buccal drug delivery system


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buccal drug delivery system

  1. 1. Buccal Drug Delivery System<br />PRESENTED BY <br />DANISH KURIEN<br />M.PHARM FIRST YEAR<br />DEPT. OF PHARMACEUTICS<br />KLE UNIVERSITY’S <br />COLLEGE OF PHARMACY BELGAUM<br />10/28/2010<br />1<br />
  3. 3. Introduction<br />The Buccal mucosa lines the inner cheek<br />Placed between the upper gingivae and cheek<br />Treat local and systemic conditions<br />An ideal dosage regimen in the drug therapy of any disease. <br />3<br />
  4. 4. 4<br />
  5. 5. Mucoadhesion can also be explained on the basis of molecular interactions composed of attractive (Vander Waal’s, Hydrogen bonding) and repulsive (Electrostatic, steric)forces.<br />Biological membrane- the membrane of internal tract e.g.-GIT, buccal cavity, eye, nose ,vagina ,rectum are covered with a thick gel like structure know as mucin<br />All polymer bind to mucin<br />5<br />
  6. 6. 6<br />Impermeable membrane (1)<br />Drug polymer layer (2)<br />Mucoadhesive polymer layer (3)<br />(1)<br />(2)<br />Mucous membrane saliva action <br />Results in swelling<br />(1)<br />(2)<br />(3)<br />Mechanism of Absorption from a MucoadhesiveBuccal Drug Delivery System<br />Drug release<br />Attachment<br />Internal jugular vein<br />Bypasses first pass metabolism<br />Systemic circulation<br />Drug Release<br />
  7. 7. Mechanism of bioadhesion<br />The bioadhesion mainly depends upon nature of bioadhesive polymer .<br />First stage involves an intimate contact between a bioadhesive & a membrane.<br />Second stage involves penetration of the bioadhesive into tissue.<br />Drug released.<br />Bypasses first pass metabolism<br />Enters systemic circulation.<br />7<br />
  8. 8. Advantages<br />1.Termination of therapy is possible <br />2. Permits localization of drug to the oral cavity for extended period of time. <br />3. Ease of administration <br />4.Avoids first pass metabolism. <br />5.Reduction in dose can be achieved <br />6.Selective use of therapeutic agents like peptides, proteins and ionized species can be achieved. <br />8<br />
  9. 9. 9<br />7. Drugs which are unstable in acidic environment of stomach or destroyed by the alkaline environment of intestine can be given by this route <br />8. Administration of drugs with poor bioavailablity<br />9. It follows passive diffusion. <br />10. Dissolution of drug is easy unlike in case of rectal and transdermal route. <br />
  10. 10. 10<br />11.Administration of Drugs with short half life.<br />12. Prolongation of contact time with mucosa.<br />13.Flexibility in shifting the position of the drug in buccal cavity. <br />
  11. 11. Disadvantages<br />11<br />1. Over hydration<br />2. Eating and drinking may become restricted <br />3. By mistake tablet can be swallowed <br />4. Saliva takes some drug into git<br />5.Only drug with small dose requirement can be administered.<br />6.Drug which irritate mucosa or have a bitter or unpleasant taste or an obnoxious odour cannot be administered by this route<br />7. Drugs which are unstable at buccal pH cannot be administered by this route. <br />8. Only those drugs which are absorbed by passive diffusion can be administered by this route <br />
  12. 12. Anatomy & Physiology of Oral Mucosa<br />The oral cavity is lined by thick dense & multilayered mucous membrane of highly vascularized nature. <br />Drug penetrating into the membrane passes through net of capillaries & arteries and reaches the systemic circulation.<br />There are mainly three functional zones of oral mucosa:-<br />12<br /><ul><li>Masticatory mucosa
  13. 13. Mucous secreting region
  14. 14. Specialized mucosa</li></li></ul><li>Oral mucosa<br />mucous membranes / mucosae / singular mucosa :-<br />That are linings of mostly endodermal origin, covered in epithelium, which are involved in absorption and secretion . <br />They line various body cavities that are exposed to the external environment and internal organs . It is at several places continuous with skin - at the nostrils , the lips , the ears , the genital area , and the anus .<br />The sticky thick fluid secreted by the mucous membranesis termed mucus . <br />13<br />
  15. 15. Structure of mucous membrane<br />14<br /> a. Fibrous covering.<br /> b. Divided fibers of<br /> longitudinal muscular<br /> coat<br /> c. Transverse muscular<br /> fibers<br /> d. Submucous or areolar<br /> layer.<br /> e. Muscularis mucosae<br /> f. Mucous membrane,<br /> with vessels and part<br /> of a lymphoid nodule<br /> g. Stratified epithelial<br /> lining<br />
  16. 16. The average thickness of various regions of the human oral mucosa<br />Epithelium :- <br /><ul><li>Basement membrane :- Boundary between basal layer (epithelium) & connective tissue (lamina propria & submucosa)
  17. 17. Submucosa layer :-</li></ul>Mucus : Secreted by goblet cells / special endocrine glands<br />Connective tissue : Collagen, elastic fibers, cellular components.<br />15<br />
  18. 18. Secretion of saliva<br />16<br />About 1.5 Liters of saliva is secreted daily<br />Chief secretions by : Parotid, sub mandibular, sublingual glands<br />Minor salivary glands are situated in buccal, palatal regions<br />The presence of saliva is more important for:-<br /><ul><li> Drug dissolution
