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)

QualityPurityTrust

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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.

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

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INTRODUCTION

Disease treatment

Health benefit

DRUG

NUTRACEUTICAL

PREVENTION

Nutrition + Pharmaceuticals= Nutraceuticals


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NUTRACEUTICAL DEFINITION

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”.

03/04/2017Namrata K. BhirudRef.- M. Prasad Palthur, Nutraceutical : conceptual definition, International journal Of pharmacy and Pharmaceutical Science vol.2 issue 3,2010.

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• “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”.

Conti..,,

Ref.- M. Prasad Palthur, Nutraceutical : conceptual definition, International journal Of pharmacy and Pharmaceutical Science vol.2 issue 3,2010. 03/04/2017Namrata K.

Bhirud.

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CLASSIFICATION OF NUTRACEUTICALS

Chyawanprash

Dietary SupplementVitamins & Minerals

Protein Supplement

Herbal Supplement

Vitamins Minerals

Protein Power & Lifestyle Product

Sport Nutrition

Ayurvedic extracts

Plant extracts & Phytochemicals


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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...

Ref.- Sateesh Kulkarni, ASA & Associates LLP, A Brief report on nutraceutical products in India 2015 03/04/2017

Namrata K. Bhirud

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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.


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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


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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.


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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.

Ref.- A. Gandhi, Solid-Dose Nutraceuticals Pose Challenges Informa Dec.17,2012 03/04/2017

Namrata K. Bhirud

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ROUTES OF NUTRACEUTICAL DELIVERY

Oral Delivery

Dermal Delivery

Ophthalmic Delivery


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Nutraceutical Formulation Strategies

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.


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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.


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• 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.

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


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MARKETED PRODUCT

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


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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.



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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.



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Supplement FactsServing Size:2Capsules (1g)Servings Per Container:15Two Tablets per day

MARKETED PRODUCT


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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.



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• 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.

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) 82-99S


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Nanotechnology-based applications for nutraceuticaldelivery

• 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.



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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.

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 03/04/2017Namrata K. Bhirud

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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



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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.

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 03/04/2017Namrata K. Bhirud

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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 a week.


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Health benefits of omega-3 fatty acid

AsthmaDiabetes ArthritisOsteoporosis Some Cancers Skin Disorders

High CholesterolHigh Blood PressureAttention Disorders Depressive DisordersMacular Degeneration Digestive Difficulties


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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

:


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CASE STUDY


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CONCLUSION

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.


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CASE STUDY


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• 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.

CONCLUSION


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Marketed Products


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REFERENCES 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

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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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03/04/2017

advances in nutraceutical

Health & Medicine