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PRACTICE SCHOOL REPORT
ON
HERBS AND NATURAL PRODUCTS IN HEALTH CARE
Submitted in Partial Fulfillment of the Requirements for the Degree of
Bachelors of Pharmacy
By
Priyansha Singh
B. Pharm 7th Semester, 2020-2021
(Registration no. 40317000025)
University Institute of Pharmaceutical Sciences
Panjab University, Chandigarh.
Subject expert- Prof. Maninder Karan
(University Institute of Pharmaceutical Sciences)
NOVEL DRUG DELIVERY SYSTEMS IN HERBAL DRUGS
Introduction
Recent advances in the understanding of pharmacokinetic & pharmacodynamic behavior of drug have offer a more rational approach
to the development of optimal drug delivery system. The novel drug delivery systems (NDDS) are carriers which maintain the drug
concentration in therapeutic range for longer period of time. NDDS aim to minimize drug degradation or loss, to prevent harmful side
effects and to improve drug bioavailability and also to favor and facilitate the accumulation of the drug in the required site.
The several advantages of novel drug delivery systems over conventional drug delivery are- Optimum therapeutic- drug concentration
in the blood or in tissue may be maintained over a prolonged period of time; Pre- determined release rates of extended period of time
may be achieved ;Duration for short half- life drug may be increased; By targeting the site of action, side effects may be eliminated;
Frequent dosing and wastage of the drug may be reduced or excluded and Better patient compliance may be ensured
Plants are nature remedies and have been used by human beings on earth since ancient times for food and medicine. Novel drug
delivery systems (NDDS) open the door towards the development of herbal drug delivery systems. Incorporation of herbal drugs in the
delivery system also aids to increase in solubility, enhanced stability, protection from toxicity, enhanced pharmacological activity,
improved tissue macrophage distribution, sustained delivery and protection from physical and chemical degradation.
Various kinds of novel herbal formulations such as polymeric nanoparticles, nano-capsules, liposomes, Phytosomes, nanoemulsions,
microsphere, Transferosomes, and Ethosomes have been prepared using bioactive plant extracts. Herbal products are considered as a
potential candidate for delivery through the novel delivery system because many natural compounds were shown to produce better
results without having side effects than many other drugs or surgical procedure; they can deliver mixtures of multi-functional
molecules with potentiating and synergistic effects and also they have a strong traditional or conceptual base and the potential to be
useful as drugs in terms of safety and effectiveness whereas modern medicines have a very strong experimental basis for their use but
are potentially toxic.
S.
No.
Name of
formulation
Overview Structure Advantages Disadvantages Applications
1. Phytosomes Encapsulates the plant
material or extract
within the spherical call
like structure thus
forming a cell form of
herbal products.
1. Enhances the absorption
of lipid insoluble polar
phytoconstituents (oral and
topical route) showing
better bioavailability.
2. Required in small
quantity with desired
results.
3. Have good skin
penetration and high lipid
profile so can be widely
used as a cosmetic product.
4. Used to give liver
protectant flavonoids.
_ 1. Phytosomes of
Silybummarianum which contains
liver-protectant flavonoids.
2. Phytosomes of Grape, the main
properties of procyanidin
flavonoids of grape seed are an
increase in total antioxidant
capacity and stimulation of
physiological defenses of plasma.
3. Phytosomes of naringenin
produced better antioxidant activity
with prolonged duration of action.
2. Nanoemulsion
s
Defined as oil-in-water
emulsions with mean
droplet diameters
ranging from 50-
1000nm.
1. Have higher surface area
and free energy.
2. Do not show creaming,
flocculation, coalescence
and sedimentation.
3. Can be taken by enteric
route because they are
formulated with surfactants.
4. Are non-toxic and non-
irritant.
1. Expensive
process.
2. Stability is
unacceptable.
3. Less
availability of
surfactant
required for
manufacturing.
1. Cosmetic preparations
Antimicrobial nanoemulsions
3. Prophylactic in bio terrorism
attack.
4. For mucosal vaccines.
5. For non toxic disinfectant
cleaner.
3. Ethosomes Vesicles composed of
phospholipids and high
concentration of ethanol.
