Development of Nutrient Delivery Systems: Ingredients & Challenges
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1 Development of Nutrient Delivery Systems David Julian McClements and Hang Xiao Department of Food Science University of Massachusetts Development of Nutrient Delivery Systems: Ingredients & Challenges Vitamins Nutraceuticals Peptides & Proteins Probiotics Minerals Functional Foods Challenges: Low water solubility Crystalline Chemical instability Enzyme digestibility Low bioavailability Flavor modulation Matrix incompatibility Targeted Delivery 1
2 Nutrient Delivery Systems: Structural Design Approaches Nanoemulsions Lipid Droplets Filled Lipid Droplets Multilayer Droplets Multilayer Liposomes Functional Microclusters Colloidomes Delivery Systems McClements Laboratory Hydrogel Beads Filled Hydrogel Beads Solid Lipid Nanoparticles Filled Liposomes Nutrient Delivery System Design: Performance Criteria Matrix Compatibility - Optical - Rheological - Stability - Flavor Processing - Heating - Cooling - Drying - Shearing Storage - Temperature - Mechanical stress - Light - Oxygen - Time Consumption - Appearance - Texture - Taste and Aroma - Convenience Ingestion - Digestion - Absorption - Toxicity Stable DELIVERY SYSTEM CRITERIA: Fabricated from food grade ingredients using economic processing operations. Designed to function over wide range of conditions in food product and human body. Sensory acceptance Controlled Instability 2
3 Enhancing Bioavailability: Designing Food Matrices to Control GIT Fate of Nutrients Bioavailability & Targeted Delivery Ensure nutrients remain stable within the product during storage Create molecular environment in GIT that increases bioavailability Deliver bioactive components to site of action within GIT: mouth, stomach, small intestine or colon Mouth, Stomach, Small Intestine Engineered Lipid Nanoparticles Digestion Colon Mixed Micelles Chylomicrons Improving Nutraceutical Bioactivity: Major Factors Limiting Bioavailability O O O α-tocopherol acetate Efflux Absorption HO O α-tocopherol Bioaccessibility Liberation & Solubilization Absorption Transport across Mucus Layer & Epithelium Cells Transformation Chemical or Biochemical Changes BA = B* A* T* B* = Bioaccessibility A* = Absorption T* = Transformation 3
4 Food Design to Improve Bioavailability: Delivery Systems versus Excipient Foods Nutrients Food Matrix Design & Structure Nutrient-Rich Food Dispersed within Physicochemical Properties Consumed with Delivery Systems Sensory Attributes Excipient Food GIT Fate Bioavailability McClements, D. J. and H. Xiao (2014). "Excipient foods: designing food matrices that improve the oral bioavailability of pharmaceuticals and nutraceuticals." Food & Function 5(7): Emulsion-based Delivery An emulsion consists of two immiscible liquids (usually oil and water), with one liquid being dispersed as very small spherical droplets in the other liquid. Potential Advantages: Incorporating Hydrophobic Nutrients & Nutraceuticals into Broad Range of Foods and Beverages Increased Bioavailability High energy methods Nanoemulsion Emulsion Low energy methods 4
5 Emulsion Design for Bioavailability Improvement: Tailoring Functionality Oil Type Particle Size Lipid Droplet Aggregation State Interfacial Properties Negative Neutral Positive Emulsion Design for Bioavailability Improvement: Liquid and Powdered Forms Spray Drop Feed Fluid Atomizer Solvent Drying Chamber Wall Material Encapsulated Oil Droplet Powder Particle Powder Collection Finishing: Agglomeration Coating Microencapsulation of nutrients by spray drying 5
6 Emulsion Design for Bioavailability Improvement: Effect of Particle Size Coarse Medium Fine Heptadecanoic Acid (mg/g tissue) Duodenum Jejunum Ileum Coarse (CO) Medium Fine (CO) Fine (MO) (CO) Droplet Properties Coenzyme Q10 nanoemulsions made from digestible or indigestible oils Emulsion Design for Bioavailability Improvement: Effect of Particle Bioaccessibility (%) Effect of Particle Corn oil MCT Orange Oil Type oil Small Mixed Micelles (MCT) Too large to fit inside micelle Effect of Particle Size Larger Mixed Micelles (Corn Oil) Fits in micelle -carotene nanoemulsions made from LCT (corn oil), MCT or indigestible oil (orange oil). 6
7 Food Design to Improve Bioavailability: Delivery Systems versus Excipient Foods Nutrients Food Matrix Design & Structure Nutrient-Rich Food Dispersed within Physicochemical Properties Consumed with Delivery Systems Sensory Attributes Excipient Food GIT Fate Bioavailability McClements, D. J. and H. Xiao (2014). "Excipient foods: designing food matrices that improve the oral bioavailability of pharmaceuticals and nutraceuticals." Food & Function 5(7): Excipient Emulsions: Impact of Lipid Content & Type on Carotenoid Bioaccessibility from Carrots 7
8 Excipient Emulsions: Enhanced Carotenoid Bioaccessibility in Supplements ENHANCED BIOACCESSIBILITY β-carotene BA (%) C BC A Tablet Soft gel Tablet + LCT ne Tablet + MCT ne Soft gel + LCT ne BC B Laura Salvia-Trujillo Conclusions Structural design principles are being developed to create food-grade delivery systems with improved efficacy These structurally designed systems can be fabricated from food grade ingredients using simple processing operations. These systems can be designed to improve food performance: Digestibility Controlled and Targeted Release Increased Bioavailability Modulate Satiety Economics and robustness of new functional foods needs to be assessed 8
9 Mechanism: Effect of Lipid on Carotenoid Bioaccessibility Does not fit Fits Well Digestion Lipase Fat Droplets Mixed micelles Digestion Micellization Solubilization Bioaccessible Testing Bioavailability & Bioactivity: In Vitro & In Vivo Methods Simulated Oral & Gastric Fluids Encapsulated Bioactive Simulated Intestinal Fluid Digestion Rate & Extent Fraction Released Time (s) Lipid phase Micelle phase Cell Culture Absorption (F A ) Bioaccessibility (F B ) Digestion ph-stat Titration Sediment phase Centrifugation Concentration Analysis Establish Physicochemical Mechanisms 9
10 Excipient Emulsion Design: Boosting Bioavailability Fat Droplet Size Fat Droplet Proteins Carbohydrates Acids, Bases, Buffers Chelating Agents Surfactants Antioxidants, Minerals Aqueous Phase Interfacial Properties Phospholipids Surfactants Polysaccharides & Proteins 10
Excipient Foods: Designing Food Matrices that Improve the Oral Bioavailability of Pharmaceuticals and Nutraceuticals
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- Most nutrients are absorbed before reaching the ileum. - Colon is responsible for final removal of electrolytes and water.
University of Jordan Department of physiology and Biochemistry Gastro-Intestinal physiology, Medical, Pt III. ---------------------------------------------------------------------------- Academic year:
The Digestive System. Prepares food for use by all body cells.
The Digestive System Prepares food for use by all body cells. Digestion The chemical breakdown of complex biological molecules into their component parts. Lipids to fatty acids Proteins to individual amino