DEVELOPMENT AND CHARACTERIZATION OF SILDENAFIL CITRATE ORAL THIN FILMS
Abstract
The current work aimed to develop sildenafil citrate (SC) oral thin films. SC oral thin films (OTF) were prepared by solvent casting method. The ingredients include hydroxypropyl methylcellulose (HPMC), E4 (as film former), glycerol (as lubricating agent), polyethylene glycol 600 (as plasticizer), rose oil (as flavoring agent), and de-ionized water (as solvent). The SC-OTFs were successfully prepared by the solvent casting method. The drug excipient compatibility studies showed the absence of drug excipient interactions in fourier transform infrared spectroscopy (FTIR) spectra. All the prepared formulations (F1 to F6) were evaluated for several physicochemical parameters like morphology (i.e., size, shape, color), thickness, uniformity (i.e., content and weight), surface pH measurement, in vitro disintegration time, in vivo studies (i.e., taste), tensile strength, folding endurance and in vitro drug release and all were found within pharmacopoeial limits. In vitro, drug release studies (F1 to F6) in simulated salivary fluid (6.8 pH phosphate buffer) showed that 98 ± 1.26% drug was released from F4 in 60 sec. The OTF is a promising formulation for SC that results in high solubility, rapid onset of action, and enhanced systemic bioavailability (BA).
Keywords:
Sildenafil citrate, oral thin films, solvent casting, dyspepsia, tensile strength, folding enduranceDOI
https://doi.org/10.25004/IJPSDR.2021.130205References
DiMasi JA , Grabowsk i HG, Hansen RW. Innovat ion in t he pharmaceutical industry: new estimates of R and D costs. J Health Economics, 2016; 47:20-33.
Borges AF, Silva C, Coelho JF, Simões S. Oral films: current status and future perspectives: I-galenical development and quality attributes. J Control Release, 2015; 206:1-9.
Bhattarai M, Gupta AK. Fast dissolving oral films: a novel trend to oral drug delivery system. Sunsari Technical College J, 2015; 2:58-68.
Barnhart SD, Full AP, Moritz CM, inventors; Adhesives Research Inc, assignee. Rapidly disintegrating films for delivery of pharmaceutical or cosmetic agents. United States patent US 9,937,123. 2018.
Bala R, Pawar P, Khanna S, Arora S. Orally dissolving strips: A new approach to oral drug delivery system.Int. J Pharm Invest, 2013; 3:67.
Arya A, Chandra A, Sharma V, Pathak K. Fast dissolving oral films: an innovative drug delivery system and dosage form. Int J ChemTech Res, 2010; 2:576-583.
Ghosh T, Ghosh A, Prasad D. A rev iew on new generation orodispersible tablets and its future prospective. Int J Pharm Pharm Sci, 2011; 3:1-7.
Sharma D. Fast Disintegrating Tablets: A review on an emerging trend in novel oral drug delivery technology and new market opportunities. J Drug Delivery Ther, 2012; 2:74-86.
Sudhakar Y, Kuotsu K, Bandyopadhyay AK. Buccal bio-adhesive drug delivery—a promising option for orally less efficient drugs. J Control Release, 2006; 114:15-40.
Madhav NS, Shakya AK, Shakya P, Singh K. Oro-transmucosal drug delivery systems: a review. J Control Release, 2009; 140:2-11.
Batchelor HK, Fotaki N, Klein S. Paediatric oral bio-pharmaceutics: key considerations and current challenges. Adv Drug Delivery Rev, 2014; 73:102-126.
Kathpalia H, Gupte A. An introduction to fast dissolving oral thin film drug delivery systems: a review. Curr Drug Deliv, 2013; 10:667-684.
Geetha A, Rajendra Kumar J, Pavani U, Kalyani CH, Design and in vivo characterization of amlodipine besylate orodispersible tablets. J Global Trends Pharm Sci, 2017; 8:4325- 4336.
Karki S, Kim H, Na SJ, Shin D, Jo K, Lee J. Thin films as an emerging platform for drug delivery. Asian J Pharm Sci, 2016; 11:559-574.
Trofimiuk M, Wasilewska K, Winnicka K. How to modify drug release in paediatric dosage forms? Novel technologies and modern approaches with regard to children’s population. Int J Mol Sci, 2019; 20:3200.
Hof fmann EM, Breitenbach A , Breit k reut z J. Advances in orodispersible films for drug delivery. Expert Opin Drug Deliv, 2011; 8:299-316.
Nagaraju T, Gowthami R, Rajashekar M, Sandeep S, Mallesham M, Sathish D, Shravan Kumar Y. Comprehensive review on oral disintegrating films. Curr Drug Deliv, 2013; 10:96-108.
Dixit RP, Puthli SP. Oral strip technology: overview and future potential. J Control Release, 2009; 139:94-107.
Han X, Zhang S, Chai Z, Dong Y, He W, Yin L, Yang L, Qin C. In vitro and in vivo evaluation of the taste-masking efficiency of Amberlite IRP88 as drug carries in chewable tablets. J Drug Deliv Sci Technol, 2019; 49:547-555.
Carson CC. Sildenafil: a 4-year update in the treatment of 20 million erectile dysfunction patients. Curr Urol Reports, 2003; 4:488- 496.
Lue TF. Erectile dysfunction. New England journal of medicine. 2000; 342:1802-1813.
Hatzimouratidis K, Hatzichristou DG. A comparative review of the options for treatment of erectile dysfunction. Drugs, 2005; 65:1621-1650.
Porst H, Burnett A, Brock G, Ghanem H, Giuliano F, Glina S, Hellstrom W, Martin-Morales A, Salonia A, Sharlip I. SOP conservative (medical and mechanical) treatment of erectile dysfunction. The J Sex Med, 2013; 10:130-171.
Hatzimouratidis K, Hatzichristou DG. Looking to the future for erectile dysfunction therapies. Drugs, 2008; 68:231-250.
Aversa A, Bruzziches R, Pili M, Spera G. Phosphodiesterase 5 inhibitors in the treatment of erectile dysfunction. Curr Pharm Des, 2006; 12:3467-3484.
Kamenov ZA. Comparison of the first intake of vardenafil and tadalafil in patients with diabetic neuropathy and diabetic erectile dysfunction. The J Sex Med, 2011; 8:851-864.
Ghasemian E, Vatanara A, Najafabadi AR, Rouini MR, Gilani K, Darabi M. Preparation, characterization and optimization of sildenafil citrate loaded PLGA nanoparticles by statistical factorial design. DARU J Pharm Sci, 2013; 21:1-10.
Hosny KM, El-Say KM, Ahmed OA. Optimized sildenafil citrate fast orodissolvable film: a promising formula for overcoming the barriers hindering erectile dysfunction treatment. Drug delivery, 2016; 23:355-361.
Patel H, Panchal M, Shah S, Vadalia KR. Formulation and evaluation of transdermal gel of sildenafil citrate. Int J Pharm Res Allied Sci, 2012; 1:103-118.
Elshafeey AH, Bendas ER, Mohamed OH. Intranasal microemulsion of sildenafil citrate: in vitro evaluation and in vivo pharmacokinetic study in rabbits. AAPS Pharm Sci Tech, 2009; 10:361-367.
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