Vesicular Formulation Covalent Bonding Transdermal Delivery
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Solution Overview
Problem
Current vesicular formulations for transdermal delivery of therapeutic agents often require the agent to be incorporated within the vesicle, necessitating vesicle disruption for release, which is inefficient for large molecules or those with incompatible chemistry, and PEG-containing surfactants affect vesicle flexibility.
Innovation Solution
A vesicular formulation where the therapeutic agent is covalently bonded to a component of the vesicle, such as a lipid or surfactant, ensuring at least 5% of the agent is external to the vesicle, allowing it to act as a mechanical device for penetration without disruption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If the therapeutic agent is incorporated within the vesicle lumen or membrane, then the vesicle can transport the agent through the skin, but the agent requires vesicle disruption for release which is inefficient for large molecules or those with incompatible chemistry
Solution Approach 1:
The patent segments the therapeutic agent from the vesicle internal structure by bonding it to the external surface of the vesicle membrane. This allows the agent to be delivered without requiring vesicle disruption, solving the problem of inefficient release for large or chemically incompatible molecules while maintaining transport capability through the skin.
Solution Approach 2:
The patent moves the therapeutic agent from the traditional intraluminal or membrane-incorporated position to the external surface of the vesicle. This spatial repositioning allows the agent to be delivered intact without vesicle disruption, enabling compatibility with large molecules and those with incompatible chemistry while maintaining delivery efficiency.
2Quantity of substance
If PEG-containing surfactant components are replaced with the therapeutic agent, then the agent can be incorporated into the vesicle, but this affects the flexibility of the vesicle and removes some of the motive power
Solution Approach 1:
The patent separates the functional roles of the surfactant and therapeutic agent by bonding the agent to the external surface rather than replacing surfactant components. This maintains the PEG-containing surfactant's flexibility and motive power functions while still achieving high therapeutic agent loading capacity on the vesicle surface.
Solution Approach 2:
The vesicle structure is designed to perform multiple functions simultaneously: the PEG-containing surfactant maintains flexibility and motive power for skin penetration, while the external surface provides binding sites for therapeutic agents. This multi-functionality resolves the contradiction between agent incorporation and vesicle performance.
3Productivity
If the therapeutic agent is bonded to the vesicle component, then the vesicle acts purely as a mechanical device for penetration without disruption, but the orientation of the modified molecule cannot be controlled during manufacture
Solution Approach 1:
The patent accepts that only a portion of the externally bonded therapeutic agents will be in the correct orientation for optimal delivery. By bonding agents to the external surface, sufficient quantities in the correct orientation are achieved to maintain high delivery efficiency without requiring complete orientation control during manufacture.
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
Enhances the speed, depth, and amount of agent penetration through the skin, overcoming limitations of size and chemistry incompatibility, with minimal systemic absorption and prolonged action.
Implementation Method 1
the AOI is bonded to a component of the vesicle such that at least a portion of the AOI is on the external surface of the vesicle, and is external to the vesicle membrane
Implementation Method 2
These vesicles have been tested as vehicles for transporting other AOIs into the body via the transdermal route... by placing the AOI to be transported inside the lumen of the vesicle or incorporating the AOI into the membrane of the vesicle
Data Source
AI summary
The present invention relates to vesicular formulations for use in the topical administration of a therapeutic, metabolic, cosmetic or structural Agent Of Interest ("AOI") and methods of administering an AOI.