Indian Journal of Pharmaceutical Education and Research Association of Pharmaceutical Teachers of India

Potential of Novel Drug Delivery Systems for Herbal Drugs

Ashwani Goyal1, Sandeep Kumar1, Manju Nagpal1*, Inderbir Singh2 and Sandeep Arora 1
1
School of Pharmaceutical Sciences, Chitkara University, Solan-174103 (HP)
2
Chitkara College of Pharmacy, Rajpura- 140401, Patiala (Punjab)

ABSTRACT Submitted: 23/7/2010 Revised: 1/2/2011 Accecpted: 3/4/2011

Recently the use of herbal medicines has been increased all over the world due to their miraculous therapeutic effects and fewer adverse effects
as compared to the modern medicines. However, delivery of herbal drugs also requires modifications with the purpose to achieve sustained
release, to increase patient compliance etc. Previously herbal drugs could not attract scientists towards the development of novel drug delivery
systems due to processing, standardising, extracting and identification difficulties. But now days with the advancement in the technology, novel
drug delivery systems opens the door towards the development of herbal drug delivery systems. Novel drug delivery technologies have gained
the importance to achieve modified delivery of herbal drugs thereby increasing the therapeutic value as well as reducing toxicity. For last one
decade many novel carriers such as liposomes, nanoparticles, phytosomes and implants have been reported for successful modified delivery
of various herbal drugs e.g. curcumin, quercetin, silybin, ginkgo etc. The objective of this review article is to summarize various novel drug
delivery technologies which have been developed for delivery of herbal drugs, to achieve better therapeutic response.
Key words: Phytosome, polymeric micelles, ethosomes, curcumin, nanoparticles, novel carriers.

INTRODUCTION the ease of administration in the paediatric and geriatric

patients. Various novel drug delivery systems such as
In the past few decades, considerable attention has been
liposomes, niosomes, microspheres and phytosomes have
focussed on the development of novel drug delivery systems
been reported for the delivery of herbal drugs. Incorporation
for herbal drugs. Novel herbal drug carriers cure particular
of herbal drugs in the delivery system also aids to increase in
disease by targeting exactly the affected zone inside a
solubility, enhanced stability, protection from toxicity,
patient's body and transporting the drug to that area. Novel
enhanced pharmacological activity, improved tissue
drug delivery system is advantageous in delivering the herbal
macrophage distribution, sustained delivery and protection
drug at predetermined rate and delivery of drug at the site of
from physical and chemical degradation. For example,
action which minimizes the toxic effects with the increase in
liposomes act as potential vehicles to carry anti cancer agents
bioavailability of the drugs. In novel drug delivery
by increasing amount of drug in tumour area and decrease the
technology, control of the distribution of drug is achieved by
exposure or accumulation of drug in normal cells/tissues
incorporating the drug in carrier system or in changing the
thereby preventing tissue toxicity effects4. The phytosomal
structure of the drug at molecular level1. Herbal drugs are carriers have been studied for effective delivery of herbal
becoming more popular in the modern world for their extracts of ginseng, ginkgo biloba etc. Direct binding of
application to cure variety of diseases with less toxic effects phosphatidylcholine to herbal extract components led to
and better therapeutic effects2. However some limitations of better absorption characteristics as compared to conventional
herbal extracts/ plant actives like instability in highly acidic delivery of herbal extracts. Other vesicular assemblies like
pH, liver metabolism etc. led to drug levels below therapeutic microspheres, nanoemulsions, polymeric nanoparticles etc.
concentration in the blood resulting in less or no therapeutic have been proved beneficial to carry herbal components. The
effect3. Incorporation of novel drug delivery technology to present review article was aimed to provide an overview of
herbal or plant actives minimizes the drug degradation or different types of drug delivery systems incorporating active
presystemic metabolism, and serious side effects by ingredients and potential advantages of such systems.
accumulation of drugs to the non targeted areas and improves
LIPOSOMES:

*Address for Correspondence: Liposomes are biodegradeable, colloidal and spherical

Manju Nagpal, Asst. Prof. (Pharmaceutics), School of Pharmaceutical Sciences, Chitkara vesicles (0.05-5.0 µm in diameter) composed of a bilayer
University, Solan-174103 (HP) membrane entrapping an aqueous core. Liposome
E-mail: [email protected] membranes can be composed of naturally-derived

