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Published in: Polymer Bulletin 5/2019

30-08-2018 | Original Paper

Design, characterization and evaluation of oral fast dissolving polymeric films of isradipine inclusion complex

Authors: Sayed H. Auda, Abdullah H. Al-Omrani, Fars K. Alanazi, Mohamed M. Badran, Faiyaz Shakeel

Published in: Polymer Bulletin | Issue 5/2019

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Abstract

This study aimed to enhance the dissolution rate of isradipine and to avoid the problem of first-pass metabolism using oral fast dissolving films (OFDFs). Isradipine was complexed with hydroxypropyl-beta-cyclodextrin (HP-β-CD) using the solvent co-evaporation technique to produce an isradipine inclusion complex with increased solubility. This complex was evaluated for its solubility and dissolution behavior compared with the free drug. Then, the inclusion complex was formulated in OFDFs. The fabricated films were evaluated for their drug content uniformity, surface pH, thickness, tensile strength, percent elongation, disintegration time and in vitro drug release profile. Additionally, Fourier transform infrared spectroscopy and differential scanning calorimetry were utilized to characterize the medicated films and the corresponding physical mixture as well as the individual components. The results indicated that the inclusion complexation of isradipine enhances its solubility and dissolution rate. Films were found to be faint yellow, elastic, compatible and palatable and to have acceptable tensile strength. The complexed drug with HP-β-CD in the presence of a high level of disintegrants enhanced the drug dissolution compared to the plain film.

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Literature
1.
go back to reference Zhang H, Zhang J, Streisand JB (2002) Oral mucosal drug delivery: clinical pharmacokinetics and therapeutic applications. Clin Pharmacokinet 41:661–680CrossRefPubMed Zhang H, Zhang J, Streisand JB (2002) Oral mucosal drug delivery: clinical pharmacokinetics and therapeutic applications. Clin Pharmacokinet 41:661–680CrossRefPubMed
2.
go back to reference Gavaskar B, Kumar SV, Sharan G, Rao YM (2010) Overview of fast dissolving films. Int J Pharm Pharm Sci 2:29–33 Gavaskar B, Kumar SV, Sharan G, Rao YM (2010) Overview of fast dissolving films. Int J Pharm Pharm Sci 2:29–33
3.
go back to reference Irfan M, Rabel S, Bukhtar Q, Qadir MR, Jabeen F, Khan A (2016) Orally disintegrating films: a modern expansion in drug delivery system. Saudi Pharm J 24:537–546CrossRefPubMed Irfan M, Rabel S, Bukhtar Q, Qadir MR, Jabeen F, Khan A (2016) Orally disintegrating films: a modern expansion in drug delivery system. Saudi Pharm J 24:537–546CrossRefPubMed
4.
go back to reference Papamichael K, Karatzas P, Theodoropoulos I, Kyriakos N, Archavlis E, Mantzaris GJ (2015) Simethicone adjunct to polyethylene glycol improves small bowel capsule endoscopy imaging in non-Crohn’s disease patients. Ann Gastroenterol 28:464–468PubMedPubMedCentral Papamichael K, Karatzas P, Theodoropoulos I, Kyriakos N, Archavlis E, Mantzaris GJ (2015) Simethicone adjunct to polyethylene glycol improves small bowel capsule endoscopy imaging in non-Crohn’s disease patients. Ann Gastroenterol 28:464–468PubMedPubMedCentral
5.
go back to reference Otero-Espinar FJ, Torres-Labandeira JJ, Alvarez-Lorenzo C, Blanco-Mendez J (2010) Cyclodextrins in drug delivery systems. J Drug Deliv Sci Technol 20:289–301CrossRef Otero-Espinar FJ, Torres-Labandeira JJ, Alvarez-Lorenzo C, Blanco-Mendez J (2010) Cyclodextrins in drug delivery systems. J Drug Deliv Sci Technol 20:289–301CrossRef
6.
go back to reference Mura P, Faucci MT, Parrini PL (2001) Effects of grinding with microcrystalline cellulose and cyclodextrins on the ketoprofen physicochemical properties. Drug Dev Ind Pharm 27:119–128CrossRefPubMed Mura P, Faucci MT, Parrini PL (2001) Effects of grinding with microcrystalline cellulose and cyclodextrins on the ketoprofen physicochemical properties. Drug Dev Ind Pharm 27:119–128CrossRefPubMed
7.
