Transdermal Andrographolide-EGCG Emulsion for Low Bioavailability
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Solution Overview
Problem
Andrographolides and epigallocatechin gallate exhibit low bioavailability and poor solubility, leading to limited biodistribution and short half-life, and oral administration results in low absorption and adverse effects.
Innovation Solution
Topical formulations comprising Andrographolides, epigallocatechin gallate, and additional ingredients like glycerin, vegetable oils, and silicone oils, formulated using a cold emulsion process to enhance transdermal delivery.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If andrographolides are administered orally, then therapeutic effects can be achieved, but bioavailability is low and half-life is short
Solution Approach 1:
The patent uses a transdermal delivery system as an intermediary mechanism to transport andrographolides from the skin surface through the stratum corneum and into systemic circulation, bypassing the gastrointestinal tract and first-pass metabolism that cause rapid elimination and low bioavailability
2Reliability
If epigallocatechin gallate is taken orally, then potential therapeutic benefits can be obtained, but absorption is poor and adverse effects occur
Solution Approach 1:
The transdermal delivery system serves as an intermediary pathway that delivers epigallocatechin gallate directly to the bloodstream through the skin, avoiding the gastrointestinal tract where degradation and adverse effects occur, while maintaining therapeutic efficacy
Solution Approach 2:
The invention extracts epigallocatechin gallate from its traditional oral administration route and delivers it through an alternative transdermal pathway, removing it from the harmful gastrointestinal environment while preserving its therapeutic properties
3Quantity of substance
If andrographolides are extracted from plant material, then active compounds are obtained, but water solubility is poor and biodistribution is limited
Solution Approach 1:
The patent creates a composite transdermal formulation combining andrographolides with penetration enhancers, emollients, and carriers that improve water solubility and facilitate biodistribution while maintaining the integrity and concentration of the active compounds
Solution Approach 2:
The invention modifies the physical and chemical parameters of andrographolide delivery by changing from oral to transdermal administration, and by formulating with solubility-enhancing agents, thereby improving water solubility and biodistribution without altering the core active compound structure
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
Enhances localized, deep-tissue, and systemic delivery of these bioactive compounds, providing therapeutic benefits for conditions like arthritis, neuropathies, and cancers, while avoiding oral absorption issues.
Implementation Method 1
formulating purified andrographolides and/or epigallocatechin gallate in an oil-in-water emulsion
Implementation Method 2
comprising: andrographolides (ANGL) (i.e., Andrographis paniculata, full spectrum extract), epigallocatechin gallate (EGCG), or a combination thereof; a wetting/hydrating agent; a vegetable oil
Data Source
AI summary
Described herein are compositions (e.g., topical formulations) including andrographolides (ANGL), epigallocatechin gallate (EGCG), or a combination thereof, and methods of making and using the same.