1. Delivery of large
molecule is possible.
2. Non-toxic raw material
in formulation.
3. Enhances permeation of
the drug through the skin
(dermal and transdermal
delivery).
5. Low risk profile.
1. Poor Yield.
2. Loss of product
during transfer
from organic to
water media.
3. Drug that
require high blood
levels cannot be
administered.
1. Hormones transdermal delivery.
2. Enhanced topical delivery of
Tetrandrine for treatment of
arthritis.
3. Increase in Quercetin
bioavailability.
4. Nanoparticles The IUPAC defines a
nanoparticle as a particle
of any shape with
dimensions in the 1 ×
10−9
and 1 × 10−7
m
range.
The shapes of
nanoparticles may be
determined by the
intrinsic crystal habit of
the material, or by the
influence of the
environment around their
creation, such as the
inhibition of crystal
growth on certain faces
by coating additives, the
shape
of emulsion droplets
and micelles in the
precursor preparation, or
the shape of pores in a
surrounding solid matrix.
Nanoparticles occur in a
great variety of shapes,
which have been given
many informal names
such as nanospheres,
nanorods, etc.
1.improved bioavailability
by enhancing aqueous
solubility,
2. Increasing resistance
time in the body (increasing
half life for
clearance/increasing
specificity for its receptors)
targeting drug to specific
location in the body (its site
of action).
1. Difficult to
manufacture on a
large scale.
2. Nanoparticles
have bio-
acceptability
restrictions.
3. Physical
handling of
nanoparticles is
difficult due to
their size and
aggregation
property.
Nanoparticles are used for
biosensing, imaging, and drug
delivery; while for
environmental applications, they
are used for bioremediation of
diverse contaminants, water
treatment, and production of clean
energy.
5. Microspheres Microspheres are small
spherical particles
having diameter
between 1 to 1000
microns.
1. Size reduction leads to
increase in surface area
which can enhance solubili-
ty of the poorly soluble
drug.
2. Protects the GIT from
irritant effects of the drug.
3. Provide constant drug
concentration in blood
1. The costs of the
materials and
processing of the
controlled release
preparation are
higher.
2. Reproducibility
is less.
3. Process condi-
tions may influ-
ence the stability
of core particles
to be encapsulat-
ed.
1. Microspheres in drug delivery
are used for targeted as well as
prolonged drug release in the
diseased area. They are also used in
immunoassays.
2. They can also be used as a
platform to monitor coagulation by
light scattering.
6. Carbon
nanotubes
Carbon nanotubes are
allotrope of carbon with
a cylindrical
nanostructure. These can
be defined as seamless
cylindrical hollow
fibers, comprised of a
single sheet of pure
graphene.
1. CNTs are resistant to
temperature changes
therefore can be used in
extreme hot and cold
temperatures.
2. CNTs have good strength
and conductivity, therefore
can be used in preparing
improved composites.
3. CNTs can be
manufactured at a very low
cost with a small amount of
material.
1. In certain cases
nanotubes can
cross BBB which
can result in
toxicity and
therefore can lead
to serious immune
reactions.
2. Carbon
nanotubes show
crystallographic
defects which are
the defects related
to atomic
vacancies.
1. In medical science, Carbon
nanotubes are have been used in
drug delivery, as biosensors and in
cancer therapy.
2. Due to the thermal and
conductive properties of CNTs they
are also employed in making
antennas for radios, brushes for
commercial electric motors etc.
7. Niosomes Niosomes are
microscopic lamellar
structures formed on
admixture of anionic
surfactant, cholesterol
and a charge inducing
agent with subsequent
hydration in aqueous
media. These are formed
usually by non-ionic
surfactant of the alkyl or
dialkyl polyglycerol and
cholesterol.
1. Niosomes are able to
encapsulate large amount of
materials in a small volume
of vesicles.
2. Niosomes have better
patient adherence and
satisfaction and also better
effectiveness than
conventional oily
formulations.
3. Niosomes can entrap
wide range of chemicals
(hydrophilic, lipophilic and
amphiphilic drugs) due to
its unique structure.
1. Fusion
2. Aggregation
3. Leaking of
entrapment.
