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Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1871-5230
ISSN (Online): 1875-614X

Research Article

Hydroxypropyl Methylcellulose Orodispersible Film Containing Desloratadine for Geriatric Use: Formulation and Evaluation

Author(s): Aya Yahya Fayez Al-Oran and Evrim Yenilmez*

Volume 22, Issue 2, 2023

Published on: 18 September, 2023

Page: [79 - 91] Pages: 13

DOI: 10.2174/1871523022666230816090942

Price: $65

Abstract

Background: Oral strip is very similar to thin strip of postage stamp in shape, size and thickness. The strip is designed to be placed on the tongue or any oral mucosal tissue which immediately gets wet and hydrated after being in contact with the saliva. Desloratadine is one of the better- known second-generation antihistamines that has been studied for being effective in relieving the allergic nasal and skin symptoms.

Objective: The aim of this study is to develop desloratadine orodispersible film (ODF) with fast disintegration time and suitable mechanical strength to treat allergic symptoms in geriatric patients in order to increase compliance and convenience.

Methods: Solvent casting method using hydroxypropyl methylcellulose (HPMC) as the film forming polymer was applied. Polyethylene glycol 400 (PEG 400) and glycerol (Gly) were used as the plasticizers and citric acid (CA) was used as saliva stimulating agent. The resultant films were evaluated for disintegration time, folding endurance, surface pH, weight variation, thickness, surface morphology using scanning electron microscopy, drug content, content uniformity, moisture loss, moisture uptake, and drug-excipient compatibility using DSC and FT-IR.

Results: All the selected films started to disintegrate in less than 14 seconds. Selected optimum films exhibited good mechanical properties with a folding endurance value greater than 100. The uniformity in weight, thickness, and drug content in the selected films was obtained. Surface pH was within the normal range (6.4 - 6.8). A smooth surface of the films was obtained and drugexcipient compatibility was proved using DSC and FT-IR. The dissolution test was done for optimum film formulations by simulating the oral cavity physiological conditions using the conventional dissolution test apparatus. More than 87% of the drug was released by the 4th minute.

Conclusion: Orodispersible film of desloratadine was successfully prepared by solvent casting method in order to improve the disintegration/dissolution of the drug in oral cavity and hence better patient compliance and effective therapy.

Keywords: Orodispersible film, desloratadine, oral strip, oral film, allergic symptoms, geriatric.

