This document discusses novel drug delivery systems for herbal medicines. It begins by introducing how novel delivery can help herbal drugs be delivered at specific rates and sites of action, improving bioavailability. It then discusses various novel delivery approaches for herbal drugs like nanoparticles, liposomes, phytosomes, and nanoemulsions that can enhance solubility, bioavailability, stability and targeting of herbal medicines. Several studies examining specific herbal extract formulations employing these approaches are also summarized. The document concludes by discussing some commercialized herbal extract formulations utilizing novel delivery approaches.
2. INTRODUCTION
Novel drug delivery system is advantageous in delivering the
herbal drug at predetermined rate and delivery of drug at the site
of action which minimizes the toxic effects with the increase in
bioavailability of the drugs.
In novel drug delivery technology , control of the distribution of
drug is achieved by incorporating the drug in carrier system or in
changing the structure of the drug at molecular level .
. Herbal drugs are becoming more popular in the modern world
for their application to cure variety of diseases with less toxic
effects and better therapeutic effects.
3. The novel carriers should ideally fulfill two
prerequisites .
Firstly, it should deliver
the drug at a rate
directed by the needs of
the body, over the period
of treatment .
Secondly , it should
channel the active entity
of herbal drug to the site
of action
4. Scope.
In phyto -formulation research, developing nano dosage
forms (polymeric nanoparticles and nanocapsules ,
liposomes , solid lipid nanoparticles , phytosomes and
nanoemulsion etc .) have a number of advantages for
herbal drugs, including enhancement of solubility and
bioavailability, protection from toxicity, enhancement of
pharmacological activity, enhancement of stability,
improving tissue macrophages distribution , sustained
delivery, protection from physical and chemical
degradation etc . Thus the nano sized novel drug delivery
systems of herbal drugs have a potential future for
enhancing the activity and overcoming problems
associated with plant medicines
5. Drawbacks of conventional dosage forms
Poor patient compliance, increased chances of missing the
dose of a drug with short half life for which frequent
administration is necessary.
The unavoidable fluctuation of drug conc may lead to
under medication or over medication.
A typical peak valley plasma conc time profile is obtained
which make attainment of steady state condition difficult.
The fluctuations in drug levels may lead to precipitation of
adverse effects especially of a drug with small therapeutic
index whenever over medication occur .
6. Advantage of NDDS
Enhancement of solubility.
Increased bioavailability.
Protection from toxicity.
Enhancement of pharmacological activity
Enhancement of stability.
Improved tissue macrophages distribution.
Sustained delivery.
Protection from physical and chemical
degradation
7. Herbal formulation means a dosage form consisting of
one or more herbs or processed herb in specified
quantities to provide specific nutritional, cosmetic
benefits, and other benefits meant for use to diagnose
treat, or to alter the structure or physiology of human
beings or animals.
Herbal preparations are obtained by subjecting whole
plants, fragmented or cut plants, plants part to
treatment such as extraction, distillation, expression
fractionation, purification, concentration or
fermentation. This include comminuted or powdered
herbal substances , extract, essential oils, expressed
juices etc.
8. Advantages of herbal drugs
Low risk of side effect
More effectiveness.
Lower cost
Widespread availability
Limitation of Herbal drug
Not suitable for many disease
Lack of dosage instruction
Poison risk associated with wild herbs
Lack of regulation
Longer duration of treatment
9. Different novel drug delivery system for
herbal drug
Liposomes
Phytosomes
Ethosomes
Transferosomals
Nanoparticles
Microemulsions.
10. Liposomal formulations
Formulation Application Biological use Method of
Prepraation
Route of
administratio
n
Liposomes
encapsulated
silymarin
Improve
bioavailability
Hepatoprotecti
ve
Reverse
Evaporation
technique
Buccal
Curcumin liposome Long-circulating
with high
entrapment
efficiency
Anticancer Ethanol
injection
Garlicin liposome Increase
efficiency
Lungs
treatment
Reverse-phase
evaporation
Paclitaxel liposome High entrapment
efficiency
and PH sensitive
Anticancer Thin film
hydration
method
Catechins liposomes Increased
permeation
through skin
Antioxidant and
chemopreventive
Rotary
evaporation
sonication
method
Transdermal
Breviscapine
liposomes
Sustained delivery of
breviscapine
Cardiovascular
diseases
Double
emulsification
process
Intramuscular
11. Nano-structured herbal formulation
Formulation Application Biological use Method of
prepration
Route of
administration
Nanoparticles of
Cuscuta
chinensis
(Flavonoids
and lignans)
Improve water
solubility
Hepatoprotective and
antioxidant effects
Nanosuspension
method
Oral
Glycyrrhizic acid-
loaded
nanoparticles
Improve the
bioavailability
Anti-inflammatory,
antihypertensive
Rotary-evaporated
Film
ultrasonication
method
Curcuminoids solid
lipid
nanoparticles
Prolonged-
release of the
curcuminoids
Anticancer and
antioxidant
Micro-emulsion
technique
Zedoary turmeric oil
nanocapsule
Increase the
drug loading and
stability of ZTO
Hepatoprotection
Anticancer and
anti-bacterial
High pressure
Homogenization
method
Ginkgo biloba
nanoparticles
Improving the cerebral
blood flow and
metabolism
Brain function
activation.
