DESIGN AND IN VITRO CHARACTERIZATION OF MUCOADHESIVE BUCCAL PATCHES OF DULOXETINE HYDROCHLORIDE
DOI:
https://doi.org/10.22159/ijpps.2017v9i2.13793Keywords:
Mucoadhesive buccal patches, Duloxetine hydrochloride, Ex vivo permeation studiesAbstract
Objective: Buccal mucosa is a potential site for the delivery of drugs to the systemic circulation, a drug administered through the buccal mucosa enters directly to the systemic circulation, thereby which bypass the drug from the ï¬rst-pass hepatic metabolism and adverse gastrointestinal effect. Duloxetine hydrochloride (DLX HCL) is a selective serotonin and noradrenaline reuptake inhibitor (SSNRI). It is used in the treatment of depression, diabetic peripheral neuropathic pain and in moderate to severe stress urinary incontinence in women.
However, it undergoes extensive first-pass metabolism, and it is susceptible to undergo degradation in the acidic environment of the stomach, which results in the poor bioavailability. The objective of the present investigation is to design and evaluate the mucoadhesive buccal patches of DLX HCL with a goal of to increase the bioavailability and improve the patient compliance.
Methods: Mucoadhesive buccal patches were prepared by solvent casting technique using mucoadhesive polymers. The patches were evaluated for weight variation, thickness, surface pH, folding endurance, moisture absorption, drug content uniformity, in vitro drug release, mechanical properties and ex vivo permeation studies.
Results: The results of the optimised buccal patch F4 indicate that the mucoadhesive buccal patches of duloxetine hydrochloride may be a good choice for improving the bioavailability by bypassing the extensive first pass metabolism and acid degradation in the stomach.
Conclusion: Duloxetine hydrochloride can be delivered through the buccal route of drug administration through the buccal patches.
Downloads
References
Harris D, Robinson JR. Drug delivery via the mucous membranes of the oral cavity. J Pharm Sci 1992;81:1-10.
Gandhi RB, Robinson JR. Oral cavity as a site for bioadhesive drug delivery. Adv Drug Delivery Rev 1994;13:43–74.
Shojaei AH, Zhuo SL, Li X. Transbuccal delivery of acyclovir (II): feasibility, system design, and in vitro permeation studies. J Pharm Sci 1998;1:66–73.
Senel S, Hıncal AA, Squier CA. Effect of chitosan in enhancing drug delivery across buccal mucosa. Adv Chitin Sci, University Potsdam 2000;4:254–8.
Merkle HP, Anders R, Wermerskirchin A. In: Bioadhesive drug delivery systems, CRC Press: Boca Raton, Florida; 1990. p. 105.
Rojanasakul Y, Wang LY, Bhat M, Glover DD, Malanga CJ, Ma JKH. The transport barrier of epithelia; a comparative study on membrane permeability and charge selectivity in the rabbit. Pharm Res 1992;9:1029–34.
Davis SS, Daly PB, Kennerley JW, Frier M, Hardy JG, Wilson CG. Design and evaluation of sustained release formulations for oral and buccal administration. In: Bussmann WD, Dries RR, Wagner W. editors. Controlled release nitroglycerin in buccal and oral form. Basle: Karger; 1982. p. 17–25.
Schor JM, Davis SS, Nigalaye A, Bolton S. Susadrin transmucosal tablets. Drug Dev Ind Pharm 1983;9:1359–77.
Ishida M, Nambu N, Nagai T. Mucosal dosage form of lidocaine for a toothache using hydroxypropyl cellulose. Chem Pharm Bull 1982;30:980–4.
Bremecker KD, Strempel H, Klein G. Novel concept for a mucosal adhesive ointment. J Pharm Sci 1984;73:548–52.
Anders R, Merkle HP. Evaluation of laminated mucoadhesive patches for buccal drug delivery. Int J Pharm 1989;49:231–40.
Tanaka M, Yanagibashi N, Fukuda H, Nagai T. Absorption of salicylic acid through the oral mucous membrane of hamster cheek pouch. Chem Pharm Bull 1980;28:1056–61.