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 Ashwani Goyal et al Potential of Novel Drug Delivery Systems for Herbal Drugs

phospholipids with mixed lipid chains and a variation of head polyethylene glycol. Both of the liposomal formulations
groups or of pure synthetic lipids with defined acyl chains and showed the increase in anxiolytic and cognitive effects.
head groups. The phospholipids align themselves side-by- Reduction in dose as well as increase in the bioavailability
side with their lipophilic heads orienting themselves towards was observed with the intranasal liposomes as compared to
each other. Drugs with widely varying lipophilicities can be oral administration. Hence, these proved to be potential
encapsulated in the liposomes, either in the phospholipids systems for delivery of quercetin to the central nervous
bilayer, in the entrapped aqueous volume or at bilayer system7. Hybrid liposomes of the silymarin extract were
interface. Liposomes usually formed from phospholipids reported for buccal administration using cholesterol and
have been used to change the pharmacokinetic profile of not stearyl amine for the treatment of liver disease. The
only drugs, but herbs, enzymes etc. Liposomal based drug interaction between the silymarin and phosopholipids led to
delivery is advantageous specifically in enhancing the increased permeation thereby increased bioavailability. An
therapeutic index of anti-cancer agents, either by increasing increase in mucoadhesion of these liposomal formulations led
the drug concentration in the tumour cells and by decreasing to the increase in hepatoprotective activity8.
the exposure to normal cells. Various targeting strategies can
Liposomes of Artemisia arborescens L. essential oil
be exploited using liposomal drug delivery. A variety of
(exhibiting antiviral activity) has been prepared by sonication
herbal liposomal formulations have been reported for herbal
technique using hydrogenated and non hydrogenated soy
drugs where liposome are able to enhance product
phosphotidylcholine. Increase in the stability and antiherpetic
performance by solubility enhancement, improving
activity was observed when liposomes were made using
bioavailability, targeting at site of action and prolonged
hydrogenated soy phosphotidylcholine9. Liposomes have
release of drug (Table 1).
also been used for the topical application of the capsaicin
Essential oil from rhizomes of Atractylodes Macrocephala where increase in the skin permeation as well as prolongation
Koidz has been entrapped into liposomes by using rapid of the duration of action was observed with the liposomal
expansion of supercritical solutions (RESS) technique. The formulation10. Inclusion of taxanes (antitumor activity) into
rhizome contains the essential oil and their oxide derivatives the liposomes led to decreased tissue related toxicities of the
which are useful for the treatment of various digestive drug with the increase in the efficacy of drug11.
diseases and tumours. Incorporation of oil into liposomes
MICROSPHERES:
improved the solubility thereby enhancing the bioavailability
of the essential oil obtained from Atractylodes Macrocephala Microspheres are spherical particles consisting of size ideally
Koidz with reduction in side effects. Similarily, the 1-300 µm. Each particle is matrix of the drug dispersed in the
antimicrobial activity of essential oil obtained from O. polymer and drug is released as a first order process. The
Dictamnus has been found to be increased after encapsulation polymers used for the fabrication of the microspheres are
into liposomes5. Extracts of Tripterygium wilfordi has been biodegradable or non biodegradeable. Various polymers have
incorporated into liposomes by thin film dispersion method, been used for fabrication of these microparticulate carriers
which led to increased stability at suitable temperature and such as Albumin, Gelatin, Modified Starch, Polypropylene,
reduced side effects6. Quercetin liposomes have been Dextran, Polylactic acid and Polylactide- co-glycolide etc.
prepared for oral and intranasal delivery by using mixture of The drug release is controlled by the dissolution and
egg phosphotidylcholine, quercetin and dispersion in degradation of the matrix. The release is effected by the size,

Table 1: Liposomal herbal formulations and their applications

Name of Bioactive Application Reference
Component/ Plant
Essential oil from Atractylodes Increase in solubility and bioavailability 5
macrocephala Koidz
Essential oil of O. dictamnus Increase in activity 5
Extracts of Tripterygium wilfordi Reduction in side effects 6
Quercetin Increase in bioavailability and 7
reduction in side effects
Silymarin extract Increase in hepatoprotective activity 8
Essential oil of Artemisia arborescens L. Increase in stability 9
Capsaicin Increase in permeation as prolongation of action 10
Taxanes Decrease in toxicity 11

