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Novel drug delivery system based herbal formulations
Presented byAnirudh Padiyar
INTRODUCTIONNovel drug delivery system is advantageous in delivering theherbal drug at predetermined rate and delivery of drug at the siteof action which minimizes the toxic effects with the increase inbioavailability of the drugs. In novel drug delivery technology , control of the distribution ofdrug is achieved by incorporating the drug in carrier system or inchanging the structure of the drug at molecular level .. Herbal drugs are becoming more popular in the modern worldfor their application to cure variety of diseases with less toxiceffects and better therapeutic effects.
The novel carriers should ideally fulfill twoprerequisites . Firstly, it should deliverthe drug at a ratedirected by the needs ofthe body, over the periodof treatment . Secondly , it shouldchannel the active entityof herbal drug to the siteof action
Scope. In phyto -formulation research, developing nano dosageforms (polymeric nanoparticles and nanocapsules ,liposomes , solid lipid nanoparticles , phytosomes andnanoemulsion etc .) have a number of advantages forherbal drugs, including enhancement of solubility andbioavailability, protection from toxicity, enhancement ofpharmacological activity, enhancement of stability,improving tissue macrophages distribution , sustaineddelivery, protection from physical and chemicaldegradation etc . Thus the nano sized novel drug deliverysystems of herbal drugs have a potential future forenhancing the activity and overcoming problemsassociated with plant medicines
Drawbacks of conventional dosage forms Poor patient compliance, increased chances of missing thedose of a drug with short half life for which frequentadministration is necessary. The unavoidable fluctuation of drug conc may lead tounder medication or over medication. A typical peak valley plasma conc time profile is obtainedwhich make attainment of steady state condition difficult. The fluctuations in drug levels may lead to precipitation ofadverse effects especially of a drug with small therapeuticindex whenever over medication occur .
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 chemicaldegradation
Herbal formulation means a dosage form consisting ofone or more herbs or processed herb in specifiedquantities to provide specific nutritional, cosmeticbenefits, and other benefits meant for use to diagnosetreat, or to alter the structure or physiology of humanbeings or animals. Herbal preparations are obtained by subjecting wholeplants, fragmented or cut plants, plants part totreatment such as extraction, distillation, expressionfractionation, purification, concentration orfermentation. This include comminuted or powderedherbal substances , extract, essential oils, expressedjuices etc.
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
Different novel drug delivery system forherbal drug Liposomes Phytosomes Ethosomes Transferosomals Nanoparticles Microemulsions.
Emulsion herbal formulation.Formulation Application Biological use Method routeSelf-nanoemulsifyingZedoary essential oilImproved aqueousdispersibility,stability and oralbioavailability.Hepatoprotectionanticancer andanti-bacterialDrawing ternary phaseDiagramOralDocetaxel submicronemulsionImprove residencetimeAnticancer High pressureHomogenizationmethodIntravenousQuercetinmicroemulsionEnhancepenetration intostratum corneumand epidermisAntioxidant High speedHomogenizationmethodTopicalTriptolidemicroemulsionEnhance thepenetration ofdrugs through thestratum corneumby increasedhydrationAntiinflammatory High pressureHomogenizationmethodTopical
Transferosomes and EthosomesFormulation Application Biological use Droplet size routeCapsaicintransferosomesIncrease skinpenetrationAnalgesic 150.6 nm TopicalColchicinetransferosomesIncrease skinpenetrationAntigoutVincristinetransferosomespermeation yIncreaseentrapmentefficiency andskinAnticancer 120 nmMatrine ethosome Improve thepercutaneouspermeationAntiinflammatory110±8 nmAmmoniumglycyrrhizinateethosomesIncrease of the in vitropercutaneouspermeationAntiinflammatory350 nm to100 nmTopical
Marketed novel drug deliveryformulations of plant active and extracts.Brand name Plantactive/extractType of NDDS CompanyWhite tealiposomeHerbasec®Camellia sinensisextractLiposome CosmetochemGreen tealiposomeHerbasec®ExtractCamellia sinensis Liposome CosmetochemWhite hibiscusliposomeHerbasec®White hibiscusextractLiposome CosmetochemAloe veraliposomeHerbasec®Aloe veraExtractLiposome CosmetochemGuaranaliposomeGuarana extract Liposome Cosmetochem
Brand name Plant active/extract Type of NDDS CompanyEscin ß-sitosterolPhytosome®Escin ß-sitosterolfrom horsechestnut fruitPhytosome IndenaLeucoselect® Polyphenols fromgrape seedPhytosome IndenaGinselect® Ginsenosides fromPanax ginsengrhizomePhytosome IndenaVisnadex ® Visnadin fromAmmi visnagaumbelPhytosome Indena
Patented Formulations.Siliphos® Bioavailable silybinSilymarin, the active ingredient of the plant (Silybummarianum, Family Asteraceae)Unfortunately, silymarin, and even more silybin, have a poorintestinal absorption, that limits their benefits.To overcome the poor bioavlability of silybin, Indena hascomplexed it with soy phospholipids (non-GMO)exploiting the Phytosome® technol
Pharmacokinetic studyPlasma levels of total silybin after oral Silipide® and silybin in rats, where Silipide® (200mg/kg as silybin) and silybin (200 mg/kg) wmale rats were administered by gavage asaqueous suspensions to 6
Ginkgoselect® Phytosome®Bioavailable standardized extract of Ginkgobiloba leaves.Pharmacokinetic Study Fifteen healthy volunteers were randomly divided into twogroups and administered respectively 160 mg of free formulationof GBE (corresponding to 9.6 mg of terpene lactone) and 160 mgof Ginkgoselect® Phytosome® (corresponding to the sameamount of terpee lactone). The subjects switched formulations after a week of wash out.Blood samples were collected at 30, 60, 120, 180, 240, 300 and400 min after ingestion. Ginkgolides A, B and bilobalide were absorbed to a higher extent(about three-fold) after administration ofGinkgoselect®Phytosome®.
As an example, the here reported chart, reports plasmaconcentrations of ginkgolide A which, according to AUC,shows a 3.5 folds higher absorption of theGinkgoselect®Phytosome®.
Meriva® Bioavailable curcumin Meriva® is a patented formulation of curcumin, adietary phenolic, with soy lecithin. The twocompounds form a non-covalent adduct in a 1:2weight ratio, and two parts of microcrystallinecellulose are then added to improve formulation,with an overall contents of curcumin of 20%.
Conclusion Novel drug delivery systems of herbal drugs have apotential future for enhancing the activity andovercoming problems associated with plantmedicines.