Buccal &Sublingual Drug Delivery System
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This document provides an overview of buccal and sublingual drug delivery systems. It discusses the anatomy of the buccal mucosa and some of the advantages of buccal/sublingual routes, including avoidance of first-pass metabolism and protection from digestive enzymes. Various formulations are described, including tablets, patches, films, and semisolids. Evaluation methods like drug release studies, permeation studies, and bioadhesion tests are also summarized. The document provides a comprehensive introduction to buccal and sublingual drug delivery.
![Bioadhesion studies
Swelling study
Percentage hydration = [(W2-W1)/ W1] ×100
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Buccal &Sublingual Drug Delivery System
- 1. Prepared by: Motivaras Ashish M.Pharm II sem Roll No: 05 Guided by: Dr. jaydeep Patel B.K.MODY GOVT. PHARMACY COLLEGE, RAJKOT. BSDDS
- 2. o INTRODUCTION o WHY BUCCAL/SUBLINGUAL? o ANATOMY OF BUCCAL MUCOSA o TRANSPORT ROUTES o BIOADHESION MECHANISMS o BASIC COMPONENTS FOR BDDS o FORMULATIONS o EVALUATION o RECENT INNOVATIONS o REFERENCE2
- 3. The oral mucosa lines includes inner cheek, sublingual, gingival, palatal Sublingual delivery: floor of the mouth Buccal delivery: lining of the cheek Local delivery:cavity, principally ulcers, fungal conditions and periodontal disease. 3
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- 6. To avoid first-pass metabolism Protection from pH and digestive enzymes Improved patient compliance Rapid onset of action Ease of drug administration Rapid and extensive drug absorption Easy termination of therapy 6
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- 9. Diffusion Theory Entanglements of the polymer Electronic Theory Attractive forces Wetting Theory Fracture Theory the force necessary to seaparate two surfaces Adsorption Theory Secondary chemical bonds 9
- 10. Drug substance Bioadhesive polymers Backing membrane Permeation enhancers Other excipient 10
- 11. dose of the drug should be small half-life between 2-8 hours exhibit first pass effect or presystemic drug elimination. absorption should be passive when given orally Nicotine Nifedipine Propranolol Diclofenac sodium Cyanocobalamin11
- 12. must not decompose on storage inert and compatible with the environment polymer and its degradation products should be non-toxic absorbable from the mucous layer. adhere quickly to moist tissue surface 1.Natural polymers Ex.: Gelatin, sodium alginate. 2. Synthetic and semisynthetic polymers Ex.: PVA, PEG, HPMC, PVP, Na-CMC etc12
- 13. plays a major role in the attachment of bioadhesive devices to the mucus membrane inert, and impermeable to the drug and penetration enhancer. Eg.carbopol, magnesium stearate, HPMC, HPC, CMC, polycarbophil 13
- 14. Mechanism Changing mucus rheology Increasing the fluidity of lipid bilayer membrane Acting on the components at tight junctions Increasing the thermodynamic activity of drugs 14
- 15. Types 1.Bile salts (Sodium glycocholate, sodium taurocholate) 2.Fatty acids(oleic acid, capric acid, lauric acid) 3.Surfactants 4.Chelators(EDTA, citric acid) 5.Others(aprotinin, hyaluronidases,neuraminidase) 6.Thiolated polymers (chitosan-cysteine, polycarbophil-cysteine) 15
- 16. 1)Polymer related factors: Molecular weight: bioadhesive strength of a polymer increases with molecular weights above 100,000 Flexibility: substantial degree of flexibility in order to achieve the desired entanglement with the mucus Hydrogen bonding capacity Cross-linking density: increasing density of cross-linking, diffusion of water into the polymer net-work occurs at a lower rate which, causes an insufficient swelling of the polymer and a decreased rate of interpenetration between polymer and mucin 16
- 17. Charge: Some generalizations about the charge of bioadhesive polymers have been made previously, where nonionic polymers appear to undergo a smaller degree o f adhesion compared to anionic polymers Concentration Hydration (swelling): Polymer swelling permits a mechanical entanglement by exposing the bioadhesive sites for hydrogen bonding and/or electrostatic interaction between the polymer and the mucous network 2)Environmental factors Saliva pH Mucin turnover Rate 17
- 18. Buccal and Sublingual Tablets Buccal and Sublingual Patches and Films Buccal Semisolids (ointments and gels) Buccal Powders 18
- 19. Fast-disintegrating sublingual tablets: (Sublingual) there is a need to formulate a dosage form which gives fast relief from angina & headache, while at the same minimising the first pass effect to improve its bioavailability. Fast disintegration sublingual tablet fullfil this criteria. Bioadhesive Sublingual tablets:a risk that the patient will swallow part of the dose before the active substance has been released Sublingual vitamin tablet Lipid matrix sublingual tablet19
- 20. S-DBMP-T(slow dissolving buccal mucoadhesive plain tablet) BCTS(buccal covered tablet system) Dosage forms are soften and lose its shape due to mouth movement, which hindered control of the disintegration of the tablet over long administration periods . The improved technology involved covering the S-DBMP-T system with a polyethylene film that had a hole in it. We refer to this technology as the buccal covered-tablet system (BCTS ) and have demonstrated that this technology can prolong the duration of absorption of glyceryl trinitrate and isosorbide dinitrate. 20
- 21. Buccal tablets are small, flat, and oval, with a diameter of approximately 5–8 mm. Tablets are usually prepared by direct compression, but wet granulation techniques can also be used 21