High pressure
homogenization
method
Oral
12. Phytosomal formulations.
Formulation Application Biological use Method Route of
administration
Ginseng
phytosome
(Ginsenosides)
Increase
absorption
Nutraceutical,
immunomodulator
Phospholipids
complexation
150 mg Oral
Green tea
phytosome
(Epigallocatechin)
Increase
absorption
Nutraceutical,
systemic
antioxidant, anticancer
Phospholipids
complexation
50–100 mg
Oral
Grape seed
phytosome
Procyanidins
The blood TRAP
nTotalRadical-trapping
Antioxidant Parameter)
were significantly
elevated over the
control
Systemic
antioxidant,
cardio-protective
Phospholipids
complexation
50–100 mg
Oral
Curcumin
phytosomes
360 mg/
kg
Oral
Increase antioxidant
activity and
Increase bioavailability
Antioxidant,
anticancer
phospholipid
complexation
Antioxidant,
anticancer
Ginkgo biloba
phytosomes
Flavonoids
Flavonoids of
GBP stabilize
the ROS
Cardio-protective,
antioxidant
activity
Phospholipids
complexation
100 mg
and
200 mg/
kg
Subcutaneous
13. Emulsion herbal formulation.
Formulation Application Biological use Method route
Self-nanoemulsifying
Zedoary essential oil
Improved aqueous
dispersibility,
stability and oral
bioavailability.
Hepatoprotection
anticancer and
anti-bacterial
Drawing ternary phase
Diagram
Oral
Docetaxel submicron
emulsion
Improve residence
time
Anticancer High pressure
Homogenization
method
Intravenous
Quercetin
microemulsion
Enhance
penetration into
stratum corneum
and epidermis
Antioxidant High speed
Homogenization
method
Topical
Triptolide
microemulsion
Enhance the
penetration of
drugs through the
stratum corneum
by increased
hydration
Antiinflammatory High pressure
Homogenization
method
Topical
14. Transferosomes and Ethosomes
Formulation Application Biological use Droplet size route
Capsaicin
transferosomes
Increase skin
penetration
Analgesic 150.6 nm Topical
Colchicine
transferosomes
Increase skin
penetration
Antigout
Vincristine
transferosomes
permeation y
Increase
entrapment
efficiency and
skin
Anticancer 120 nm
Matrine ethosome Improve the
percutaneous
permeation
Antiinflammator
y
110±8 nm
Ammonium
glycyrrhizinate
ethosomes
Increase of the in vitro
percutaneous
permeation
Antiinflammator
y
350 nm to
100 nm
Topical
15. Marketed novel drug delivery
formulations of plant active and extracts.
Brand name Plant
active/extract
Type of NDDS Company
White tea
liposome
Herbasec®
Camellia sinensis
extract
Liposome Cosmetochem
Green tea
liposome
Herbasec®
Extract
Camellia sinensis Liposome Cosmetochem
White hibiscus
liposome
Herbasec®
White hibiscus
extract
Liposome Cosmetochem
Aloe vera
liposome
Herbasec®
Aloe vera
Extract
Liposome Cosmetochem
Guarana
liposome
Guarana extract Liposome Cosmetochem
16. Brand name Plant active/extract Type of NDDS Company
Escin ß-sitosterol
Phytosome®
Escin ß-sitosterol
from horse
chestnut fruit
Phytosome Indena
Leucoselect® Polyphenols from
grape seed
Phytosome Indena
Ginselect® Ginsenosides from
Panax ginseng
rhizome
Phytosome Indena
Visnadex ® Visnadin from
Ammi visnaga
umbel
Phytosome Indena
17. Patented Formulations.
Siliphos® Bioavailable silybin
Silymarin, the active ingredient of the plant (Silybum
marianum, Family Asteraceae)
Unfortunately, silymarin, and even more silybin, have a poor
intestinal absorption, that limits their benefits.
To overcome the poor bioavlability of silybin, Indena has
complexed it with soy phospholipids (non-GMO)
exploiting the Phytosome® technol
18. Pharmacokinetic study
Plasma levels of total silybin after oral Silipide® and silybin in rats, where Silipide® (200
mg/kg as silybin) and silybin (200 mg/kg) wmale rats were administered by gavage as
aqueous suspensions to 6
19. Ginkgoselect® Phytosome®
Bioavailable standardized extract of Ginkgo
biloba leaves.
Pharmacokinetic Study
Fifteen healthy volunteers were randomly divided into two
groups and administered respectively 160 mg of free formulation
of GBE (corresponding to 9.6 mg of terpene lactone) and 160 mg
of Ginkgoselect® Phytosome® (corresponding to the same
amount of terpee lactone).
The subjects switched formulations after a week of wash out.
Blood samples were collected at 30, 60, 120, 180, 240, 300 and
400 min after ingestion.
Ginkgolides A, B and bilobalide were absorbed to a higher extent
(about three-fold) after administration of
Ginkgoselect®Phytosome®.
20. As an example, the here reported chart, reports plasma
concentrations of ginkgolide A which, according to AUC,
shows a 3.5 folds higher absorption of the
Ginkgoselect®Phytosome®.
21. Meriva® Bioavailable curcumin
Meriva® is a patented formulation of curcumin, a
dietary phenolic, with soy lecithin. The two
compounds form a non-covalent adduct in a 1:2
weight ratio, and two parts of microcrystalline
cellulose are then added to improve formulation,
with an overall contents of curcumin of 20%.
22. Conclusion
Novel drug delivery systems of herbal drugs have a
potential future for enhancing the activity and
overcoming problems associated with plant
medicines.