High Penetration Compositions for Biological Barrier Crossing
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Solution Overview
Problem
Current drug delivery methods face challenges in effectively penetrating biological barriers, leading to inadequate treatment of conditions due to limited drug penetration and resulting in adverse reactions and inefficiencies, particularly for non-steroidal anti-inflammatory agents, prostaglandins, peptides, mustards, and beta-lactam antibiotics.
Innovation Solution
Development of a high penetration composition (HPC) comprising a functional unit covalently linked to a transportational unit through a linker, which includes a protonatable amine group to facilitate crossing of biological barriers, allowing for efficient delivery of parent drugs or related compounds across biological barriers with reduced systemic exposure.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If drugs are administered through systematic route (oral or parenteral) to reach distal action sites, then the drugs can reach the target location, but higher dosage is required which causes adverse reactions
Solution Approach 1:
The patent uses a penetration enhancer as an intermediary substance that facilitates drug penetration across biological barriers. The penetration enhancer temporarily modifies the barrier properties of membranes (such as skin, mucosa, or blood-brain barrier) to allow therapeutic agents to pass through more efficiently, reducing the need for high systemic doses and thereby minimizing adverse reactions while maintaining effective drug delivery to distal sites
2Reliability
If higher dosage of drugs is used to achieve effective concentration at distal locations, then the treatment efficacy is improved, but side effects increase
Solution Approach 1:
The patent changes the physical-chemical parameters of the drug delivery system by incorporating penetration enhancers that alter membrane permeability. This parameter change allows the same drug to achieve effective concentrations at the target site with lower administered doses, thereby maintaining treatment efficacy while reducing dose-dependent side effects
3Ease of operation
If drugs are administered orally for convenient delivery, then ease of administration is improved, but drug penetration across biological barriers is limited
Solution Approach 1:
The patent employs penetration enhancers as mediators that bridge the gap between oral administration and effective drug penetration. These enhancers are incorporated into the oral formulation and act at the site of absorption (gastrointestinal mucosa) to facilitate drug penetration across biological barriers, thereby maintaining the convenience of oral administration while improving penetration reliability
4Object-affected harmful factors
If conventional formulations are used for transdermal application to reduce side effects, then localized drug administration is achieved, but therapeutically effective plasma levels are difficult to deliver
Solution Approach 1:
The patent modifies the formulation parameters by incorporating penetration enhancers that significantly increase transdermal permeability. This allows the formulation to deliver therapeutically effective plasma levels of drugs through the skin while maintaining localized administration benefits and minimizing systemic side effects
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 HPC achieves higher local concentrations of drugs at the target site with lower dosages, reducing adverse effects and enhancing bioavailability, enabling effective treatment of conditions previously difficult to reach, such as spinal cord injuries and autoimmune disorders, with improved pharmacological effects compared to traditional delivery methods.
Implementation Method 1
a transportational unit to facilitate the crossing of one or more biological barriers
Data Source
AI summary
High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.