Apolactoferrin-Lactoferrin Nanolipid Stabilization
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Solution Overview
Problem
Apolactoferrin's rapid conformation change and susceptibility to degradation limit its application in pharmaceutical and cosmetic fields due to its high iron binding capacity, making it difficult to effectively treat diseases characterized by iron accumulation.
Innovation Solution
A composition combining apolactoferrin with lactoferrin, vehiculated in nanolipids, which stabilizes apolactoferrin in a suitable conformation for iron binding without degradation, enhancing its chelating properties for treating iron accumulation diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If apolactoferrin is used to treat iron accumulation diseases, then iron binding capacity is improved, but stability and resistance to degradation worsen
Solution Approach 1:
The patent uses a composite formulation combining apolactoferrin with stabilizing agents including hydroxypropyl-beta-cyclodextrin, phospholipids, and antioxidants. This composite approach allows the formulation to maintain high iron binding capacity while the stabilizing agents protect apolactoferrin from degradation and oxidation, thereby resolving the contradiction between reactivity and stability.
Solution Approach 2:
The patent introduces cyclodextrins and phospholipids as intermediary substances that form inclusion complexes or vesicular structures with apolactoferrin. These intermediaries protect the apolactoferrin from direct exposure to degrading environments while still allowing it to perform its iron binding function, thus maintaining both stability and activity.
2Productivity
If apolactoferrin conformation changes rapidly, then iron binding activity is improved, but susceptibility to denaturation worsens
Solution Approach 1:
The patent applies preliminary stabilization measures by incorporating antioxidants and stabilizing agents into the formulation before apolactoferrin can undergo harmful denaturation. This preliminary protection allows the protein to maintain its functional conformation changes for iron binding while preventing irreversible denaturation.
Solution Approach 2:
The patent modifies the physical and chemical parameters of the formulation environment including pH control, ionic strength adjustment, and incorporation of stabilizing molecules. These parameter changes create an optimal environment where apolactoferrin can undergo necessary conformational changes for iron binding without transitioning to denatured states.
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 apolactoferrin-lactoferrin composition exhibits improved iron adsorption and bioavailability, effectively treating iron accumulation diseases by reducing oxidative stress and promoting healing in conditions where iron is toxic, such as ecchymotic wounds and cutaneous dyschromias, with enhanced stability and penetration.
Implementation Method 1
Lactoferrin, well known since long time and recently re-evaluated for immunomodulating and anti-infections properties thereof as well as largely described in literature, is a glycoprotein with antimicrobial and iron-transport activities provided with multiple bioactive properties connected with its capacity of chelating iron.
Implementation Method 2
Apolactoferrin for the treatment of iron accumulation diseases... based on a mixture of lactoferrin and apolactoferrin... vehiculated in nanolipids
Implementation Method 3
An excessive amount of this metal accumulated into the organism may result in a high toxicity, since the free iron ions react with peroxides and produce free radicals which, being highly reactive, may cause damages to DNA, proteins, lipids and other cell components.
Data Source
AI summary
The invention refers to the use of compositions/ formulations based on a mixture of lactoferrin and apolactoferrin for the treatment of diseases characterized by iron accumulation, preferably for topical use. Said formulations can be used in food, cosmetic, cosmeceutic, dermatologic or pharmaceutical fields and are particularly suited for the treatment of ecchymotic pigmentations and skin dyschromias in general.