4.Physical
instability
5. Hydrolysis of
encapsulated
drugs which
limiting the shelf
life of the
dispersion.
6. inefficient drug
1. Drug-delivery systems using
Niosomes through transdermal,
parenteral, and ophthalmic routes
are available.
2. Niosomal delivery via
transdermal routes is able to
overcome the slow penetration rate
of conventional transdermal
approaches.
3. Colchicine as Prolonged release
niosomal preparation used to treat
rheumatic patients.
4. Silymarin niosomal preparation
Increases drug bioavailability and is
loading
7. Time
consuming.
used to treat liver and gallbladder
disorders.
8. Hydrogels Hydrogels are three-
dimensional network
structures able to imbibe
large amounts of water.
Hydrogels do not
typically dissolve due to
chemical or physical
cross-links and/or chain
entanglements. They
exist naturally in the
form of polymer
networks such as
collagen or gelatin, or
can be made
synthetically.
Typical chemical cross-
linked hydrogels are
often fabricated by
thermal, photo or
radiation initiated free
radical polymerization,
while physically cross-
linked hydrogels are
resulted from non-
covalent bonding
interaction at molecular
scale.
1. These were employed in
the field of pharmaceutics.
2. These may provides
several advantageous
properties such as inherent
biocompatibility,
biodegradability, and
biologically recognizable
moieties that support
cellular activities.
3. It can be modified to
yield the tailorable
degradability and
functionality.
1. The amount of
water Hydrogels
absorb decreases
greatly if there are
any ions in the
water.
2. Hydrogels are
very costly, which
limits their use to
high value crops
such as potted
ornamental plants,
landscape trees.
1. Skin wounds: Provides effective
photo thermal for the treatment of
infected wounds.2.Transparent
interpenetrating network (IPN)
Hydrogel: IPN shows real time
monitoring of wounds.
3. Rapid tissue repair of bacterial
infected wound: The antibacterial
ratio of the hydrogels could reach
up to 99.97% and 99.93% against
Staphylococcus aureus and
Escherichia coli. Thus, the
synthesized hydrogels have great
potential as a safe and efficient
wound dressing.
9. Liposomes Microsized spheres in
which aqueous core is
surrounded by
phospholipid bilayer.
Size- 100-1000 nm
Cholesterol acts as a
fluidity buffer on
addition to the
Solubility enhancement
Enhancement of
bioavailability
Programmed targeting
Stability associated
problems can also be
solved.
Absorption and disposition
of the constituents can also
be tailored.
Leakage and
fusion of
encapsulated drug
during storage.
Shorter half lives.
Production cost is
very high
Low stability.
1 Quercetin liposomes with
antioxidant properties for intranasal
administration.
2. Liposomes encapsulated
silymarin with hepato-protective
properties.
3. Colchicine liposomes with
antigout properties.
membrane.
10. Proliposomes They include a dry, free-
flowing, granular
material that
immediately forms a
uni- or multilamellar
liposomal dispersion on
contact with water or a
biological fluid within
the body.
Lipid and carrier are
coated into a soluble
carrier to form free
flowing granular
material.
Increase the dissolution of
a poorly soluble drug
Increase lipophilicity
Improve the permeability
Improve intestinal uptake
Decrease hepatic first-pass
metabolism
Ease of translating into a
desired dosage form
- -
11. Transferosome
s
Transferosomes is a
novel, elastic or ultra-
deformable vesicular
drug carriers system
composed of
phospholipid, surfactant
and water for enhanced
transdermal delivery.
Transferosomes are a
special type of
liposomes, consisting of
phosphatidylcholine and
an edge activator.
They are soft malleable
vesicles tailored for
enhanced delivery of
active agents.
They are biocompatible and
biodegradable as they are
made from natural
phospholipids similar to
liposomes.
They have high entrapment
efficiency, in case of
lipophilic drug around
90%.
They act as depot, releasing
their contents slowly and
gradually.
They protect the
encapsulated drug from
metabolic degradation.
Transferosomes
are chemically
unstable because
of their
predisposition to
oxidative
degradation.
