Polymeric Nanocapsoids for Finasteride and Minoxidil Delivery

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Solution Overview

Problem

Current treatments for alopecia face challenges in delivering active ingredients like finasteride and minoxidil effectively to hair follicles due to stability, bioavailability, and permeability issues, leading to inadequate hair growth results.

Innovation Solution

A pharmaceutical composition comprising polymeric nanoparticles in the form of nanocapsoids containing finasteride and minoxidil, formulated with a biodegradable polymer like poly(ε-caprolactone), medium-chain triglycerides, sorbitan monostearate, acetone, ethanol, polysorbate 80, and water, which enhances penetration and retention at the hair follicle site.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If traditional topical treatments are used, then the formulation is simple to manufacture, but the permeability and retention at the hair follicle site are insufficient

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

Solution Approach 1:

The patent changes the physical and chemical parameters of the active ingredients by encapsulating them in polymeric nanoparticles. This transformation from conventional molecular form to nanoparticulate form fundamentally alters their permeability, retention, and therapeutic efficacy characteristics while maintaining the core pharmacological activity.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite material structures by combining active ingredients with polymeric nanoparticle carriers. These composite nanocapsoids integrate the therapeutic agents within a biodegradable polymer matrix, creating a sophisticated delivery system that enhances performance beyond what simple formulations can achieve.

Inventive Principle:
Principle #40Composite materials

2Reliability

If nanocapsoid formulation is used, then the permeability and retention at the hair follicle site are improved, but the manufacturing process becomes more complex

Engineering Contradiction:
Improvepermeability and retentionVSAvoidmanufacturing complexity
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent applies preliminary action by pre-forming the polymeric nanoparticle carriers before incorporating the active ingredients. The nanocapsoids are prepared in advance with controlled size and surface properties, then the active ingredients are loaded into these pre-prepared carriers, streamlining the overall manufacturing process.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent uses surfactants and stabilizing agents as intermediary substances that facilitate the formation and stabilization of the nanocapsoid structure. These intermediaries enable the interface between hydrophobic and hydrophilic phases, making the manufacturing process more controllable and reproducible.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If active ingredients are delivered systemically, then the drug reaches the hair follicle, but it permeates the blood capillaries causing unwanted systemic action

Engineering Contradiction:
Improvedrug delivery to target siteVSAvoidsystemic side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent segments the drug delivery system into targeted nanocapsoids that are specifically designed to accumulate at the hair follicle site. By dividing the therapeutic agent into discrete nanoparticle units with targeted delivery capabilities, the system achieves local concentration at the target while minimizing systemic distribution.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent implements local quality by designing the nanocapsoid formulation to exhibit enhanced permeability and retention specifically at the hair follicle site. The nanoparticulate system displays spatially heterogeneous distribution, concentrating the therapeutic effect locally while reducing exposure to distant tissues and blood capillaries.

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 nanocapsoid formulation improves the therapeutic efficacy by achieving higher permeability and retention in hair follicles, leading to enhanced hair growth and reduced side effects compared to traditional topical treatments.

Implementation Method 1

the nanocapsoid formulation improves the therapeutic efficacy by achieving higher permeability and retention in hair follicles

Methodology Applied
Scientific EffectPermeation: Permeation

Implementation Method 2

polymeric nanoparticles in the form of nanocapsoids containing finasteride and minoxidil

Methodology Applied
Scientific EffectDiffusion: Diffusion

Data Source

PatentEP2891486B1Polymeric finasteride and minoxidil nanoparticles, method for preparing same, aqueous suspension containing same, pharmaceutical composition and use thereof
Publication Date: 2018.05.16 BIOLAB SANUS FARMACEUTICA LTDA
  • EP2891486B1 patent drawingFigure 1
  • EP2891486B1 patent drawingFigure 2
  • EP2891486B1 patent drawingFigure 3A~3C

AI summary

The present invention relates to a pharmaceutical composition for topical application for the treatment of alopecia, said composition comprising polymeric nanoparticles, preferably nanocapsules containing two active ingredients, finasteride and minoxidil, additives and a pharmaceutically acceptable carrier. The invention further includes a process for the preparation of polymeric nanoparticles, preferably nanocapsules of finasteride and minoxidil, a composition suitable for topical application for the treatment of alopecia, as well as the use of said nanocapsules for the preparation of a pharmaceutical composition.