PCA-PVA-PEG Graft Copolymer Solubilization in Ophthalmic Formulations
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Solution Overview
Problem
Topically applied ophthalmic formulations face challenges due to poor solubility and stability of therapeutically active agents in aqueous solutions, which limits their effectiveness and requires improved solubilization and stabilization methods.
Innovation Solution
The use of a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PCA-PVA-PEG) to enhance the solubility and stability of therapeutically active agents, while also providing antimicrobial properties and reducing the need for traditional preservatives.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If traditional aqueous formulations are used, then the formulation is simple and easy to manufacture, but the solubility of therapeutically active agents is poor
Solution Approach 1:
The patent uses a nonionic surfactant as an intermediary substance to mediate between the hydrophobic therapeutically active agent and the aqueous formulation medium. The surfactant forms micelles that solubilize the active agent in the aqueous phase, enabling improved solubility without fundamentally changing the aqueous formulation system.
Solution Approach 2:
The patent modifies the physical-chemical parameters of the formulation by introducing a surfactant that changes the surface tension and micelle formation characteristics of the aqueous solution. This parameter change enables the system to accommodate hydrophobic active agents that would otherwise be insoluble.
2Reliability
If traditional preservatives are used at effective concentrations, then antimicrobial protection is adequate, but the preservative may cause irritation or reduce preservative effectiveness when solubility is improved
Solution Approach 1:
The nonionic surfactant acts as a protective intermediary that prevents direct interaction between the preservative and the therapeutically active agent, thereby maintaining preservative effectiveness while reducing potential irritation. The surfactant micelles can also help distribute the preservative more uniformly throughout the formulation.
3Quantity of substance
If solubility is improved using a nonionic surfactant, then the solubility of therapeutically active agents is enhanced, but further improvement is needed
Solution Approach 1:
The patent employs a composite approach by combining the nonionic surfactant with specific ophthalmic excipients and active agents in a multi-component formulation system. This composite formulation synergistically enhances solubility beyond what the surfactant alone could achieve, while maintaining formulation stability and safety.
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
PCA-PVA-PEG significantly improves the solubility and stability of active agents, maintains preservative effectiveness at lower concentrations, and demonstrates antimicrobial activity, making it suitable for self-preserved ophthalmic compositions that meet stringent preservative efficacy criteria.
Implementation Method 1
Some embodiments include a method of solubilizing a therapeutically active agent comprising providing a composition including the therapeutically active agent and a PCA-PVA-PEG
Implementation Method 2
Some embodiments include a method of stabilizing a therapeutically active agent comprising combining the therapeutically active agent with a PCA-PVA-PEG to thereby improve stability of the therapeutically active agent
Implementation Method 3
demonstrates antimicrobial activity, making it suitable for self-preserved ophthalmic compositions
Data Source
AI summary
Compositions and methods related to ophthalmic use of polyvinyl capralactam-polyvinyl acetate-polyethylene glycol graft copolymers and therapeutic uses are described herein.