Transmucosal Delivery of Duloxetine Hydrochloride for Prolonged Release: Preparation, in vitro, ex vivo Characteri-zation and in vitro-ex vivo Correlation
DOI:
https://doi.org/10.37285/ijpsn.2018.11.5.5Abstract
Duloxetine hydrochloride is a selective serotonin and nor adrenaline reuptake inhibitor. 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 hepatic first-pass metabolism and susceptible to undergo degradation in acidic environment of stomach, which results in the poor bioavailability. The objective of the present study was to develop and evaluate the mucoadhesive buccal tablets (transmucosal delivery) of duloxetine hydrochloride with a goal of to increase the bioavailability and improve the patient compliance. Mucoadhesive buccal tablets were prepared by a wet granulation technique using mucoadhesive polymers like HPMC K4M, Carbopol 934P and PEO WSR 303. The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, swelling index, drug content uniformity, in vitro drug release, in vitro bioadhesion and ex vivo permeation studies. The physicochemical properties of all the formulations were shown to be within the limits. The optimized buccal tablets AA1, AB3 and AC1 showed prolonged drug release for a period of 6 h with the Higuchi model release profile. Further, ex vivo permeation studies for optimized tablets were conducted and shown enhanced drug permeation. Therefore, these results demonstrated that the optimized buccal formulation of duloxetine hydrochloride enhances the oral bioavailability by delivered through the buccal route.
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Keywords:
Mucoadhesive buccal tablets, Duloxetine, Wet granulation, Ex vivo permeation
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Published
2018-09-30
How to Cite
1.
Banala N, Peddapalli H, Dudhipala N, Chinnala KM. Transmucosal Delivery of Duloxetine Hydrochloride for Prolonged Release: Preparation, in vitro, ex vivo Characteri-zation and in vitro-ex vivo Correlation. Scopus Indexed [Internet]. 2018 Sep. 30 [cited 2024 Dec. 22];11(5):4249-58. Available from: https://ijpsnonline.com/index.php/ijpsn/article/view/390
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Research Articles
References
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Arjun N, Narendar D, Sunitha K, Harika K, Madhusudan Rao Y and Nagaraj B (2016). Development, evaluation and influence of formulation and process variables on in vitro performance of oral elementary osmotic device of atenolol. Int J Pharm Invest 6(4): 1-9.
Arun Butreddy and Narendar Dudhipala (2015). Enhancement of solubility and dissolution rate of trandolapril sustained release matrix tablets by liquisolid compact approach. Asian J Pharma 9(4): 290-297.
Bromberg LE, Buxton DK and Friden PM (2001). Novel periodontal drug delivery system for treatment of periodontitis. J Control Rel 71: 251-259.
Chandra Sekhar K, Naidu KVS, Ramesh G, Vamshi Vishnu Y and Madhusudan Rao Y (2008). Transbuccal Delivery of chlorpheniramine maleate from Mucoadhesive Buccal Patches. Cur Drug Del 15: 185-91.
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Chinna Reddy Palem, Narendar D, Sunil Kumar Battu, Michael A Repka and Madhusudan Rao Yamsani (2016). Development, optimization and in vivo characterization of domperidone controlled release hot melt extruded films for buccal delivery. Drug Dev Ind Pharm 42(3): 473-484.
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Codd JE and Deasy PB (1998). Formulation development and in vivo evaluation of a novel bioadhesive lozenge containing a synergistic combination of antifungal agents. Int J Pharm 173: 13-24.
Dudhipala N, Arjun N, Karthik Yadav J and Ramesh B (2016). Amoxycillin trihydrate floating-bioadhesive drug delivery system for eradication of helicobacter pylori: preparation, in vitro and ex vivo evaluation. J Bioequ Avail 8(3): 118-124.
Dudhipala N, Chinna Reddy P, Sunil R and Madhusudan Rao Y (2011). Pharmaceutical Development and Clinical Pharmacokinetic Evaluation of Gastroretentive Floating Matrix Tablets of Levofloxacin. Int J Pharm Sci Nanotech 4(3): 1461-1467.
