formulation of Buccal Drug Delivery System.pptx

Prepare BY: Chrishmita
M.Pharmacy , 1st Year
Pharmaceutics Department
RR COLLEGE OF PHARMACY.
Thanks to PAWAN DHAMALA

1. 30-04-2022 © R R INSTITUTIONS , BANGALORE 1 MODERN DRUG DELIVERY SYSTEM B UCCAL DRUG DELIVERY SYSTEM RR COLLEGE OF PHARMACY Submitted by: Chrishmitha 1 st M.Pharm . Dept. of Pharmaceutics Submitted to: Dr. Geethalaxmi HOD. Dept of pharmaceutics

2. 30-04-2022 © R R INSTITUTIONS , BANGALORE 2 CONTENTS Introduction Types of dosage forms Basic formulation components Formulations of BDDS

3. Buccal drug delivery system Delivery of drug through buccal mucosa of oral cavity is called BDDS. Buccal mucosa lines the inner region of cheeks. In biological term, the product is placed between upper gums and cheek to treat local and systemic conditions. Buccal route provides one of the potential routes for typically large, hydrophilic and unstable proteins, oligonucleotides and polysaccharides as well as conventional small drug molecules . 30-04-2022 © R R INSTITUTIONS , BANGALORE 3

4. Formulation of BDDS 3 Types of dosage forms : Solid Dosage forms : Tablets Patches / Films Wafers Lozenges Powders Semi-Solid Dosage forms: Gels Ointments Liquid Dosage forms: sprays 30-04-2022 © R R INSTITUTIONS , BANGALORE 4

5. Basic Formulation Components Pure Drug Muco-adhesive Polymers Permeation enhancers Diluents Plasticizer 30-04-2022 © R R INSTITUTIONS , BANGALORE 5

6. Selection of DRUG for BDDS MW should be less than 1000da It should be having both nature i.e. hydrophilic-lipophilic type Should be potent {low dose so that formulation is not bulky } Non-irritant to mucosa Drugs that degrades in GIT. List of API’s delivered via Buccal route : Acyclovir Metronidazole Metoprolol tartrate Carbamazepine Morphine sulphate Chlorpheniramine maleate Nifedipine Danazol Omeprazole Diclofenac sodium Pentazocine Diltiazem Pindolol Flurbiprofen Piroxicam Hydrocortisone acetate Insulin Testosterone Lignocaine Terbutaline sulphate 30-04-2022 © R R INSTITUTIONS , BANGALORE 6

7. Mucoadhesive Polymers These are the main component for adhesion. they attract water from the biological surrounding, get swells & adhere to the membrane. Normally they should be having hydrophilicity, numerous H-bonding groups, flexibility, interpenetration with mucus & tissues. Examples Hydrogels : Polyacrylates, Carbopol, polycarbophils, PVA, Ethylene Vinyl alcohol, cellulose derivatives, alginates. Thiolated Polymers : Eg : Thiomers of chitosan & polyacrylic acid etc. 30-04-2022 © R R INSTITUTIONS , BANGALORE 7

8. Ideal characteristics Non-toxic, non-irritant & pure. Good spreadability, wetting, swelling, solubility,& biodegradable if possible. Adhesion should be quick & with sufficient mechanical strength. Should have peel, tensile, shear strength. Should easily incorporate drug in formulation & it should not be obstacle in drug release. Cost effective. 30-04-2022 © R R INSTITUTIONS , BANGALORE 8

9. Permeation Enhancers Permeation is very limiting factor in BDDS. Substances that facilitates permeation through Buccal mucosa are called PE. Epithelium & Lamina Propria are very effective barrier to absorption. They should be used with very care & in optimum concentration (<1%), above this concentration toxicity due to membrane damage may occur & histopathological study should be done. 30-04-2022 © R R INSTITUTIONS , BANGALORE 9

10. Mechanisms of PE’s Increasing fluidity & integrity of cell membrane. Extracting inter/intra cellular lipids. Altering cellular lipids. Altering mucus rheology. Acting at the tight junctions. Increasing thermodynamic activity of drugs. Surface tension decreasing. 30-04-2022 © R R INSTITUTIONS , BANGALORE 10

11. Permeation Enhancers TYPES EXAMPLES Chelators EDTA, Citric acid, Sodium salicylate, methoxy salicylates Surfactants SLS, Polyoxyethylene , Cetylpyridinium chloride, Benzalkonium chloride, Cetyltrimethyl ammonium bromide. Bile salts sodium glycocholate, sodium deoxycholate, sodium taurocholate, sodium deoxycholate, sodium taurodeoxycholate . Fatty acids Oleic acid, Capric acid, Lauric acid, PG, methyloleate , Phosphatidylcholine. Non-surfactants Unsaturate cyclic ureas . Inclusion complexes Cyclodextrins. 30-04-2022 © R R INSTITUTIONS , BANGALORE 11

