Liposomal Formulation Sustained Release Ocular Drug Delivery

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Conventional treatments for ocular hypertension and glaucoma, such as topical eye drops and surgery, face challenges including patient compliance issues and inefficient drug delivery, leading to suboptimal control of intraocular pressure and systemic side effects.

Innovation Solution

A stable liposomal formulation containing phosphatidylcholine liposomes encapsulating prostaglandin F2α, specifically latanoprost, is developed for subconjunctival injection, allowing for slow and sustained release of the drug, reducing the frequency of administration and enhancing drug delivery directly to the eye.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If topical eye drops are used to deliver IOP-reducing drugs, then the drug can be administered easily and repeatedly, but patient compliance deteriorates and drug penetration efficiency worsens

Engineering Contradiction:

Improveease of administrationVSAvoidpatient compliance

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The drug is pre-encapsulated in liposomes with sustained-release properties before administration. This preliminary encapsulation action enables the drug to be delivered in a form that maintains therapeutic levels over extended periods (months), eliminating the need for frequent re-administration and ensuring consistent patient compliance without requiring daily drops.

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The invention changes the physical and chemical parameters of drug delivery by transitioning from free drug in aqueous solution to drug encapsulated in lipid bilayers. This parameter change enables controlled release kinetics, improving both ease of administration and reliability of therapeutic effect maintenance.

Inventive Principle:

Principle #35Parameter changes

2Quantity of substance

If topical eye drops are used to deliver IOP-reducing drugs, then the drug can reach the cornea, but drug penetration efficiency deteriorates and systemic absorption increases

Engineering Contradiction:

Improvedrug delivery efficiencyVSAvoidsystemic side effects

Core Design Contradiction:

Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

Liposomes serve as intermediary carriers between the administered drug and the ocular tissues. The lipid bilayer structure of liposomes facilitates targeted delivery to the cornea and aqueous humor while the encapsulation prevents premature release and systemic absorption, thereby improving delivery efficiency and reducing harmful systemic effects.

Inventive Principle:

Principle #24Intermediary (Mediator)

3Reliability

If subconjunctival injection is used to deliver IOP-reducing drugs, then patient compliance improves and corneal penetration efficiency improves, but formulation stability requirements worsen

Engineering Contradiction:

Improvepatient complianceVSAvoidformulation stability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The invention uses composite liposomal structures combining phospholipid bilayers with encapsulated prostaglandin analogs. This composite material approach provides both the sustained-release functionality needed for monthly injection intervals and the structural stability required to maintain formulation integrity during storage and after injection.

Inventive Principle:

Principle #40Composite materials

4Reliability

If repeated topical eye drop administration is used to maintain therapeutic drug levels, then therapeutic efficacy can be maintained, but patient compliance deteriorates and treatment complexity increases

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidtreatment simplicity

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The liposomal formulation enables periodic action with extended intervals between administrations. Instead of requiring daily or multiple-times-daily drops, the sustained-release liposomes maintain therapeutic drug levels for months, transforming the treatment regimen from frequent simple administrations to infrequent administrations with complex preparatory formulation.

Inventive Principle:

Principle #19Periodic action

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 formulation achieves a significant reduction in intraocular pressure for up to 4-6 months with a single injection, minimizing systemic side effects and maintaining therapeutic efficacy without the need for daily applications.

Implementation Method 1

a liposome containing at least one lipid bilayer that includes a phosphatidylcholine

Methodology Applied

Scientific EffectLipid bilayer encapsulation:

Implementation Method 2

prostaglandin F2α encapsulated in the liposome

Methodology Applied

Scientific EffectEncapsulation:

Implementation Method 3

The liposome also allows passive diffusion of prostaglandin F2α from its encapsulated core to its surrounding medium

Methodology Applied

Scientific EffectPassive diffusion: Diffusion

Data Source

PatentUS9956195B2Stable liposomal formulations for ocular drug delivery

Publication Date: 2018.05.01 SINGAPORE HEALTH SERVICES PTE LTD

AI summary

A stable liposomal formulation for ocular delivery. The formulation contains a liposome that includes at least one lipid bilayer containing a phosphatidylcholine, and a prostaglandin F2α encapsulated in the liposome. Also provided is a method for treating an ocular disorder with the formulation.