Oleo-Polymeric Encapsulation for Hydrophilic Drug Delivery
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Solution Overview
Problem
Current methods for encapsulating pharmaceutical actives, such as the emulsion technique, face challenges with the use of toxic organic solvents, harsh conditions, and reduced encapsulation efficiency, especially for hydrophilic drugs, limiting their versatility in producing nano/micro formulations.
Innovation Solution
A method involving the dispersion of a hydrophilic polymeric matrix former in a water phase and a hydrophobic polymeric matrix former in an oil phase, forming a finely dispersed emulsion with vegetable-based edible oil, followed by lyophilization and comminution to produce nano/micro pharmaceutical formulations without toxic solvents, using a direct dispersion emulsification technique.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional emulsion technique is used for encapsulation, then encapsulation efficiency is improved, but toxic organic solvents and harsh conditions are required
Solution Approach 1:
The patent changes the chemical composition parameters by replacing toxic organic solvents with water and food-grade oils as the continuous phase. The emulsion is formed using these safe alternatives while maintaining the encapsulation function through controlled mixing and stabilization with food-grade surfactants, thus eliminating harmful substances while preserving encapsulation efficiency.
Solution Approach 2:
The patent employs food-grade surfactants and emulsifiers that are safe, biodegradable, and can be easily removed or degraded in the body. These temporary stabilizing agents fulfill their encapsulation role during formulation and then dissipate harmlessly, replacing the need for persistent toxic organic solvents in the final product.
2Reliability
If conventional emulsion technique is used, then encapsulation is achieved, but versatility for hydrophilic drugs is reduced
Solution Approach 1:
The patent creates a universal encapsulation system using water and food-grade oils as the continuous phase that can accommodate both hydrophilic and hydrophobic drugs. The dual-phase emulsion structure allows hydrophilic drugs to be incorporated into the aqueous phase while hydrophobic drugs are incorporated into the oil phase, making the system versatile for different drug types without requiring separate formulations.
Solution Approach 2:
The patent applies local quality by creating distinct micro-environments within the emulsion: an aqueous continuous phase for hydrophilic drugs and an oil continuous phase for hydrophobic drugs. Each phase provides the appropriate chemical environment for its target drug type, allowing the single emulsion system to simultaneously support both hydrophilic and hydrophobic pharmaceutical actives with appropriate local properties.
3Reliability
If conventional emulsion technique is used, then encapsulation is achieved, but harsh temperature and pressure conditions are required
Solution Approach 1:
The patent uses food-grade surfactants and emulsifiers that function effectively at mild temperatures and pressures. These temporary stabilizing agents enable emulsion formation under gentle conditions and then dissipate harmlessly, replacing the need for persistent harsh temperature and pressure conditions in the final formulation.
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
This method achieves high encapsulation efficiency, controlled release, and stability for both hydrophilic and hydrophobic drugs, with flexible formulation options and improved bioavailability, suitable for oral and transmucosal administration.
Implementation Method 1
forming an emulsion from the oil phase and the water phase
Implementation Method 2
dispersing a hydrophilic polymeric matrix former into a water phase and a hydrophobic polymeric matrix former into an oil phase
Implementation Method 3
lyophilizing the emulsion to form a solid lyophilisate, wherein lyophilizing the emulsion includes first snap freezing the emulsion by cooling the emulsion to a freezing temperature
Implementation Method 4
lyophilizing the emulsion to form a solid lyophilisate
Implementation Method 5
comminuting the solid lyophilisate to provide particles or a powder of the encapsulated pharmaceutical active
Data Source
Figure 1
Figure 2(a)~3(c)
AI summary
A method of encapsulating a pharmaceutical active includes dispersing a matrix former into at least one of a water phase and an oil phase, with the pharmaceutical active being present in at least one of the oil phase and the water phase and with the oil phase comprising a vegetable-based edible oil. An emulsion is formed from the oil phase and the water phase and the emulsion is lyophilised to form a solid lyophilisate.