Zwitterionic PLGA Microparticles for Alveolar Delivery

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Solution Overview

Problem

Current drug delivery systems face challenges in efficiently reaching the alveoli in the lungs without being removed by the mucin mucus layer in the airways.

Innovation Solution

Development of amphoteric surface-modified microparticles made of poly(lactic-co-glycolic acid) (PLGA) with an average diameter of 1 to 4 micrometers, modified with sulfobetaine methacrylate (SBMA), 2-methacryloyloxyethyl phosphorylcholine (MPC), or carboxybetaine methacrylate (CBMA), which form a water film to prevent mucin adsorption and enhance delivery to the alveoli.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If conventional drug delivery systems are used, then the delivery process is simple, but the delivery efficiency to alveoli is low due to removal by mucin mucus layer

Engineering Contradiction:

Improvedelivery efficiencyVSAvoidsurface modification complexity

Core Design Contradiction:

ProductivityVSDevice complexity

Solution Approach 1:

The patent modifies the surface charge parameter of PLGA microparticles from neutral to amphoteric by incorporating zwitterionic monomers (SBMA, MPC, or CBMA) during polymerization. This parameter change enables the particles to resist mucin mucus layer removal while maintaining delivery efficiency to alveoli, resolving the contradiction between simple delivery and high efficiency.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates composite PLGA microparticles by combining traditional PLGA matrix with zwitterionic monomers (SBMA, MPC, or CBMA) during polymerization. This composite structure provides both the mechanical integrity of PLGA and the mucin-resisting amphoteric surface properties, achieving high delivery efficiency without excessive complexity.

Inventive Principle:

Principle #40Composite materials

2Productivity

If amphoteric surface modification is applied, then delivery efficiency to alveoli is improved, but manufacturing precision requirements increase

Engineering Contradiction:

Improvedelivery efficiencyVSAvoidsurface modification precision

Core Design Contradiction:

ProductivityVSManufacturing precision

Solution Approach 1:

The patent controls surface modification precision by adjusting the polymerization parameters (monomer ratio, initiator concentration, reaction time) to achieve optimal amphoteric surface density. This parameter optimization ensures consistent surface properties while maintaining manufacturing feasibility, resolving the contradiction between high delivery efficiency and precision requirements.

Inventive Principle:

Principle #35Parameter changes

3Reliability

If zwitterionic monomers are used for surface modification, then mucin mucus layer removal is prevented, but production cost increases

Engineering Contradiction:

Improveresistance to mucin removalVSAvoidproduction cost

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent optimizes the ratio of zwitterionic monomers (SBMA, MPC, or CBMA) to conventional monomers in the polymerization reaction to achieve sufficient amphoteric surface density at lower costs. This parameter optimization balances resistance to mucin removal with production cost effectiveness.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent uses composite PLGA particles with incorporated zwitterionic monomers that provide mucin resistance through their amphoteric properties. The composite structure leverages the cost-effectiveness of PLGA while adding functional zwitterionic components, achieving reliable mucin resistance without excessive production cost increase.

Inventive Principle:

Principle #40Composite materials

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 amphoteric surface-modified microparticles achieve high delivery efficiency to the alveoli, avoiding removal by the mucin mucus layer, and can be loaded with both hydrophobic and hydrophilic drugs for targeted lung disease treatment.

Implementation Method 1

modified with sulfobetaine methacrylate (SBMA), 2-methacryloyloxyethyl phosphorylcholine (MPC), or carboxybetaine methacrylate (CBMA), which form a water film to prevent mucin adsorption and enhance delivery to the alveoli

Methodology Applied

Scientific EffectWater film formation:

Implementation Method 2

The microparticles of the present invention for achieving the aforementioned objectives may have a surface of poly(lactic-co-glycolic acid) (PLGA) modified with amphoteric ions

Methodology Applied

Scientific EffectZwitterionic modification:

Data Source

PatentUS20250152514A1Microparticles having zwitterionically modified surface, drug delivery system comprising the same, and a process for preparing the same

Publication Date: 2025.05.15 UI (UNIVERSITY IND FOUNDATION) YONSEI UNIVERSITY

AI summary

The present invention relates to microparticles, drug delivery systems, and methods of preparing the same, wherein the surface of poly(lactic-co-glycolic acid) (PLGA) is modified with amphoteric ions, Due to the water film formed by the modification of the amphoteric ions, the delivery of microparticles (or drug delivery systems) to the lungs through nebulizing can reach the alveoli with high delivery efficiency without being removed by the mucin mucus layer present in the airway.