Soluplus Micelle Encapsulation for Poorly Soluble Drug Delivery

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Solution Overview

Problem

Glutaminase inhibitors with flexible structures have low solubility in solvents, leading to poor bioavailability and stability issues, including rapid metabolism and precipitation, which hampers their effectiveness as anti-cancer drugs.

Innovation Solution

A poorly soluble chain-like drug-entrapped polymeric micelle is developed using Soluplus as a carrier, which increases solubility and bioavailability by entrapping the drug within hydrophobic cores, enhancing tumor treatment effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If chain-like selenium-containing glutaminase inhibitors are used as anti-cancer drugs, then they show targeted inhibitory effect on tumor cells, but they have low solubility in solvents including water

Engineering Contradiction:

Improveanti-tumor effectVSAvoidsolubility

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

The patent uses Soluplus as an intermediary carrier to solve the solubility problem. Soluplus is a polymeric carrier that forms micelles in aqueous solution, with hydrophobic cores that can encapsulate the poorly soluble chain-like selenium-containing glutaminase inhibitors. This mediator enables the drug to be delivered in water-based formulations without compromising its anti-tumor efficacy.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite drug delivery system combining Soluplus polymer carrier with chain-like selenium-containing glutaminase inhibitors. The composite micelle structure integrates the hydrophilic exterior of Soluplus for water solubility with the hydrophobic core for drug encapsulation, resolving the solubility-activity contradiction.

Inventive Principle:

Principle #40Composite materials

2Ease of operation

If chain-like selenium-containing glutaminase inhibitors are administered orally, then they can be delivered systemically, but they are metabolized quickly in blood and liver microsomes resulting in reduced bioavailability

Engineering Contradiction:

Improveadministration routeVSAvoidbioavailability

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent changes the physical and chemical parameters of the drug delivery system by encapsulating the drug in polymeric micelles. This alters the drug's apparent molecular size, hydrophobicity, and recognition patterns by metabolic enzymes, thereby reducing metabolism in blood and liver microsomes and improving bioavailability while maintaining oral or injectable administration routes.

Inventive Principle:

Principle #35Parameter changes

3Speed

If chain-like selenium-containing glutaminase inhibitors are used in injection administration, then they can achieve direct delivery, but they show low bioavailability and poor stability with precipitation and degradation

Engineering Contradiction:

Improvedelivery speedVSAvoidstability

Core Design Contradiction:

SpeedVSReliability

Solution Approach 1:

The patent applies beforehand cushioning by pre-encapsulating the chain-like selenium-containing glutaminase inhibitors in Soluplus micelles before administration. This protective encapsulation prevents precipitation and degradation during storage and injection, cushioning the drug from adverse environmental conditions and maintaining its stability throughout the delivery process.

Inventive Principle:

Principle #11Beforehand cushioning (Prior cushioning)

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 polymeric micelle improves the solubility and bioavailability of selenium-containing glutaminase inhibitors, stabilizes them in blood and liver microsomes, and enhances their anti-tumor effects with prolonged circulation and reduced metabolism, leading to improved therapeutic outcomes.

Implementation Method 1

the poorly soluble chain-like drug is entrapped by hydrophobic cores of polyvinylcaprolactam and polyvinyl acetate of the carrier

Methodology Applied

Scientific EffectHydrophobic interaction: Hydrophobe

Implementation Method 2

polyvinylcaprolactam-polyvinyl acetate-polyethylene glycol (trade name: Soluplus) is used as a coating carrier

Methodology Applied

Scientific EffectMicelle formation: Microemulsion

Data Source

PatentUS20240173255A1Polymeric Micelle Coated with Chain-Like Poorly Soluble Drug, Preparation Method and Application

Publication Date: 2024.05.30 HANGZHOU HANJING BIOTECHNOLOGY CO LTD

AI summary

Provided are a poorly soluble chain-like drug-entrapped polymeric micelle, and a preparation method and use thereof. In the polymeric micelle, a chain-like selenium-containing glutaminase inhibitor is entrapped by a carrier of polyvinylcaprolactam-polyvinyl acetate-polyethylene glycol. The prepared poorly soluble chain-like drug-entrapped polymeric micelle could effectively increase a solubility of the chain-like selenium-containing glutaminase inhibitor, and could also improve stability of the selenium-containing glutaminase inhibitor in blood and liver microsomes, thereby enhancing a bioavailability of the chain-like selenium-containing glutaminase inhibitor.