Zwitterionic Polymer Particles for Oral Protein Absorption
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Solution Overview
Problem
There is a need for improved compositions for oral and mucosal delivery of biologically active agents such as proteins, peptides, and dietary supplements that enhance absorption and trans-mucosal delivery.
Innovation Solution
The use of zwitterionic polymer particles, including micelles, liposomes, or hydrogel particles, with zwitterionic polymers or copolymers, to facilitate the delivery of biologically active agents by oral and mucosal administration, utilizing zwitterionic polymers with lipid-derived polymers and crosslinkers to improve absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional delivery compositions are used, then the biologically active agent can be administered, but oral absorption and trans-mucosal delivery are insufficient
Solution Approach 1:
The patent employs zwitterionic copolymers comprising both hydrophilic zwitterionic segments and hydrophobic lipid-derived segments. This composite structure enables the formulation to simultaneously interact with aqueous mucosal environments and facilitate membrane permeation, thereby improving oral absorption and trans-mucosal delivery without requiring overly complex multi-component systems.
Solution Approach 2:
The patent utilizes the amphiphilic nature of zwitterionic copolymers to self-assemble into nanostructured formulations with specific micellar or vesicular morphologies. By controlling parameters such as copolymer composition, molecular weight, and hydrophobic-hydrophilic balance, the formulation achieves optimal size, surface charge, and stability characteristics that enhance mucosal penetration and intestinal absorption.
2Reliability
If zwitterionic polymers are used to improve oral bioavailability, then trans-mucosal delivery is enhanced, but the formulation complexity increases
Solution Approach 1:
The zwitterionic copolymer is segmented into distinct functional domains: hydrophilic zwitterionic segments that provide aqueous solubility and mucosal surface interaction, and hydrophobic lipid-derived segments that facilitate membrane integration and trans-mucosal transport. This segmentation allows each segment to perform its specific function while the overall copolymer structure remains relatively simple.
Solution Approach 2:
The zwitterionic copolymer structure serves multiple functions simultaneously: it acts as a solubilizing agent, a mucosal permeation enhancer, a stabilizer for the biologically active agent, and a potential targeting moiety. This multi-functionality reduces the need for additional excipients or complex formulation components.
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 oral bioavailability and trans-mucosal delivery of biologically active agents by improving interaction with mucosal surfaces and intestinal absorption.
Implementation Method 1
the exterior surface having at least one type of zwitterionic polymer disposed thereon and/or extending therefrom
Data Source
AI summary
Compositions and methods for oral and/or mucosal administration of a biologically active agent are provided according to aspects of the present disclosure which include: a plurality of particles, wherein each particle has an exterior surface, the exterior surface defining a particle interior, the exterior surface having at least one type of zwitterionic polymer and/or zwitterionic copolymer disposed thereon and/or extending therefrom; and a biologically active agent disposed on the exterior surface and/or in the particle interior, wherein the biologically active agent is or includes a protein, peptide, or dietary supplement. According to particular aspects, compositions and methods for oral and/or mucosal administration of an anti diabetes biological agent, such as insulin and/or an insulin analog.