Modified Microemulsion Hormone Delivery for Liver-Safe Oral Absorption
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Solution Overview
Problem
Conventional delivery systems for nonderivatized hormones face challenges in achieving therapeutically effective bloodstream concentrations due to poor solubility in water or oil, leading to liver stress, variable absorption rates, and inconsistent hormone release profiles, especially for oral and transdermal applications.
Innovation Solution
A modified oil-in-water microemulsion (MOIW) system is developed, using a specific ratio of DHEA to polyphenol (1:1 to 12:1) solubilized in a modified oil phase with phospholipid, polyethylene glycol derivative, alcohol, and dispersed in a sugar or sugar alcohol and water continuous phase, allowing stable oral delivery without liver stress and consistent hormone release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If nonderivatized hormones are delivered orally using conventional delivery systems, then the liver is subjected to extensive metabolism and stress, but achieving therapeutically effective bloodstream concentrations becomes difficult
Solution Approach 1:
The patent changes the physical and chemical parameters of the hormone delivery system by converting conventional macroemulsions into microemulsions with droplet sizes of 50-500 nanometers. This parameter change in droplet size enables the hormones to bypass liver metabolism via lymphatic absorption, simultaneously protecting the liver and achieving therapeutically effective bloodstream concentrations
Solution Approach 2:
The patent segments the hormone delivery system into microemulsion droplets with specific size ranges (50-500 nanometers). This segmentation allows the hormones to be absorbed through the lymphatic system rather than undergoing extensive liver metabolism, resolving the contradiction between liver safety and achieving effective bloodstream concentrations
2Quantity of substance
If greater than medically necessary dosages of nonderivatized hormones are taken orally in solid or suspended form, then therapeutically effective bloodstream concentrations may be achieved, but systemic side effects and liver stress increase
Solution Approach 1:
By changing the delivery system from conventional macroemulsions to microemulsions with 50-500 nanometer droplet sizes, the patent enables efficient lymphatic absorption at medically necessary dosages. This parameter change eliminates the need for excessive dosing, thereby preventing systemic side effects and liver stress while achieving therapeutically effective bloodstream concentrations
3Reliability
If transdermal creams and gels are used to bypass liver metabolism, then liver stress is reduced, but absorption rates become poor and variable
Solution Approach 1:
The patent uses microemulsion droplets as an intermediary delivery system that can be orally administered. These microemulsions facilitate rapid absorption through the lymphatic system, serving as a mediator that combines the liver-protection benefit of non-oral delivery with the convenience and consistent absorption of oral delivery, eliminating the poor and variable absorption rates of transdermal applications
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 MOIW microemulsion achieves therapeutically effective bloodstream concentrations of DHEA and pregnenolone within 60 minutes, doubling DHEA and increasing testosterone levels by 30%, while reducing estradiol levels by 12%, effectively alleviating menopausal symptoms such as hot flashes, mood swings, and weight gain.
Implementation Method 1
the alcohol-soluble species is solubilized in the modified oil phase
Implementation Method 2
A modified oil-in-water microemulsion (MOIW) system is developed
Implementation Method 3
the modified oil phase including a phospholipid, a polyethylene glycol derivative, an oil, and an alcohol
Data Source
AI summary
Microemulsions are described where hydrophobic liquid droplets are distributed in a continuous hydrophilic liquid phase. In relation to conventional oil-in-water (OIW) microemulsions, the described microemulsions may be thought of as modified oil-in-water (MOIW) microemulsions, where both the “oil” and “water” phases of the microemulsion are modified. The oil phase droplets of the MOIW microemulsion are modified with alcohol and can solubilize alcohol-soluble species, including nonderivatized hormones. More preferably, the modified oil phase droplets of the MOIW microemulsion directly solubilize nonderivatized hormones. The oil phase droplets of the MOIW microemulsion include DHEA, pregnenolone, and a polyphenol, where a ratio of DHEA to polyphenol is from 1:1 to 12:1 by weight. Methods of supporting and/or increasing bloodstream hormone levels in perimenopausal and postmenopausal females and improving menopausal symptoms also are disclosed.