Enhanced Ocular Delivery of Cell Permeant Therapeutics for Retinal Edema Treatment

Publication ID: 24-11857609_0006_PTD
Published: October 28, 2025
Category:Direct Improvements & Enhancements

Legal Citation

pr1or.art Inc., “Enhanced Ocular Delivery of Cell Permeant Therapeutics for Retinal Edema Treatment,” Published Technical Disclosure No. 24-11857609_0006_PTD, Published October 28, 2025, available at https://archive.pr1or.art/24-11857609_0006_PTD
This technical disclosure describes improvements that would be readily apparent to a Person Having Ordinary Skill In The Art (PHOSITA) when considered in combination with the foundational architecture disclosed in U.S. Patent No. 11,857,609.

Summary of the Inventive Concept

The present disclosure relates to novel compositions and methods for the enhanced ocular delivery of cell permeant therapeutics for the treatment of retinal edema, overcoming limitations of existing treatments by providing sustained release formulations, targeted delivery, and improved bioavailability.

Background and Problem Solved

Retinal edema is a prevalent condition characterized by fluid accumulation in the retina, often leading to vision loss. Current treatments, such as those described in the original patent, have limitations, including short duration of action, inadequate penetration, and systemic toxicity. The present inventive concept addresses these limitations by introducing novel formulations, delivery methods, and bioavailability enhancers.

Detailed Description of the Inventive Concept

The new inventive concept comprises a system for treating retinal edema, featuring a therapeutic composition containing a cell-penetrating peptide conjugate administered to the eye in a sustained release formulation. This allows for prolonged treatment duration, reducing the need for frequent administrations. Additionally, the conjugate may be combined with a permeation enhancer to increase transport across the blood-retina barrier, further enhancing bioavailability. The inventive concept also encompasses methods for reducing inflammation in the retina by administering a caspase-9 inhibitor conjugated to a cell-penetrating peptide, and compositions for treating diabetic macular edema using an XIAP-MTS conjugate.

Novelty and Inventive Step

The new claims introduce novel and non-obvious improvements over the original patent, including sustained release formulations, targeted delivery, and bioavailability enhancers. These innovations provide a significant advancement in the treatment of retinal edema, overcoming the limitations of existing therapies.

Alternative Embodiments and Variations

Alternative embodiments of the inventive concept may include varying the type and concentration of cell-penetrating peptides, conjugate structures, and delivery formulations. Additionally, the inventive concept could be adapted for use in treating other ocular conditions, such as age-related macular degeneration or uveitis.

Potential Commercial Applications and Market

The enhanced ocular delivery system for retinal edema treatment has significant commercial potential in the ophthalmology market, with potential applications in treating various retinal diseases and disorders. The targeted delivery and improved bioavailability of the therapeutic composition may lead to improved treatment outcomes, reduced healthcare costs, and enhanced patient quality of life.

CPC Classifications

SectionClassGroup
A A61 A61K38/55
A A61 A61K9/0048
A A61 A61K47/64
A A61 A61P27/02

Field of Art

Pharmaceutical biotechnology, specifically ocular drug delivery systems, focusing on therapeutic peptide conjugates for retinal disease treatment

Person of Ordinary Skill (PHOSITA) Profile

A skilled practitioner with advanced degrees in pharmaceutical sciences, biochemistry, or biomedical engineering, having expertise in peptide chemistry, drug delivery mechanisms, and ocular pharmacology

Obviousness Rationale

A person of ordinary skill would recognize that the published technical disclosure represents predictable variations on the source patent's core technology of cell-penetrating peptide conjugates for retinal treatment. The PTD's extensions involve standard pharmaceutical formulation techniques like sustained release, permeation enhancement, and conjugate modifications that would be readily apparent to a skilled practitioner in the field of ocular therapeutics.

Obvious Combinations & Variations

Source Patent Element
Cell-penetrating peptide conjugate for retinal vein occlusion treatment using Penetratinl-XBIR3
PTD Variation
Sustained release formulation of cell-penetrating peptide conjugates
Obviousness Reasoning
Sustained release is a known pharmaceutical technique for improving drug delivery, and a PHOSITA would find it obvious to apply standard controlled-release technologies to the existing peptide conjugate to extend treatment duration
Source Patent Element
Eye drop composition containing XIAP-BIR3 conjugate
PTD Variation
Adding permeation enhancers to improve blood-retina barrier transport
Obviousness Reasoning
Enhancing drug transport across biological barriers is a well-established pharmaceutical strategy, and a PHOSITA would recognize the predictable benefit of improving conjugate bioavailability
Source Patent Element
Cell-penetrating peptide conjugates using Penetratinl
PTD Variation
Expanding conjugate design to include alternative cell-penetrating peptides like membrane translocating sequences (MTS)
Obviousness Reasoning
Selection of alternative cell-penetrating peptides represents an obvious design choice within a finite set of known peptide sequences with similar transport properties
Source Patent Element
Treatment of retinal vein occlusion using peptide conjugates
PTD Variation
Diagnostic monitoring of treatment efficacy through caspase-9 signaling activity measurement
Obviousness Reasoning
Developing companion diagnostic techniques to monitor therapeutic response is a standard approach in personalized medicine and would be an obvious extension to the existing treatment method
35 U.S.C. § 103 Summary: Based on the teachings of US Patent 11857609, the present published technical disclosure demonstrates that the claimed variations in ocular drug delivery systems involving cell-penetrating peptide conjugates would have been obvious to a person having ordinary skill in the art at the time of invention. The disclosed modifications represent predictable applications of known pharmaceutical formulation techniques to the existing therapeutic approach, thereby rendering potential patent claims obvious and anticipatable as prior art.

Original Patent Information

Patent NumberUS 11,857,609
TitleOcular delivery of cell permeant therapeutics for the treatment of retinal edema
Assignee(s)The Trustees of Columbia University in the City of New York