Formononetin Solid Lipid Nanoparticles for Bioavailability

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Solution Overview

Problem

Formononetin exhibits poor oral bioavailability and instability in existing formulations, leading to inadequate pharmacological activity due to its poor biocompatibility and formulation instability.

Innovation Solution

A dispersion of formononetin solid lipid nanoparticles is developed, comprising a core system with formononetin, a lipid base, and a fluid medium, along with an emulsifier system, which enhances biocompatibility, stability, and controlled release profiles, with particle sizes ranging from 200 nm to 350 nm and zeta potentials between −25.00 mv to −45.00 mv, achieving an entrapment efficiency of 40% to 75% and controlled drug release of 70% to 90%.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If formononetin is formulated in conventional formulations, then the formulation can be prepared, but the oral bioavailability is poor and stability is insufficient

Engineering Contradiction:
ImprovestabilityVSAvoidoral bioavailability
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent transforms formononetin from a conventional formulation into solid lipid nanoparticles with specific physical parameters (particle size 200-350 nm, zeta potential -25 to -45 mV). This parameter transformation resolves the contradiction by improving both stability through the nanoparticle matrix and oral bioavailability through enhanced solubility and cellular uptake characteristics of the nanoscale formulation

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite material system combining formononetin with lipid bases (such as stearic acid, glyceryl monostearate) and emulsifiers (such as Tween 80, Span 20). This composite approach resolves the contradiction by providing both the stability of the lipid matrix and the bioavailability enhancement through the amphiphilic emulsifier system that facilitates absorption

Inventive Principle:
Principle #40Composite materials

2Reliability

If formononetin is formulated in conventional formulations, then the formulation can be prepared, but biocompatibility is poor

Engineering Contradiction:
ImprovebiocompatibilityVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent achieves improved biocompatibility by transforming the formulation into nanoscale particles (200-350 nm) that exhibit better cellular compatibility and reduced toxicity. The specific parameter of particle size in the nanorange resolves the contradiction by enhancing biocompatibility while the standardized preparation protocol maintains ease of manufacture

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces biocompatible lipid bases and emulsifiers as intermediary materials between formononetin and the biological system. These intermediaries (lipid bases and emulsifiers) resolve the contradiction by providing a biocompatible interface that enhances cellular acceptance while the materials are readily available and easy to work with

Inventive Principle:
Principle #24Intermediary (Mediator)

3Duration of action of moving object

If formononetin is formulated in conventional formulations, then the formulation can be prepared, but controlled release profile is not achieved

Engineering Contradiction:
Improvecontrolled release profileVSAvoidformulation structure
Core Design Contradiction:
Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The patent achieves controlled release by transforming the formulation into solid lipid nanoparticles with specific physical parameters. The nanoparticle structure with controlled size (200-350 nm) and surface charge (-25 to -45 mV) provides sustained release kinetics, resolving the contradiction by enabling controlled release through nanoscale physics while maintaining relatively simple formulation composition

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses the lipid matrix as a flexible shell or matrix that controls drug release. The lipid base forms a semi-permeable structure around the formononetin, providing controlled release through diffusion and erosion mechanisms while keeping the formulation structure relatively simple compared to multi-layered systems

Inventive Principle:
Principle #30Flexible shells and thin films

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 dispersion of formononetin solid lipid nanoparticles improves bioavailability, stability, and biocompatibility, providing a controlled release profile and enhanced solubility, making them biodegradable and suitable for pharmacological applications.

Implementation Method 1

a dispersion of formononetin solid lipid nanoparticles comprises (a) a core system comprising formononetin in an amount in the range of 15 wt % to 25 wt % of the total weight of the dispersion, a lipid base in an amount in the range of 15 wt % to 35 wt % of the total weight of the dispersion

Methodology Applied
Scientific EffectSelf-assembly: Self-Assembly

Implementation Method 2

an emulsifier system comprising an emulsifier, and water

Methodology Applied
Scientific EffectEmulsion: Emulsion

Implementation Method 3

Drug Release Kinetics: The system in which drug release and concentration exhibit zero dependency was well explained by Zero order equation. Whereas, First order rate equation explains the system release which is dependent on concentration. Likewise, Higuchi equation postulated theory for insoluble drug matrix, proposing that rate of release as square root of time following a fickian diffusion.

Methodology Applied
Scientific EffectDiffusion: Diffusion

Data Source

PatentUS10973798B2Dispersion of formononetin solid lipid nanoparticles and process for its preparation
Publication Date: 2021.04.13 SRM INST OF SCI & TECH
  • US10973798B2 patent drawing
  • US10973798B2 patent drawing
  • US10973798B2 patent drawing

AI summary

A dispersion of formononetin solid lipid nanoparticles and process for its preparation, namely having (i) a core system comprising formononetin, a lipid base, and a fluid medium, and (ii) an emulsifier system comprising an emulsifier, and water. The dispersion of formononetin solid lipid nanoparticles of the present disclosure can be used for treating cancer, osteoporosis, diabetes, and inflammation. The dispersion of formononetin solid lipid nanoparticles of the present disclosure are biocompatible, biodegradable, has improved solubility, has enhanced controlled drug release profile and are stable.