Hypericin Liquid Formulation for Safer Photodynamic Therapy

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Solution Overview

Problem

Current photodynamic therapy for skin conditions like psoriasis and cutaneous T cell lymphoma using UV-A light is associated with undesirable side effects, including skin tumors and carcinogenic risks due to the mutagenic properties of psoralen and UV exposure.

Innovation Solution

The use of hypericin in a liquid formulation, activated by visible light, which generates singlet oxygen and induces apoptosis in lymphocytic cells, offering a safer alternative with deeper skin penetration and reduced side effects compared to traditional UV-A therapy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If UV-A light and psoralen are used for photodynamic therapy, then treatment efficacy for psoriasis and cutaneous T cell lymphoma is improved, but carcinogenic side effects and skin tumor risk increase

Engineering Contradiction:
Improvetreatment efficacyVSAvoidcarcinogenic side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the wavelength parameter from UV-A (315-400 nm) to visible light (400-700 nm), specifically targeting wavelengths that activate hypericin while avoiding the carcinogenic UV range. This parameter change maintains photodynamic therapy efficacy while eliminating the mutagenic effects associated with UV radiation

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent extracts and eliminates the harmful psoralen component from the treatment system, replacing it with hypericin as the photosensitizing agent. This substitution removes the mutagenic DNA intercalation property while retaining the ability to generate singlet oxygen and induce apoptosis in lymphocytic cells

Inventive Principle:
Principle #2Taking out (Extraction)

2Ease of operation

If ointment formulations are used for hypericin delivery, then application ease is improved, but treatment efficacy and skin penetration are reduced

Engineering Contradiction:
Improveapplication easeVSAvoidtreatment efficacy
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent changes the physical state parameter of the formulation from semi-solid ointment to liquid solution. This parameter change enhances skin penetration capability and treatment efficacy while maintaining ease of topical application, as the liquid formulation can be more effectively distributed and absorbed

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs a composite liquid formulation containing hypericin dissolved in a suitable solvent system, potentially combined with penetration enhancers or adjuvants. This composite approach optimizes both delivery efficiency and therapeutic effect, overcoming the limitations of simple ointment bases

Inventive Principle:
Principle #40Composite materials

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 study demonstrates that hypericin in a liquid formulation, applied topically and activated by visible light, achieves significant reductions in psoriasis and cutaneous T cell lymphoma lesions, with higher efficacy and safety compared to conventional ointment formulations, and is effective in treating inflammatory skin diseases characterized by lymphocytic infiltrates.

Implementation Method 1

hypericin in a liquid formulation, activated by visible light, which generates singlet oxygen and induces apoptosis in lymphocytic cells

Methodology Applied
Scientific EffectPhotodynamic therapy: Photo-oxidation

Implementation Method 2

hypericin... activated by visible light, which generates singlet oxygen

Methodology Applied
Scientific EffectSinglet oxygen generation: Photo-oxidation

Data Source

PatentEP2932973B1Formulations for use in the treatment of skin conditions
Publication Date: 2020.04.01 SOLIGENIX INC

AI summary

The present invention provides a liquid formulation for the treatment of a skin condition associated with leukocyte accumulation in the skin, comprising a therapeutic compound selected to reduce leukocyte accumulation in the skin; and an aqueous solution of an organic solvent, wherein the organic solvent increases skin permeability. The present invention also provides a method of treating a skin condition associated with leukocyte accumulation in the skin, comprising the steps of applying topically a liquid formulation of a photosensitizer to a skin lesion of a patient afflicted with the skin condition; and exposing the skin lesion to a light source.