Purity of natural
phospholipids
also proves as a
limitation.
Transferosomes
formulations and
manufacturing
aspects are
expensive.
1. Have been widely used as a
carrier for the transport of other
proteins and peptides.
2. Have the potential for the
controlled release of the
administered drug and increasing
the stability of labile drugs due to
incorporation of phospholipids.
3. Human serum albumin
encapsulated in Transferosomes
delivered by transdermal route.
4. Transferosomes improve the
overall safety margin of
corticosteroids.
Hndds (cognosy)

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Hndds (cognosy)

  • 1. PRACTICE SCHOOL REPORT ON HERBS AND NATURAL PRODUCTS IN HEALTH CARE Submitted in Partial Fulfillment of the Requirements for the Degree of Bachelors of Pharmacy By Priyansha Singh B. Pharm 7th Semester, 2020-2021 (Registration no. 40317000025) University Institute of Pharmaceutical Sciences Panjab University, Chandigarh. Subject expert- Prof. Maninder Karan (University Institute of Pharmaceutical Sciences)
  • 2. NOVEL DRUG DELIVERY SYSTEMS IN HERBAL DRUGS Introduction Recent advances in the understanding of pharmacokinetic & pharmacodynamic behavior of drug have offer a more rational approach to the development of optimal drug delivery system. The novel drug delivery systems (NDDS) are carriers which maintain the drug concentration in therapeutic range for longer period of time. NDDS aim to minimize drug degradation or loss, to prevent harmful side effects and to improve drug bioavailability and also to favor and facilitate the accumulation of the drug in the required site. The several advantages of novel drug delivery systems over conventional drug delivery are- Optimum therapeutic- drug concentration in the blood or in tissue may be maintained over a prolonged period of time; Pre- determined release rates of extended period of time may be achieved ;Duration for short half- life drug may be increased; By targeting the site of action, side effects may be eliminated; Frequent dosing and wastage of the drug may be reduced or excluded and Better patient compliance may be ensured Plants are nature remedies and have been used by human beings on earth since ancient times for food and medicine. Novel drug delivery systems (NDDS) open the door towards the development of herbal drug delivery systems. Incorporation of herbal drugs in the delivery system also aids to increase in solubility, enhanced stability, protection from toxicity, enhanced pharmacological activity, improved tissue macrophage distribution, sustained delivery and protection from physical and chemical degradation. Various kinds of novel herbal formulations such as polymeric nanoparticles, nano-capsules, liposomes, Phytosomes, nanoemulsions, microsphere, Transferosomes, and Ethosomes have been prepared using bioactive plant extracts. Herbal products are considered as a potential candidate for delivery through the novel delivery system because many natural compounds were shown to produce better results without having side effects than many other drugs or surgical procedure; they can deliver mixtures of multi-functional molecules with potentiating and synergistic effects and also they have a strong traditional or conceptual base and the potential to be useful as drugs in terms of safety and effectiveness whereas modern medicines have a very strong experimental basis for their use but are potentially toxic.
  • 3.
  • 4. S. No. Name of formulation Overview Structure Advantages Disadvantages Applications 1. Phytosomes Encapsulates the plant material or extract within the spherical call like structure thus forming a cell form of herbal products. 1. Enhances the absorption of lipid insoluble polar phytoconstituents (oral and topical route) showing better bioavailability. 2. Required in small quantity with desired results. 3. Have good skin penetration and high lipid profile so can be widely used as a cosmetic product. 4. Used to give liver protectant flavonoids. _ 1. Phytosomes of Silybummarianum which contains liver-protectant flavonoids. 2. Phytosomes of Grape, the main properties of procyanidin flavonoids of grape seed are an increase in total antioxidant capacity and stimulation of physiological defenses of plasma. 3. Phytosomes of naringenin produced better antioxidant activity with prolonged duration of action. 2. Nanoemulsion s Defined as oil-in-water emulsions with mean droplet diameters ranging from 50- 1000nm. 1. Have higher surface area and free energy. 2. Do not show creaming, flocculation, coalescence and sedimentation. 3. Can be taken by enteric route because they are formulated with surfactants. 4. Are non-toxic and non- irritant. 1. Expensive process. 2. Stability is unacceptable. 3. Less availability of surfactant required for manufacturing. 1. Cosmetic preparations Antimicrobial nanoemulsions 3. Prophylactic in bio terrorism attack. 4. For mucosal vaccines. 5. For non toxic disinfectant cleaner. 3. Ethosomes Vesicles composed of phospholipids and high concentration of ethanol. 1. Delivery of large molecule is possible. 2. Non-toxic raw material in formulation. 3. Enhances permeation of the drug through the skin (dermal and transdermal delivery). 5. Low risk profile. 1. Poor Yield. 2. Loss of product during transfer from organic to water media. 3. Drug that require high blood levels cannot be administered. 1. Hormones transdermal delivery. 2. Enhanced topical delivery of Tetrandrine for treatment of arthritis. 3. Increase in Quercetin bioavailability.