go back to reference Moyano JR, Arias-Blanco MJ, Gines JM, Giordano F (1997) Solid-state characterization and dissolution characteristics of gliclazide-b-cyclodextrin inclusion complexes. Int J Pharm 157:239–243CrossRefPubMed Moyano JR, Arias-Blanco MJ, Gines JM, Giordano F (1997) Solid-state characterization and dissolution characteristics of gliclazide-b-cyclodextrin inclusion complexes. Int J Pharm 157:239–243CrossRefPubMed
8.
go back to reference Pandit V, Gorantla R, Devi K, Pai RS, Sarasija S (2011) Preparation and characterization of pioglitazone cyclodextrin inclusion complexes. J Young Pharm 3:267–274CrossRefPubMedPubMedCentral Pandit V, Gorantla R, Devi K, Pai RS, Sarasija S (2011) Preparation and characterization of pioglitazone cyclodextrin inclusion complexes. J Young Pharm 3:267–274CrossRefPubMedPubMedCentral
9.
go back to reference Pose-Vilarnovo B, Perdomo-Lopez L, Echezarreta-Lopez M, Schroth-Pardo P, Torres-Labandeira JJ (2001) Improvement of water solubility of sulfamethizole through its complexation with beta- and hydroxypropyl-beta-cyclodextrin. characterization of the interaction in solution and solid state. Eur J Pharm Sci 13:325–331CrossRefPubMed Pose-Vilarnovo B, Perdomo-Lopez L, Echezarreta-Lopez M, Schroth-Pardo P, Torres-Labandeira JJ (2001) Improvement of water solubility of sulfamethizole through its complexation with beta- and hydroxypropyl-beta-cyclodextrin. characterization of the interaction in solution and solid state. Eur J Pharm Sci 13:325–331CrossRefPubMed
10.
go back to reference Saito M, Ugajin T, Nozawa Y, Sadzuka Y, Miagishima A, Sonobe T (2002) Preparation and dissolution characteristics of griseofulvin solid dispersions with saccharides. Int J Pharm 249:71–79CrossRefPubMed Saito M, Ugajin T, Nozawa Y, Sadzuka Y, Miagishima A, Sonobe T (2002) Preparation and dissolution characteristics of griseofulvin solid dispersions with saccharides. Int J Pharm 249:71–79CrossRefPubMed
11.
go back to reference Yang P, Li Y, Li W, Zhang H, Gao J, Sun J, Yin X, Zheng A (2018) Preparation and evaluation of carfentanil nasal spray employing cyclodextrin inclusion technology. Drug Dev Ind Pharm 44:953–960CrossRefPubMed Yang P, Li Y, Li W, Zhang H, Gao J, Sun J, Yin X, Zheng A (2018) Preparation and evaluation of carfentanil nasal spray employing cyclodextrin inclusion technology. Drug Dev Ind Pharm 44:953–960CrossRefPubMed
12.
go back to reference Mangolim CM, Moriwaki C, Nogueira AC, Sato F, Baesso ML, Neto AM, Matioli G (2014) Curcumin-β-cyclodextrin inclusion complex: stability, solubility, characterisation by FT-IR, FT-Raman, X-ray diffraction and photoacoustic spectroscopy, and food application. Food Chem 153:361–370CrossRefPubMed Mangolim CM, Moriwaki C, Nogueira AC, Sato F, Baesso ML, Neto AM, Matioli G (2014) Curcumin-β-cyclodextrin inclusion complex: stability, solubility, characterisation by FT-IR, FT-Raman, X-ray diffraction and photoacoustic spectroscopy, and food application. Food Chem 153:361–370CrossRefPubMed
14.
go back to reference Miyashita Y, Peterson D, Rees JM, Flynn JT (2010) Isradipine for the treatment of acute hypertension in hospitalized children and adolescents. J Clin Hypertens 12:850–855CrossRef Miyashita Y, Peterson D, Rees JM, Flynn JT (2010) Isradipine for the treatment of acute hypertension in hospitalized children and adolescents. J Clin Hypertens 12:850–855CrossRef
15.
