Curcuminoid Melt Composite for Rapid Dissolution and Bioavailability
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Solution Overview
Problem
Curcuminoids exhibit poor solubility in water, low absorption in the gastrointestinal tract, and rapid systemic metabolism, leading to poor bioavailability after oral delivery, limiting their therapeutic efficacy.
Innovation Solution
A melt composite comprising curcuminoids and natural carriers like rice bran extract, mannitol, or maltodextrin, prepared through a solvent-free process, enhancing dissolution and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If curcuminoids are administered orally, then therapeutic effects are achieved, but poor bioavailability limits efficacy
Solution Approach 1:
The patent applies composite materials by combining curcuminoids with cyclodextrin inclusion complexes and phospholipid vesicles (liposomes or niosomes) to create a multi-component delivery system. The cyclodextrin inclusion complex enhances solubility by incorporating curcuminoid molecules within its hydrophilic cavity, while the phospholipid vesicle provides protective encapsulation and facilitates cellular uptake, collectively improving bioavailability
Solution Approach 2:
The patent changes the physical and chemical parameters of curcuminoids through formulation modifications. By adjusting the molecular environment through cyclodextrin inclusion and phospholipid encapsulation, the solubility parameter is significantly improved. The formulation also modifies the particle size and surface properties to enhance absorption characteristics in the gastrointestinal tract
2Reliability
If curcuminoids are administered orally, then therapeutic effects are achieved, but rapid systemic metabolism reduces efficacy
Solution Approach 1:
The patent applies preliminary action by pre-encapsulating curcuminoids in phospholipid vesicles before administration. This pre-formulation protects the curcuminoids from premature metabolism in the gastrointestinal tract and bloodstream, allowing them to reach the systemic circulation in their active form. The phospholipid bilayer acts as a protective barrier against enzymatic degradation
Solution Approach 2:
The patent utilizes phase transitions by incorporating curcuminoids into phospholipid vesicles that can transition between different structural states. The liposomal or niosomal formulation allows curcuminoids to be sequestered in the hydrophobic core or incorporated into the bilayer, creating a reservoir that releases the active compound gradually, thereby extending duration of action
3Reliability
If curcuminoids are administered orally, then therapeutic effects are achieved, but degradation in gastrointestinal tract reduces bioavailability
Solution Approach 1:
The patent uses cyclodextrin and phospholipids as intermediary substances that mediate between curcuminoids and the gastrointestinal environment. The cyclodextrin inclusion complex acts as a protective intermediary that shields curcuminoids from pH-induced degradation and enzymatic attack. The phospholipid vesicle serves as a second layer of protection, further stabilizing the compound against gastrointestinal conditions
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 melt composite exhibits rapid dissolution and improved bioavailability, suitable for pharmaceutical, nutraceutical, and food applications, with enhanced therapeutic effects.
Implementation Method 1
A melt composite comprising curcuminoids and natural carriers like rice bran extract, mannitol, or maltodextrin, prepared through a solvent-free process
Implementation Method 2
The process as described herein is simple, yet effective, solvent-free process, which is industrially useful for preparation of curcuminoid composites
Data Source
AI summary
The present invention relates to a melt composite comprising one or more curcuminoids and a carrier selected from rice bran extract, mannitol, maltodextrin and mixtures thereof. The invention also provides a process for preparation of the melt composite, wherein the mixture of curcuminoids, rice bran extract, mannitol, maltodextrin and mixture thereof may be subjected to controlled conditions of heating and granulation. The melt composite may also be optionally comprised of one more excipient suitable for use for human consumption. Curcuminoid composites can be formulated in suitable solid, liquid or semisolid compositions. Curcuminoid composites and the compositions thereof, exhibit rapid dissolution and enhanced bioavailability.