Polyamine-Mediated Drug Delivery Across Mucosal Barriers
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Solution Overview
Problem
Existing drug delivery systems struggle to efficiently transport pharmaceutically active agents across complex biological barriers such as mucosal and epithelial surfaces, particularly for conditions like burns, trauma, and chronic eye diseases, with limited effectiveness in multi-layered systems.
Innovation Solution
A drug delivery system comprising a pharmaceutically effective moiety and a polyamine or amine moiety, where the polyamine or amine moiety does not include two or more contiguous basic amino acid residues, utilizing polyamines or amines as carrier agents to enhance transport across membranes.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If conventional polypeptides or cell penetrating peptides are used to transport pharmaceutically active agents across biological barriers, then some transport capability is achieved, but the transport efficiency is insufficient for complex multi-layered systems such as skin, cornea, and mucosal membranes
Solution Approach 1:
The patent introduces polyamine or amine moieties as intermediary carrier agents that facilitate the transport of pharmaceutically active agents across biological barriers. These carrier agents act as mediators between the drug molecules and the membrane structures, enabling efficient translocation without direct penetration by the drug itself. The carrier agents interact with both the pharmaceutically active moieties and the membrane components, creating a facilitated transport mechanism that overcomes the inefficiency of conventional direct penetration approaches.
Solution Approach 2:
The patent modifies the chemical parameters of the carrier agents by specifying polyamines or amines with particular structural characteristics (such as molecular weight, charge distribution, and functional group composition) that optimize their ability to facilitate transport across different biological barriers. By carefully controlling these parameters, the system achieves enhanced transport efficiency while maintaining compatibility with various membrane types including skin, cornea, and mucosal membranes.
2Reliability
If polypeptides with basic amino acid residues are used as carrier agents, then interaction with biological membranes is enhanced, but the complexity of the system increases and manufacturing becomes more difficult
Solution Approach 1:
The patent extracts and isolates the essential functional characteristics needed for membrane interaction from complex polypeptides, separating these functions into simpler polyamine or amine moieties. By taking out only the critical interactive elements (basic amino acid-like functionality) while excluding the complex polypeptide structure, the system achieves membrane interaction capability with significantly reduced synthesis complexity and improved manufacturability.
Solution Approach 2:
The patent segments the carrier agent function into discrete polyamine or amine moieties that can be independently synthesized and optimized. Rather than working with single large polypeptide molecules, the system divides the functional requirements into separate, manageable chemical units that can be manufactured more easily and combined as needed, thereby reducing overall synthesis complexity while maintaining membrane interaction effectiveness.
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 system significantly enhances the transport of active agents across single or multi-layered membranes, demonstrating improved delivery of peptides, lutein, and bevacizumab into target tissues, with increased efficacy in transmucosal and transepithelial drug delivery.
Implementation Method 1
utilizing polyamines or amines as carrier agents to enhance transport across membranes
Data Source
AI summary
The present invention relates to a drug delivery system and methods of using the delivery system, particularly a delivery system for transporting pharmaceutically active agents across, for example, the skin, the surface of the eye or mucosal membranes. The drug delivery system comprises a pharmaceutically effective moiety and a polyamine or amine moiety, wherein the polyamine or amine moiety does not comprise two or more contiguous basic amino acid residues. The drug delivery system may be provided for use as a medicament, or for use in the treatment of a disease or condition selected from eye disease, burns, infection, and trauma. The invention also provides a method comprising administering a pharmaceutically effective amount of the drug delivery system of the invention to a patient in need thereof.