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type of matrix and polymer concentration etc12. These industrial scale for the encapsulation of the herbal extracts18.
microparticulate systems are also advantageous as they can be Site specific delivery of rutin from its microspheres (rutin-
ingested or injected and tailored for desired release profiles. alginate-chitosan) was observed via targeting to
Various methods such as evaporation technique, ionic cross- cardiovascular and cerebrovascular regions19. Oxidised
linking technique have been reported for preparation of cellulose microspheres containing Camptothecin were
mucoadhesive, buoyant microspheres 1 3 - 1 4 . These prepared by using spray drying process, Oxidised cellulose
microparticulate systems are advantageous as they can be microspheres have been successfully used to enhance
ingested or injected, produce sustained release action and site solubility and cytotoxicity of Camptothecin20.
specific delivery. A number of plant ingredients have been NANOPARTICLES:
microencapsulated for various applications (Table 2).
Nanoparticles are the submicron size particles having size
Gastroretentive floating microspheres of silymarin have been
range 10 to 1000 nm.The main advantages of the
reported for sustained delivery of the drug. Prolonged release
nanoparticles is their stability and long term storage. The
of drug (12 hours) was achieved in simulated gastric fluid and
particle size and surface characteristics of nanoparticles can
resulted in increased drug bioavailability as well as patient
be easily modified for controlled and targeted drug delivery21.
compliance15. Microencapsulation of Zedoary turmeric oil
Nanosizing led to increased solubility of components,
into microspheres via emulsion-solvent diffusion has used
reduction in the dose via improved absorption of active
been used for bioavailability enhancement and sustained ingredient. Nanoparticles are efficient delivery systems for
release application16. Microspheres of turmeric oleoresin the delivery of both hydrophilic and hydrophobic drugs22.
were prepared after emulsification by using spray drying Some examples of nanoparticulate drug delivery system
technique. The stable emulsion product protected the resin incorporating herbal ingredients are depicted in Table 3.
from degradation from light, oxygen, heat and alkaline Controlled and sustained delivery of the paclitaxel
conditions and showed increased therapeutic effect17. nanoparticles is observed with reduction in toxic effects23.
Encapsulation of the herbal extracts of Piper sarmentosumn Curcumin obtained from the rhizomes of turmeric (Curcuma
was done by absorption with calcium alginate beads and it longa) has the anticancer activity but it is limited due to its
was found that there is no effect of method of encapsulation poor aqueous solubility which led to the poor bioavailability.
on the encapsulation efficiency so the process can be used at Nanoparticles containing Curcumin was prepared by using

Table 2: Microsphere herbal formulation and their applications

Name of Bioactive Application Reference
component/ Plant
Silymarin Sustained release 15
Zedoary turmeric oil Increase in bioavailability as well 16
sustained release occurs
Extract of Piper sarmentosumn Used for industrial scale 18
Rutin Specific delivery to cardiovascular 19
and cerebrovascular region
Campothecin Significant decrease in dose 20

Table 3: Nanoparticle containing herbal drugs and their applications

Name of Bioactive Application Reference
component/ Plant
Paclitaxel Reduction in side effects 23
Curcumin Increase in solubility 24
Cuscuta chinensis Increase in solubility 25
Triptolide Increase in solubility 26
Zedoary turmeric oil Increased stability and drug loading 27
Quercetin Increased drug release and antioxidant effect. 28
Taxol Sustained release 29
Silybinin Increase in circulation time 30
Paclitaxel and Doxorubicin Inhibition of resistance 31

