Polymeric Microparticles for Sustained Anti-Cancer Drug Release

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Solution Overview

Problem

Current drug delivery systems face challenges in targeting anti-cancer drugs to tumor sites and sustaining effective drug concentrations over an extended period, often requiring frequent administration.

Innovation Solution

Nanoparticle-drug conjugates encapsulated in biocompatible polymeric microparticles, where metal-core nanoparticles with carbohydrate and glutathione ligands are encapsulated, allowing for targeted delivery and sustained release of chemotherapeutic agents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If conventional drug delivery systems are used, then drug administration can be performed, but frequent repeat administration is required and effective drug concentration cannot be sustained over extended period

Engineering Contradiction:
Improveduration of drug actionVSAvoidfrequency of administration
Core Design Contradiction:
Duration of action of moving objectVSLoss of time

Solution Approach 1:

The invention employs a multi-layered nested structure where metal-core nanoparticles with carbohydrate ligands are encapsulated within polymeric microparticles. This nested configuration allows the inner nanoparticle to provide targeted delivery while the outer microparticle matrix enables sustained release over extended periods, thereby reducing administration frequency and maintaining effective drug concentrations.

Inventive Principle:
Principle #7Nested doll (Nesting)

Solution Approach 2:

The invention utilizes composite material systems combining metal cores, carbohydrate ligands (such as glucosamine), and biocompatible polymeric matrices. This composite structure integrates the targeting capability of metal nanoparticles with the sustained release properties of polymeric microparticles, achieving both prolonged duration of action and reduced administration frequency.

Inventive Principle:
Principle #40Composite materials

2Reliability

If anti-cancer drugs are administered systemically, then tumor treatment can be achieved, but drug targeting to specific tumor site is insufficient leading to reduced therapeutic efficacy

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoiddrug targeting capability
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The invention applies local quality by functionalizing the nanoparticle surface with specific carbohydrate ligands (such as glucosamine) that exhibit selective affinity for tumor tissue. This localized functionalization enables the drug delivery system to preferentially accumulate at the tumor site through receptor-mediated endocytosis, thereby enhancing therapeutic efficacy while reducing systemic exposure.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The carbohydrate ligands on the nanoparticle surface act as intermediaries that mediate the interaction between the drug delivery system and tumor cells. These ligands facilitate selective binding and uptake by tumor cells through carbohydrate-receptor interactions, enabling targeted delivery without requiring complex external guidance systems.

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentEP3217958B1Sustained release encapsulated nanoparticles
Publication Date: 2020.02.26 MIDATECH LTD
  • EP3217958B1 patent drawingFigure 1
  • EP3217958B1 patent drawingFigure 2
  • EP3217958B1 patent drawingFigure 3

AI summary

The present invention provides a microparticle comprising at least one biocompatible polymer, the microparticle encapsulating at least one nanoparticle, the nanoparticle comprising: (i) a core comprising a metal and/or a semiconductor; and (ii) a corona comprising a plurality of ligands covalently linked to the core, wherein said ligands comprise at least one carbohydrate and/or glutathione. The nanoparticle may additionally comprise a biologically active agent or detectable label covalently linked or non-covalently bound to said corona and/or said core. Also disclosed are pharmaceutical compositions comprising the microparticles, processes for their production and uses of the microparticles in methods of therapy.