muco-adhesive drug delivery systems by -deepak kumar

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MUCO ADHESIVE DRUG DELIVERY SYSTEM 1.BUCCAL DDS 2.NASAL DDS

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MUCO ADHESIVE DRUG DELIVERY SYSTEM 1.BUCCAL DDS 2.NASAL DDS

MUCO ADHESIVE DRUG DELIVERY SYSTEM1.BUCCAL DDS2.NASAL DDS

1. BUCCAL DRUG DELIVERY SYSTEMSNovel drug delivery systems (NDDS) are the system where the man searches for new method of entry of drug into the body in order to show its activity in the body.The buccal mucosa lines the inner cheek and buccal formulation are placed in mouth between the upper gums and cheek to treat local and systemic conditions.It is richly vascularized and more accessible for the administration and removal of dosage form. High patient acceptability, extensive first pass metobolism.

1. BUCCAL TABLETSBuccal tablets are small, flat, oval (5-8mm) shaped dosage forms.Buccal tablets soften

Adhere to the mucosa

Retained in position until dissolution or release is complete

Tablets applied to various sites in oral cavity:-1.Palate 2.Mucosa lining the cheek 3. Between the lip and gum

Prepared by direct compression and sometimes wet granulation.Formulation of Nicorandil buccal tabletNicorandil HPMC K100M PVP K30 Magnesium stearateMannitol Carbopol 934P Aspartane Ethyl Cellulose

2. BUCCAL PATCH / FILMBuccal patch/film are laminates consisting of an impermeable backing layer, a drug containing reservoir layer from which the drug is released in a controlled manner, and a bioadhesive surface for mucosal attachment. Effective in oral disease.Two methods used to prepare adhesive patches- 1.Solvent casting 2.Direct Milling1.Solvent casting method

2.Direct Milling

An impermeable backing layer may also be applied to control, - The direction of drug release - Prevent drug loss - Minimize deformation and disintegration of the device during application periodFormulation of buccal patch of Atenolol - Atenolol - NaCMC - PVA - Sodium alginate - HPMC - Glycerine

2. BUCCAL GEL / OINTMENTBuccal gel or ointment such semisolids dosage forms have the advantage of easy dispersion throughout the oral mucosa.It has been overcome by using bioadhesive formulations.Certain bioadhesive polymers undergo a phase change from liquid semisolid this change enhances viscosity results in sustained and controlled release drugs.Formulation of in-situ gel of clotrimazole- - Clotrimazole - Carbopol - Sodium citrate - Gellan gum - HPMC - Calcium chloride

DOSAGE FORMSTABLETSPATCHESSEMI-SOLIDSSPRAYS1. Weight variationYY2. AssayYYYY3. ThicknessYY4. FriabilityY5. Disintegration timeYY6. Residue timeYY7. Tensile strengthY8. Folding enduranceY9. Viscosity10. Droplets sizeYY11. DissolutionYY12. Mucoadhesion stre.YY13. Permeability testYYYY

APPLICATIONS OF BUCCAL DELIVERY SYSTEMSSmoking cessation therapy. Eg- Nicotine patchesHormone replacement therapy. Hypertension. Eg- Atenolol patches.Angina pectoris. Eg- Nitroglycerine tablets / patches.Cancer. Eg- Opoid Analgesics.

1. NASAL DRUG DELIVERY SYSTEMSNasal route is an attractive alternative to invasive administrations and provides a direct access to the systemic circulation.About 2% of the overall drug delivery is administered via the nasal route.Drugs which are getting degraded in the acidic pH can be given through this route.

Parameters of Nasal AbsorptionMolecular size-(MW-1000 daltons, then molecular size is optimum-good absorption.Perfusion ratePerfusion volumeSolution pH - Nasal absorption is pH dependent.Drug Lipophilicity - Lipid soluble drugs are highly absorbed.Drug concentration Absorption depends on the initial concentration of drug.Particle size - (3-7 microns)reach the actual site of action.

MECHANISM OF NASAL ABSORPTION1.First MechanismIt involves an hydrophilic route of transportation.The absorption here is slow.It is also known as the paracellular route.2.Second MechanismIt involves a lipoidal route of transportation.Drug cross cell membranes by an active transport route via carrier mediated means or transport through the opening of tight junctions.It is also known as the transcellular process.

Enhancement in absorption Use of absorption enhancers Absorption enhancers works by increasing the rate at which the drug pass through the nasal mucosa. Ex- Surfactants, bile, salts, fatty-acids, phospholipids, etc.Increase in residence time Increase in residence time Increase in the higher local drug concentration in the mucous lining of the nasal mucosa is obtained. Ex-CMC, Methylcellulose, Polyacrylic acid

Administration of drug in form of microspheres Microspheres Good bioadhesive property Swell in contact with mucosa Advantages of using microspheres - Control the rate of clearance - Protect drug from enzymatic degradationEx Microspheres made of starch, albumin, gelatin and dextran.

4) Use of Physiological modifying agents These agents are vasoactive agents Exert their action by increasing nasal blood flow. Ex Histamine, terbutaline, etc.

EVALUATION OF NASAL FORMULATIONNasal diffusion cell is fabricated in glassLid has 3 opening in the diffusion-cell3 Opening Sampling, Thermometer, Donor tube chamberNasal mucosa of sheep was separated and stored in distilled water containing few drops at gentamycin injectionMucosal surface is attached to donor chamber tubeDonor chamber tube is placed in such a way that, it just touches the diffusion medium in recipient chamber(0.5 ml) Samples are withdrawnSamples are transferred to amber coloured ampoulesSamples subjected to suitable analytical techniques

IN-VITRO NASAL ABSORPTION STUDIES(RAT MODEL)Rat is anaesthesizedIncision is made in the neckTrachea is cannulated with a polyethylene tubeAnother tube is inserted through the oesophagus towards posterior region of nasal cavityDrug delivery toNostril / cannulation tubingBlood samples collected from femoral vein

RABBIT MODELRabbit is anaesthetized(IM Injection ketamine + xylazine)Rabbits head is held in an upright positionDrug deliveryNostrilBody temperature is maintained at 37oC,with the help of a heating pad.Blood samples collectedBy an catheter in the marginal ear vein or artery

MARKETED PRODUCTSOtrivin Spray ( Xylometazoline )Miacalcin Spray ( Calcitonin )Vibrocil Gel ( Phenylephrine, dimethindene maleate)Naset - P Drop ( Xylometazoline HCl )Nasoval H1N1 - Vaccine.

APPLICATIONS OF NASAL DRUG DELIVERY SYSTEMSDelivery of Non - peptide PharmaceuticalsDelivery of Peptide - based PharmaceuticalsDelivery of Diagnostic drugsCNS Delivery through nasal routeNasal Vaccination

REFERENCESY . W . CHEIN (NOVEL DRUG DELIVERY SYSTEMS)Google ImagesN .K. Jain, Introduction to Novel Drug Delivery Systems; 1st edition, 2010, page no: 223-242.www.authorstream.in

QUESTIONSWrite a note on nasal drug delivery system, describe about the development, evaluation and applications?

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