drivers comprising an amino benzoate local anesthetic, ethoxydiglycol and methylsulfonylmethane (MSM) that in combination are effective to synergistically deliver the therapeutic agent; and (c) a depot component for keeping the pharmaceutical composition in the skin. Methods for delivering an active therapeutic agent into skin, for keeping it in the skin, for reducing systemic side effects attributable to entry of the active agent into the blood stream, and a method for treating a condition, disease or disorder of skin topically also are described in accordance with the embodiments of the described invention.