  • 5. 4. Nanoparticles The IUPAC defines a nanoparticle as a particle of any shape with dimensions in the 1 × 10−9 and 1 × 10−7 m range. The shapes of nanoparticles may be determined by the intrinsic crystal habit of the material, or by the influence of the environment around their creation, such as the inhibition of crystal growth on certain faces by coating additives, the shape of emulsion droplets and micelles in the precursor preparation, or the shape of pores in a surrounding solid matrix. Nanoparticles occur in a great variety of shapes, which have been given many informal names such as nanospheres, nanorods, etc. 1.improved bioavailability by enhancing aqueous solubility, 2. Increasing resistance time in the body (increasing half life for clearance/increasing specificity for its receptors) targeting drug to specific location in the body (its site of action). 1. Difficult to manufacture on a large scale. 2. Nanoparticles have bio- acceptability restrictions. 3. Physical handling of nanoparticles is difficult due to their size and aggregation property. Nanoparticles are used for biosensing, imaging, and drug delivery; while for environmental applications, they are used for bioremediation of diverse contaminants, water treatment, and production of clean energy. 5. Microspheres Microspheres are small spherical particles having diameter between 1 to 1000 microns. 1. Size reduction leads to increase in surface area which can enhance solubili- ty of the poorly soluble drug. 2. Protects the GIT from irritant effects of the drug. 3. Provide constant drug concentration in blood 1. The costs of the materials and processing of the controlled release preparation are higher. 2. Reproducibility is less. 3. Process condi- tions may influ- ence the stability of core particles to be encapsulat- ed. 1. Microspheres in drug delivery are used for targeted as well as prolonged drug release in the diseased area. They are also used in immunoassays. 2. They can also be used as a platform to monitor coagulation by light scattering.
  • 6. 6. Carbon nanotubes Carbon nanotubes are allotrope of carbon with a cylindrical nanostructure. These can be defined as seamless cylindrical hollow fibers, comprised of a single sheet of pure graphene. 1. CNTs are resistant to temperature changes therefore can be used in extreme hot and cold temperatures. 2. CNTs have good strength and conductivity, therefore can be used in preparing improved composites. 3. CNTs can be manufactured at a very low cost with a small amount of material. 1. In certain cases nanotubes can cross BBB which can result in toxicity and therefore can lead to serious immune reactions. 2. Carbon nanotubes show crystallographic defects which are the defects related to atomic vacancies. 1. In medical science, Carbon nanotubes are have been used in drug delivery, as biosensors and in cancer therapy. 2. Due to the thermal and conductive properties of CNTs they are also employed in making antennas for radios, brushes for commercial electric motors etc. 7. Niosomes Niosomes are microscopic lamellar structures formed on admixture of anionic surfactant, cholesterol and a charge inducing agent with subsequent hydration in aqueous media. These are formed usually by non-ionic surfactant of the alkyl or dialkyl polyglycerol and cholesterol. 1. Niosomes are able to encapsulate large amount of materials in a small volume of vesicles. 2. Niosomes have better patient adherence and satisfaction and also better effectiveness than conventional oily formulations. 3. Niosomes can entrap wide range of chemicals (hydrophilic, lipophilic and amphiphilic drugs) due to its unique structure. 1. Fusion 2. Aggregation 3. Leaking of entrapment. 4.Physical instability 5. Hydrolysis of encapsulated drugs which limiting the shelf life of the dispersion. 6. inefficient drug 1. Drug-delivery systems using Niosomes through transdermal, parenteral, and ophthalmic routes are available. 2. Niosomal delivery via transdermal routes is able to overcome the slow penetration rate of conventional transdermal approaches. 3. Colchicine as Prolonged release niosomal preparation used to treat rheumatic patients. 4. Silymarin niosomal preparation Increases drug bioavailability and is