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the mixture of crosslinked and random copolymers of N- range (limited/no passive diffusion) or due to poor
isopropylacrylamide (NIPAAM) with N-vinyl-2-pyrrolidone permeability through the lipid membranes resulting in poor
(VP) and polyethylene glycol monoacrylate (PEG-A). In vitro bioavailability. Some herbal components in extracts get
release studies revealed 40% curcumin release in 24 hours in destroyed in gastric environment, led to low bioavailability
phosphate buffer at physiological pH and no tissue related thereby limiting the clinical utility of these plant extracts.
toxicity was observed even at 20-fold void range of Complexation with some clinically useful nutrients such as
nanoparticles. The dispersion of nanocurcumin in aqueous phospholipids substantially improves the bioavailability of
media proved them as potential carrier for the treatment of the these active components. So these water soluble components
cancer as compared to free drug24. Cuscuta chinensis is a could be converted into the lipid compatible complexes by
Chinese drug containing flavonoids and lignins as active u s i n g t h e p h o s p h o l i p i d s f r o m s o y, m a i n l y
ingredients, used for nourishment of liver and kidney. Poor phosphotidylcholine. These are called as Phytosomes and can
aqueous solubility of active ingredients led to the poor easily cross the lipid membranes32. Phytosomes led to
absorption upon oral administration. C. chinensis enhanced solubility of the poorly lipid soluble drugs and
nanoparticles were prepared by using nanosuspension increase in the bioavailability was reported due to increased
method and compared with C. chinensis ethanolic extract for absorption in the GIT33. A number of methods have been
hepatoprotective and antioxidant effects upon oral reported for preparation of the Phytosomes 34-35 . In
administration. An oral dose of C.chinensis nanoparticles at phytosomes, the complexation of phospholipids and water
25 and 50 mg/kg showed almost similar hepatoprotective soluble active plant components involve chemical bond
activity as that of ethanolic extract of C. chinensis at 125 and formation and therefore more stable. Whereas in liposomes
250 mg/kg, fivefold reduction in dose was observed with no chemical bond is formed; phosphatidylcholine molecules
C.Chinensis nanoparticles25. Triptolide is known for the anti- simply surrounds the water soluble components.
inflammatory, immunosuppressive, anti-fertility and anti- Phospholipids are also employed as natural digestive aids and
neoplastic activities. The aqueous solubility of the drug is carriers for water soluble and lipid soluble nutrients36-38. Due
very poor and it shows some of the undesirable toxic effects. to improved absorption characteristics, phytosomes are more
Nanoparticles and microemulsions containing triptolide were bioavailable than conventional herbal extracts. A number of
prepared and evaluated for anti-inflammatory activity. The phytosomal formulations have been reported for the delivery
solid lipid nanoparticle formulation showed more anti- of poorly lipid soluble drugs like extracts of Ginkgo biloba,
inflammatory activity than the microemulsion when grape seed, hawthorn, milk thistle, green tea and ginseng34, 39-41
evaluated in the rat paw oedema model26. Nanocapsules of as shown in Table 4.
Zedoary turmeric oil was found to produce increased
TRANSFEROSOMES:
hepatoprotective and anticancer effect as they showed
improved stability and increased drug loading27. Quercetin Transferosomes are phospholipid vesicles which act as
nanoparticles were prepared by precipitation technique. potential carriers for the transdermal delivery of the drug as
Increased antioxidant activity was achieved via improved they overcome the difficulty of penetration through the
released characteristics of the drug (74 times higher drug stratum corneum and can easily penetrate through the
release)28. Taxol loaded nanoparticles were produced by intracellular pores of the skin due to their flexibility42-43
emulsion solvent evaporation method and enhanced Increased penetration through stratum corneum results from
bioavailability and sustained release of drug was observed hydration or osmotic force in the skin. Transferosomes are
with nanoparticles29. Solid lipid nanoparticles of silibinin fabricated by using phospholipids (act as vesicle forming
were prepared by using hand shaking method. The solid lipid material), surfactant (providing flexibility), alcohol (solvent)
nanoparticles show the hepatoprotective effects as well as and buffering agent (as Hydrating medium)42. Capsaicin
increase in the bioavailability due to increase in the transferosomes were prepared by the high shear dispersion
circulation time and solubility of the silybinin30. Inclusion of technique and the penetration of the capsaicin transferosomes
paclitaxel and doxorubicin to nanoparticles by using brij 78 was found to be more resulting better topical absorption as
surfactant led to the inhibition of p-gp mediated drug compared to pure drug44. Curcumin is used as potent anti-
resistance and hence increase in the anticancer activity of the inflammatory drug, but it shows poor bioavailability when
drugs31. given orally due to less absorption through GI tract.
Transferosomes containing the curcumin gel was prepared
PHYTOSOMES: and an increase in the permeation was observed when
Most of the biologically active components of herbal drugs compared with the simple gel through the skin, hence they act
are water soluble e.g. flavonoids, terpenoids etc. However, as potential carriers for the transdermal delivery of the
these are poorly absorbed due to their large molecular size curcumin45.Transferosomes of the vincristine sulphate were