go back to reference Cipriani A, Saunders K, Attenburrow MJ, Stefaniak J, Panchal P, Stockton S, Lane TA, Tunbridge EM, Geddes JR, Harrison PJ (2016) A systematic review of calcium channel antagonists in bipolar disorder and some considerations for their future developments. Mol Psychiatry 21:1324–1332CrossRefPubMedPubMedCentral Cipriani A, Saunders K, Attenburrow MJ, Stefaniak J, Panchal P, Stockton S, Lane TA, Tunbridge EM, Geddes JR, Harrison PJ (2016) A systematic review of calcium channel antagonists in bipolar disorder and some considerations for their future developments. Mol Psychiatry 21:1324–1332CrossRefPubMedPubMedCentral
16.
go back to reference Peter EP, Shirley CS, Antone FS (1988) Isradipine in the treatment of angina pectoris. Am J Med 84:62–66CrossRef Peter EP, Shirley CS, Antone FS (1988) Isradipine in the treatment of angina pectoris. Am J Med 84:62–66CrossRef
17.
go back to reference Christensen HR, Antonsen K, Simonsen K, Lindekaer A, Bonde J, Angelo HR, Kampmann JP (2000) Bioavailability and pharmacokinetics of isradipine after oral and intravenous administration: half-life shorter than expected. Pharmacol Toxicol 86:178–182CrossRefPubMed Christensen HR, Antonsen K, Simonsen K, Lindekaer A, Bonde J, Angelo HR, Kampmann JP (2000) Bioavailability and pharmacokinetics of isradipine after oral and intravenous administration: half-life shorter than expected. Pharmacol Toxicol 86:178–182CrossRefPubMed
18.
go back to reference Rekha MS, Sultana SKS, Mahathi K, Parveen P, Prathima B, Devi AS (2015) Formulation and evaluation of fast dissolving buccal film containing isradipine solid dispersion. Am J PharmTech Res 5:222–247 Rekha MS, Sultana SKS, Mahathi K, Parveen P, Prathima B, Devi AS (2015) Formulation and evaluation of fast dissolving buccal film containing isradipine solid dispersion. Am J PharmTech Res 5:222–247
19.
go back to reference Kaewnopparat N, Chuchom T, Sunthornpit A, Jangwang A, Kaewnopparat S (2009) Enhanced bromhexine hydrochloride solubility and dissolution by inclusion complexation with methylated β-cyclodextrin. Asian J Pharm Sci 5:114–122 Kaewnopparat N, Chuchom T, Sunthornpit A, Jangwang A, Kaewnopparat S (2009) Enhanced bromhexine hydrochloride solubility and dissolution by inclusion complexation with methylated β-cyclodextrin. Asian J Pharm Sci 5:114–122
20.
go back to reference Bergstrom CAS, Larsson P (2018) Computational prediction of drug solubility in water-based systems: qualitative and quantitative approaches used in the current discovery and development setting. Int J Pharm 540:185–193CrossRefPubMedPubMedCentral Bergstrom CAS, Larsson P (2018) Computational prediction of drug solubility in water-based systems: qualitative and quantitative approaches used in the current discovery and development setting. Int J Pharm 540:185–193CrossRefPubMedPubMedCentral
21.
go back to reference Katariya H, Prajapati J (2013) Development and validation of UV spectrophotometric method for determination of isradipine loaded into solid lipid nanoparticles. Int J Pharm Sci Rev Res 20:162–166 Katariya H, Prajapati J (2013) Development and validation of UV spectrophotometric method for determination of isradipine loaded into solid lipid nanoparticles. Int J Pharm Sci Rev Res 20:162–166
22.
go back to reference Barbic U, Verdenik I, Marolt M, Hren NI (2016) Three-dimensional ultrasound evaluation of tongue volume. Zdrav Vestn 85:228–236 Barbic U, Verdenik I, Marolt M, Hren NI (2016) Three-dimensional ultrasound evaluation of tongue volume. Zdrav Vestn 85:228–236
23.
go back to reference Tomar A, Sharma K, Chauhan NS, Mittal A, Bajaj U (2012) Formulation and evaluation of fast dissolving oral film of dicyclomine as potential route of buccal delivery. Int J Drug Dev Res 4:408–417 Tomar A, Sharma K, Chauhan NS, Mittal A, Bajaj U (2012) Formulation and evaluation of fast dissolving oral film of dicyclomine as potential route of buccal delivery. Int J Drug Dev Res 4:408–417
24.