Harris D and Robinson JR (1992). Drug delivery via the mucous membranes of the oral cavity. J Pharm Sci 81: 1-10.
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Nagaraj K, Narendar D and Kishan V (2017). Development of olmesartan medoxomil optimized nanosuspension using Box-Behnken design to improve oral bioavailability. Drug Dev Ind Pharm 43(7): 1186-1196.
Narendar D and Kishan V (2016). Candesartan cilexetil loaded solid lipid nanoparticles for oral delivery: characterization, pharmacokinetic and pharmacodynamic evaluation. Drug Delivery 23(2): 395-404.
Narendar D and Kishan V (2017). Improved anti-hyperlipidemic activity of Rosuvastatin Calcium via lipid nanoparticles: pharmacokinetic and pharmacodynamic evaluation. Euro J Pharm Biopharm 110(1): 47-57.
Narendar D, Arjun N, Dinesh S and Karthik J (2016). Biopharmaceutical and preclinical studies of efficient oral delivery of zaleplon as semisolid dispersions with self-emulsifying lipid surfactants. Int J Pharm Sci Nanotech 9(1): 1-8.
Narendar D, Someshwar K, Arjun N and Rao YM (2016). Quality by design approach for development and optimization of Quetiapine Fumarate effervescent floating matrix tablets for improved oral delivery. J Pharm Investigation 46(3): 253-263.
Palem CR, Narendar D, Satyanarayana G and Varsha BP (2016). Development and optimization of Atorvastatin calcium-cyclodextrin inclusion complexed oral disintegrating tablets for enhancement of solubility, dissolution, pharmacokinetic and pharmacodynamic activity by central composite design. Int J Pharm Sci Nanotech 9(2): 1-11.
Palem CR, Ramesh G, Narender D, Vamshi V Y and Madhusudan RY (2011). Transmucosal delivery of domperidone from bilayered buccal patches: in vitro, ex vivo and in vivo characterization. Arch Pharm Res 34(10): 1701-1710.
Peppas NA (1985). Analysis of Fickian and non-Fickian drug release from polymers. Pharma Acta Helvetiae 60: 110-111.
Pitta Sravan, Dudhipala Narendar, Narala Arjun and Veerabrahma Kishan (2018). Development and evaluation of zolmitriptan transfersomes by Box-Behnken design for improved bio-availability by nasal delivery. Drug Dev Ind Pharm 44(3): 484-492.
Reddy ND, Reddy CP, Sunil R and Madhusudan Rao Y (2012). Development of floating matrix tablets of Ofloxacin and Ornidazole in combined dosage form: in vitro and in vivo evaluation in healthy human volunteers. Int J Drug Deli 4: 462-469.
Rojanasakul Y, Wang LY, Bhat M, Glover DD, Malanga CJ and Ma JKH (1992). The transport barrier of epithelia; a comparative study on membrane permeability and charge selectivity in the rabbit. Pharma Res 9: 1029-1034.
Schor JM, Davis SS, Nigalaye A and Bolton S (1983). Susadrin Transmucosal tablets. Drug Dev Ind Pharmacy 9: 1359-1377.
Senel S, Hıncal AA and Squier CA (2000). Effect of chitosan in enhancing drug delivery across buccal mucosa. Adv Chitin Sci 4: 254-258.
Shayeda, Ramesh G, Chinna Reddy P and Madhusudan Rao Y (2009). Development of novel bioadhesive buccal formulation of diltiazem: in vitro and in vivo characterization. PDA J Pharm Sci Tech 63(4): 1-9.
Shojaei AH, Zhuo SL and Li X (1998). Transbuccal delivery of acyclovir (II): feasibility, system design, and in vitro permeation studies. J Pharm Sci 1: 66–73.
