Negatively Charged PLGA Particles for API Surface Attachment
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Solution Overview
Problem
Conventional methods for producing carboxylated PLGA particles result in biocompatibility issues and insufficient surface carboxyl groups for attaching APIs, limiting their therapeutic efficacy.
Innovation Solution
A method involving emulsion or precipitation processes in an aqueous solution with pH promotion and use of pharmaceutically acceptable polymers with controlled molecular weight and multiple negatively charged terminal groups to enhance surface charges on microparticles and nanoparticles.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional methods are used to produce carboxylated PLGA particles, then the particles can be manufactured, but they exhibit poor biocompatibility and insufficient surface carboxyl groups
Solution Approach 1:
The patent changes the pH parameter of the aqueous solution to promote ionization of the polymer, creating negative surface charges on the particles. This parameter change improves biocompatibility while maintaining manufacturability through controlled ionization processes
Solution Approach 2:
The patent uses composite polymer systems with multiple negatively charged terminal groups combined with pharmaceutically acceptable polymers. This composite approach enhances surface charge density and biocompatibility while ensuring safety for human and animal use
2Quantity of substance
If conventional PLGA particles are used, then they can be produced, but they do not contain sufficient carboxyl groups for attaching APIs
Solution Approach 1:
The patent concentrates negative charges and carboxyl groups specifically at the surface and terminal regions of the polymer chains. This local concentration of functional groups provides sufficient attachment sites for APIs without requiring complex polymer structures throughout the entire molecule
Solution Approach 2:
The patent incorporates multiple negatively charged terminal groups into the polymer structure during synthesis, preparing the particles in advance with sufficient carboxyl groups for API attachment. This preliminary functionalization eliminates the need for additional complex modification steps
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 method produces PLGA particles with increased negative surface charges, improving biocompatibility and facilitating API attachment, suitable for treating inflammatory diseases.
Implementation Method 1
said emulsion process or said precipitation process is carried out in an aqueous solution having a pH that promotes ionization of said pharmaceutically acceptable polymer
Implementation Method 2
emulsifying the polymer solution in a solution of a second solvent to form an emulsion, wherein the first solvent is not miscible or partially miscible with the second solvent
Implementation Method 3
combining (e.g., adding) the polymer solution to the solution of the second solvent while mixing, thus forming said microparticles or nanoparticles having negative surface charges
Data Source
AI summary
This invention provides methods for producing a polymer particle which contains unusually high negative charges on the surface of the particle. Preferably, the polymer is pharmaceutically acceptable. The negative charges can be conferred by chemical groups such as carboxyl, sulfonate, nitrate, fluorate, chloride, iodide, persulfate, and many others, with carboxyl group being preferred. The invention also provides polymer particle produced by the methods of the invention.