Peptide–Surfactant Compositions for Membrane Permeability
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Solution Overview
Problem
Existing methods to enhance the membrane permeability and absorbability of peptide compounds, such as those containing N-substituted amino acid residues, have not been effectively addressed, particularly in compositions combining peptide compounds with surfactants without altering the peptide's functional properties.
Innovation Solution
A composition comprising peptide compounds with specific characteristics, such as N-substituted amino acid residues and C log P values, combined with surfactants having linear alkylene structures and carnitine residues, along with solubility improvers like polyoxyethylene structures, to enhance membrane permeability and absorbability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a peptide compound with medium molecular weight is used to target tough proteins, then binding ability to target protein is improved, but membrane permeability and absorbability deteriorate
Solution Approach 1:
The patent introduces surfactants as intermediary substances that mediate between the peptide compound and the membrane. The surfactants form complexes with the peptide compounds, facilitating their transport across the membrane without altering the peptide's binding function. This mediator approach allows the peptide to maintain its therapeutic activity while improving membrane permeability.
Solution Approach 2:
The patent creates composite formulations by combining peptide compounds with surfactants in specific ratios. This composite material approach leverages the complementary properties of both components: the peptide provides target-specific binding activity while the surfactant contributes membrane permeabilizing properties, achieving both therapeutic efficacy and improved bioavailability.
2Object-generated harmful factors
If the structure of the peptide compound is modified to improve membrane permeability, then absorbability is improved, but the function of the peptide compound (binding ability) may be affected
Solution Approach 1:
The patent separates the functions of membrane permeability and target binding into different components. The peptide compound is dedicated to binding function, while the surfactant component handles membrane permeability. This functional segmentation allows each component to optimize its specific role without compromising the other, avoiding the need to compromise peptide structure for permeability.
3Object-generated harmful factors
If a surfactant is combined with a peptide compound to enhance absorbability, then membrane permeability is improved, but the complexity of the composition increases
Solution Approach 1:
The patent optimizes the concentration ratios and physical parameters of the surfactant-peptide complex to achieve effective permeability enhancement with minimal complexity. By carefully controlling the surfactant-to-peptide ratio and selecting appropriate surfactant molecular weights and structures, the formulation achieves improved absorbability while maintaining reasonable compositional simplicity for practical application.
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 composition significantly improves the membrane permeability and absorbability of peptide compounds, as evidenced by increased Caco-2 Papp values and solubility in phosphate buffer, facilitating effective peptide delivery.
Implementation Method 1
a combination of a peptide compound with a surfactant has been attempted to improve absorbability
Implementation Method 2
a solubility improver containing a polyoxyethylene structure
Data Source
AI summary
The present invention relates to a composition containing components (1) and (2) below:(1) at least one or more peptide compounds selected from the group consisting of (i), (ii), and (iii) below:(i) a peptide compound containing one or more N-substituted amino acid residues,(ii) a peptide compound having C log P of 4 or more and 25 or less, and(iii) a peptide compound having a solubility of 10 mg/mL or less in 50 mM phosphate buffer (pH 6.5) under the conditions of 37° C., 1 atm; and(2) at least one or more surfactants selected from the group consisting of (iv) and (v) below:(iv) a surfactant having a linear alkylene structure and having 5 or more and 13 or less carbon atoms in the linear alkylene structure, and(v) a surfactant having a carnitine residue.