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[1]
Darji, M.A.; Lalge, R.M.; Marathe, S.P.; Mulay, T.D.; Fatima, T.; Alshammari, A.; Lee, H.K.; Repka, M.A.; Narasimha Murthy, S. Excipient stability in oral solid dosage forms: A review. AAPS PharmSciTech, 2018, 19(1), 12-26.
[http://dx.doi.org/10.1208/s12249-017-0864-4] [PMID: 28895106]
[2]
Kulkarni, A.S.; Deokule, H.A.; Mane, M.S.; Ghadge, D.M. Exploration of different polymers for use in the formulation of oral fast dissolving strips. J. Curr. Pharm. Res. JCPR., 2010, 2(1), 33-35.
[3]
Stegemann, S.; Ecker, F.; Maio, M.; Kraahs, P.; Wohlfart, R.; Breitkreutz, J.; Zimmer, A.; Bar-Shalom, D.; Hettrich, P.; Broegmann, B. Geriatric drug therapy: Neglecting the inevitable majority. Ageing Res. Rev., 2010, 9(4), 384-398.
[http://dx.doi.org/10.1016/j.arr.2010.04.005] [PMID: 20478411]
[4]
Wahlich, J.; Stegemann, S.; Orlu-Gul, M. Meeting commentary—“Medicines for older adults: Learning from practice to develop patient centric drug products”. Int. J. Pharm., 2013, 456(1), 251-257.
[http://dx.doi.org/10.1016/j.ijpharm.2013.07.038] [PMID: 23916726]
[5]
Okuda, Y.; Irisawa, Y.; Okimoto, K.; Osawa, T.; Yamashita, S. A new formulation for orally disintegrating tablets using a suspension spray-coating method. Int. J. Pharm., 2009, 382(1-2), 80-87.
[http://dx.doi.org/10.1016/j.ijpharm.2009.08.010] [PMID: 19686825]
[6]
Gryczke, A.; Schminke, S.; Maniruzzaman, M.; Beck, J.; Douroumis, D. Development and evaluation of orally disintegrating tablets (ODTs) containing Ibuprofen granules prepared by hot melt extrusion. Colloids Surf. B Biointerfaces, 2011, 86(2), 275-284.
[http://dx.doi.org/10.1016/j.colsurfb.2011.04.007] [PMID: 21592751]
[7]
Dixit, R.P.; Puthli, S.P. Oral strip technology: Overview and future potential. J. Control. Release, 2009, 139(2), 94-107.
[http://dx.doi.org/10.1016/j.jconrel.2009.06.014] [PMID: 19559740]
[8]
Al-khattawi, A.; Mohammed, A.R. Compressed orally disintegrating tablets: Excipients evolution and formulation strategies. Expert Opin. Drug Deliv., 2013, 10(5), 651-663.
[http://dx.doi.org/10.1517/17425247.2013.769955] [PMID: 23387409]
[9]
Liew, K.B.; Tan, Y.T.F.; Peh, K.K. Characterization of oral disintegrating film containing donepezil for Alzheimer disease. AAPS PharmSciTech, 2012, 13(1), 134-142.
[http://dx.doi.org/10.1208/s12249-011-9729-4] [PMID: 22167416]
[10]
Patel, J.G.; Modi, A.D. Formulation, optimization and evaluation of levocetirizine dihyrochloride oral thin strip. J. Pharm. Bioallied Sci., 2012, 4(5(S1)), 35.
[http://dx.doi.org/10.4103/0975-7406.94133] [PMID: 23066198]
[11]
Irfan, M.; Rabel, S.; Bukhtar, Q.; Qadir, M.I.; Jabeen, F.; Khan, A. Orally disintegrating films: A modern expansion in drug delivery system. Saudi Pharm. J., 2016, 24(5), 537-546.
[http://dx.doi.org/10.1016/j.jsps.2015.02.024] [PMID: 27752225]
[12]
Karki, S.; Kim, H.; Na, S.J.; Shin, D.; Jo, K.; Lee, J. Thin films as an emerging platform for drug delivery. Asian J. Pharmaceut. Sci., 2016, 11(5), 559-574.
[http://dx.doi.org/10.1016/j.ajps.2016.05.004]
[13]
Gholve, S.; Savalsure, S.; Bhusnure, O.; Surywanshi, S.; Birajdar, M. Formulation and evaluation of oral fast dissolving sublingual film of formulation and evaluation of oral fast dissolving sublingual film of propranolol HCl. Int. J. Pharma Res. Heal. Sci., 2018, 6(2), 2369-2373.
[14]
Borges, A.F.; Silva, C.; Coelho, J.F.J.; Simões, S. Oral films: Current status and future perspectives. J. Control. Release, 2015, 206, 1-19.
[http://dx.doi.org/10.1016/j.jconrel.2015.03.006] [PMID: 25747406]
[15]
Łagun, A. Desloratadine in the treatment of allergic rhinitis and urticaria in a daily practice of family doctors. Lek. POZ., 2017, 3(2), 125-128.