12. Diluents: Diluents are filters used to make required bulk of the tablet when the drug dosage itself is inadequate to the bulk. Secondary reason is to provide better tablet properties such as improve cohesion, to permit use of direct compression manufacturing or to promote flow. 30-04-2022 © R R INSTITUTIONS , BANGALORE 12

13. A diluents should have following properties They must be non toxic They must be commercially available in acceptable grade There cost must be low They must be physiologically inert They must be physically & chemically stable by themselves & with the drugs They must be free from all microbial contamination They do not alter the bio availability of drug They must be color compatible. 30-04-2022 © R R INSTITUTIONS , BANGALORE 13

14. Plasticizers Plasticizers are the important excipient of the oral film. The selection of film forming polymers, is one of the most important and critical parameter for the successful development of film formulation. It improve the flexibility and a mechanical property of the film like tensile strength and elongation and reduce the brittleness of the strip. Plasticizer should be selected so that it must be compatible with the drug. Plasticizer can improve the flow and enhances the strength of polymer. Different plasticizers used in the preparation of the oral films are Glycerol, propylene glycol, polyethylene glycol400, dimethyl, dibutyl, diethyl phthalate, acetyl citrate, triacetin and castor oil. 30-04-2022 © R R INSTITUTIONS , BANGALORE 14

15. FORMULATIONS OF BDDS Tablets Is small, flat, generally oval shape with 5-8mm diameter. It is directly placed onto mucosal surface & adheres to it. Direct compression or wet granulation may be used to formulate Unlike conventional tablets, buccal mucoadhesive tablets allow for drinking and speaking without major discomfort. They soften, adhere to the mucosa and are retained in position until dissolution and/or release is complete. Example: Nitro-glycerine bio adhesive tablets 30-04-2022 © R R INSTITUTIONS , BANGALORE 15

16. Buccal Patches/films They are long, thin thickness, transparent with high surface area. Buccal patch/film are laminates consisting of an impermeable backing layer, a drug containing reservoir layer from which the drug released in a controlled manner and a bioadhesive surface for mucosal attachment. They can be prepared by two methods - Solvent casting method - Direct milling method 30-04-2022 © R R INSTITUTIONS , BANGALORE 16

17. Solvent Casting Method Here drug & all excipients are weighed and dispersed in the suitable organic solvent & coated on the release liner. The organic solvent is allowed to evaporate & after evaporation the thin layer of the backing material is laminated on to the sheet of coated release liner to form laminate. After that the whole patch is ready to cut into required size (almost 2*2cm 2 ) 30-04-2022 © R R INSTITUTIONS , BANGALORE 17

18. Direct Milling Method Here, drug & excipients are mixed mechanically by milling or kneading. After mixing the resultant material is rolled on the release liner till desired thickness is achieved. Finally, the backing material is laminated. Though there is no difference in the patch performance but with the SOLVENT method there are chance of residual solvent. Hence this Solvent free method is highly used. 30-04-2022 © R R INSTITUTIONS , BANGALORE 18

19. NOTE: Generally for unidirectional release, a backing membrane is applied, which is impermeable to liquid, to one side so that no drug release is observed from that side & non-coated surface adheres to the Buccal mucosa . Ethyl Cellulose is used as backing membrane. What does backing layer does.... Control the direction of drug release Also prevent drug losses Minimize deformation during handling & transportation Reduce the disintegration of device during the application Examples:- Nitroglycerin patches Fentanyl patches( Onsolis ) 30-04-2022 © R R INSTITUTIONS , BANGALORE 19

20. Semisolid Preparations(Ointments and Gels) Bioadhesive gel or ointments have less patient acceptability than solid Bioadhesive dosage forms, and most of the dosage forms are used only for localized drug therapy within the oral cavity. These are having the advantage of easy dispersion throughout the oral mucosa. Certain bioadhesive polymers undergo a phase change from a liquid to a semisolid; this change enhances the viscosity, which results in sustained and controlled release of drugs. 30-04-2022 © R R INSTITUTIONS , BANGALORE 20

21. BUCCAL SPRAYS Generex bio technology have been introduced insulin spray. This technology is being used to develop a formulation for buccal delivery of insulin for treatment of type -1 diabetes. Buccal spray delivers a mist of droplets onto mucosal membrane probably on to mucin layer . E.g. Estradiol spray. 30-04-2022 © R R INSTITUTIONS , BANGALORE 21

22. Reference: International journal of pharmaceutical sciences and research vol.4,issue 3. N.K.Jain , Controlled and Novel drug delivery,CBS publishers &distributors 30-04-2022 © R R INSTITUTIONS , BANGALORE 22

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