go back to reference Maheswari KM, Devineni PK, Deekonda S, Shaik S, Uppala NP, Nalluri BN (2014) Development and evaluation of mouth dissolving films of amlodipine besylate for enhanced therapeutic efficacy. J Pharm 2014:E520949 Maheswari KM, Devineni PK, Deekonda S, Shaik S, Uppala NP, Nalluri BN (2014) Development and evaluation of mouth dissolving films of amlodipine besylate for enhanced therapeutic efficacy. J Pharm 2014:E520949
25.
go back to reference Upreti K, Kumar L, Anand SP, Chawla V (2014) Formulation and evaluation of mouth dissolving films of paracetamol. Int J Pharm Pharm Sci 6:200–202 Upreti K, Kumar L, Anand SP, Chawla V (2014) Formulation and evaluation of mouth dissolving films of paracetamol. Int J Pharm Pharm Sci 6:200–202
26.
go back to reference Kumria R, Nair AB, Al-Dhubiab BE (2014) Loratidine buccal films for allergic rhinitis: development and evaluation. Drug Dev Ind Pharm 40:625–631CrossRefPubMed Kumria R, Nair AB, Al-Dhubiab BE (2014) Loratidine buccal films for allergic rhinitis: development and evaluation. Drug Dev Ind Pharm 40:625–631CrossRefPubMed
27.
go back to reference Auda SH, Salem-Bekhit MM, Alanazi FK, Alsarra IA, Shakeel F (2017) Antimicrobial evaluation of novel buccoadhesive films containing Myrrh extract. Polym Bull 74:4041–4054CrossRef Auda SH, Salem-Bekhit MM, Alanazi FK, Alsarra IA, Shakeel F (2017) Antimicrobial evaluation of novel buccoadhesive films containing Myrrh extract. Polym Bull 74:4041–4054CrossRef
28.
go back to reference Tran PH, Tran TT, Piao ZZ, Lim JT, Oh YS, Rhee BJ (2013) Physical properties and in vivo bioavailability in human volunteers of isradipine using controlled release matrix tablet containing self-emulsifying solid dispersion. Int J Pharm 450:79–86CrossRefPubMed Tran PH, Tran TT, Piao ZZ, Lim JT, Oh YS, Rhee BJ (2013) Physical properties and in vivo bioavailability in human volunteers of isradipine using controlled release matrix tablet containing self-emulsifying solid dispersion. Int J Pharm 450:79–86CrossRefPubMed
29.
go back to reference Anwer MK, Jamil S, Ansari MJ, Al-Shdefat R, Ali BE, Ganaie MA, Abdel-Kader MS, Shakeel F (2014) Water soluble binary and ternary complexes of diosmin with β-cyclodextrin: spectroscopic characterization, release studies and anti-oxidant activity. J Mol Liq 199:35–41CrossRef Anwer MK, Jamil S, Ansari MJ, Al-Shdefat R, Ali BE, Ganaie MA, Abdel-Kader MS, Shakeel F (2014) Water soluble binary and ternary complexes of diosmin with β-cyclodextrin: spectroscopic characterization, release studies and anti-oxidant activity. J Mol Liq 199:35–41CrossRef
30.
go back to reference Aloisio C, Antimisiaris SG, Longhi MR (2017) Liposomes containing cyclodextrins or meglumine to solubilize and improve the bioavailability of poorly soluble drugs. J Mol Liq 229:106–113CrossRef Aloisio C, Antimisiaris SG, Longhi MR (2017) Liposomes containing cyclodextrins or meglumine to solubilize and improve the bioavailability of poorly soluble drugs. J Mol Liq 229:106–113CrossRef
31.
go back to reference Altamimi MA, Elzayat EM, Alhowyan AA, Alshehri S, Shakeel F (2018) Effect of β-cyclodextrin and different surfactants on solubility, stability, and permeability of hydrochlorothiazide. J Mol Liq 250:323–328CrossRef Altamimi MA, Elzayat EM, Alhowyan AA, Alshehri S, Shakeel F (2018) Effect of β-cyclodextrin and different surfactants on solubility, stability, and permeability of hydrochlorothiazide. J Mol Liq 250:323–328CrossRef
32.