Squier CA, Hall BK. The permeability of mammalian non-keratinized oral epithelial to horseradish Peroxidase applied in vivo and in-vitro. Arch Oral Biol 1984;29:45-50.
Brun PPHL, Fox PLA, Vries MED, Bodde HE. In vitro penetration of some β adrenoreceptor blocking drugs through the porcine buccal mucosa. Int J Pharm 1989;49:141–5.
Biswajit Basu1, Kevin Garala, Thimmasetty J. Formulation and evaluation of pimozide buccal mucoadhesive patches. Int J Pharm Sci Nanotechnol 2010;2:152.
Chinna Reddy P, Ramesh G, Shravan Kumar Y, Madhusudan Rao Y. Development of bioadhesive buccal tablets for felodipine and pioglitazone in combined dosage form: in vitro, ex vivo and in vivo characterization. Drug Delivery 2011;18 Suppl 5:344-52.
Chinna Reddy P, Madhusudan Rao Y. Buccal drug delivery systems. In: Advances in drug delivery, published by Pharma Book Syndicate. Vol. 1; 2010. p. 139-210.
Shayeda, Ramesh G, Chinna Reddy P, Madhusudan Rao Y. Development of novel bioadhesive buccal formulation of diltiazem: in vitro and in vivo characterization. PDA J Pharm Sci Technol 2009;63 Suppl 4:1-9.
Vamshi Vishnu Y, Chandra Sekhar K, Ramesh G, Madhusudan Rao Y. Development mucoadhesive patches for buccal administration of carvedilol. Curr Drug Delivery 2007;4:27-39.
K Chandra Sekhar, KVS Naidu, G Ramesh, Y Vamshi Vishnu, Y Madhusudan Rao. Transbuccal delivery of chlorpheniramine maleate from mucoadhesive buccal patches. Curr Drug Delivery 2008;15:185-91.
S Himabindu, D Sathish, Shayeda. Formulation and in vitro evaluation of mucoadhesive buccal patches of cyproheptadine hydrochloride. J Appl Pharm Sci 2012;2 Suppl 7:196-201.
Mona semalty, A Semalty, G Kumar. Formulation and characterization of mucoadhesive buccal films of Glipizide. Indian J Pharm Sci 2008;70 Suppl 1:43-8.
Amanpreet kaur, Gurpreet kaur. Mucoadhesive buccal patches based on interpolymer complexes of chitosan–pectin for delivery of Carvedilol. Saudi Pharm J 2012;20 Suppl 1:21-7.
Vishnu M Patel, Bhupendra G Prajapati. Design and in vitro characterization of eudragit containing mucoadhesive buccal patches. Int J PharmTech Res 2009;1 Suppl 3:783-9.
Bottenberg P, Cleymaet R, Muynek CD, Remon JP, Coomans D, Slop D. Development and testing of bioadhesive, fluoride-containing slow-release tablets for oral use. J Pharm Pharmacol 1991;43:457-64.
Chinna Reddy Palem, Ramesh Gannu, Narender Doodipala, Vamshi Vishnu Yamsani, Madhusudan Rao Yamsani. Transmucosal delivery of domperidone from bilayered buccal patches: in vitro, ex vivo and in vivo characterization. Arch Pharm Res 2011;34 Suppl 10:1701-10.
Wong CF, Yuen KH, Peh KK. An intro method for buccal adhesion studies: the importance of instrument variables. Int J Pharm 1999;180:47-57.
Parthasarathy Govindasamy, Bhaskar Reddy Kesavan, Jayaveera Korlakunta Narasimha. Formulation of unidirectional release buccal patches of carbamazepine and study of permeation through the porcine buccal mucosa. Asian Pac J Trop Biomed 2013;3:995–1002.
Peppas NA. Analysis of fickian and non-fickian drug release from polymers. Pharm Acta Helvetiae 1985;60:110–1.
Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanism of solute release from porous hydro-matrices and other factors may be responsible. Int J Pharm 1983;15 Suppl 1:25-35.