FAST DISSOLVING SUBLINGUAL PATCH OF PHENOBARBITAL SODIUM: FORMULATION AND IN VITRO EVALUATION

SUJAID THAYYILAKANDY; GAYATHRI P. S.; ARJUN K. K.; GAYATHRI KRISHNAKUMAR; SREEJA C. NAIR

doi:10.22159/ijap.2020v12i5.38872

Authors

SUJAID THAYYILAKANDY Department of Pharmaceutics, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham, AIMS Health Sciences Campus, Kochi, India
GAYATHRI P. S. Department of Pharmaceutics, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham, AIMS Health Sciences Campus, Kochi, India
ARJUN K. K. Department of Pharmaceutics, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham, AIMS Health Sciences Campus, Kochi, India
GAYATHRI KRISHNAKUMAR Department of Pharmaceutics, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham, AIMS Health Sciences Campus, Kochi, India
SREEJA C. NAIR Department of Pharmaceutics, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham, AIMS Health Sciences Campus, Kochi, India

DOI:

https://doi.org/10.22159/ijap.2020v12i5.38872

Keywords:

Epilepsy, Phenobarbital sodium, Pullulan, Fast dissolving, Sublingual patch

Abstract

Objective: To formulate and characterize. Phenobarbital sodium loaded sublingual patch using biodegradable, mucoadhesive, fast-dissolving natural polymer pullulan for immediate management of epileptic seizures.

Methods: Phenobarbital sodium loaded sublingual patches were prepared by the solvent casting method and were subjected to various physicochemical evaluation parameters to find the optimized sublingual patch. The in vitro drug release study and kinetic model of the optimized formulation was also carried out. The stability study of the optimized Phenobarbital sodium loaded sublingual patch was also done.

Results: From in vitro drug release study, it was found that Phenobarbital sodium loaded sublingual patch (S4) exhibited a maximum drug release of 96.24±1.27% at the end of 60 min compared to other formulations indicating a faster drug release from the formulation with release kinetics as Higuchi diffusion model. In fact, a notable release data was obtained between 0.5 to 8 min by all formulations, specifically S4 formulation (20.84±1.97% and 77.22±2.41% drug release at the end of 0.5 min and 8 min respectively) showed a better percentage release profile in comparison with other formulations. Such a trend is vital to deliver the drug at a faster rate to promote immediate effect for managing the fatal and complicated seizure. Considering the physicochemical property and in vitro drug release data, S4 formulation was regarded as an optimized one. The stability study also confirmed that S4 formulation is stable at refrigeration conditions.

Conclusion: The formulated Phenobarbital sodium loaded sublingual patch is an effective drug delivery carrier which enables faster drug release to manage epileptic seizure.

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References

Ryosuke H, Kazunori A. The new antiepileptic drugs: their neuropharmacology and clinical indications. Neurol Med Chir 2016;56:205–20.

Jeremy AB, Kees VM. Understanding the oral mucosal absorption and resulting clinical pharmacokinetics of asenapine. AAPS PharmSciTech 2012;13:1110–5.

Desai C. Meyler’s side effects of drugs: the international encyclopedia of adverse drug reactions and interactions. Indian J Pharmacol 2016;48:224-5.

Mark M. Recent advances in epilepsy. J Neurol 2017;264:1811-24.

Suruchi S, Vaishali D. Epilepsy-a comprehensive review. Int J Pharm Res Rev 2013;2:61-80.

Khanna R, Agarwal SP, Ahuja A. Mucoadhesive buccal delivery: a potential alternative to conventional therapy. Ind J Pharm Sci 1998;60:1-11.

John AD. Mechanisms of action of antiepileptic drugs. Seizure 1995;4:267-71.

Madhavi BR, Murthy VSN, Rani AP, Kumar GD. Buccal film drug delivery system: an innovative and emerging technology. J Mol Pharm Org Process Res 2013;1:107-9.

Sah S, Badola A, Kothiyal P. Sublingual tablets: an overview. Indian J Pharm Biol Res 2016;4:20-6.

Michael R, Joseph E, Guido Barbagli, Frank A. Oral mucosa harvest: an overview of anatomic and biologic considerations. Eau-Ebu Update Series 2007;5:179-87.

