Solid Lipid Nanoparticles for Lipase-Resistant Intracellular Release
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Solution Overview
Problem
Existing solid lipid nanoparticles (SLNs) face challenges such as large size, high lipid content, low melting point, enzymatic disintegration by lipases, and inability to target intracellular release of active substances while avoiding the p-gp efflux mechanism.
Innovation Solution
A solid lipid nanoparticle composition using natural plant wax, d-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS), and polysorbate, with a spherical diameter of 15-100 nm, designed to encapsulate active substances within a hard, insoluble core, resistant to lipases and capable of intracellular release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If solid lipid nanoparticles are used as carriers for therapeutic compounds, then drug delivery control and bioavailability enhancement are improved, but the particles are subject to enzymatic disintegration by lipases due to high lipid content
Solution Approach 1:
The patent changes the chemical composition parameters of the lipid matrix by incorporating specific solid lipids (triglycerides, fatty acids, steroids, lipid peptides, or waxes) and emulsifiers in controlled ratios. This parameter modification allows the nanoparticle to maintain structural integrity against lipase degradation while preserving drug delivery control capabilities.
Solution Approach 2:
The patent creates a composite nanoparticle system combining solid lipid matrix with emulsifier systems. This composite structure provides both the structural framework for controlled drug release and resistance to enzymatic degradation, as the emulsifier component protects the lipid core from lipase attack while maintaining the nanoparticle's drug carrier functionality.
2Quantity of substance
If the lipid core of solid lipid particles has high lipid content, then the active substances can be effectively encapsulated, but the lipid core becomes object of enzymatic disintegration by lipases preventing targeted release
Solution Approach 1:
The patent employs an emulsifier shell or film surrounding the lipid core. This protective shell prevents direct access of lipases to the encapsulated active substances, ensuring that the high lipid content necessary for encapsulation does not compromise targeted release capability. The emulsifier layer acts as a barrier while maintaining the nanoparticle's structural integrity.
3Reliability
If solid lipid nanoparticles are prepared with traditional lipid compounds, then the lipid matrix can protect labile active ingredients, but the particles exhibit large size and high melting point
Solution Approach 1:
The patent modifies the physical parameters of the lipid matrix by selecting solid lipids with appropriate melting points and incorporating them in specific concentrations. This allows the nanoparticle to maintain protection of labile active ingredients through the solid lipid structure while achieving lower overall melting point and smaller particle size through optimized formulation parameters.
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 achieves intracellular delivery of active substances with high lipophilicity, avoiding enzymatic degradation and p-gp efflux, ensuring controlled release and efficient targeting.
Implementation Method 1
designed to encapsulate active substances within a hard, insoluble core
Implementation Method 2
encapsulate active substances within a hard, insoluble core, resistant to lipases
Implementation Method 3
The lipid matrix of SLN can protect labile active ingredients from hydrolysis and/or oxidation
Implementation Method 4
The lipid matrix of SLN can protect labile active ingredients from hydrolysis and/or oxidation
Implementation Method 5
The composition achieves intracellular delivery of active substances with high lipophilicity, avoiding enzymatic degradation and p-gp efflux
Data Source
AI summary
The invention relates to solid lipid nanoparticle for intracellular release of active substances, can be used in the pharmaceutical industry, in the medicine, cosmetics, as well as for food supplements. Solid lipid nanoparticle has spherical shape with a diameter of 15-100 nm, the lipid is a solid lipid selected from natural plant wax or its synthetic analogue, as the surface acting agent is used TMDSC. The particles of solid lipid nanoparticle is characterized with high melting point, high lipophilicity and low (or lack) of in-vitro dissolution profile. The system is lipase-resistant and is capable to freely penetrate through cell membranes into cells where to release the active substance(s) due to an intracellular digestion with controllable depo-effect. In a second aspect, the invention relates to a method of production of the solid lipid nanoparticle. The preferred technology for production of the compositions is a Phase Inversion Temperature method.