The file is all about the modern and effective method for the development of natural products . and to explore the traditional system globally . the one who wants to make his product effective and stable he must follow these methods .
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Modern and effective methods in the development of natural products
1. Modern and Effective Methods In
the development of Natural
products .
• Mr. Nandkishor Rajankar .
• Mr. Tejas Sonawane .
Ty b Pharmacy , Maharashtra ,
India .
2. Intension :
Need to boost herbals and generate more potential in pharma life. No dought
there are some barriers which decreases the quality. But to give life to herbal
products . Its time to change Old methods with modern one while using
flourished techniques .
It will help to the new comers Recognize and understand the process to get
natural products in market.
The revolution in ayurveda can only brought by advancement and estab lishing
modern methods. In precise and effective way.
3. Content
Modern methods of Extraction of plant materials .
Isolation and identification of compounds .
Modern methods for distillation and chromatography .
In- vitro and in- vivo study .
Challenge and Opportunities.
In- silico study
Metabolosmicis study .
LC – NMR and LC- MS.
Conclusions.
4. Natural products.
Need To make more efforts .
1. Test large no of natural compound For therapeutic effect.
2. Discover new Ways to measure the effect of promising
effect .
3. Target drug delivery system .
4. Improve efficacy.
5. Drug Discovery and Development.
100,000 Molecules are tested By experimental Screening cost .
Cost of the screening is expensive.
Discovering new drug Is becoming Is more complex and consumes
more time .
Need to optimize all steps of the development of new drug discovery
obtained from nature.
6. Current Research in Drug Discovery
Medicinal plant drug discovery continues to
Provide new and important leads against
Various Diseases .
Several isolated compounds mainly from edible
plant species or plant used as dietary
supplement and created new form of dosage
form .
Though drug discovery from medicinal plant
continues to provide an vital source of new drug
leads numerous challenges are encountered.
7. Rejection of Natural products
in market?
There are so many reasons that herbal drugs fail to
reach to market. Lacking of safety and efficacy and
marketing .
Amongst 40% of compound fails because of poor
pharmaceutics property and too solubility ,
metabolic stability .
8. Selection of plant material.
Revives .
Traditional and ethnomedical uses.
Usage of reliable ethnobotanical data .
Collection of proper genera and species in traditional system.
9. Authentication of Raw material
Authenticated by certified botanist
Herbarium .
Chemotaxonomy and molecular biology are helpful for plant
identification
Correct identification of medicinal plant by voucher specimen herbarium
in need.
10. Basic operational steps .
Prewashing .
Drying .
Grinding .
Assure the API.
Active constituent not lost or destroyed
during extraction.
12. Solvent selection for Extraction :
Different solvent system are available to extract the active
constituent from the natural Compounds.
The extraction of hydrophilic Compound uses polar solvent Such
as ethanol methanol , ethyl acetate .
For extraction of more lipophilic compound dichloromethane
or mixture of dichloromethane and methanol in ratio 1: 1.
14. Pressurized liquid extraction:
Also known as acclerated solvent extraction,
enhanced solvent extraction, pressurized fluid
extraction .
PLE applies high pressure in extraction. High
pressure keeps solvent in a liquid state above their
boiling point. Which results in high solubility and
high diffusion And to high penetration of solvent in
matrix.
PLE has decreased consumption of of extraction time
and solvent had better repeatability compared to
other methods .
15. Supercritical fluid extraction:
SF has similar solubility to liquid and similar diffusivity to gas
and can dissolve a wide variety of natural products.
Their solvating properties dramatically changed near their
critical point due to small temp and pressure.
Supercritical carbon dioxide widely used in SEF because of
attractive merit such as low critical temp. non toxicity,
inertness, and capability to extract thermolabile compounds.
The low polarity od supercritical Carbon dioxide makes it ideal
for the extraction of non polar natural products such as lipid
and volatile oil.
16. Microwave assested extraction:
The transfer of heat and mass are in the same
direction in MAE which generates a synergistic
effect to accelerate extraction and improve
extraction yield.
The application of MEA is provide many
advantages such as increasing the extract yield
decreasing the thermal degradation and selective
heating vegetal material .
MAE is also regarded as green technology
because it reduces the usage of organic solvents.
17. Pulsed electric field extraction PEE:
PEE extraction significantly increases the
extraction yield and decreased the extraction time
.it can also increase mass transfer during
extraction by destroying membrane structures.
The effectiveness of PEE treatment depends on several
parameters include field strength , specific energy input
,pulse number and treatment temperature.
PEE extraction is non thermal method and
minimize the degradation of the thermolabile
compound .
18. Enzyme assisted extraction(EAE):
structure of cell membrane and cell wall micelles
formed by macromolecules such polysaccharides and
high temperature during extraction are the main barrier
to extraction of natural products.
The extraction efficacy can be improved by EAE due to
the hydrolytic action of enzyme on the component of
cell wall and membrane and the macromolecules inside
the cell which facilities the release of natural products.
Cellulose , α amylase and pectinase are generally
employed in EAE.
19. Isolation and identification :
TLC , column chromatography, flash
chromatography sephadex chromatography and
HPLC, should used to obtain pure compounds .
Based non chromatographic technique such as
phytochemical screening assay Fourier transform
infrared spectroscopy [FTIR ]AND Attenuated total
reflectance[ATR] can also be used to obtain and
facilitate the identification Of the bioactive
compound.
20. Concentration of the extraction
Rotary evaporator
Controlled pressure and
temperature .