Jacob NJ, Hesse GW, Shashoua VE. Synthesis, brain uptake, and pharmacological properties of a glyceryl lipid-containing gaba and the gaba-t inhibitor 7-vinyl-gaba. J Med Chem 1990;33:733-6.

Verma P, Thakur S, Deshmukh K, Verma S. Routes of drug administration. Int J Pharm Sci Res 2010;1:54-9.

Sellappan V, Sumanjali D. Buccal penetration enhancers-an overview. Asian J Pharm Clin Res 2013;6:39-47.

Susan H. Advances in nanoparticulate drug delivery approaches for sublingual and buccal administration. Fornt Pharmacol 2019;10:1328-34.

Arshad BK, Tarun K, Preeta C. Sublingual tablets and the benefits of the sublingual route of administration. J Pharm Res 2017;16:257-62.

Kalliopi D. Research and developments in buccal and sublingual drug delivery systems. Int Curr Pharm J 2012;288:446-51.

Shailesh TP, Parth BP, Chhagan NP. Formulation and evaluation of sublingual tablets containing sumatriptan succinate. Int J Pharm Investig 2012;2:162-8.

Shinkar DM, Dhake AS, Setty CM. Drug delivery from the oral cavity: a focus on mucoadhesive buccal drug delivery systems. J Pharm Sci Tech 2012;66:466-500.

Puja S, Sushma V, Pratik SD. Sublingual drug delivery: an indication of a potential alternative route. Int J Curr 2017;9:5-7.

Pankil GA, Patel MR, Patel NM. A review article on mucoadhesive buccal drug delivery system. Int J Pharm Res Dev 2011;3:159-73.

Patel KV, Patel KR, Patel MR, Patel Nm. A review article on mucoadhesive buccal drug delivery system: an overview. Int J Pharm Bio Arch 2011;2:600-9.

Pooja M, Aparna R, Kamal S, Kanchan M. Sublingual route: an approach to administered drugs in systemic circulation. Int J Pharma Res Health Sci 2019;7:2869-73.

Priya VB, Kanchan PU, Gouri D. Formulation and evaluation of fast dissolving oral melt-in-mouth of lorazepam for sublingual use. World J Pharm Pharm Sci 2016;5:763-75.

Ming TS, Chien MH, Ray NC, Po YC. Rapid-onset sildenafil sublingual drug delivery systems: in vitro evaluation and in vivo pharmacokinetic studies in rabbits. J Pharm Sci 2016;105:2774-81.

Prateek K, Uday B, Panchaxari MD. Development and characterization of fast dissolving sublingual films containing midazolam. World J Pharm Res 2014;2:123139.

Khanusiya AQ, Charyulu RN, Prabhu P, Batt S, Shastry CS. Formulation and evaluation of fast dissolving films of loratadine for sublingual use. Int Res J Pharm 2012;3:157-61.

Neha N, Jyothi S. Sublingual mucosa as a route for systemic drug delivery. Int J Pharm 2011;3:18-22.

Priyanka N, Iti C, Mohd Y. Insights into polymers: films formers in mouth dissolving films. Drug Invent 2011;3:280-9.

Bhyan B, Jangra S. Formulation and evaluation of fast dissolving sublingual films of rizatriptan benzoate. Int J Drug Dev Res 2012;4:133-43.

Mattson RH, Cramer JA, Collins JF. Comparison of carbamazepine, phenobarbital, phenytoin and primidone in partial and secondarily generalized tonic-clonic seizures. N Engl J Med 1985;313:145–51.

Abhilash M, Deepu T. Biopolymers for biocomposites and chemical sensor applications. Biopolymer composites in electronics. Amsterdam: Elsevier; 2017. p. 405-35.

Nithin GK, Mokal D, Patil K, Bhandurge P, Prashant D. A review on citric acid production and its applications. Int J Curr Adv Res 2017;6:5880-3.

Darwin LH, Paul FP, Don EF. Propylene glycol. Am J Health Syst Pharm 1950;7:8-17.

Qiao H, Meifang Z, Shuyong W. Progress on the antimicrobial activity research of clove oil and eugenol in the food antisepsis field. J Food Sci 2018;83:1476-83.