  • 7. loading 7. Time consuming. used to treat liver and gallbladder disorders. 8. Hydrogels Hydrogels are three- dimensional network structures able to imbibe large amounts of water. Hydrogels do not typically dissolve due to chemical or physical cross-links and/or chain entanglements. They exist naturally in the form of polymer networks such as collagen or gelatin, or can be made synthetically. Typical chemical cross- linked hydrogels are often fabricated by thermal, photo or radiation initiated free radical polymerization, while physically cross- linked hydrogels are resulted from non- covalent bonding interaction at molecular scale. 1. These were employed in the field of pharmaceutics. 2. These may provides several advantageous properties such as inherent biocompatibility, biodegradability, and biologically recognizable moieties that support cellular activities. 3. It can be modified to yield the tailorable degradability and functionality. 1. The amount of water Hydrogels absorb decreases greatly if there are any ions in the water. 2. Hydrogels are very costly, which limits their use to high value crops such as potted ornamental plants, landscape trees. 1. Skin wounds: Provides effective photo thermal for the treatment of infected wounds.2.Transparent interpenetrating network (IPN) Hydrogel: IPN shows real time monitoring of wounds. 3. Rapid tissue repair of bacterial infected wound: The antibacterial ratio of the hydrogels could reach up to 99.97% and 99.93% against Staphylococcus aureus and Escherichia coli. Thus, the synthesized hydrogels have great potential as a safe and efficient wound dressing. 9. Liposomes Microsized spheres in which aqueous core is surrounded by phospholipid bilayer. Size- 100-1000 nm Cholesterol acts as a fluidity buffer on addition to the Solubility enhancement Enhancement of bioavailability Programmed targeting Stability associated problems can also be solved. Absorption and disposition of the constituents can also be tailored. Leakage and fusion of encapsulated drug during storage. Shorter half lives. Production cost is very high Low stability. 1 Quercetin liposomes with antioxidant properties for intranasal administration. 2. Liposomes encapsulated silymarin with hepato-protective properties. 3. Colchicine liposomes with antigout properties.
  • 8. membrane. 10. Proliposomes They include a dry, free- flowing, granular material that immediately forms a uni- or multilamellar liposomal dispersion on contact with water or a biological fluid within the body. Lipid and carrier are coated into a soluble carrier to form free flowing granular material. Increase the dissolution of a poorly soluble drug Increase lipophilicity Improve the permeability Improve intestinal uptake Decrease hepatic first-pass metabolism Ease of translating into a desired dosage form - - 11. Transferosome s Transferosomes is a novel, elastic or ultra- deformable vesicular drug carriers system composed of phospholipid, surfactant and water for enhanced transdermal delivery. Transferosomes are a special type of liposomes, consisting of phosphatidylcholine and an edge activator. They are soft malleable vesicles tailored for enhanced delivery of active agents. They are biocompatible and biodegradable as they are made from natural phospholipids similar to liposomes. They have high entrapment efficiency, in case of lipophilic drug around 90%. They act as depot, releasing their contents slowly and gradually. They protect the encapsulated drug from metabolic degradation. Transferosomes are chemically unstable because of their predisposition to oxidative degradation. Purity of natural phospholipids also proves as a limitation. Transferosomes formulations and manufacturing aspects are expensive. 1. Have been widely used as a carrier for the transport of other proteins and peptides. 2. Have the potential for the controlled release of the administered drug and increasing the stability of labile drugs due to incorporation of phospholipids. 3. Human serum albumin encapsulated in Transferosomes delivered by transdermal route. 4. Transferosomes improve the overall safety margin of corticosteroids.