Vitamin D Micro-Emulsion for Ocular Retention and Low Irritation

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Solution Overview

Problem

Existing ophthalmic compositions struggle to efficiently deliver lipophilic agents like Vitamin D to the eye, as they cause irritation and have a short retention time due to the eye's aqueous environment and polar nature, making it difficult to achieve therapeutic concentrations.

Innovation Solution

Phospholipid nano-emulsions are used to create a dynamic structure on the eye's surface, allowing Vitamin D to be administered without irritation and maintaining prolonged contact, enhancing delivery and absorption by forming a localized environment where oily molecules can penetrate the corneal epithelium.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If lipophilic agents like Vitamin D are administered to the eye, then therapeutic benefits are achieved, but irritation occurs and retention time is short

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoideye irritation
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

Phospholipid nano-emulsions serve as an intermediary carrier between the lipophilic Vitamin D and the aqueous ocular environment. The phospholipid structure with amphiphilic properties (hydrophilic head and hydrophobic tail) enables the nano-emulsion to solubilize lipophilic agents while maintaining compatibility with the polar eye surface, thereby delivering therapeutic benefits without irritation

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the physical and chemical parameters of Vitamin D by encapsulating it within phospholipid nano-emulsion particles of specific size (100-300 nm). This transformation alters the delivery characteristics, enabling prolonged retention time on the ocular surface and enhanced penetration through the corneal epithelium without causing irritation

Inventive Principle:
Principle #35Parameter changes

2Reliability

If lipophilic agents are administered to the eye, then therapeutic benefits are achieved, but retention time on the ocular surface is short

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidretention time
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The phospholipid nano-emulsion acts as a mediator that prolongs the residence time of lipophilic agents on the ocular surface. The nano-emulsion structure interacts with the tear film and corneal epithelium, maintaining contact for extended periods and enabling sustained delivery of therapeutic agents

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention uses composite phospholipid nano-emulsion structures combining hydrophilic and hydrophobic components. This composite material properties enable the formulation to maintain stability in the aqueous ocular environment while retaining lipophilic agents, thereby extending retention time on the ocular surface

Inventive Principle:
Principle #40Composite materials

3Reliability

If phospholipid nano-emulsions are used to deliver Vitamin D, then prolonged contact and enhanced absorption are achieved, but formulation complexity increases

Engineering Contradiction:
Improvedelivery efficiencyVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The invention segments the delivery system into nano-sized phospholipid emulsion particles (100-300 nm). This segmentation enables the complex formulation to interact more effectively with the ocular surface and corneal epithelium, improving delivery efficiency while the small size allows for simpler administration compared to larger complex systems

Inventive Principle:
Principle #1Segmentation

Data Source

PatentEP3890746B1Vitamin d micro-emulsions and uses thereof
Publication Date: 2026.02.04 CHEMIPAL GLOBAL ENTREPRENEURSHIP LTD
  • EP3890746B1 patent drawingFigure 1
  • EP3890746B1 patent drawingFigure 2
  • EP3890746B1 patent drawingFigure 3

AI summary

Pharmaceutical compositions designed to deliver Vitamin D efficiently to the eyes and methods for using same are described herein. More particularly, ophthalmic pharmaceutical compositions for use in protecting eyes from the harmful effects of light exposure, in maintaining a healthy ocular state, and in treating disorders of the eye are described herein. The composition may also be used as a medical device which, once on the surface of the eye, creates a layer that filters electro-magnetic radiation in different wave lengths. The composition may also be used as a medical device which eases the symptoms and signs of eye-surface conditions.