Liposomal Sedative Composition With Remote Loading for Sustained Release

Solution Overview

Problem

Existing sustained-release formulations for sedative drugs like dexmedetomidine face challenges in achieving high drug to lipid ratios and encapsulation efficiency, leading to frequent dosing and potential side effects.

Innovation Solution

A sustained-release pharmaceutical composition comprising liposomes with a bilayer membrane, a trapping agent, and a sedative drug, where the drug to lipid molar ratio is equal to or higher than 0.02, utilizing remote loading techniques to enhance encapsulation efficiency.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If passive drug loading into liposomes is used, then the formulation process is simple, but the drug to lipid ratio and encapsulation efficiency are low

Engineering Contradiction:

Improveformulation process simplicityVSAvoiddrug to lipid ratio

Core Design Contradiction:

Ease of manufactureVSQuantity of substance

Solution Approach 1:

The patent applies preliminary action by pre-forming liposomes with trapping agents (such as polyethylene glycol or cholesterol) before drug loading. This preliminary preparation creates a structured lipid bilayer that facilitates subsequent remote loading of the sedative drug, thereby achieving high drug to lipid ratios without compromising formulation simplicity

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The patent uses trapping agents as intermediaries within the liposome structure. These agents (polyethylene glycol or cholesterol) are incorporated into the lipid bilayer during liposome formation and serve as mediators that enhance the encapsulation efficiency and drug to lipid ratio during the remote loading process

Inventive Principle:

Principle #24Intermediary (Mediator)

2Ease of manufacture

If passive drug loading into liposomes is used, then the formulation process is simple, but the encapsulation efficiency is low

Engineering Contradiction:

Improveformulation process simplicityVSAvoidencapsulation efficiency

Core Design Contradiction:

Ease of manufactureVSManufacturing precision

Solution Approach 1:

The patent applies preliminary action by pre-forming liposomes with trapping agents (such as polyethylene glycol or cholesterol) before drug loading. This preliminary preparation creates a structured lipid bilayer that facilitates subsequent remote loading of the sedative drug, thereby achieving high drug to lipid ratios without compromising formulation simplicity

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The patent uses trapping agents as intermediaries within the liposome structure. These agents (polyethylene glycol or cholesterol) are incorporated into the lipid bilayer during liposome formation and serve as mediators that enhance the encapsulation efficiency and drug to lipid ratio during the remote loading process

Inventive Principle:

Principle #24Intermediary (Mediator)

3Speed

If short-acting sedative formulations are used, then the drug acts quickly, but the frequency of administration must be increased

Engineering Contradiction:

Improveonset of actionVSAvoiddosage frequency

Core Design Contradiction:

SpeedVSLoss of time

Solution Approach 1:

The patent applies periodic action by designing a sustained-release liposomal formulation that releases the sedative drug in controlled periodic intervals. The liposome structure maintains therapeutic drug levels over an extended period (at least 24 hours), converting the need for frequent administration into a once-daily or less frequent dosing regimen while preserving the therapeutic effectiveness

Inventive Principle:

Principle #19Periodic action

4Reliability

If high dosage of sedative drug is administered, then the therapeutic effect is enhanced, but the side effects increase

Engineering Contradiction:

Improvetherapeutic effectVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent uses liposomes as flexible shell structures to encapsulate the sedative drug. This lipid bilayer membrane provides a controlled release mechanism that maintains therapeutic drug levels while avoiding peak concentrations that cause side effects. The liposomal delivery system achieves reliable therapeutic effects at lower overall dosages by ensuring sustained bioavailability

Inventive Principle:

Principle #30Flexible shells and thin films

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 composition achieves prolonged drug release, reducing dosing frequency and enhancing therapeutic efficacy while minimizing side effects, thereby improving patient compliance and treatment outcomes.

Implementation Method 1

creating a transmembrane pH- or ion-gradient during liposome formation and then the drug is loaded by the driving force generated from the gradients after liposome formation

Methodology Applied

Scientific EffectConcentration gradient: Diffusion

Data Source

PatentUS12629354B2Sustained-release pharmaceutical compositions comprising of a sedative drug and uses thereof

Publication Date: 2026.05.19 TAIWAN LIPOSOME CO LTD

AI summary

The present invention relates to a pharmaceutical composition comprising at least one liposome, a trapping agent and a sedative drug with a high drug to lipid ratio and a high encapsulation efficiency. Also provided are the methods to sedate or treat pain in a subject in need thereof by administering the pharmaceutical composition disclosed herein.