Formulation development of Gymnema sylvestre

1. Development of formulation containing
Gymnena sylvestre & their
characterization for treatment of
diabetes
NAME: DIBYAJYOTI MUKHERJEE
M. PHARM. (PHARMACEUTICS)
1st Year 2nd Semester.
Dr. SUBHASISH MAITY (DIRECTOR)
and
MRS. PARAMITA PAUL (ASSISTANT PROFESSOR)
NSHM KNOWLEDGE CAMPUS, KOLKATA GROUP OF INSTITUTION
DEPARTMENT OF PHARMACEUTICAL TECHNOLOGY
Under the guidance of...

2. INTRODUCTION
Global survey:
Morbidity: Adults aged 20 and over:
• Percent with physician-diagnosed diabetes: 9.6% (2011-2014)
• Percent with undiagnosed diabetes: 3.0% (2011-2014)
• Number of deaths: 79,535
• Deaths per 100,000 population: 24.7
Treatment of Diabetes mellitus:
• Insulin and other anti-diabetic drugs
• One of the alternative medicines to both diabetes and obesity could be
Gymnema sylvestre plant preparation, as it known to have a good effect for
curbing of diabetes by blocking sugar binding sites and hence not allowing
the sugar molecules to accumulate in body.

3. OBJECTIVE
1. Development of formulation containing Gymnena
sylvestre
2. Characterization of the developed formulations for
the treatment of diabetes

4. Plan of work
• Literature survey of the plant Gymnema sylvestre, and various novel
drug delivery systems suitable to make the dosage form
• Selection and procurement of excipients
• Preformulation study
• Formulation and development of Gymnema sylvestre
• Physicochemical characterization of the developed formulations
• Compilation of data

5. “GURMAR” or SUGAR DESTROYER.
woody, climbing traditional medicinal herb which
has many therapeutic applications in Ayurvedic
system of medicine.
Best known for its leaf extract to suppress the
sweet receptors of the tongue. The active
ingredient that causes physiological reaction is
GURMARIN which is a poly-peptide made of 35
amino acids.
About Gymnena sylvestre..

6. Habitat of this plant..
•Found in the tropical forests of India and South-east Asia. It lives in
tropical temperatures with plentiful moisture.
•Common names include Gymnema, cowplant, Australian cowplant,
and Periploca of the woods. Also found in certain hilly areas of
Pakistan.
•Regarded as one of the plants with potent anti-diabetic properties.
•Gymnema sylvestre plant could be commonly distributed throughout
India in an attitude ranging from 300-700m.It is occasionally
cultivated as a medicinal plant.

7. Phytochemical constituents...
The primary chemical constituents includes:
Gymnemic acid: Anti-sweet compound
Tartaric acid: White crystalline organic acid.
Gurmarin: A polypeptide made of 35 amino acids.
Calcium oxalate: Calcium salt of oxalate.
Glucose: Sugar molecules made of six carbon atoms.
Stigmasterol: a phytosterol which have suger lowering property.
Betaine: an neutral cationic compound with positively charged
cationic functional group.
Choline: Choline is a water-soluble vitamin-like essential nutrient.

8. Mode of action..
It is an Ayurvedic plant known to act on the body’s glucose levels.
Though its mechanisms of action are not yet fully understood.
Recent studies have identified gymnemic acids and gurmarin
have hypo-glycemic properties. These compounds combat sugar
cravings by attaching themselves to specific receptors on the taste
buds and by binding to receptors in the gut, they reduces the
body’s absorption of sugar.
Other studies suggest that gymnemic acids imitate or stimulate the
activity of incretins, gastrointestinal hormones involved in insulin
secretion. The fresh leaves when chewed have the remarkable
property of paralyzing the sense of taste of sweet substance for
some time.

9. Proposed Formulation through Herbosome..
There are some benefits of herbosome formulations..
1) Potential enhancement of bioavailability.
2) Pharmacologically assured delivery to the different biological
tissues
3) Less dose requirement is due to absorption of chief constituent.
4) Drug loading efficiency can be increased by conjugating the drug
itself in with lipids in the vesicles formed.
5) Herbosomes shows better stability profile because chemical
bonds are formed between phosphatidylcholine molecules and
phytoconstituents.

