Enteric-Coated Lactoferrin Particles for Gastric Protection
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Solution Overview
Problem
Lactoferrin exhibits poor bioavailability and stability after oral administration due to enzymatic degradation and acidic gastric environment, limiting its effectiveness in treating gastrointestinal issues like food poisoning, as existing methods to enhance its delivery often decrease its activity.
Innovation Solution
Enteric-coated particles comprising a core of inert materials like cellulose polymer, sugar, or starch, a first coating layer with lactoferrin and a binder, and a second enteric coating layer to protect lactoferrin from gastric conditions, allowing for high-dose delivery and improved stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If lactoferrin is administered orally without protection, then it can reach the gastrointestinal tract, but it undergoes enzymatic degradation and is exposed to acidic gastric environment, resulting in poor bioavailability and stability
Solution Approach 1:
The particle is divided into multiple functional layers: a core layer containing lactoferrin, a first coating layer providing structural support, and a second enteric coating layer providing chemical protection. This segmentation allows each layer to perform its specific function independently, protecting lactoferrin from degradation while maintaining its activity.
Solution Approach 2:
The lactoferrin-containing core is nested within the first coating layer, which is in turn nested within the second enteric coating layer. This nested structure provides progressive protection, with each outer layer shielding the inner layers from harmful environmental factors while allowing the active ingredient to remain intact.
2Reliability
If existing methods like iron saturation, microencapsulation, or PEGylation are used to protect lactoferrin, then stability is improved, but the activity of lactoferrin against microorganisms decreases
Solution Approach 1:
By separating the protection function (provided by the coating layers) from the activity function (provided by the lactoferrin in the core), the invention allows lactoferrin to maintain its full antimicrobial activity while being protected from degradation. The coating layers act as a barrier without interfering with lactoferrin's biological function.
Solution Approach 2:
The enteric coating layers serve as an intermediary between the harsh gastrointestinal environment and the lactoferrin active ingredient. This intermediary layer protects lactoferrin from acidic and enzymatic damage while allowing it to remain bioactive when it reaches the target site in the gastrointestinal tract.
3Quantity of substance
If high dose of lactoferrin is administered to overcome poor bioavailability, then therapeutic effectiveness may be improved, but the complexity of formulation and delivery system increases
Solution Approach 1:
The segmented particle structure with distinct functional layers enables efficient delivery of high doses of lactoferrin. Each layer is optimized for its specific purpose, allowing the formulation to handle large amounts of active ingredient without proportionally increasing complexity.
Solution Approach 2:
The invention changes the physical and chemical parameters of the delivery system by using specific coating materials with controlled properties (such as enteric coating that resists acid but dissolves in intestinal pH). This allows high-dose delivery through a relatively simple two-layer coating approach rather than complex multi-component systems.
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 enteric-coated particles provide a high dose of pure lactoferrin with enhanced stability and selective antimicrobial activity, effectively targeting pathogenic microorganisms in the gastrointestinal tract while minimizing exposure to harsh stomach conditions.
Implementation Method 1
a second coating layer substantially covering the first coating layer and comprising c-1) an enteric coating material
Implementation Method 2
lactoferrin generally shows poor low bioavailability after oral administration due to its proteolysis in the gastrointestinal tract
Data Source
AI summary
The present invention generally relates to enteric-coated particles containing lactoferrin. More specifically, the present invention provides an enteric-coated particle comprising (or consisting essentially of): a) a core comprising (or consisting essentially of) an inert core-forming material selected from cellulose polymer, sugar, sugar alcohol, starch and carnauba wax; b) a first coating layer substantially covering the core and comprising (or consisting essentially of) b-1) lactoferrin, b-2) a pharmaceutically acceptable binder and optionally b-3) one or more other suitable excipients, such as a plasticizer; and c) a second coating layer substantially covering the first coating layer and comprising (or consisting essentially of) c-1) an enteric coating material, and optionally c-2) one or more suitable excipients, such as a plasticizer and/or an anti-tacking agent. The present invention further provides pharmaceutical compositions and oral dosage forms comprising one or more particles according to the present invention.