Supercritical CO2 Antisolvent Precipitation for Bioactive Lipid Dispersion
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Solution Overview
Problem
Existing methods for formulating bioactive compounds in pharmaceutical, nutraceutical, and cosmetic products face challenges due to the poor stability and low solubility of bioactive molecules, often requiring toxic organic solvents that need to be eliminated, leading to degradation of the compounds during processing.
Innovation Solution
The BIOSAS (Bioactive compounds Supercritical Antisolvent Solvent) process uses supercritical carbon dioxide to precipitate and disperse bioactive compounds into a lipid matrix, avoiding the use of toxic solvents and maintaining the stability and bioavailability of the compounds.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional encapsulation methods using organic solvents are used, then bioactive compounds can be formulated, but the solvents are toxic and must be eliminated requiring heating steps that degrade the bioactive compounds
Solution Approach 1:
The patent changes the physical state and properties of the solvent by using supercritical carbon dioxide instead of traditional organic solvents. This parameter change allows the solvent to be non-toxic and removable by simple pressure reduction without heating, thus eliminating both toxicity concerns and thermal degradation of bioactive compounds
Solution Approach 2:
The patent utilizes the phase transition properties of supercritical CO2, where it transitions from a supercritical state during formulation to a gaseous state upon pressure release. This phase transition enables complete solvent removal without heating, resolving the contradiction between solvent elimination and compound stability
2Reliability
If supercritical carbon dioxide is used as a solvent, then the process can be carried out at low temperatures preserving bioactive compounds, but the solubility of many bioactive molecules in SCCO2 is limited
Solution Approach 1:
The patent introduces a cosolvent as an intermediary substance that mediates between the supercritical CO2 and the bioactive compound. This cosolvent enhances the solubility of bioactive molecules in the supercritical fluid while maintaining the low-temperature processing conditions, thus resolving the contradiction between stability and solubility
3Manufacturing precision
If SCCO2 acts as an antisolvent in precipitation processes, then particles can be formed with controlled size and morphology, but the process complexity increases with multiple phases and components
Solution Approach 1:
The patent makes the supercritical CO2 system multi-functional by allowing it to serve both as a solvent for the cosolvent and as an antisolvent for the bioactive compound simultaneously. This universal application of SCCO2 simplifies the overall process design while maintaining precise particle formation control
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 BIOSAS process achieves high dispersion yields and stability of bioactive compounds in lipid matrices, enhancing their bioavailability and efficacy, with successful applications in dispersing pure compounds and complex mixtures like quercetin, rosemary phytochemicals, and licorice extracts, offering a more effective formulation technique compared to traditional methods.
Implementation Method 1
The application of supercritical fluids enables the control of the size and morphology of the bioactive particles. Moreover, SCCO2 processes can be carried out at low temperatures in absence of oxygen.
Implementation Method 2
In the Supercritical Anti-solvent (SAS) approach, the biomolecules have low solubility in SCCO2 but high solubility in a liquid solvent which in turn is highly soluble in SCCO2. A solution containing the biomolecules is sprayed through a nozzle into a chamber containing SCCO2 that acts as an antisolvent. The rapid contact between the two phases generates supersaturation of the droplets, and results in fast nucleation and growth of solid particles.
Data Source
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Figure 3a~3b
Figure 3c~3d
AI summary
This invention pertains to the chemical field, in particular, to the field of pharmaceutical or galenic formulation, more particularly, it relates to methods to formulate homogenous dispersions and emulsions of bioactive substances in oily matrixes.