Advances in Nutraceutical

ADVANCES IN
NUTRACEUTICAL
NAME: NAMRATA KRISHNA
BHIRUD.
F.Y.M. PHARMACY
(ROLL NO: 504)
Guided by: Dr. Mrs. N. S.
Ranpise.
(HEAD OF THE DEPARTMENT)
Quality
Purity
Trust

HISTORY
Greek physician Hippocrates, known as father of medicine.
“LET FOOD BE YOUR MEDICINE & MEDICINES BE YOUR
FOOD” the philosophy behind is: “FOCUS ON
PREVENTION.”
Modern nutraceutical industry began to develop in Japan
during the 1980s.
Ayurveda, the 5000 year old health science have mentioned
benefits of food for therapeutic purposes.
2
Ref.J. Beranal, J. A. Mendiola A Review on Advanced Anlysis of nutraceuticals, Journal of Pharmaceutical and
Biomedical Analysis55(2011)758-774
03/04/2017Namrata K. Bhirud

INTRODUCTION
Disease
treatment
Health
benefit
DRUG
NUTRACEUTICAL
PREVENTION
Nutrition + Pharmaceuticals= Nutraceuticals
3
03/04/2017
Namrata K. Bhirud

NUTRACEUTICAL DEFINITION
4
Originally, the term “Nutraceutical" was coined by
Dr. Stephen DeFelice, founder and chairman of the
foundation for innovation in medicine.
“A nutraceutical is any substance that is a food or a
part of a food and provides medical or health
benefits, including the prevention and treatment of
disease”.
Ref.- M. Prasad Palthur, Nutraceutical : conceptual definition, International journal Of pharmacy and
Pharmaceutical Science vol.2 issue 3,2010.

• “Nutraceutical” is any substance that may be considered a
food or part of a food and provides medical or health
benefits, encompassing, prevention and treatment of
diseases.
• A nutraceutical is, “any nontoxic food component that has
scientifically proven health benefits, including disease
treatment and prevention”.
5
Conti..,,
Ref.- M. Prasad Palthur, Nutraceutical : conceptual definition, International journal Of pharmacy
and Pharmaceutical Science vol.2 issue 3,2010. 03/04/2017
Namrata K. Bhirud.

CLASSIFICATION OF
NUTRACEUTICALS
Chyawanprash
Dietary Supplement
Vitamins &
Minerals
Protein Supplement
Herbal
Supplement
 Vitamins
 Minerals
 Protein Power & Lifestyle
Product
 Sport Nutrition
 Ayurvedic
extracts
 Plant extracts &
Phytochemicals
6

Functional Food
& Beverage
Market
Functional Food
Omega fatty
acid Fortified
food
Probiotic
fortified food
Branded
lodinated salt
Branded wheat
flour market
Functional
Beverage
Energy Drink Sport Drinks
Conti...
7
Ref.- Sateesh Kulkarni, ASA & Associates LLP, A Brief report on nutraceutical products in India
2015 03/04/2017
Namrata K. Bhirud

SOLID-DOSE NUTRACEUTICALS CHALLENGES
Formulating solid-dose nutraceutical products, such as
tablets, capsules and powders, can cause technical
challenges.
Most common multivitamin formulas contain up to 50 active
ingredients and two to eight excipients including coating
ingredients.
Traditional pharmaceutical formulations contain one to four
actives and five to six excipients.
8
03/04/2017
Namrata K. Bhirud

Higher numbers of active ingredients in nutraceutical
formulations bring challenges related to…
Particle size
Flow
Compressibility
Moisture sensitivity
Ingredient interaction
Content uniformity and Quality control (QC) testing
9

Active ingredients may be available in granular form, fine powder form
hydrophilic and others hydrophobic.
These ingredient blend may have many different particle sizes and
ingredients with a variety of characteristics.
Ingredient blends can also have segregation and flow issues.
Tablet production from these blends can result in-
Capping,
Sticking and
Different patterns on the faces of tablets during compression,
As well as basic content uniformity problems.
10

ACTIVE INGREDIENT TO EXCIPIENTS
RATIO
Nutraceutical formulations are likely to have more
actives present in higher weight than pharmaceutical
formulas.
The typical nutraceutical formulation has 70-90%
active drug.
While traditional pharmaceutical formulation has 70-
90 percent excipients and 10-30%active drug.
11
Ref.- A. Gandhi, Solid-Dose Nutraceuticals Pose Challenges Informa Dec.17,2012
03/04/2017
Namrata K. Bhirud