- 22. Swelling study Bioadhesion studies In vitro residence time In vitro surface pH studies In vitro drug release studies In vitro permeation studies In vitro mucoadhesion strength In vivo release studies Ex vivo mucoadhesion time Ex vivo mucoadhesion force Ex vivo transmucosal permeation studies22
- 23. Bioadhesion studies Swelling study Percentage hydration = [(W2-W1)/ W1] ×100 23
- 24. Residence time (in vitro) Modified Disintigration Apparatus Glass slab Buccal tissue Tablet Isotonic buffer 24 Glass Beaker
- 25. Release rate study(in vitro) Composition of simulated saliva KH2PO4 12mM NaCl 40mM CaCl2 1.5mM NaOH To pH 6.2 25
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- 28. Matrix type Reservoir type 28
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- 30. Thin film drug delivery is a process of delivering drugs to the systemic circulation via a thin film that dissolves when in contact with liquid, often referred to as a dissolving film or strip. Thin film strips are typically designed for oral administration, with the user placing the strip on or under the tongue. As the strip dissolves, the drug can enter the blood stream enterically, or sublingually. 30
- 31. Drug Polymers (Mucoadhesive polymers, polymers controlling rate of release and Polymers to prepare backing membrane) Backing membrane Plasticizer Penetration enhancer 31
- 32. Methods for patch preparation Solvent casting method Semisolid casting Hot melt extrusion Solid dispersion extrusion Rolling method 32
- 33. EVALUATION OF BUCCAL PATCHES Physical properties Physical appearance and surface texture of patch Weight uniformity of patches Thickness of patches Folding endurance of patches Swelling index of patches Surface pH of patches 33
- 34. CONT… Mechanical properties Bursting strength of patches In vitro residence time of patches Drug polymer interaction study of patches Drug content uniformity of patches In vitro drug release 34
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- 36. Gels are usually clear, transparent, semisolids containing solubilized active substances . e.g.Methylcellulose, carbopols, hydroxyethylcellulose etc Glibenclamide gel Buccal bioadhesive powder dosage forms are a mixture of bioadhesive polymers and the drug and are sprayed onto the buccal mucosa. eg hydroxypropylcellulose and beclomethasone- diproprionate 36
- 37. BUCCAL WAFERS novel periodontal drug delivery system that is intended for the treatment of microbial infections associated with peridontitis. The delivery system is a composite wafer with surface layers possessing adhesive properties, while the bulk layer consists of antimicrobial agents, biodegradable polymers and matrix polymers. 37
- 38. GEL FORMING LIQUIDS: This type of a formulation is liquid upon instillation and undergoes a phase transition to form a viscoelastic gel in response to stimulus such as temperature, ionic stength or pH. Carbomers become more viscous upon increased pH. Gellan gum and alginate both form gel in response to increased ionic strength (particularly with Ca+2 ions). Poloxamers and smart hydrogel are gel at approximately body temperature. BIOADHESIVE SPRAY: Buccoadhesive sprays are gaining popularity over other dosage forms because of flexibility, comfort, high surface area availability of drug in solution form. Drugs genrally given by these routes are fentanyl, buprenorphine. Naloxone etc. 38
- 39. flushing action of saliva Taste, Irritancy and ‘mouth feel’ is an issue. Allergic reactions, discoloration of teeth Antimicrobial agents, affects the natural microbes Patient cannot eat/drink/speak Swallowing of saliva lead to the loss of drug 39
- 40. Write about buccal & sublingual drug delivery systems. (DEC. 2010) Explain the structure of buccal mucosa. Give a brief account of mucoadhesive polymers for buccal delivery. (JULY 2010) Discuss the merits and demerits of mucoadhesive buccal drug delivery. How one can evaluate mucoadhesive buccal formulation? (JULY 2010) Which are potential sites and dosage forms for bioadhesion? Draw a general schematic diagram for BDDS and classify them. Write a note on exvivo and invivo methods to study BDDS system. (January 2011)40
- 41. Drug Delivery to the Oral Cavity,Drugs and The Pharmaceutical Sciences, Executive Editor James Swarbrick PharmaceuTech, Inc.Pinehurst, North Carolina Enhancement in Drug DeliveryEdited by Elka Touitou Brian W. Barry, Page no: 173-215 Encyclopedia of PHARMACEUTICAL TECHNOLOGY, Third Edition, VOLUME 1, Page no:2664-2676 Marcel Dekker, Inc. Modified-Release Drug Delivery Technology, chapter no: 30 Patel V. F., Liu F., et al. (2011). "Advances in oral transmucosal drug delivery." Journal of Controlled Release 153: 106-116.41
- 42. Miller N., Chittchang M., et al. (2005). "The use of mucoadhesive polymers in buccal drug delivery." Advanced Drug Delivery Reviews 57: 1666– 1691. Sudhakar Y., Kuotsu K., et al. (2006). "Buccal bioadhesive drug delivery — A promising option for orally less efficient drugs " Journal of Controlled Release 114: 15-40. Pankil A. Gandhi,Dr. M.R.Patel, Dr. K.R. Patel, Dr. N. M. Patel , 2011, A REVIEW ARTICLE ON MUCOADHESIVE BUCCAL DRUG DELIVERY SYSTEM IJPRD, 2011; Vol 3(5): July 2011 (159 - 173) 42
- 43. http://www.novadel.com/pipeline/index.htm http://www.medpharm.co.uk http://www.biodeliverysciences.com/pipeline. php http://www.generex.com/technology.php http://www.snoreeze.com/the-snoreeze- range/snoreeze-oral-strips 43
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