[16]
Buczak, K.; Sybilski, A.J. The role of desloratadine in the treatment of allergic rhinitis and urticaria. Lek. POZ., 2018, 4(2), 119-126.
[17]
Singh, H.; Kaur, M.; Verma, H. Optimization and evaluation of desloratadine oral strip: An innovation in paediatric medication. ScientificWorldJournal, 2013, 2013, 1-9.
[http://dx.doi.org/10.1155/2013/395681] [PMID: 24235887]
[18]
Joshua, J.M.; Hari, R.; Jyothish, F.K.; Surendran, S.A. Fast dissolving oral thin films: An effective dosage form for quick releases. Int. J. Pharm. Sci. Rev. Res., 2016, 38(1), 282-289.
[19]
Chaudhary, H.; Gauri, S.; Rathee, P.; Kumar, V. Development and optimization of fast dissolving oro-dispersible films of granisetron HCl using Box–Behnken statistical design. Bull. Fac. Pharm. Cairo Univ., 2013, 51(2), 193-201.
[http://dx.doi.org/10.1016/j.bfopcu.2013.05.002]
[20]
Rençber, S.; Karavana, S.Y.; Yilmaz, F.F.; Eraç, B.; Nenni, M.; Gurer-Orhan, H.; Limoncu, M.H.; Güneri, P.; Ertan, G. Formulation and evaluation of fluconazole loaded oral strips for local treatment of oral candidiasis. J. Drug Deliv. Sci. Technol., 2019, 49, 615-621.
[http://dx.doi.org/10.1016/j.jddst.2018.12.035]
[21]
Centkowska, K.; Ławrecka, E.; Sznitowska, M. Technology of orodispersible polymer films with micronized loratadine—influence of different drug loadings on film properties. Pharmaceutics, 2020, 12(3), 250.
[http://dx.doi.org/10.3390/pharmaceutics12030250] [PMID: 32164345]
[22]
Alhayali, A.; Vuddanda, P.R.; Velaga, S. Silodosin oral films: Development, physico-mechanical properties and in vitro dissolution studies in simulated saliva. J. Drug Deliv. Sci. Technol., 2019, 53, 101122.
[http://dx.doi.org/10.1016/j.jddst.2019.06.019]
[23]
Bondili, S.; Ramya, M. Method development and validation of desloratadine in bulk and its tablet dosage forms. Int. J. Pharm. Ind. Res., 2011, 1(3), 245-250.
[24]
Patil, A.B.; Charyulu, R.N.; Shastry, C.S. Development and characterization of atenolol fast dissolving orodispersible films. World J. Pharm. Res., 2013, 2(6), 3284-3295.
[25]
Bharti, K.; Mittal, P.; Mishra, B. Formulation and characterization of fast dissolving oral films containing buspirone hydrochloride nanoparticles using design of experiment. J. Drug Deliv. Sci. Technol., 2019, 49, 420-432.
[http://dx.doi.org/10.1016/j.jddst.2018.12.013]
[26]
Sudhakara Reddy, P.; Koteswara Rao, G.S.N.; Ramana Murthy, K.V. Formulation and evaluation of oral fast dissolving films of poorly soluble drug loperamide HCl using transcutol HP. Int. J. Adv. Pharma. Biotechnol., 2016, 2(2), 15-31.
[http://dx.doi.org/10.38111/ijapb.20160202003]
[27]
Al-Mogherah, A.I.; Ibrahim, M.A.; Hassan, M.A. Optimization and evaluation of venlafaxine hydrochloride fast dissolving oral films. Saudi Pharm. J., 2020, 28(11), 1374-1382.
[http://dx.doi.org/10.1016/j.jsps.2020.09.001] [PMID: 33250644]
[28]
Panchal, M.S.; Patel, H.; Bagada, A.; Vadalia, K.R. Formulation and evaluation of mouth dissolving film of ropinirole hydrochloride by using pullulan polymers. Int. J. Pharm. Res. Allied Sci., 2012, 1(3), 60-72.
[29]
Adrover, A.; Pedacchia, A.; Petralito, S.; Spera, R. in vitro dissolution testing of oral thin films: A comparison between USP 1, USP 2 apparatuses and a new millifluidic flow-through device. Chem. Eng. Res. Des., 2015, 95, 173-178.
[http://dx.doi.org/10.1016/j.cherd.2014.10.020]
[30]
Yenilmez, E.; Öztürk, A.A.; Başaran, E. Preparation and in vitro, ex vivo evaluation of benzidamine hydrochloride loaded fast dissolving oral strip formulations: Treatment of oral mucositis due to side effects of chemotherapy and radiotherapy. Lett. Drug Des. Discov., 2023, 20(8), 1147-1157.