  19. 19. Drug permeation (across mucous membrane).</li></li></ul><li>17<br />Function of oral mucosa <br />Provide protection<br />Acts as a barrier<br />Provides adhesion<br />Keep the mucosal membrane moist<br />Regional Differences In Mucosal Permeability<br />Permeability : Intermediate between epidermis & intestinal mucosa<br />Permeability of oral mucosa :<br />sublingual > buccal > palate<br />Palate(keratinized), sublingual (thinner & immersed in saliva)<br />
  20. 20. Transport of Material Across the Oral Mucosa (Transmucosal Permeability)<br />Drugs may cross a cell membrane by <br />Passive diffusion, <br />Facilitated diffusion, <br />Active transport <br />Pinocytosis<br />Factors To Be Considered In The Transmucosal Permeability<br />Liphophilicity of drug<br />Salivary secretion<br />pH of saliva : Around 6 favour absorption<br />Binding to oral mucosa<br />Oral epithelium thickness<br />18<br />
  21. 21. Routes of Drug Transport<br />19<br />CELL MEMBRANE<br />Two routes of drug transport :-<br />Paracellular<br />Transcellular<br />Paracellular Route :-<br />Primary route for hydrophilic drugs Intercellular spaces is the preferred route<br />Transcellular Route :-<br />Route for lipophillic compounds Lipophillic drugs passes through lipid rich plasma membranes of the epithelial cells. <br />TRANSCELLULAR<br />PARACELLULAR<br />
  22. 22. Ideal Candidates for Buccal Drug Delivery System<br />Molecular size <br />Molecular weight.<br />Drug nature.<br />BuccalpH.<br />Taste<br />Drug should be odourless.<br />Drugs following passive diffusion be used.<br />10/28/2010<br />Department Of Pharmaceutics<br />20<br />
  23. 23. Mimosa Membrane<br />
  24. 24. The Fluid Mosaic Model is used to describe the interactions of lipids and proteins in biological membranes.<br />Fluid mosaic model is two dimensional model, which depicts a biological membrane composed of a fluid state lipid bilayer embedded with globular integral proteins.<br />The integral membrane protein may also exist as sub-unit aggregates, which span through entire thickness of the lipid bilayer to form a continuous water-filled channels.<br />
  25. 25. Permeability Enhancers <br />Definition :<br />Substances added to pharmaceutical formulation in order to increase the membrane permeation rate or absorption rate of coadministered drug.<br />E.g. :By using di- and tri-hydroxy bile salts, the permeability of buccal mucosa to fluorescein isothiocynate (FITC) increased by 100-200 fold compared to FITC alone.<br />Applications -Bioavailability of drugs – 5% - 40%<br />Limitations -Potential membrane damage.<br />10/28/2010<br />Department Of Pharmaceutics<br />23<br />
  27. 27. DESIGN OF BUCCAL DOSAGE FORM<br />Matrix type: The Buccal patch designed in a matrix configuration contains drug, adhesive, and additives mixed together <br />Bi-directional patches release drug in both the mucosa and the mouth <br />Drug + Mucoadhesive Matrix<br />………………………………………………………………….<br />………………………………………………………………….<br />
  28. 28. Contd…<br />Reserviour type: The buccal patch designed in a reservoir system contains a cavity for the drug and additives separate from the adhesive<br />Impermeable backing is applied to control the direction of drug delivery; to reduce patch deformation and disintegration while in the mouth; and to prevent drug loss<br />Backing Layer<br />MucoadhesiveMatrix+Drug<br />~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~<br />
  29. 29. BuccalMucoadhesive Dosage Forms<br />Three types based on their geometry<br />
  30. 30.
  31. 31. BUCCAL FORMULATION<br />Buccal patches <br /><ul><li>laminates consisting of an impermeable backing layer, a drug-containing reservoir layer, a bioadhesive surface for mucosal attachment
  32. 32. similar to those used in transdermal drug delivery
  33. 33. Backing layer control the direction of drug release, prevent drug loss, minimize deformation and disintegration</li></li></ul><li>Buccal gels <br /><ul><li>Semisolid dosage forms, have the advantage of easy dispersion throughout the oral mucosa
  34. 34. may not be as accurate as from tablets, patches, or films
  35. 35. Poor retention of the gels at the site of application has been overcome by using bioadhesive formulations</li></li></ul><li>PRODUCT<br />Oral bioadhesive formulation<br />Corlan – hydrocortisone succinate<br />Bonjela – hypromellose<br />Daktarin – miconazole<br />Corsodyl – chlorohexidine<br />Buccal mucosa formulation<br />Buccastem – nausea , vomiting, vertigo<br />Suscard- angina<br />31<br />
  36. 36. REFERENCES<br />Y.W. Chein , Novel Drug Delivery Systems, 2 nd edition, revised and expanded , Marcel Dekker , Inc. New York , 1992(pg. no. 195 – 224)<br />N.K. Jain , Controlled and Novel drug delivery , CBS Publishers & Distributors, New Delhi, First edition 1997 (reprint in 2001)<br />S.P. Vyas and R.K.Khar, Controlled Drug Delivery, CBS Publishers & Distributors, New Delhi, First edition 1997.pg no. 259- 260<br />
  37. 37. THANK<br />YOU<br />