10. Development of Formulation (Herbosome)..
Physicochemical characterization
Drug loading
Drug encapsulation efficiency
percentage drug released
Chemical composition
Preformulation study
FTIR: Fourier Transform Infrared Spectroscopy
DSC: Differential scanning calorimetry & etc.
Zeta potential (electrokinetic)
Particle size
Particle morphology
Membrane permeability,

11. Conclusion..
The leaves of the plant are widely used for the treatment of diabetes in India
proprietary medicine. G. Sylvestre, an ayurvedic herb, came to known as
“destroyer of sugar” from ancient times. Ayurveda physicians observed that
chewing a few leaves of G. sylvestre suppressed the taste of sugar. It is used
totally all over India for controlling blood sugar. Several bio-active
compounds have been isolated from the herb for diabetes care. Thus
formulation of G. Sylvestre could be a novel approach to enhance the
therapeutic activity of the active moiety present in it for prolonged time
period and to reduce its toxicity.

12. Literature survey
i. As early as 1980s, researchers have started to study the anti-diabetic effects of G. sylvestre leaf
extracts. G. sylvestre leave extract appears to have the benefits on supporting blood glucose
homeostasis of diabetic rats through increased serum insulin levels via repair or regeneration of
the endocrine pancreas. In diabetic rabbits, dried leaf powder of G. sylvestre regulated the blood
sugar levels by increasing the enzyme activities affording the utilisation of glucose by insulin
dependent pathways. Thus, G. sylvestre appears to correct the metabolic defects in liver, kidney
and muscle.
ii. In 1990, researchers started to conduct study of G. sylvestre leaf extract on human beings.
Researchers from India administered a water-soluble extract of the leaves of Gymnema sylvestre
to 27 patients with insulin-dependent diabetes mellitus (IDDM) on therapy63. They found that
the G. Sylvestre leaves extract enhance endogenous insulin. In another study of 22 Type 2
diabetic patients on conventional oral anti-hyperglycaemic agents, researchers applied G.
sylvestre leave extracts as supplements to these patients and five of the 22 diabetic patients were
able to discontinue their conventional drug and maintain their blood glucose homeostasis with
G. sylvestre leaf extract alone.
iii. Thousands of years ago, Type II diabetes was treated with Gymnema. The plant's sugar-
destroying property was revealed when a person chewed one or two leaves. Gymnema was said
to paralyze a person's tongue to the taste of sugar and bitter tastes. That taste-blocking reaction
lasted for several hours85-90. During that time, leaves supposedly provided a slight block to the
taste for salty foods, while the taste for acidic foods was not affected. By blocking the taste
buds from tasting sugar, Gymnema blocked sugar in the digestive system, resulting in a decrease
in blood sugar, also known as a hypoglycemic effect. This medicinal action has been studied
since the late 1930sR

13. Reference
1) Kokate CK, Purohit AP and Gokhale SB. Pharmacognosy, Nirali Prakashn. 21st edn,
Pune; 2002: pp 105-106, 111-113
2) Mall GK, Mishra PK, Prakash V. Antidiabetic and hypolipidemic activity of Gymnema
sylvestre in alloxan induced diabetic rats. Global journal of biotechnology &
biochemistry. 2009;4(1):37-42.
3) Duke JA. Handbook of medicinal herbs. CRC press; 2002 Jun 27.
4) Wiersema, John Harry; León, Blanca (1999). World Economic Plants: A Standard
Reference. CRC Press. p. 661
5) "Gymnema - Uses and Effectiveness". WebMD. Retrieved 2 June 2016.
6) Drury H. Hand-book of the Indian flora.
7) Fabio GD, Romanucci V, De Marco A, Zarrelli A (2014). "Triterpenoids from
Gymnema sylvestre and their pharmacological activities". Molecules (Review). 19 (8)
8) The Wealth of India. Raw materials, vol. IV. Council of Scientific and Industrial
Research; New Delhi: 1956. A Dictionary of Indian Raw materials and Industrial
products; pp. 276–277.
9) Komalavalli N., Rao M.V. In vitro micropropagation of Gymnema sylvestre:
multipurpose medicinal plant. Plant Cell, Tissue and Organ Culture. 2000;61:97–105.