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prepared by using lecithin and sodium deoxycholate in 70/20 be safe for the use. The increased permeability of the drug via
ratio. The in vitro tests showed that they can penetrate at zero ethosomal preprations led to increase in the bioavailability of
order rate through the skin46. Colchicine transferosomes were the drug as compared to the ethanolic solution of the drug50.
prepared by using hand shaking method. The transferosomal Ethosomes of the Triptolide were prepared for topical
preparation of colchicine prevents from the gastrointestinal delivery of the triptolide and evaluated in the rat model of
side effects associated with oral administration of the erythema. The ethosomal formulation showed an increase in
colchicine and provides the local, sustained and site specific bioavailability due to increase in the accumulation and
delivery of the colchicines47. reduction in erthema more rapidly as compared to the other
ETHOSOMES: formulations 51 . Ethosomes of alkaloids of Sophora
alopencerides were prepared by transmembrane pH gradient
Ethosomes are vesicles composed of phospholipids and high
concentration of ethanol. High concentration of ethanol in the technique. The ethosomal formulations led to increase in the
vesicles led to enhancement in their permeability through the permeability through the stratun corenum and are useful for
skin by fluidising the lipid domain of the skin. These carriers topical delivery of alkaloids52.
can penetrate through the skin deeply leading to improved NANOEMULSIONS/ MICROEMULSIONS:
drug delivery into deeper layers of skin and even into blood
circulation. These features make them as efficient carriers for Nanoemulsions and Microemulsions are the emulsions of
topical as well as transdermal route. They can be formulated O/W type having the size range of several microns. They are
by hot and cold methods and can be used for both lipophilic as prepared by using the surfactants which are considered safe
well as hydrophilic drugs. Ethosomes has been reported for for the human use and approved by the FDA. These types of
transdermal delivery of the hydrophilic and impermeable emulsions have higher surface area and hence can easily
drugs such as minoxidil, testosterone, bacitracin and penetrate through the skin. They are also non toxic and non
cannabidol48-49. Ethosomal suspensions of the ammonium irritant in nature and can be used in the animals and veterinary
glycyrrhizinate (Table 5) was prepared for the dermal purpose53.Nanoemulsions can be prepared by the high
administration and used for the treatment of the inflammatory pressure homogenization and microfluidisation technique54-57.
diseases of the skin. The ethosomal suspension showed no Nanoemulsions have been reported for the delivery of drugs
toxicity when applied for 24 hours (dermal) and was found to to cell culture, cancer therapy and as disinfectants58-59.

Table 4: Phytosomal Herbal Products

Phytosomes Source Use
Silybin Phytosomes Silybin flavonoids from Silybium marianum Hepatoprotective, antioxidant
for liver
Ginkgo Phytosomes Ginkgo flavoinoids from Ginkgo biloba Protects brain and vascular
linings.
Ginseng Phytosomes Ginsenosides from Panax ginseng Nutraceutical and
immunomodulator
Green Tea Phytosomes Epigallocatechin from Thea sinensis Anti cancer, Nutraceutical
Grape Seed Phytosomes Procyanidins from Vitis vinifera Nutraceutical, systemic
antioxidant, cardio protective.
Olive oil phytosomes Polyphenols from Olea europaea oil Antioxidant, anti-inflammatory

Table 5: Herbal Transferosomal and ethosomal formulations

Name of Bioactive component/ Plant Application Reference
Capsaicin Transferosomes Increased skin penetration 44
Curcumin Transferosomes Increased skin penetration 45
Vincristine Transferosomes Increase in permeability 46
Colchicine Transferosomes Reduction in GIT side effects 47
Ammonium Glycyrrhizinate Increased drug permeation through dermis. 50
ethosomes
Triptolide Increase in Bioavailability 51
Sophora alopencerides Increase in Permeability 52