Swetha E and Narendar D (2017). Influence of β-Cyclodextrin and Hydroxypropyl-β-Cyclodextrin on Enhancement of Solubility and Dissolution of Isradipine. Int J Pharm Sci Nanotech 10(3): 3752-3757.
Thirupathi G, Swetha E and Narendar D (2017). Role of isradipine loaded solid lipid nanoparticles in the pharmacodynamic effect of isradipine in rats. Drug Res 67(3): 163-169.
Amanpreet Kaur and Gurpreet Kaur (2012). Mucoadhesive buccal patches based on inter polymer complexes of chitosan–pectin for delivery of Carvedilol. Saudi Pharm J 20(1): 21-27.
Arjun N, Narendar D, Sunitha K, Harika K, Madhusudan Rao Y and Nagaraj B (2016). Development, evaluation and influence of formulation and process variables on in vitro performance of oral elementary osmotic device of atenolol. Int J Pharm Invest 6(4): 1-9.
Arun Butreddy and Narendar Dudhipala (2015). Enhancement of solubility and dissolution rate of trandolapril sustained release matrix tablets by liquisolid compact approach. Asian J Pharma 9(4): 290-297.
Bromberg LE, Buxton DK and Friden PM (2001). Novel periodontal drug delivery system for treatment of periodontitis. J Control Rel 71: 251-259.
Chandra Sekhar K, Naidu KVS, Ramesh G, Vamshi Vishnu Y and Madhusudan Rao Y (2008). Transbuccal Delivery of chlorpheniramine maleate from Mucoadhesive Buccal Patches. Cur Drug Del 15: 185-91.
Chinna Reddy P, Narendar D, Sunil Kumar B, Satyanarayana G, Michale AR and Madhusudan Rao Y (2015). Combined dosage form of pioglitazone and felodipine as mucoadhesive pellets via hot melt extrusion for improved buccal delivery with application of quality by design approach. J Drug Del Sci Tech 30: 209-219.
Chinna Reddy Palem, Narendar D, Sunil Kumar Battu, Michael A Repka and Madhusudan Rao Yamsani (2016). Development, optimization and in vivo characterization of domperidone controlled release hot melt extruded films for buccal delivery. Drug Dev Ind Pharm 42(3): 473-484.
Chopparapu KCS, Palem CR, Dudhipala NR and Rao YM (2011). Development of Promethazine Hydrochloride Mucoadhesive Patches for Buccal Delivery: In vitro, Ex vivo and In vivo Characterization. Int J Pharm Sci Nanotech 5(2): 1697- 1705.
Codd JE and Deasy PB (1998). Formulation development and in vivo evaluation of a novel bioadhesive lozenge containing a synergistic combination of antifungal agents. Int J Pharm 173: 13-24.
Dudhipala N, Arjun N, Karthik Yadav J and Ramesh B (2016). Amoxycillin trihydrate floating-bioadhesive drug delivery system for eradication of helicobacter pylori: preparation, in vitro and ex vivo evaluation. J Bioequ Avail 8(3): 118-124.
Dudhipala N, Chinna Reddy P, Sunil R and Madhusudan Rao Y (2011). Pharmaceutical Development and Clinical Pharmacokinetic Evaluation of Gastroretentive Floating Matrix Tablets of Levofloxacin. Int J Pharm Sci Nanotech 4(3): 1461-1467.
Harris D and Robinson JR (1992). Drug delivery via the mucous membranes of the oral cavity. J Pharm Sci 81: 1-10.
Ishida M, Nambu N and Nagai T (1982). Mucosal dosage form of lidocaine for toothache using hydroxypropyl cellulose. Chem and Pharma Bul 30: 980-4.
Korsmeyer RW, Gurny R, Doelker E, Buri P and Peppas NA (1983). Mechanism of solute release from porous hydro-matrices and other factors may be responsible. Int J Pharm 15(1): 25-35.
Nagaraj K, Narendar D and Kishan V (2017). Development of olmesartan medoxomil optimized nanosuspension using Box-Behnken design to improve oral bioavailability. Drug Dev Ind Pharm 43(7): 1186-1196.
