Amorphous Solid Dispersion for Resveratrol Bioavailability
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Solution Overview
Problem
Resveratrol and curcumin, classified as Class IV compounds, exhibit low oral bioavailability due to their low solubility and permeability, making existing delivery systems ineffective in improving their bioavailability.
Innovation Solution
A hot melt extrusion (HME) process is used to create an amorphous solid dispersion of resveratrol and curcumin with lipid-based excipients and inorganic carriers, resulting in a composition that enhances solubility and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional delivery systems are used for resveratrol and curcumin, then the formulation is simple to manufacture, but the oral bioavailability remains low due to low solubility and permeability
Solution Approach 1:
The patent uses a composite material system combining hydrophilic polymers (such as HPMC, PEG, or chitosan) with lipophilic excipients (such as lecithin, triglycerides, or fatty acids) to create a delivery composition. This composite structure allows the hydrophilic polymer to enhance solubility while the lipophilic excipients facilitate permeability through biological membranes, thereby resolving the contradiction between improving bioavailability and maintaining manufacturability
Solution Approach 2:
The patent modifies the physicochemical parameters of the active ingredients by incorporating them into a delivery system that changes their solubility characteristics. The composition transforms the poorly soluble resveratrol and curcumin into a form with improved dissolution properties through polymer-excipipient interactions, enabling better absorption without complex manufacturing processes
2Reliability
If the solubility of resveratrol and curcumin is increased through polymer loading, then the bioavailability improves, but the complexity of the delivery system increases
Solution Approach 1:
The patent changes the physical state and solubility parameters of resveratrol and curcumin by incorporating them into an amorphous solid dispersion matrix. This transformation from crystalline to amorphous state, facilitated by the polymer-excipipient system, significantly increases solubility and bioavailability while maintaining a relatively simple formulation structure
Solution Approach 2:
The patent introduces intermediary substances (hydrophilic polymers and lipophilic excipients) that mediate between the poorly soluble active ingredients and the aqueous biological environment. These intermediaries facilitate dissolution and absorption without requiring complex delivery mechanisms, thus improving bioavailability while limiting system complexity
3Reliability
If resveratrol and curcumin are administered orally, then the treatment is easy to administer, but rapid metabolism reduces therapeutic efficacy
Solution Approach 1:
The patent applies preliminary protection to resveratrol and curcumin by encapsulating them within the polymer-excipipient delivery system before administration. This pre-protection prevents premature metabolism by enzymes and chemicals in the gastrointestinal tract, allowing the active ingredients to reach their target sites intact and maintain therapeutic efficacy over time
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 HME process significantly increases the solubility and bioavailability of resveratrol and curcumin, preventing rapid metabolism and allowing for higher therapeutic efficacy, particularly in the human intestine, independent of age.
Implementation Method 1
A hot melt extrusion (HME) process is used to create an amorphous solid dispersion of resveratrol and curcumin with lipid-based excipients and inorganic carriers
Implementation Method 2
The HME process significantly increases the solubility and bioavailability of resveratrol and curcumin, preventing rapid metabolism
Implementation Method 3
A liquid pharmaceutical composition is described, comprising a stable colloidal dispersion comprising polymeric particles of zein and β-cyclodextrin suspended in a hydroalcoholic continuous phase
Implementation Method 4
A liquid pharmaceutical composition is described, comprising a stable colloidal dispersion comprising polymeric particles of zein and β-cyclodextrin suspended in a hydroalcoholic continuous phase
Data Source
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AI summary
The invention relates to a composition containing natural lipophilic compounds, the use of this composition, in particular as a pharmaceutically active composition, and its preparation. It contains resveratrol together with curcumin as natural lipophilic compounds, as well as one or more nonionic and/or anionic emulsifiers and one or more solid matrix-forming agents. Resveratrol, together with curcumin and with one or more emulsifiers and one or more matrix-forming agents, is soluble in a solid solvent system. The composition is prepared by hot melt extraction. Lipophilic model compounds are provided that are characterized by a significantly increased release of the active ingredients in the human intestine. The otherwise usual metabolism is prevented.The uptake of resveratrol and curcumin by human cells is enhanced, and a significantly higher bioavailability of these active ingredients is achieved, regardless of age. The invention therefore has great potential for improving the efficacy of dosages, especially in pharmaceuticals. It also opens up new possibilities with improved sustainability for food technologies and, in particular, dietary supplements.