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Curcumin which is used as anti-inflammatory drug have poor drug at predetermined rate and for predetermined time. This is
solubility when given orally. To increase the oral absorption the non-invasive route of drug administration; the drug
of the curcumin self microemulsifying drug delivery system present in the formulation permeates into the systemic
was formulated using the surfactant, cosurfactant and ethyl circulation by diffusion to stratum corneum and further to the
oleate. The increase in the oral absorption of curcumin was effected organ. There are various types of the transdermal
observed with the self microemulsifying drug delivery delivery devices which can be formulated by using the
system as compared to the simple emulsion60. Self polymer matrix, adhesive bandage and permeation
nanoemulsified drug delivery system (SNEDDS) was enhancers. Transdermal delivery system provides the
developed for the delivery of the ubiquinone which is based advantage of the controlled drug delivery, enhanced
upon the eutectic properties of the drug. This system led to bioavailability, reduction in side effects and easy
increase in the solubility thereby enhancing the application68. Transdermal drug delivery systems are
bioavailability of drug as well as decrease in the precipitation potentially used for the sustained delivery of the drugs up to
of the drug in the vehicle 61 . Microemulsion and several days or even months. Various vesicular systems are
Nanoemulsion formulations for various herbal bioactives also reported for the transdermal delivery of herbal drugs and
have been reported and depicted in Table 6. to increase the penetration and sustained action e.g.
transdermal films containing boswellic acid (Boswellia
POLYMERIC MICELLE FORMULATIONS:
serrata) and curcumin (Curcuma longa) were formulated for
Micelles exhibit easily controllable and good the treatment of inflammation. The combination was used to
pharmacological properties so they can be used to carry a produce the synergistic action of the drugs. The increase in the
number of drugs62-63. Micelles consists of an inner efficacy of the drug was observed with the formulation of
hydrophobic core capable of solubilizing lipophilic transdermal films69-70.
substances and an outer hydrophilic corona which serves as
the stabilizing interface between the internal hydrophobic IMPLANTS:
core and external aqueous environment64. Polymeric micelles These are the polymeric devices which are used for the
consist of hydrophobic core stabilized by the hydrophilic controlled and sustained delivery of the drugs. These are
polymer chains exposed to the aqueous environment. The size directly placed in the body fluids/cavities and are fabricated
of the polymeric micelles ranges from 10-100 nm65. by using biodegradable polymers. A microsurgery is always
Polymeric micelles have been reported for the delivery of the required for the insertion of these devices12. Implants of the
poorly soluble herbal drugs. Artemisinin from Artemisia extract of danshen (Radix Salviae Miltiorrhizae) were
annua L. and Curcumin from the roots of Curcuma longa L. developed using the chitosan and gelatin. This drug is used for
are used as antimalarial drugs, but these are poorly soluble healing of muscles and tissues in the abdominal cavities. The
drugs. Micelles formulations of these drugs with sodium sustained action was reported with these implants upto 28
dodecyl sulphate led to 25 fold increase in solubility of these days. The wounds and tissues were observed to be healed best
drugs66.The polymeric micellar formulation of paclitaxel led with this type of implantable system and also prevented the
to increase in the solubility of the drug. The micellar patient from frequent dosing71.
formulation of paclitaxel has been used for the treatment of
MICROPELLETS:
LNcap prostate tumours67.
These are the solid particles which fall in the range of 1-
TRANSDERMAL SYSTEMS:
1000µm. Controlled release pellets are used for the delivery
Transdermal drug delivery devices are the polymeric of drugs to specific sites and for the extended period of time.
formulations which are applied over the skin and deliver the These are also used for the delivery of the two incompatible

Table 6: Nanoemulsios and Microemulsion formulation of herbal bioactives

Name of the Bioactive component Target site/ biological activity Reference
Norcantharidin microemulsion Liver 76
Puerarin Microemulsion Cardiovascular and cerebrovascular disease 77
Ligustrazine hydrochloride microemulsion Intestinal obstruction after abdominal surgery 78
Silybin Nanoemulsion Liver 79
Berberine Nanoemulsion Tumor 80
Matrine Nanoemulsion Anti-bacterial, Anti- inflammatory, anti-virus 81