[http://dx.doi.org/10.2174/1570180820666230207122755]
[31]
Ullah, W.; Nawaz, A.; Akhlaq, M.; Shah, K.U.; Latif, M.S.; Doolaanea, A.A.; Alfatama, M. Transdermal delivery of gatifloxacin carboxymethyl cellulose-based patches: Preparation and characterization. J. Drug Deliv. Sci. Technol., 2021, 66, 102783.
[http://dx.doi.org/10.1016/j.jddst.2021.102783]
[32]
Galgatte, U.C.; Khanchandani, S.S.; Jadhav, Y.G.; Chaudhari, P.D. Investigation of different polymers, plasticizers and superdisintegrating agents alone and in combination for use in the formulation of fast dissolving oral films. Int. J. Pharm. Tech. Res., 2013, 5(4), 1465-1472.
[33]
Abdelbary, A.; Bendas, E.R.; Ramadan, A.A.; Mostafa, D.A. Pharmaceutical and pharmacokinetic evaluation of a novel fast dissolving film formulation of flupentixol dihydrochloride. AAPS PharmSciTech, 2014, 15(6), 1603-1610.
[http://dx.doi.org/10.1208/s12249-014-0186-8] [PMID: 25142820]
[34]
Garsuch, V.; Breitkreutz, J. Comparative investigations on different polymers for the preparation of fast-dissolving oral films. J. Pharm. Pharmacol., 2010, 62(4), 539-545.
[http://dx.doi.org/10.1211/jpp.62.04.0018] [PMID: 20604845]
[35]
Speer, I.; Steiner, D.; Thabet, Y.; Breitkreutz, J.; Kwade, A. Comparative study on disintegration methods for oral film preparations. Eur. J. Pharm. Biopharm., 2018, 132, 50-61.
[http://dx.doi.org/10.1016/j.ejpb.2018.09.005] [PMID: 30201569]
[36]
Liew, K.B.; Tan, Y.T.F.; Peh, K.K. Effect of polymer, plasticizer and filler on orally disintegrating film. Drug Dev. Ind. Pharm., 2014, 40(1), 110-119.
[http://dx.doi.org/10.3109/03639045.2012.749889] [PMID: 23311593]
[37]
Raju, P.N.; Kumar, M.S.; Reddy, C.M.; Ravishankar, K. Formulation and evaluation of fast dissolving films of loratidine by solvent casting method. Pharma Innov., 2013, 2(2), 31-35.
[38]
Bhyan, B.; Jangra, S.; Kaur, M.; Singh, H. Orally fast dissolving films: Innovations in formulation and technology. Int. J. Pharm. Sci. Rev. Res., 2011, 9(2), 50-57.
[39]
Takeuchi, Y.; Ikeda, N.; Tahara, K.; Takeuchi, H. Mechanical characteristics of orally disintegrating films: Comparison of folding endurance and tensile properties. Int. J. Pharm., 2020, 589, 119876.
[http://dx.doi.org/10.1016/j.ijpharm.2020.119876] [PMID: 32927004]
[40]
Morales, J.O.; McConville, J.T. Manufacture and characterization of mucoadhesive buccal films. Eur. J. Pharm. Biopharm., 2011, 77(2), 187-199.
[http://dx.doi.org/10.1016/j.ejpb.2010.11.023] [PMID: 21130875]
[41]
Hl, R.; Kumar, G.P. Development and evaluation of polymer-bound glibenclamide oral thin film. J. Bioequivalence Bioavailab., 2016, 9(1), 324-330.
[http://dx.doi.org/10.4172/jbb.1000319]
[42]
Garcia, V.A.S.; Borges, J.G.; Maciel, V.B.V.; Mazalli, M.R.; Lapa-Guimaraes, J.G.; Vanin, F.M.; de Carvalho, R.A. Gelatin/starch orally disintegrating films as a promising system for vitamin C delivery. Food Hydrocoll., 2018, 79, 127-135.
[http://dx.doi.org/10.1016/j.foodhyd.2017.12.027]
[43]
Sjöholm, E.; Sandler, N. Additive manufacturing of personalized orodispersible warfarin films. Int. J. Pharm., 2019, 564, 117-123.
[http://dx.doi.org/10.1016/j.ijpharm.2019.04.018] [PMID: 30974195]
[44]
Nair, A.B.; Kumria, R.; Harsha, S.; Attimarad, M.; Al-Dhubiab, B.E.; Alhaider, I.A. In vitro techniques to evaluate buccal films. J. Control. Release, 2013, 166(1), 10-21.
[http://dx.doi.org/10.1016/j.jconrel.2012.11.019] [PMID: 23219961]
[45]
Dharmasthala, S.; Shabaraya, A.R.; Andrade, G.S.; Shriram, R.G.; Hebbar, S.; Dubey, A. Fast dissolving oral film of piroxicam: Solubility enhancement by forming an inclusion complex with β-cyclodextrin, formulation and evaluation. J. Young Pharm., 2018, 11(1), 1-6.
