Biodegradable Polymeric Particles for Urinary Tract Intracellular Delivery
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Solution Overview
Problem
Urinary tract infections (UTIs), particularly in vulnerable populations, are challenging due to recurrent nature, inadequate treatment by standard oral antibiotics, and resistance issues, including biofilm formation and intracellular bacterial reservoirs, leading to high recurrence rates and complications.
Innovation Solution
A composition of biodegradable and hydrolysable polymer particles, 1-30 μm in size, dispersing medicaments for intracellular delivery, specifically designed for urinary tract treatment, using an electrohydrodynamic device to produce particles that penetrate cells and disrupt biofilms effectively.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If standard oral antibiotic therapy is used, then treatment can be administered systemically, but the drugs are poorly absorbed, require prolonged exposure, and high dosages lead to side effects
Solution Approach 1:
The patent uses polymeric particles as an intermediary carrier system. These particles are administered orally and serve as a vehicle to deliver antibiotics to the urinary tract, overcoming the poor absorption issue. The particles protect the drug from degradation in the GI tract and enable targeted delivery, improving absorption efficiency while maintaining ease of oral administration.
Solution Approach 2:
The patent changes the physical form of the antibiotic from conventional oral tablets to polymeric particles with specific size parameters (1-30 μm). This parameter change improves absorption characteristics and enables the drug to reach the urinary tract more effectively, reducing the required dosage and eliminating side effects associated with high dosages.
2Adaptability or versatility
If cell-permeant antibiotics are used to access intracellular reservoirs, then intracellular delivery is achieved, but the antibiotics do not accumulate to high enough levels within cells
Solution Approach 1:
The polymeric particles act as an intermediary delivery system that facilitates intracellular access. The particles are taken up by cells through endocytosis and then fuse with intracellular membranes, releasing the antibiotic inside the cell. This intermediary mechanism enables both intracellular access and high intracellular concentration accumulation, solving the limitation of cell-permeant antibiotics.
Solution Approach 2:
The patent employs a nested structure where the antibiotic is embedded within the polymeric particle, which itself is taken up by the cell. This nested arrangement (cell → particle → drug) enables the drug to reach intracellular reservoirs and accumulate at high levels, overcoming the barrier of cell membrane permeability while maintaining high intracellular concentration.
3Device complexity
If free diffusion is used for drug delivery, then simple delivery is achieved, but delivery efficiency is markedly inefficient compared with directed delivery
Solution Approach 1:
The polymeric particles serve as an intermediary that enables directed delivery while maintaining relative simplicity. The particles are designed to be taken up by cells through endocytosis and then fuse with intracellular membranes, providing a simple yet efficient delivery mechanism that outperforms free diffusion in terms of delivery efficiency and intracellular concentration accumulation.
4Reliability
If antibiotics are used to treat biofilm infections, then bacterial killing is attempted, but biofilms are naturally resistant due to physical barrier to drug diffusion
Solution Approach 1:
The polymeric particles act as an intermediary that penetrates the biofilm barrier. The particles are taken up by cells within the biofilm and fuse with intracellular membranes, delivering the antibiotic directly to the bacterial cells inside the biofilm. This mechanism overcomes the physical barrier to drug diffusion that protects biofilm-forming bacteria, improving antibacterial efficacy while addressing biofilm resistance.
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 particles achieve robust and efficient intracellular delivery of medicaments, significantly reducing bacterial populations, including in biofilms, with improved efficacy compared to free diffusion methods, and demonstrate low cytotoxicity, addressing the limitations of traditional UTI treatments.
Implementation Method 1
using an electrohydrodynamic device to produce particles
Implementation Method 2
biodegradable and hydrolysable polymer
Data Source
AI summary
Described herein is a composition comprising a particle comprising a biodegradable and hydrolysable polymer, wherein a medicament for the treatment of a disease of the urinary tract is dispersed in the polymer, wherein the particle has a dimension of from 1 μm to 30 μm. Also described herein is a composition for the treatment of a disease, the composition comprising a particle comprising a biodegradable and hydrolysable polymer, wherein a medicament is dispersed in the polymer, wherein the particle has a dimension of from 1 μm to 30 μm, wherein the composition is for use in a method for treating the disease and the method involves the intracellular delivery of the particle or the medicament from the particle. Also described herein is a composition comprising a particle comprising a biodegradable and hydrolysable polymer, wherein a medicament is dispersed in the polymer, wherein the particle has a dimension of from 1 μm to 30 μm, wherein the composition is for use in a method for treating bacteria and optionally the method involves the intracellular delivery of the particle or the medicament from the particle.