ROUTES OF NUTRACEUTICAL DELIVERY
Oral Delivery
Dermal Delivery
Ophthalmic Delivery
12

Nutraceutical Formulation Strategies
13
Formulation design will assist in improving the
physicochemical characteristics of nutraceutical
compounds and aid in the design of products that are
more efficacious in the treatment and prevention of
disease.
03/04/2017
Namrata K. Bhirud

Liposomal carrier systems
• Liposomes are ideal cosmetic delivery system used in
treatment and prevention of skin conditions.
• Liposomal phospholipid membrane is used to transport
active agents across the stratum corneum.
• And has proved to have successful improved dermal delivery
and deposition of vitamins to the skin.
14

• Drug delivery advantages to the similarity of liposomal
membranes to biological membranes.
• This property enables formulations to circumvent the barrier of
the skin and assists in protecting sensitive nutraceuticals from
UV exposure.
• Liposomal systems have also been employed in oromucosal
sprays for sublingual absorption of some nutraceuticals like
melatonin that showed improvements in bioavailability when
compared to the conventional tablet formulations.
15
Ref.- Miles C. Braithwaite, Charu Tyagi, Nutraceutical-based therapeutics and formulation strategies augmenting
their efficiency to complement modern medicine: An overview Journal of functional Foods 6 (2014) 82-99
03/04/2017
Namrata K. Bhirud

MARKETED PRODUCT
16
 NutraSpray Melatonin - Natural
Orange Flavor
 Dose: 1.3mg
 Sublingual
 Approximately 80 sprays
 Suggested Use: 1 to 3 sprays
before bedtime.
 It governs the body's circadian
rhythms, helping the body to
ease into restful sleep

Microsponges and Nanosponges
Micro and nano sponges are ‘‘non-collapsible’’ delivery systems that
contain porous micro and nanospheres.
It provide immense benefits in terms of their high internal surface area
and bioactive loading capacity.
The nanosponge complexes improve-
The in vitro release
Permeation
Efficacy and stability
And propose as suitable formulations for topical as well as buccal
delivery of the nutraceutical.
17

CYCLODEXTRIN COMPLEXATION
• Cyclodextrins (CD) and their derivatives have been widely
utilized as carrier compounds to improve the inherent
solubility, stability, permeation and bioavailability of
nutraceuticals to the body
• The liver protective nutraceutical, silymarin has particularly
low water solubility and bioavailability and also requires novel
formulation approaches for effective oral delivery.
• Silymarin-β CD complexes formed by a co-precipitation
method resulted in increased dissolution rates compared to
the nutraceutical.
18

19
Supplement Facts
Serving Size:2
Capsules (1g)
Servings Per Container:15
Two Tablets per day
MARKETED PRODUCT

BIODEGRADABLE HYDROGELS
• Many pharmaceutical polymers are stimuli-responsive and
degrade or swell to varying extents depending on the
physiological environment and changing thermal, pH, and
hydration stimuli.
• For most nutritive molecules, preferential absorption occurs in
the small intestine, and hydrogels may be used to facilitate
this process by protecting nutraceuticals from degradation or
denaturation and facilitating their controlled release.
20

• Milk protein gels are adept at pH-triggered release with
various bioactives.
• Vitamin B12 has been included in the casein hydrogel
matrix to facilitate the controlled release of the vitamin in
the body.
21Ref.- Miles C. Braithwaite, Charu Tyagi, Nutraceutical-based therapeutics and formulation strategies augmenting
their efficiency to complement modern medicine: An overview Journal of functional Foods 6 (2014) 82-99S
03/04/2017
Namrata K. Bhirud

Nanotechnology-based applications for
nutraceutical
delivery
• Nanotechnology has often been used to enhance the
solubility of poorly soluble nutraceuticals for
administration within a variety of dosage forms and is
also stated to achieve good bioavailability and
targeted delivery of the bioactives.
22

Nanosuspensions and Nanoemulsions
 Preparing nanosuspensions and nanoemulsions of
hydrophobic nutraceuticals, with poor solubility, improves
and enhances two key factors: dissolution velocity and
saturation solubility.
The nanosuspension can be lyophilised and incorporated in
creams and gels for dermal application and modified into
pellets to fill into hard gelatine capsules for oral dosing.
23

