Internal Structured Self-Assembling Liposomes for Drug Delivery
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Solution Overview
Problem
Current drug delivery methods, particularly for large molecules like DNA, RNA, and proteins, face challenges such as poor pharmacodynamics, instability in blood serum, immune system targeting, low delivery efficiency, and structural instability during storage, which limits their effectiveness and practicality.
Innovation Solution
The development of internal structured self-assembled liposomes (ISSALs) with a nuclear core molecule and a lipid bilayer containing phospholipid-affinity enhancing complexes, allowing for stepwise assembly and targeting of sub-cellular addresses, while maintaining structural stability during freeze-thaw cycles and storage.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional liposomes are used for drug delivery, then they can protect drugs from hostile environment, but they suffer from low delivery efficiency and poor structural stability during storage
Solution Approach 1:
The liposome is segmented into multiple functional layers: an internal structured core containing the drug payload, and an external self-assembling bilayer shell. This segmentation allows each layer to perform specialized functions - the core provides structural stability and drug loading, while the shell provides delivery efficiency and cellular uptake, resolving the contradiction between delivery efficiency and structural complexity
Solution Approach 2:
The patent implements a nested structure where the drug payload is embedded within the internal core, which is then enclosed by the lipid bilayer shell. This nested arrangement protects the drug while maintaining a compact, stable structure that improves both delivery efficiency and storage stability without excessive complexity
2Reliability
If liposomes are modified with targeting molecules and membrane fusion proteins to improve delivery efficiency, then cellular uptake is enhanced, but structural stability during storage and freeze-thaw cycles deteriorates
Solution Approach 1:
The internal structured core is pre-assembled with the drug payload before the external bilayer shell forms around it. This preliminary structuring creates a stable nucleus that maintains integrity during storage and freeze-thaw cycles, while still allowing the external shell to provide enhanced delivery and cellular uptake functions
Solution Approach 2:
The liposome combines different material properties: the internal core uses materials optimized for structural stability and drug loading, while the external shell uses lipid bilayer materials with incorporated targeting molecules and fusion proteins for enhanced delivery. This composite structure resolves the contradiction between stability and delivery efficiency
3Ease of operation
If nucleic acids are delivered directly into the body, then they can be administered easily, but they are destroyed by nucleases in blood serum
Solution Approach 1:
The nucleic acid payload is nested within the internal structured core of the liposome, which is then enclosed by the protective lipid bilayer shell. This nested protection prevents nucleases in blood serum from accessing and degrading the nucleic acids, maintaining drug stability while preserving easy administration through intravenous injection
4Reliability
If foreign protein drugs are delivered into the body, then they can provide therapeutic effects, but they are targeted by the humoral immune system
Solution Approach 1:
The flexible lipid bilayer shell acts as a protective film that shields the foreign protein drug from immune system recognition. The shell's fluid nature allows it to adapt and protect the payload while circulating in the body, reducing immune targeting and extending therapeutic 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
ISSALs enable efficient delivery of various-sized molecules to specific sub-cellular locations, overcoming issues of low delivery efficiency and structural instability, and allowing for the use of membrane fusion proteins to avoid cytotoxicity, thereby enhancing the delivery of nucleic acids and proteins into cells.
Implementation Method 1
a nuclear core molecule or complex including a first affinity enhancing molecule; and a liposome encompassing the nuclear core molecule or complex, the liposome containing a lipid bilayer containing a phospholipid-affinity enhancing complex having a phospholipid coupled to second affinity enhancing molecule, wherein the second affinity enhancing molecule couples to the first affinity enhancing molecule
Data Source
AI summary
The specification relates to an internal structured self assembled liposome (ISSAL), containing a nuclear core molecule or complex including a first affinity enhancing molecule; and a phospholipid-affinity enhancing complex having a phospholipid coupled to second affinity enhancing molecule, wherein the second affinity enhancing molecule couples to the first affinity enhancing molecule. The ISSAL's can be used in, for example and without limitation, the field of drug delivery, vaccination, imaging contrast agents, and nanotechnology, in which liposomes of ordered, self-assembling structure are employed to deliver soluble or insoluble molecules to any sub-cellular address.