go back to reference Loftsson T, Magnúsdóttir A, Másson M, Sigurjónsdóttir JF (2002) Self-association and cyclodextrin solubilization of drugs. J Pharm Sci 91:2307–2316CrossRefPubMed Loftsson T, Magnúsdóttir A, Másson M, Sigurjónsdóttir JF (2002) Self-association and cyclodextrin solubilization of drugs. J Pharm Sci 91:2307–2316CrossRefPubMed
33.
go back to reference Conceicao J, Adeoye O, Cabral-Marques HM, Lobo JMS (2018) Cyclodextrins as excipients in tablet formulations. Drug Discov Today 23:1274–1284CrossRefPubMed Conceicao J, Adeoye O, Cabral-Marques HM, Lobo JMS (2018) Cyclodextrins as excipients in tablet formulations. Drug Discov Today 23:1274–1284CrossRefPubMed
34.
go back to reference Soltani N, Shaynafar A, Djozan D, Jouyban A (2013) Solubility of three basic drugs in propylene glycol + water mixtures in the presence of β-cyclodextrin. J Drug Deliv Sci Technol 23:187–190CrossRef Soltani N, Shaynafar A, Djozan D, Jouyban A (2013) Solubility of three basic drugs in propylene glycol + water mixtures in the presence of β-cyclodextrin. J Drug Deliv Sci Technol 23:187–190CrossRef
35.
go back to reference Ramasahayam B, Eedara BB, Kandadi P, Jukanti R, Bandari S (2015) Development of isradipine loaded self-nano emulsifying powders for improved oral delivery: in vitro and in vivo evaluation. Drug Dev Ind Pharm 41:753–763CrossRefPubMed Ramasahayam B, Eedara BB, Kandadi P, Jukanti R, Bandari S (2015) Development of isradipine loaded self-nano emulsifying powders for improved oral delivery: in vitro and in vivo evaluation. Drug Dev Ind Pharm 41:753–763CrossRefPubMed
36.
37.
go back to reference Shazly GA, Ibrahim MA, Badran MM, Zoheir KA (2012) Utilizing Pluronic F-127 and G elucire 50/13 solid dispersions for enhanced skin delivery of flufenamic acid. Drug Dev Res 73:299–307CrossRef Shazly GA, Ibrahim MA, Badran MM, Zoheir KA (2012) Utilizing Pluronic F-127 and G elucire 50/13 solid dispersions for enhanced skin delivery of flufenamic acid. Drug Dev Res 73:299–307CrossRef
38.
go back to reference Teotia A, Ikram S, Gupta B (2012) Structural characterization of chitosan and oxidized carboxymethyl cellulose based freeze-dried films. Polym Bull 69:175–188CrossRef Teotia A, Ikram S, Gupta B (2012) Structural characterization of chitosan and oxidized carboxymethyl cellulose based freeze-dried films. Polym Bull 69:175–188CrossRef
39.
go back to reference Sahiner M, Alpaslan D, Bitlisli BO (2014) Collagen-based hydrogel films as drug-delivery devices with antimicrobial properties. Polym Bull 71:3017–3033CrossRef Sahiner M, Alpaslan D, Bitlisli BO (2014) Collagen-based hydrogel films as drug-delivery devices with antimicrobial properties. Polym Bull 71:3017–3033CrossRef
40.
go back to reference Maslakci NN, Ulusoy S, Uygun E, Cevikbas H, Oksuz L, Can HK, Oksuz AU (2017) Ibuprofen and acetylsalicylic acid loaded electrospun PVP-dextran nanofiber mats for biomedical applications. Polym Bull 74:3283–3299CrossRef Maslakci NN, Ulusoy S, Uygun E, Cevikbas H, Oksuz L, Can HK, Oksuz AU (2017) Ibuprofen and acetylsalicylic acid loaded electrospun PVP-dextran nanofiber mats for biomedical applications. Polym Bull 74:3283–3299CrossRef
Metadata
Title
Design, characterization and evaluation of oral fast dissolving polymeric films of isradipine inclusion complex
Authors
Sayed H. Auda
Abdullah H. Al-Omrani
Fars K. Alanazi
Mohamed M. Badran
Faiyaz Shakeel
Publication date
30-08-2018
Publisher
Springer Berlin Heidelberg
Published in
Polymer Bulletin / Issue 5/2019
Print ISSN: 0170-0839
Electronic ISSN: 1436-2449
DOI
https://doi.org/10.1007/s00289-018-2503-y

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