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drugs simultaneously at same or different sites. The main oral use is limited owing to its solubility. The solubility of the
advantage of the pellets is that it prevents dose dumping Curcumin was increased by the formation of the curcumin
which occurs with the conventional dosage forms. Pellets are soya lecithin complex and evaluated for the hepatoprotective
also used for the coating and taste masking of the activity. The in vitro permeation study of the complex showed
formulations 72 . Pectin-hydroxypropyl methylcellulose increase in the permeability of the drug leading to greater
(HPMC) coated curcumin pellets were prepared for delivery hepatoprotective activity as compared to the pure curcumin75.
of the curcumin in the colon to treat the inflammatory disease.
RECENT PATENTS ON HERBAL CONTROLLED
The release rate of the drug was found to be dependent on ratio
RELEASE FORMULATIONS:
of the Pectin and HPMC. The drug release from the pellets is
induced by the pectinolytic enzymes present in the colon. Some of recent patents on controlled release novel herbal
Therefore, these pellets were used for the delivery of the drug formulations are depicted in Table 7. This also illustrates plant
specifically to the colon73. Andrographolide (Andrographis actives along with type of dosage form that can be fabricated.
paniculata wall.) micropellets were prepared by adding CONCLUSION
sodium alginate into the sodium chloride solution. The
micropellets have been found to release the drug away from Herbal drugs/plant actives possess a lot of therapeutic
the upper part of GIT and prevents the GIT irritation problems potential that should be explored via application of novel drug
i.e. vomiting, loss of appetite and nausea74. delivery technology. Large molecular size, lipid solubility,
degradation in acidic stomach are certain problems which
COMPLEXATION:
limit the therapeutic activity of these extracts in vivo though
Solubility of the poorly soluble herbal drugs is the major these possess excellent bioactivity in vitro. Application of
problem in the formulation of appropriate dosage form. An novel drug delivery systems led to enhanced bioavailability of
appropriate solubility is must for the achievement of desired plant actives by increasing the permeability and solubility as
therapeutic concentration of the drug in systemic circulation. well as reduction in side effects. A number of plant
There are various methods by which solubility of the poorly constituents like flavanoids, tannins, terpenoids etc. showed
soluble drugs can be enhanced i.e. solid dispersions, enhanced therapeutic effect at similar or less dose when
microemulsions, eutectic mixtures and complexation etc. incorporated into novel drug delivery vehicles as compared to
Complexation is the association between the two or more conventional plant extracts. Hence there is great potential in
molecules to form a nonbonded entity with a well defined development of novel drug delivery system for valuable
stochiometry. Various complexing agents such as EDTA, herbal drugs as it provides efficient and economical drug
cyclodextrins and polymers have been used for the delivery and the trends of incorporating NDDS for herbal
complexation12. Curcumin is poorly soluble drug hence its drugs have also been adopted at industrial scale.

Table 7: Recent patents on novel herbal formulations

US patent No. Active ingrediant Novel System incorporate Reference
US 5948414 Opioid analgesic and aloe Nasal Spray 82
US 6340478 B1 Ginsenosides Microencapsulated and controlled 83
release formulations
Us6890561 B1 Isoflavones Microencapsulated formulation 84
US6896898 B1 Alkaloids of Aconitum Species Transdermal delivery system 85
US patent 2005/ Oleaginous oil of Sesamum Brain Tonic 86
0142232 A1 indicum and alcoholic extract of
Centella asiatica
US patent 2007/ Glycine max containing 7s Herbal Tablet dosage form 87
0042062 A1 globulin protein extract,
curcumin, Ginger officinalis
US patent 2007/ Opioid analgesic Transdermal patch 88
0077284A1 (phenanthrene gp)
US patent Flavonoids(such as quercetin) Microgranules 89
7569236132 and Terpenes (ginkgolide
A, B, C and J)

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ACKNOWLEDGEMENT 13. Kanan K, Karar PK, Manavalan R. Formulation and

evaluation of sustained release microspheres of
The authors are grateful to Dr. Ashok Chitkara, Chancellor,
acetazolamide by solvent evaporation technique. J
Chitkara University, HP, India and Dr. Madhu Chitkara, Pro
Chancellor, Chitkara University, HP, India, for support and Pharm Sci Res 2009; 1(1):36-39.
institutional facilities. 14. Das MK, Senapati PC. Furosemide loaded alginate
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