FP2110 – Nutraceutical and Functional Foods

• Nutraceutical delivery through oral route is considered to be the most

acceptable and preferred route as it follows the same natural process of food
and nutrient consumption in the body, is non-invasive, and involves neither
special technique nor complex instructions.

• Functional foods and food supplements enriched with nutraceutical

compounds are effective in preventing chronic diseases such as diabetes,
obesity, cardio-vascular disease, inflammation, cancer.

• Functional foods are those that when consumed regularly exert a specific
health-beneficial effect beyond their nutritional properties.

• According to the International Food Information Council (IFIC),

functional foods are “foods or dietary components that may provide a
health benefit beyond basic nutrition”.
• As a vital macronutrient in food, protein possesses unique functional
properties which allow them to be an ideal material for encapsulation
of Nutraceutical compounds.

• Food biopolymers, specifically food proteins, are widely used in

formulated foods because they have high nutritional value and are
generally recognized as safe (GRAS) and possess unique functional
properties such as gelation, emulsification, foaming, water binding
capacity and stabilize food texture.

• Among the food proteins, Soy proteins are used extensively in food
manufacturing, because of their functional properties, low cost,
availability, and high nutritional value and degradable by digestive
enzyme
• Soybean (Glycine max L.) is currently one of the most abundant
sources of plant proteins.

• The enriched form of soy protein, known as soy proteins isolate (SPI),
has been reported to have high nutritional values and ingredient
functionalities.

• Soy protein Isolate (SPI) is an important component of soybeans and

provides an abundant source of dietary protein.

• Soy protein is unique among the plant-based protein because it is

associated with isoflavone, a group of compounds with a variety of
biological properties that may potentially benefit human health.
• Soy protein is considered a complete protein that it contains most of
the essential amino acids that are found in animal proteins.

• The nutritional value of soy protein is roughly equivalent to that of

animal protein of high biological value.

• SPI possesses a balanced composition of polar, nonpolar, and charged

amino acids, allowing a variety of drugs to be incorporated.

• In an aqueous environment, glycinin and β-conglycinin exist as

globular structures consisting of a hydrophilic shell and hydrophobic
kernel, together with a certain amount of small water-soluble
aggregates.
• Upon addition of dissolvent or cross linking agents, SPI molecules
continue to aggregate and form various structures such as
microspheres, hydrogels and polymer blends.

• Soy protein nanoparticles can be prepared either from a freshly

prepared SPI by desolvation or from the glycinin fraction of defatted
soy flour extraction using a simple coacervation method.

• Gel property makes the Soy protein an ideal coating material for the
encapsulation of bioactive compounds in the form of hydrogel, Tablet
and Microspheres.

• Gels of diverse mechanical and micro structural properties can be

formed by controlling the assembly of protein molecular chains, thus
offering the possibility of developing GRAS biocompatible carriers for
oral administration of sensitive nutraceuticals in a wide variety of
foods.
• Protein hydrogels are undoubtedly the most convenient and widely
used matrix in food applications.

• Soy protein hydrogel has the ability to protect the nutraceutical

compounds from hostile environment and to deliver them in response
to environmental stimuli such as pH and temperature.

• Soya protein acts as a substrate for the development of nutraceutical

delivery systems.

• Various strategies have been developed to protect and deliver

bioactive molecules such as Protein hydrogel, microparticles,
nanoparticles, etc.
 Hydrogel

• Biodegradable hydrogels have been widely researched to carry, protect

and modify the delivery of a wide variety of pharmaceutical
compounds including nutraceuticals.

• Over the past decade, hydrogels have been studied extensively in

biomedical and pharmaceutical applications, due primarily to their
ability to protect drugs from hostile environments and to deliver them
in response to environmental stimuli such as pH and temperature.

• A hydrogel is an infinite water-swollen network of hydrophilic

polymers that can swell in water and hold a large amount of water
while maintaining a network structure.
• New synthetic methods have been used to prepare hydrogels for a
wide range of drug delivery applications.

• Although successful as oral drug delivery systems, one of the inherent

limitations of these hydrogels for food applications is that they contain
components that are not generally recognized as safe for regular
consumption by healthy individuals.

• In the food industry, the use of food proteins to develop

environment-sensitive hydrogels for nutraceutical delivery constitutes
an interesting strategy.

• A fundamental advantage of this approach is that nutraceutical carrier

gels can stabilize food texture, which is a highly desirable
characteristic in the manufacturing of food products.
• Gelation of food proteins and particularly of globular proteins e.g.
soybean has attracted much attention over the years because of its
physicochemical and industrial significance.

• It is traditionally achieved through heat treatment.

• Depending on preparation technique, gels can exhibit different

microstructural properties, which are strongly related to aggregate
molecular structure.

• However, the heat needed to produce these gels limits their application
to formulations that do not contain heat-sensitive ingredients.
 Microparticles

• Protein-based Microparticles have found wide and rapidly increasing

applications in the food industry because they can be precisely
designed for use in many food formulations and virtually any
ingredient can be encapsulated, whether hydrophobic, hydrophilic, or
even microbial.

• A wide variety of processes have been developed to prepare

protein-based micro (sub-micro) particles.

• The most common techniques are spray drying, emulsifying-cross

linking or coacervation and cold-gelation.

• Soy protein isolate (SPI) use in microencapsulation has already been

studied by various authors.
• SPI is generally used as an individual coating material, but can also be
mixed with polysaccharides.

• The combination of proteins with carbohydrates as a carrier material

favors better protection, oxidative stability and drying properties.