[http://dx.doi.org/10.5530/jyp.2019.11.1]
[46]
Mushtaque, M.; Muhammad, I.N.; Fareed Hassan, S.M.; Ali, A.; Masood, R. Development and pharmaceutical evaluation of oral fast dissolving thin film of escitalopram: A patient friendly dosage form. Pak. J. Pharm. Sci., 2020, 33(1), 183-189.
[http://dx.doi.org/10.36721/PJPS.2020.33.1.REG.183-189.1] [PMID: 32122847]
[47]
Thakur, R.R.; Rathore, D.S.; Narwal, S. Orally disintegrating preparations: Recent advancement in formulation and technology. J. Drug Deliv. Ther., 2012, 2(3), 87-96.
[http://dx.doi.org/10.22270/jddt.v2i3.130]
[48]
Castro, P.M.; Sousa, F.; Magalhães, R.; Ruiz-Henestrosa, V.M.P.; Pilosof, A.M.R.; Madureira, A.R.; Sarmento, B.; Pintado, M.E. Incorporation of beads into oral films for buccal and oral delivery of bioactive molecules. Carbohydr. Polym., 2018, 194, 411-421.
[http://dx.doi.org/10.1016/j.carbpol.2018.04.032] [PMID: 29801856]
[49]
Vuddanda, P.R.; Montenegro-Nicolini, M.; Morales, J.O.; Velaga, S. Effect of surfactants and drug load on physico-mechanical and dissolution properties of nanocrystalline tadalafil-loaded oral films. Eur. J. Pharm. Sci., 2017, 109, 372-380.
[http://dx.doi.org/10.1016/j.ejps.2017.08.019] [PMID: 28823854]
[50]
Sharma, A.; Agarwal, D. Formulation and evaluation of montelukast sodium oral dissolving film. Asian J. Pharmaceut. Res. Develop., 2021, 9(1), 130-140.
[http://dx.doi.org/10.22270/ajprd.v9i1.893]
[51]
Pimparade, M.B.; Vo, A.; Maurya, A.S.; Bae, J.; Morott, J.T.; Feng, X.; Kim, D.W.; Kulkarni, V.I.; Tiwari, R.; Vanaja, K.; Murthy, R.; Shivakumar, H.N.; Neupane, D.; Mishra, S.R.; Murthy, S.N.; Repka, M.A. Development and evaluation of an oral fast disintegrating anti-allergic film using hot-melt extrusion technology. Eur. J. Pharm. Biopharm., 2017, 119, 81-90.
[http://dx.doi.org/10.1016/j.ejpb.2017.06.004] [PMID: 28596037]
[52]
Reddy, P.S.; Murthy, K.V.R. Formulation and evaluation of oral fast dissolving films of poorly soluble drug ezetimibe using transcutol Hp, Indian J. Indian J. Pharmaceut. Edu. Res., 2018, 52(3), 398-407.
[http://dx.doi.org/10.5530/ijper.52.3.46]
[53]
Sheikh, F.A.; Aamir, M.N.; Shah, M.A.; Ali, L.; Anwer, K.; Javaid, Z. Formulation design, characterization and in vitro drug release study of orodispersible film comprising BCS class II drugs. Pak. J. Pharm. Sci., 2020, 33(1), 343-353.
[http://dx.doi.org/10.36721/PJPS.2020.33.1.SUP.343-353.1] [PMID: 32122867]
[54]
Bala, R.; Khanna, S.; Pawar, P. Design optimization and in vitro-in vivo evaluation of orally dissolving strips of clobazam. J. Drug Deliv., 2014, 2014, 1-15.
[http://dx.doi.org/10.1155/2014/392783] [PMID: 25328709]
[55]
Yenılmez, E. Desloratadine-Eudragit® RS100 nanoparticles: formulation and characterization. Turkish J. Pharmaceut. Sci., 2017, 14(2), 148-156.
[http://dx.doi.org/10.4274/tjps.52523] [PMID: 32454606]
[56]
Speer, I.; Preis, M.; Breitkreutz, J. Dissolution testing of oral film preparations: Experimental comparison of compendial and non-compendial methods. Int. J. Pharm., 2019, 561, 124-134.
[http://dx.doi.org/10.1016/j.ijpharm.2019.02.042] [PMID: 30826424]
[57]
Öztürk, A.A.; Kıyan, H.T. Treatment of oxidative stress-induced pain and inflammation with dexketoprofen trometamol loaded different molecular weight chitosan nanoparticles: Formulation, characterization and anti-inflammatory activity by using in vivo HET-CAM assay. Microvasc. Res., 2020, 128, 103961.
[http://dx.doi.org/10.1016/j.mvr.2019.103961] [PMID: 31758946]

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