Design, characterization and evaluation of oral fast dissolving polymeric films of isradipine inclusion complex
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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.
KeywordsIsradipine Hydroxypropyl-β-cyclodextrin Inclusion complex Oral fast dissolving films Polymers
The authors are thankful to the Deanship of Scientific Research and Research Center, College of Pharmacy, King Saud University.
Compliance with ethical standards
Conflict of interest
The authors report no conflicts of interest associated with this work.
- 2.Gavaskar B, Kumar SV, Sharan G, Rao YM (2010) Overview of fast dissolving films. Int J Pharm Pharm Sci 2:29–33Google Scholar
- 4.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 28:464–468Google Scholar
- 9.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 13:325–331CrossRefGoogle Scholar
- 12.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 153:361–370CrossRefGoogle Scholar
- 15.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 21:1324–1332CrossRefGoogle Scholar
- 18.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 5:222–247Google Scholar
- 19.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 5:114–122Google Scholar
- 21.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 20:162–166Google Scholar
- 22.Barbic U, Verdenik I, Marolt M, Hren NI (2016) Three-dimensional ultrasound evaluation of tongue volume. Zdrav Vestn 85:228–236Google Scholar
- 23.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 4:408–417Google Scholar
- 24.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:E520949Google Scholar
- 25.Upreti K, Kumar L, Anand SP, Chawla V (2014) Formulation and evaluation of mouth dissolving films of paracetamol. Int J Pharm Pharm Sci 6:200–202Google Scholar