Volume : 12, Issue : 02, February – 2025

Title:

FORMULATION AND EVALUATION OF BUCCAL MUCOADHESIVE TABLET OF DALFAMPRIDINE
‬

Authors :

Maheen Afroze, Sameena Begum, Niranjan Panda

Abstract :

Objective: The study aimed to formulate and evaluate mucoadhesive buccal tablets of dalfampridine to avoid the first-pass metabolism. The goal of the current investigations was to create a buccal mucoadhesive tablet combining sustained release and mucoadhesive polymers like guar gum, HPMC K100LV, ethyl cellulose, Eudragit RLPO, and Carbopol 934P. Dalfampridine, a medication used to treat multiple sclerosis, was taken as a model drug while the tablets were being manufactured using the direct compression method. To guarantee flow characteristics during tablet punching, precompression settings for the dry combination of medication and polymers were assessed. The model medication and the mucoadhesive polymers employed in formulations did not interact, according to the results of FTIR and DSC investigations. The physicochemical parameters, including hardness, thickness uniformity, weight variation, and moisture absorption investigations, were assessed for the mucoadhesive buccal tablets that were created. The produced buccal tablets were assessed for ex vivo drug permeability via cellulose acetate membrane, mucoadhesive strength, and in vitro drug release. For additional kinetic and stability investigations, the four best formulations from each medication category have been selected and tested based on bioadhesive strength, Ex vivo mucoadhesive strength, and in vitro release studies. The medicines and the produced mucoadhesive buccal tablets were found to be stable in fake human saliva when the stability of the tablets was assessed. Therefore, by preventing first-pass metabolism, the mucoadhesive polymers under study can be utilized in different ratios to make mucoadhesive buccal tablets of Dalfampridine, which should have a prolonged therapeutic impact and better patient compliance.
Keywords: Multiple sclerosis, Mucoadhesion, Dalfampridine, HPMC K100LV, Carbopol 934P, Ethyl Cellulose, Eudragit RLPO, Guar gum

Cite This Article:

Please cite this article in press Niranjan Panda et al., Formulation And Evaluation Of Buccal Mucoadhesive Tablet Of Dalfampridine.,Indo Am. J. P. Sci, 2025; 12 (02).

Number of Downloads : 10

References:

1. Jain NK. Controlled and novel drug delivery. 1stEd. New Delhi: CBS Publishers & Distributors; 1997: 52-81.
2. Patel VM, Prajapati BG, Patel MM. Formulation, evaluation and comparison of bilayered and multilayered mucoadhesive buccal devices of propranolol hydrochloride. AAPS Pharm Sci Tech. 2007; 8(1): 1-8.
3. Miller NS, Chittchang M, Johnston TP. The use of mucoadhesive polymers in buccal drug delivery. Adv Drug Deliv Rev. 2005; 57: 1666-1691.
4. Vyas SP, Khar RK. Controlled drug delivery- concepts and advances. 1sted. New Delhi: Vallabh Prakashan; 2002.
5. Shojaei HA. Buccal mucosa as a route for systemic drug delivery: A Review. J Pharm Sci.1998; 1(1): 15-30.
6. Ballard, B.E. and Robinson, J.R., Eds., In; An overview of prolonged action drug dosage form, In sustained and controlled release drug delivery systems, Marcel Dekker, New York,795, 1978.
7. Vyas, S. P. and Roop, K.Khar. Controlled Drug Delivery: Concepts and Advances, 1st Ed., 258, 2004.
8. R. Khanna, S.P. Agarwal, Alka Ahuja., Mucoadhesive Buccal Drug Delivery: A Potential Alternative to Conventional Therapy. Indian J. Pharm. Sci., 1998; 60(1); 1-11.
9. Ahuja.A, Khar.R.K, Ali.J., Muccoadhesive Drug Delivery Systems. Drug Dev. Ind. Pharm., 1997; 23(5); 489-515.
10. Smart JD. The basics and underlying mechanisms of mucoadhesion. Adv Drug Del Rev.2005; 57: 1556–1568
11. Hans.E, Junginger, Bioadhesive polymer Systems for peptide delivery. Acta Pharm. Technol.1990; 36(3), 110-126.
12. Patil SB, Murthy RSR, Mahajan HS, Wagh RD, Gattani SG. Mucoadhesive polymers: means of improving drug delivery. Pharma Times. 2006; 38(4): 2.
13. Peppas NA, Buri PA. Surface, interfacial and molecular aspects of polymer bioadhesion on soft tissues. J Cont Rel. 1985; 2: 257-275.
14. Gu JM, Robinson JR, Leung SH. Binding of acrylic polymers to mucin/epithelial surfaces: structure-property relationships. Crit Rev Ther Drug Carr Syst. 1998; 5: 21-67.
15. Park H, Amiji M, Park K. Mucoadhesive hydrogels effective at neutral pH. Proc Int Symp Cont Rel Bioact Mater. 1989; 16: 217-218.
16. Rathbone MJ, Drummond BK, Tucker IG. The oral cavity as a site for systemic drug delivery. Adv Drug Deliv Rev. 1994; 13: 1-22.
17. Lehr CM, Poelma FG, Junginger HE, Tukker JJ. An estimate of turnover time of intestinal mucus gel layer in the rat in situ loop. Int J Pharm. 1991; 70: 235- 240. Forstner JF. Intestinal mucins in health and disease. Digestion 1978; 17:234- 263.
18. Ho NF, Barsuhn CL, Burton PS, Merkle HP. Routes of delivery: case studies (3) Mechanistic insights to buccal delivery of proteinaceous substances. Adv Drug Deliv Rev. 1992; 8: 197-235.
19. David Haris, Robinson JR. Buccal drug delivery via the mucous membranes of the oral cavity. J Pharm Sci. 1992; 81(1): 1-9.
20. Ross & Wilson. Anatomy & physiology in health and illness. 9th ed. Edited by Anne Waugh and Allison Goraw: Churchill Livingstone Edinburgh Publishers; 2001: 289-293.
21. Chatterjee CC. Human physiology. 10th ed. Calcutta: Medical Allied Agency; 1985: 427-434.
22. Pramod KTM, Shivakumar HG and Desai KG. Oral transmucosal drug delivery systems. Indian Drugs. 2004; 41(2): 63-67.
23. Chen YS, Squier CA. The ultra structure of the oral epithelium. In: J.Meyer, CA. Squier, SJ. Gerson (Eds), The structure and function of oral mucosa, Pergamon Press, Oxford. 1984: 7-30.
24. Swarbrick James. Bioadhesive drug delivery systems. 1st ed. New York: Marcel Dekker Inc; 1999: 541-562.
25. Hayward AF. Membrane-coating granules . Int Rev Cyt. 1979; 59: 97-127.
26. Squier CA, Eady RA, Hopps RM. The permeability of epidermis lacking normal membrane- coating granules: an ultra structural tracer study of Kyrle-Flegel disease. J Invest Dermatol.1978; 70: 361-364.
27. Gurny R, Ryser JE, Tabatabay C, Martenet M, Edman P, Camber O. Precorneal residence time in humans of sodium hyaluronate as measured by gamma scintigraphy. Graefe Arch Clin Exp Ophthalmol 1990; 228; 510-512.
28. Meseguer G, Gurny R, Buri P. Gamma scintigraphic evaluation of precorneal clearance in human volunteers and in rabbits. Eur J Drug Meta Pharma. 1993; 18: 190-194.
29. Martin L, Wilson CG, Koosha F, Uchegbu IF. Sustained buccal delivery of the hydrophobic drug denbufylline using physically cross- linked palmitoyl glycol chitosan hydrogels. Eur J Pharm Biopharm. 2003; 55: 35-45.