24
 The nanoformulation provided enhanced penetration
due to improved solubility and larger surface area.
 Nanoemulsions have also been used to effectively
deliver micronutrients such as carotenoids and fat
soluble vitamins (A, D, E, and K) within liposomes via
the oral route

SELF-EMULSIFYING DRUG DELIVERY
SYSTEMS (SEDDS)
Novel self-emulsifying DDs (SEDDSS) have been developed
and documented by different research groups as a means to
enhance the oral bioavailability of the nutraceuticals.
SEDDS of vitamin E to enhance bioavailability of the vitamin
after oral dosing has been investigated.
The researchers found that vitamin E delivered as SEDDS
resulted in a 2.5–4.5 times higher Cmax, a higher AUC and a
reduced lag time to absorption when compared to the non-
SEDDS formulation.
25

WHAT IS OMEGA-3 FATTY ACID?
Omega-3 fatty acid is an essential fatty acid
that plays an important role in brain function
and may help fight against cardiovascular
disease.
The American heart association recommends
a diet in which fatty fish, like salmon, herring,
sardines and tuna are consumed at least twice
26

Health benefits of omega-3 fatty acid
 Asthma
 Diabetes
 Arthritis
 Osteoporosis
 Some Cancers
 Skin Disorders
 High Cholesterol
 High Blood Pressure
 Attention Disorders
 Depressive Disorders
 Macular Degeneration
 Digestive Difficulties
27

Omega-3 fatty acids are found naturally
•Grains
•Spirulina
•Brazil nuts
•Hempseed oil
•Mustard seeds
•Pumpkin seeds
•Chia seed oil
•Wheat germ oil
•Canola oil (rapeseed)
•Green leafy vegetables
•Raw walnuts & walnut oil
•Flaxseeds or flaxseed oil
:
28

CASE STUDY
29
03/04/2017
Namrata K. Bhirud

CONCLUSIO
N
Compactible powders comprising β-cyclodextrin and ethyl esters or
triglycerides of omega-3 fatty acids dried utilizing various drying methods.
From freeze dried powders, the maximum amount of oil in a compactible
powder is up to 20% (w/w) for an ethyl ester powder and 30% (w/w) for a
powder.
The properties of tablets made from spray granulated powders show that
increased oil load.
Spray granulation is hence the superior drying method with respect to
obtaining a compactible omega-3 containing powder.
30

CASE STUDY
31

• Microsphere structures used as a versatile food-grade vehicle for
nutraceutical products is an important challenge to improve the uptake
and bioavailability of D3
• Optimal initial protein concentration βlactoglobulin : lysozyme ratio (v/v)
was 2:1.
• Microspheres effectively protected D3 against degradation during long-
term storage (4˚c) and against photochemical degradation.
• Storage (4̊ c) and against photochemical degradation.
• Versatile food-grade vehicle significantly increased the concentration of
25% D3 recovered in blood of rats compared to the free vitamin
treatments.
CONCLUSIO
N
32

Marketed Products
33

REFERENCES
34
 J. Beranal, J. A. Mendiola A Review on Advanced
Analysis of nutraceuticals, Journal of Pharmaceutical and
Biomedical Analysis55(2011)758-774
 M. Prasad Palthur, Nutraceutical : conceptual definition,
International journal Of pharmacy and Pharmaceutical
Science vol.2 issue 3,2010.
 Sateesh Kulkarni, ASA & Associates LLP, A Brief report
on nutraceutical products in India 2015
 A. Gandhi, Solid-Dose Nutraceuticals Pose Challenges
Informa Dec.17,2012
03/04/2017

35
Miles C. Braithwaite, Charu Tyagi, Nutraceutical-
based therapeutics and formulation strategies
augmenting their efficiency to complement modern
medicine: An overview Journal of functional Foods 6
(2014) 82-99
Tina Lien Vestlend, Oyvind Jacobsen, compactible
Power Of Omega-3 and β-cyclodextrin, Food
Chemistry185(2015) 151-158
F. Diarrassouba, G. Garrait, Food Protein-base
microspheres for increased uptake of vitamin D3,
Food Chemistry 173 (2015) 1066-1072
03/04/2017

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