Peptide Granule Composition for Sustained Intraocular Release
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Solution Overview
Problem
Existing treatments for ocular inflammation, such as corticosteroids, have severe side effects, and there is a need for solid formulations of Phosphorylcholine-tuftsin conjugate that provide a sufficient storage shelf-life and gradual release of the active agent at the application site.
Innovation Solution
A composition of poly(glycolide-co-lactide)-based solid particles containing Phosphorylcholine-tuftsin conjugate with a controlled particle size and ester-end-capped PLGA, which results in improved drug loading efficiency and sustained release profile.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If corticosteroids are used to treat ocular inflammation, then anti-inflammatory effect is achieved, but severe side effects occur
Solution Approach 1:
The invention changes the chemical parameter from corticosteroids to Phosphorylcholine-tuftsin conjugate, which has different pharmacological properties. The conjugate provides anti-inflammatory effects through immunomodulation rather than steroid mechanisms, thereby avoiding steroid-related side effects while maintaining therapeutic efficacy
Solution Approach 2:
The invention uses a composite structure of Phosphorylcholine conjugated to tuftsin peptide. This composite molecule combines the immunomodulatory properties of tuftsin with the anti-inflammatory characteristics of phosphorylcholine, creating a new therapeutic agent that achieves anti-inflammatory effects without the harmful side effects of corticosteroids
2Duration of action of stationary object
If solid formulations of Phosphorylcholine-tuftsin conjugate are developed, then storage shelf-life is improved, but gradual release at application site must be maintained
Solution Approach 1:
The invention segments the drug delivery system into solid particulate formulations with controlled size distribution. The particles are segmented to specific size ranges (e.g., 1-50 μm, 10-30 μm) that enable both stable storage and controlled gradual release at the application site, resolving the contradiction between shelf-life stability and sustained release
Solution Approach 2:
The invention changes the physical state parameter from liquid or solution to solid particulate form. This parameter change enables long-term stable storage while the controlled particle size and surface properties ensure gradual release kinetics at the application site, simultaneously achieving both extended shelf-life and sustained release
3Quantity of substance
If particle size is reduced to improve drug loading efficiency, then release control must be maintained
Solution Approach 1:
The invention optimizes the particle size parameter to specific ranges (e.g., 1-50 μm, 10-30 μm) that maximize drug loading efficiency while maintaining sustained release. The precise control of this physical parameter enables high drug capacity within small particles while the surface-to-volume ratio and surface chemistry ensure controlled gradual release rather than burst release
Data Source
AI summary
Provided herein is a composition comprising solid particles or granules comprising Phosphorylcholine-tuftsin conjugate including a salt thereof, and ester end-capped poly(glycolide-co-lactide), wherein the Phosphorylcholine-tuftsin conjugate is an amorphous solid; is characterized by any one of: (i) average particle size less than 30 um, as determined by SEM; (ii) a powder XRD devoid of a corresponding peak having a net intensity peak height of above about 30 counts. Additionally, method for treating an ocular disease or disorder in a subject via intraocular administration of a therapeutically effective amount of the composition of the invention to the subject.