30. Rudnic EM, Schwartz JD. Oral solid dosage forms. In: Gennaro AR (editor). Remington: the science and practice of pharmacy. 20th ed. Lippincott Williams & Wilkins, Baltimore; 2000:858-859.
31. Hannan Butchelov. Novel bioadhesive formulation in drug delivery an oral presentation at the British pharmaceutical conference. The drug delivery companies pharmaventures Ltd.2004: 22-26.
32. Dkinci G, Çapan Y, Senel S, Alaaddinogu E, Dalkara T, Hıncal AA. In vitro/in vivo studies on a buccal bioadhesive tablet formulation of carbamazepine. Pharmazie. 2000; 55: 762-765.
33. Nagai T, Konishi R. Buccal/gingival drug delivery systems. J Cont Rel.1987; 6: 353-360.
34. S. Roy, K. Pal, A. Anis3, K. Pramanik and B.Prabhakar. Polymers in Mucoadhesive Drug Delivery System: A Brief Note. Designed monomers and polymers. 2009 ; 12: 483- 95.
35. Lueben HL, Lehr CM, Rentel CO, Noach AB, Boer AG, Verhoef JC, Junginger HG. Bioadhesive polymers for the per oral delivery of peptide drugs. J Cont Rel. 1994; 29: 329-338
36. Dkinci G, Çapan Y, Senel S, Alaaddinogu E, Dalkara T, Hıncal AA. In vitro/in vivo studies on a buccal bioadhesive tablet formulation of carbamazepine. Pharmazie. 2000; 55: 762-765.
37. Giunchedi P, Juliano C, Gavini E, Cossu M, Sorrenti M. Formulation and in vivo evaluation of chlorhexidine buccal tablets prepared using drug loaded chitosan microspheres. Eur J Pharmbiopharm.2002; 53:233-239.
38. Cassidy J, Berner B, Chan K, John V, Toon S, Holt B, Rowland M. Human transbuccal absorption of diclofenac sodium from a prototype hydrogel delivery device. Pharm Res.1993; 10: 126-129.
39. Ahuja A, Dogra M, Agarwal SP. Development of buccal tablets of diltiazem hydrochloride. Ind J Pharm Sci. 1995; 57: 26-30.
40. Tsutsumi K, Obata Y, Nagai T, Loftsson T, Takayama K. Buccal absorption of ergotamine tartrate using the bioadhesive tablet system in guinea-pigs. Int J Pharm. 2002; 238: 161-170.
41. Ceschel GC, Maffei P, Lombardi SB, Ronchi C. Design and evaluation of buccal adhesive hydrocortisone acetate (HCA) tablets. Drug Deliv. 2001; 8: 161- 171.
42. Hosny EA, Elkheshen SA, Saleh S. Buccoadhesive tablets for insulin delivery: in- vitro and in- vivo studies. Boll Chim Farm. 2002; 141: 210-217.
43. Kuipers ME, Heegsma J, Bakker HI, Meijer DK, Swart PJ, Frijlink EW, Eissens AC, Vries- Hospers HG, Berg J. Design and fungicidal activity of mucoadhesive lactoferrin tablets for the treatment of oropharyngeal candidosis. Drug Deliv. 2002; 9: 31-38.
44. Parvez N, Ahuja A, Khar RK. Development and evaluation of mucoadhesive buccal tablets of lignocaine hydrochloride. Ind J Pharm Sci. 2002; 64(6): 563- 567.
45. Ahuja A, Khar RK, Chaudhry R. Evaluation of buccoadhesive metronidazole tablets: microbiological response. Pharmazie 1998: 53:264-267.
46. Mohammed FA, Khedr K. Preparation and in vitro/in vivo evaluation of the buccal bioadhesive properties of slow release tablets containing miconazole nitrate. Drug Dev Ind Pharm. 2003; 29: 321-337.
47. Anlar S, Capan Y, Guven O, Gogus A, Dalkara T, Hıncal AA. Formulation and in vitro-in vivo evaluation of buccoadhesive morphine sulfate tablets. Pharm Res. 1994; 11: 231-236.
48. Park CR, Munday DL. Development and evaluation of a biphasic buccal adhesive tablet for nicotine replacement therapy. Int J Pharm. 2002; 237:215-226.
49. Cho HG, Kim CK. Development of omeprazole buccal adhesive tablets with stability enhancement in Saliva. J Cont Rel. 2000; 68: 397–404.
50. Dortunç B, Ozer L, Uyanik N. Development and in vitro evaluation of a buccoadhesive pindolol tablet formulation. Drug Dev Ind Pharm. 1998; 24: 281- 288.
51. Celebi N, Kislal O. Development and evaluation of a buccoadhesive propranolol tablet formulation.Pharmazie.1995; 50:470-472.
52. Mohamed MI, Mortada ND. Development and characterization of a buccoadhesive dosage form of terbutaline sulphate. Mansoura J Pharm Sci. 2000; 16: 69-81.
53. Jug M, Becirevic L. Influence of hydroxypropyl-β-cyclodextrin complexation on piroxicam release from buccoadhesive tablets. Eur J Pharm Sci. 2004; 21: 251-260.
54. Lachman L, Libermann HA, Kanig JL. Pharmaceutical dosage forms tablets volume 1, 2nd ed. New York: Marcel Dekker Inc; 1991: 133-195.
55. Gautam singhvi, Mahaveer Singh, In vitro drug release characterization models. International Journal of Pharmaceutical Studies and Research/ Vol. II/ IssueI/Jan-march, 2011.