• Due to SPI hydro solubility, microparticles are mainly produced using

the spray-drying technique but coacervation and gelation have also
been investigated.

• For Soy protein isolate, microencapsulation is carried out by spray

drying and coacervation technique.
 Nanoparticle

• In the last decades, the growth of nanotechnology has opened several

new possibilities in medical sciences, especially in the field of drug
delivery.

• Different new drug carrier systems in the micro- and nanometer size
range have been developed and the number of patents and products in
the drug delivery field has increased tremendously.

• Various nanotechnology platforms are being investigated at either the

developmental or clinical stages in order to obtain more effective and
safer therapeutics for a myriad of clinical applications.

• Nanoparticles have increasingly been used for a variety of applications,

most notably for the delivery of therapeutic and diagnostic agents.
• Natural biomolecules such as proteins are an attractive alternative to
synthetic polymers which are commonly used in drug formulations
because of their safety.

• In general, protein nanoparticles offer a number of advantages

including biocompatibility and biodegradability.

• They can be prepared under mild conditions without the use of toxic
chemicals or organic solvents.

• Moreover, due to their defined primary structure, protein-based

nanoparticles offer various possibilities for surface modifications
including covalent attachment of drugs and targeting ligands.
• Nanoparticles are solid colloidal particles ranging in size from about 10
nm to 1000 nm.

• The major goal in designing nanoparticles as a delivery system is to

control particle size, surface properties, and release of
pharmacologically active agents in order to achieve the site-specific
action of drugs at a therapeutically optimal rate and dosage regimen.

• Nanoparticle delivery systems offer certain distinct advantages for

drug delivery.

• First, the particle size, particle morphology, and surface charge of

nanoparticles can be controlled.

• Secondly, nanoscale drug delivery systems can carry or deliver a

variety of therapeutic and diagnostic agents such as small molecules
(hydrophilic or hydrophobic), peptides, proteins, and nucleic acids
while releasing the active molecules in a controlled manner.
• The entrapped molecules can be released from the nanocarriers in a
precise manner over time to maintain drug concentrations within a
therapeutic window, or they can be triggered to be released by some
stimuli unique to the delivery site.

• Thirdly, these nanocarriers can improve the solubility and stability of

encapsulated drugs, providing an opportunity to reevaluate drug
candidates that were previously ignored because of poor
pharmacokinetics.

• Lastly, site-specific drug delivery can be achieved using nanoparticles

delivered through various routes of administration.

• The nanocarriers can be engineered to have a prolonged circulation

time or to have enhanced cellular uptake and targeting abilities.
• The development of nanoparticle-based drug delivery systems is
rapidly growing due to their great therapeutic potential.

• Various types of materials including polymers, lipids, polysaccharides,

and proteins have been explored as drug delivery carriers.

• The selection of nanoparticle materials is dependent on many factors

including

(a) the size of nanoparticles needed,

(b) inherent properties of the drug such as aqueous solubility and
stability,
(c) drug release profile desired,
(d) surface charge and hydrophobicity of nanoparticles,
(e) biocompatibility and biodegradability of nanomaterials, and
(f) antigenicity and toxicity of the product.
• Biopolymer-based nanoparticles including protein nanoparticles have
gained considerable interest in recent years due to their many
desirable properties such as low toxicity and biodegradability.

• They are actively being developed for both pharmaceutical and

nutraceutical delivery.

• Proteins are a class of natural molecules that have unique

functionalities and potential applications in both biomedical and
material sciences.
• Nanoparticles derived from natural proteins are biodegradable,
metabolizable, and are easily amenable to surface modifications to
allow attachment of drugs and targeting ligands.

• Preparation of protein nanoparticles is based on balancing the

attractive and repulsive forces in the protein.

• It is generally accepted that increasing protein unfolding and

decreasing intramolecular hydrophobic interactions are crucial to the
formation of protein nanoparticles.

• Organic solvents such as acetone and ethanol have been used as

anti-solvents for the preparation of protein nanoparticles.
• Crosslinking stabilizes the protein nanoparticles and reduces
enzymatic degradation and drug release from the nanoparticles.

• Drugs can be loaded into particles by surface adsorption or by

entrapping the drugs in the particles during the preparation process.
Table: Typical composition of Soya Protein Isolate (Moisture-free basis)

Components % Weight

Protein 90.0

Fat 0.5

Ash 4.5

Total Carbohydrate 0.3

 Table: Soya Protein as carrier for nutraceutical compounds

Wall Material Core Material Dosages Form

Soy Protein isolate Riboflavin Tablets and Hydrogel

Soy Protein isolate Riboflavin Microspheres

Soy Protein isolate Curcumin Tablet

 Table: Microencapsulation with SPI based wall Materials

Microencapsulation Wall materials Core Materials

process
Spray - drying SPI Orange oil

Spray - drying SPI Flavour

Spray - drying SPI Casein Hydrolysate

Spray - drying SPI Alpha Tocopherol

Spray - drying SPI Fish oil

Spray - drying SPI Riboflavin

 Conclusions

• Delivery of nutraceuticals through oral route is considered to be the

most acceptable and preferred route.

• It follows the same natural process of food and nutrient consumption

in the body.

• This processing of soy protein does not require any special technique.

• Soy protein can be used as nanoparticles, coating materials for the

encapsulation of bioactive compounds, hydrogel in the formulation of
tablet and microspheres.

• Hence soy protein based nutraceutical delivery system has excellent

potential.