Triblock Copolymer Emulsion for Controlled API Release
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Solution Overview
Problem
Current bioresorbable polymers for controlled release of pharmaceutical ingredients face challenges such as laborious incorporation processes that can inactivate active ingredients, high burst releases due to low molecular weight polymers, and short release times for hydrophilic APIs, especially when used in liquid formulations.
Innovation Solution
A stable water-in-oil emulsion composed of a bioresorbable triblock copolymer, a bioresorbable surfactant, and water, where the triblock copolymer is fluid at ambient conditions, allowing for the encapsulation and controlled release of hydrophilic active pharmaceutical ingredients, reducing burst releases and improving injectability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If laborious incorporation processes are used to incorporate active ingredient into polymer interior, then controlled release is achieved, but active ingredient may be inactivated during the process
Solution Approach 1:
The patent uses an emulsion system as an intermediary medium to incorporate hydrophilic active ingredients into the polymer matrix. The emulsion comprises water, surfactant, and polymer in a specific configuration that allows gentle incorporation of the active ingredient without requiring harsh solvents or high temperatures, thereby maintaining ingredient efficacy while achieving controlled release
Solution Approach 2:
The patent changes the physical state parameters by formulating the polymer as a liquid at ambient conditions rather than a solid, and controlling the emulsion droplet size and distribution. This allows the active ingredient to be incorporated in a gentler, more uniform manner that prevents inactivation while enabling controlled release through the emulsion structure
2Ease of operation
If low molecular weight polymers are added to make composition injectable, then injectability is improved, but burst release increases and fast release of polymer occurs
Solution Approach 1:
The patent changes the molecular weight parameter of the polymer to a specific range (1,000-10,000 Da) that balances injectability with sustained release performance. This optimized molecular weight range allows the polymer to remain sufficiently fluid for injection while maintaining structural integrity to prevent burst release and fast polymer degradation
Solution Approach 2:
The patent creates a composite emulsion system combining polymer, surfactant, and water in specific proportions. This composite structure provides the rheological properties needed for injectability while the emulsion architecture and surfactant stabilization prevent premature polymer release and burst effects
3Ease of manufacture
If water is added and mixed through liquid polymer to incorporate hydrophilic API, then API incorporation is achieved, but burst release and short release times occur
Solution Approach 1:
The patent segments the formulation into distinct emulsion droplets with specific internal and external phases. Hydrophilic active ingredients are incorporated within the aqueous phase of the emulsion droplets, which are then dispersed in the polymer matrix. This segmentation creates a structured release pathway that prevents burst release while maintaining ease of manufacturing through simple mixing
Solution Approach 2:
The patent uses surfactant as an intermediary substance that mediates between the hydrophilic active ingredient and the hydrophobic polymer matrix. The surfactant forms a stable emulsion interface that allows gentle incorporation of the API while controlling its release kinetics, preventing both burst release and excessive retention
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 formulation provides a controlled release of active pharmaceutical ingredients with reduced burst effects, improved injectability, and extended release times for hydrophilic APIs, forming a cohesive mass in the body suitable for medical applications.
Implementation Method 1
a water in oil (w/o) emulsion of at least one bioresorbable triblock copolymer, a bioresorbable surfactant and water
Implementation Method 2
0.1-15 wt % of at least one surfactant (B)
Implementation Method 3
slowly release said active pharmaceutical ingredient
Implementation Method 4
bioresorbable triblock copolymer
Data Source
AI summary
A composition including a) 55-98.9 wt % of at least one type of triblock copolymer (A) of formula (1)R—B-A-B—R (1)b) 0.1-15 wt % of at least one surfactant (B) and c) 1-30 wt % of water, wherein A is a hydrophilic block having a number average molecular weight (Mn) of 100-1,000 Da, B is a hydrophobic block made from monomers having at least a monomer B1 and a monomer B2, wherein B1 and B2 have the largest weight contents in the hydrophobic block and B1 has a lower molecular weight than B2, wherein R is an end group which is H or a C1-C30 organic moiety, wherein the composition is fluid in a temperature range of 0° C. to 37° C., wherein the weight % are relative to the sum of a), b) and c), and wherein the sum of components a), b) and c) is at least 80 wt % of the entire composition, preferably at least 90 wt %; to the use of the composition and to pharmaceutical compositions having said composition and an active pharmaceutical ingredient.