Topical Finasteride Minoxidil Formulation for Alopecia

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Solution Overview

Problem

Current treatments for androgenic alopecia, such as Minoxidil and Finasteride, have limitations including significant side effects and limited efficacy, with Finasteride's oral use posing risks and Minoxidil's mechanism of action not fully understood, necessitating a more effective and safer topical formulation.

Innovation Solution

A topical formulation combining Finasteride with silicones and Minoxidil, potentially incorporating retinol, to enhance hair growth with reduced systemic side effects, using an anhydrous vehicle and porous polymers for slow release to improve transdermal penetration and efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If Finasteride is used orally to treat androgenic alopecia, then hair growth is stimulated, but significant side effects occur including impotence, erection failure, decreased libido, and gynecomastia

Engineering Contradiction:
Improvehair growthVSAvoidsystemic side effects
Core Design Contradiction:
ProductivityVSObject-generated harmful factors

Solution Approach 1:

The patent applies Finasteride topically to the scalp rather than systemically through oral administration. This localized application ensures that the drug acts only at the site of hair growth, stimulating hair growth in the scalp while avoiding systemic circulation that causes impotence, erection failure, decreased libido, and gynecomastia.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent uses a topical formulation system as an intermediary to deliver Finasteride to the scalp. This formulation acts as a mediator that allows the drug to penetrate the scalp and reach the hair bulb without entering the systemic circulation, thus achieving hair growth stimulation while preventing systemic side effects.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Object-generated harmful factors

If Finasteride is applied topically to reduce DHT formation, then hair growth is stimulated without systemic side effects, but penetration to the hair bulb level is insufficient

Engineering Contradiction:
Improvesystemic side effectsVSAvoidpenetration efficacy
Core Design Contradiction:
Object-generated harmful factorsVSReliability

Solution Approach 1:

The patent modifies the physical and chemical parameters of the Finasteride molecule and its formulation to enhance penetration. This includes adjusting the molecular properties of Finasteride and the formulation characteristics (such as using anhydrous vehicles and porous polymers) to improve transdermal penetration and ensure reliable delivery to the hair bulb level.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent incorporates porous polymers in the topical formulation to enhance the penetration of Finasteride through the scalp. The porous structure provides pathways that facilitate drug permeation while maintaining controlled release, ensuring reliable delivery to the hair bulb without causing systemic side effects.

Inventive Principle:
Principle #31Porous materials

3Productivity

If Minoxidil is used topically to treat alopecia, then hair growth is stimulated through vasodilation and potassium channel opening, but the mechanism of action is not fully clarified and response is limited to 40% of individuals

Engineering Contradiction:
Improvehair growthVSAvoidmechanism of action understanding
Core Design Contradiction:
ProductivityVSLoss of information

Solution Approach 1:

The patent combines Finasteride and Minoxidil in a single topical formulation. This combination merges the DHT inhibition mechanism of Finasteride with the vasodilation and potassium channel opening mechanism of Minoxidil, providing synergistic effects that enhance hair growth stimulation and expand the responsive population beyond the 40% limit of Minoxidil alone.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent creates a composite topical formulation that integrates multiple active ingredients (Finasteride, Minoxidil, and potentially retinol) with specific carriers and adjuvants. This composite system enhances the overall efficacy by combining different mechanisms of action while improving delivery and penetration characteristics.

Inventive Principle:
Principle #40Composite materials

4Object-affected harmful factors

If Finasteride is used at 1 mg daily for oral treatment, then teratogenesis risk is reduced, but hormonal function is not completely prevented and limited efficacy is achieved

Engineering Contradiction:
Improveteratogenesis riskVSAvoidhormonal function inhibition
Core Design Contradiction:
Object-affected harmful factorsVSProductivity

Solution Approach 1:

The patent applies Finasteride locally to the scalp through topical formulation rather than systemically through oral administration. This localized application allows the drug to inhibit 5α-reductase specifically at the scalp level, providing more effective hormonal function inhibition in the target area while maintaining safety by avoiding systemic circulation.

Inventive Principle:
Principle #3Local quality

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 combination of Finasteride and Minoxidil in a silicone-based formulation significantly increases hair growth efficacy, reduces side effects, and improves hair properties like softness and shine, as demonstrated by clinical studies, providing a safer and more effective treatment for both men and women.

Implementation Method 1

This compound is an inhibitor of 5a: -reductase types II and III, which prevents the transformation of testosterone into DHT, significantly reducing the concentration of DHT in the scalp

Methodology Applied
Scientific EffectEnzyme inhibition: Enzyme

Implementation Method 2

it is postulated that it works by producing local vasodilation and opening the cellular potassium channels. This allows the blood to containing oxygen and nutritional elements, it reaches the hair follicle more easily

Methodology Applied
Scientific EffectVasodilation:

Implementation Method 3

Finasteride could be applied topically and penetrate the scalp at the level of the hair bulb in order to locally reduce the formation of DHT

Methodology Applied
Scientific EffectTransdermal penetration: Permeation

Data Source

PatentUS12029811B2Formulation and method for the treatment of androgenic alopecia
Publication Date: 2024.07.09 CENT INT DE COSMIATRIA S A P I DE CV

AI summary

The present invention relates to a topical formulation intended to be used for the treatment of androgenic or androgenetic baldness is men and women, with reduced side effects, especially with fewer collateral effects in the female population. The topical formulation comprises 0.01% to 10% by weight of Finasteride and a concentration of 1% to 5% by weight of Minoxidil in its free form or in an inert porous polymer. The combination of Finasteride and Minoxidil provides a synergistic effect against baldness. The formulation also comprises 0.15% by weight of retinol and is suitable for being applied to the scalp of the patient that requires it.