Narendar D and Kishan V (2016). Candesartan cilexetil loaded solid lipid nanoparticles for oral delivery: characterization, pharmacokinetic and pharmacodynamic evaluation. Drug Delivery 23(2): 395-404.
Narendar D and Kishan V (2017). Improved anti-hyperlipidemic activity of Rosuvastatin Calcium via lipid nanoparticles: pharmacokinetic and pharmacodynamic evaluation. Euro J Pharm Biopharm 110(1): 47-57.
Narendar D, Arjun N, Dinesh S and Karthik J (2016). Biopharmaceutical and preclinical studies of efficient oral delivery of zaleplon as semisolid dispersions with self-emulsifying lipid surfactants. Int J Pharm Sci Nanotech 9(1): 1-8.
Narendar D, Someshwar K, Arjun N and Rao YM (2016). Quality by design approach for development and optimization of Quetiapine Fumarate effervescent floating matrix tablets for improved oral delivery. J Pharm Investigation 46(3): 253-263.
Palem CR, Narendar D, Satyanarayana G and Varsha BP (2016). Development and optimization of Atorvastatin calcium-cyclodextrin inclusion complexed oral disintegrating tablets for enhancement of solubility, dissolution, pharmacokinetic and pharmacodynamic activity by central composite design. Int J Pharm Sci Nanotech 9(2): 1-11.
Palem CR, Ramesh G, Narender D, Vamshi V Y and Madhusudan RY (2011). Transmucosal delivery of domperidone from bilayered buccal patches: in vitro, ex vivo and in vivo characterization. Arch Pharm Res 34(10): 1701-1710.
Peppas NA (1985). Analysis of Fickian and non-Fickian drug release from polymers. Pharma Acta Helvetiae 60: 110-111.
Pitta Sravan, Dudhipala Narendar, Narala Arjun and Veerabrahma Kishan (2018). Development and evaluation of zolmitriptan transfersomes by Box-Behnken design for improved bio-availability by nasal delivery. Drug Dev Ind Pharm 44(3): 484-492.
Reddy ND, Reddy CP, Sunil R and Madhusudan Rao Y (2012). Development of floating matrix tablets of Ofloxacin and Ornidazole in combined dosage form: in vitro and in vivo evaluation in healthy human volunteers. Int J Drug Deli 4: 462-469.
Rojanasakul Y, Wang LY, Bhat M, Glover DD, Malanga CJ and Ma JKH (1992). The transport barrier of epithelia; a comparative study on membrane permeability and charge selectivity in the rabbit. Pharma Res 9: 1029-1034.
Schor JM, Davis SS, Nigalaye A and Bolton S (1983). Susadrin Transmucosal tablets. Drug Dev Ind Pharmacy 9: 1359-1377.
Senel S, Hıncal AA and Squier CA (2000). Effect of chitosan in enhancing drug delivery across buccal mucosa. Adv Chitin Sci 4: 254-258.
Shayeda, Ramesh G, Chinna Reddy P and Madhusudan Rao Y (2009). Development of novel bioadhesive buccal formulation of diltiazem: in vitro and in vivo characterization. PDA J Pharm Sci Tech 63(4): 1-9.
Shojaei AH, Zhuo SL and Li X (1998). Transbuccal delivery of acyclovir (II): feasibility, system design, and in vitro permeation studies. J Pharm Sci 1: 66–73.
Swetha E and Narendar D (2017). Influence of β-Cyclodextrin and Hydroxypropyl-β-Cyclodextrin on Enhancement of Solubility and Dissolution of Isradipine. Int J Pharm Sci Nanotech 10(3): 3752-3757.
Thirupathi G, Swetha E and Narendar D (2017). Role of isradipine loaded solid lipid nanoparticles in the pharmacodynamic effect of isradipine in rats. Drug Res 67(3): 163-169.