21. Distillation.
Molecular distillation:
Molecular distillation separates the
molecule by distillation under vaccum at
temperature far below its boiling point .
It is suitable distillation method for
separating thermosensitive and high
molecular weight compounds .
23. Preparative gas chromatography
Gas chromatography with high separation efficacy and
fast separation and analysis makes potentially the ideal
preparative method for separation of volatile
compounds.
The injection port column split device and trap device
of GC equipment must be modified for preparative
separation due to a lack of commercial prep- GS .
Prep- GS has become an important separation method
for natural volatile compound.
24. Molecular imprinted technology
Many complementary cavities with the memory of size
shape and functional group of the template molecule are
removed from the molecular imprinted polymer (MIP).
Thus the template molecule and its analogs will have the
specific recognition and selective adsorption for the MIP.
MIP have been widely used in the separation of natural
products or as solid phase extraction sorbents for sample
preparation Of herbal material to enrich the minor
compounds.
25. Stimulated moving bed chromatography:
Stimulated moving bed chromatography uses multiple
column with stationary phases .
The countercurrent movement the bed is stimulated
through rotary valves which periodically switch the inlet
( feed and eluent) And outlet ( extract and raffinate )
The SMB process is a continuous separation method and a
powerful tool for the large scale separation of natural
products with the advantage of lower solvent consumption
over the shorter period of time .
26. Multi dimensional chromatography
separation.
The component In the extract subjected to separation were complex and generally no pure compound will
be separated in one column chromatography.
Multi dimensional separation based on the solid phase extraction and coupling of multiple columns with
different stationary phases greatly improves the separation efficacy.
With more commercial multiple Dimensional separation equipment entering the market the separation of
natural product is becoming more rapid ,efficient and automated .
27. Supercritical fluid chromatography
SFC uses supercritical fluid as the mobile phase.
SFC integrates the advantages of both GC and liquid
chromatography as a supercritical fluid process properties of high
dissolving property, high difficuity and low viscosity , which
allows rapid and efficient separation.
The SFC can use a longer column and smaller particles of the
stationary phase than HPLC which provide greater numbers of
theoretical plates and better separation.
SFC can be used for the separation of non volatile or thermally
labile compounds to which GC is not applicable.
28. Identification and characterization of
isolated compound
UV visible spectroscopy
IR Spectroscopy
1D and 2D NMR
spectroscopy
Mass spectroscopy
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29. In-vitro and In-vivo studies:
IN- VITRO : The data can provide meaningful insights to the
potential target and mechanism of action for a proposed active
compound . It considers all the pharmacodynamics and
pharmacokinetic .
The tests performed outside the living body ,with evaluation
parameter.
In vitro testing are may lead to further testing in in-vivo studies.
IN- VIVO: The study in which the effects of various biological entities
are tasted on whole living organism or cells and the product is
investigated .
The are many reasons to believe in in vivo studies have the potential
to offer conclusive insights about the nature of drug .
31. Challenges and opportunities in development of
natural products
Challenges: Natural products are typically isolated in small quantities
Insufficient for lead optimization, lead development and clinical trials.
Drug discovery of medicinal plant has been time consuming
Opportunities : collaborating with synthetic and medicinal chemist is necessary to determine if
synthesis or semi synthesis might be possible
Innovative and better methodologies for plant collection bioassay Screening.
Another technique to improve natural product and natural product like libraries that combine the
features of natural products with combinatorial chemistry.
32. Acceptance of natural products
Before there can be acceptance of natural products (NPs) Or
phytomedicines .
Questions related to.
1. Active ingredient .
2. Mechanism if action .
3. Toxicology .
4. Drug interactions.
Will need to be satisfactorily addressed .
35. In – Silico study
Increases the number of data base in order to reduce the number of
biological tests .
Use the drug ability laws (lipinskis< rule of five> ADME )to have
compound with good pharmacokinetic and pharmacodynamics
properties
Have specific database for a class of target .
Have a predictive binding modes of the molecule within the target
(docking).
36. In –silico study
Proper estimation of drugs- likeness features and profiling of potential
toxicity .
Promising therapeutic molecule binding energy scores and its non
toxic attritbutes .
in silico and studies of natural products strength the drug development
platform .
38. Metabolomicis study
Metabolomicis has been defined as “comprehensive and quantative
analysis of all metabolites.
it is used to study about natural products ‘’drug ability ‘’including
metabolites derived from natural products .
metabolic changes induced by natural products .
toxicity related to natural product
39. Metabolomicis study
Metabolomicis has the potential to make a powerful impact in preclinical
drug development studies including.
identification of new target .
elucidation of the mechanism of action of new drug .
development of safety and efficacy profile of new drug .
Absorption , distribution , metabolism , excretion of new drug .
40. LC- NMR AND LC-MS
Analysis of crude extract of natural products derived component the
technique is optimized for rapid identification of potential drug
candidates in plant product .
Detection of bulk drug impurities during drug stability tests the data
from LC-NMR /MS allows full characterization of all impurities
present in the drug .
42. Conclusions
o Natural products discovered from medicinal plants [and their
derivatives] have provided numerous clinically used medicines .
o Even with all the challenges facing drug discovery from medicinal
plants natural products isolated from medicinal plant can be predicted
to remain an essential component in the search for new medicines .
o As technology continues to develop more new automatic and rapid
technique have been created to extract and separete natural products
which might reach the requirement of high throught screening .