Rajni B, Pravin P, Sushil K, Sandeep A. Orally dissolving strips: a new approach to oral drug delivery system. Int J Pharm Investig 2013;3:67–76.

Prasanna PG, Kailas MK, Riyaz AO, Rohit RB, Bhargav RH, Birudev BK. Mouth dissolving films: innovative vehicle for oral drug delivery. Int J Pharm Sci Rev Res 2013;2:41-7.

De CV, Ajovalasit A, Sutera Fm, Murgia D, Sabatino MA, Dispenza C, et al. Development and characterization of an amorphous solid dispersion of furosemide in the form of a sublingual bioadhesive film to enhance bioavailability. Pharmaceutics 2017;9:22-7.

Eldridge JE, Burdick DC, Jones RH, Hossack KF. Comparison of nitroglycerin patches and nifedipine. J Cardiovasc Pharm T 1987;10:315-9.

Naresh K, Kishan P, Sriram P, Adukondalu D. Formulation and evaluation of sublingual strips of naratriptan. Indo Am J Pharm 2016;3:759-66.

Kalia V, Garg T, Rath G, Goyal AK. Development and evaluation of a sublingual film of the antiemetic granisetron hydrochloride. Artif Cells Nanomed Biotechnol 2014;44:842-6.

Tayel SA, Nabarawi MA, Amin MM, Abou Ghaly MH. Sumatriptan succinate sublingual fast dissolving thin films: formulation and in vitro/in vivo evaluation. Pharm Dev Technol 2015;21:328-37.

Arya A, Chandra A, Sharma V, Pathak K. Fast dissolving oral films: an innovative drug delivery system and dosage form. J Chem Tech Res 2010;2:576–83.

Hearnden V, Sankar V, Hull K. New developments and opportunities in oral mucosal drug delivery for local and systemic disease. Adv Drug Delivery Rev 2012;64:16–28.

Liew KB, Tan YT, Peh KK. Characterization of oral disintegrating film containing donepezil for Alzheimer's disease. AAPS PharmSciTech 2012;13:134–42.

Yeola GS, Darandale S, Khire A. Fabrication and statistical optimization of a polysaccharide-based sublingual film of buprenorphine hydrochloride for breakthrough pain management: in vitro and in vivo performance. Drug Delivery Transl Res 2014;4:116–25.

Marina K, Narayana CR, Vijayanarayana K, Prabhakara P. In vitro and in vivo evaluation of chitosan buccal films of ondansetron hydrochloride. Int J Pharm Investig 2011;1:164–71.

Fawzia H, Salah ES, Maha AA, Gihan F, Mohamed S. Mucoadhesive buccal patches of lornoxicam: ii–in vivo evaluation and clinical efficacy. Bull Pharm Sci 2011;34:21-30.

Siddiqui MN, Garg G, Sharma PK. A short review on “a novel approach in oral fast-dissolving drug delivery system and their patents”. Adv Biol Res 2011;5:291–303.

Sayed S, Ibrahim HK, Mohamed MI. Fast-dissolving sublingual films of terbutaline sulfate: formulation and in vitro/in vivo evaluation. Mol Pharm 2013;10:2942–7.

Tong Q, Xiao Q, Lim LT. Preparation and properties of pullulan–alginate–carboxymethylcellulose blend films. Food Res Int 2008;41:1007–14.

Murata Y, Isobe T, Kofuji K, Norihisa N, Ryosei K. Preparation of fast dissolving films for oral dosage from natural polysaccharides. Materials 2010;3:4291–9.

Sachin G, Sonali S, Omprakash GB, Sandeep S. Formulation and evaluation of oral fast dissolving sublingual film of Propranolol Hcl. Int J Pharm Res Health Sci 2018;6:2369-73.

Priya YS, Hastak VS, Bajaj AN. Polymers used for disintegrating oral film: a review. Int J Pharm Sci Rev Res 2013;21:169-78.

Rita NW, Farheen A, Pranita K. Formulation and evaluation of fast dissolving sublingual film of paroxetine hydrochloride for treatment of depression. Asian J Pharm Clin Res 2019;12:126-32.

Soha S, Howida KI, Magdy IM, Mohamed FM. Fast-dissolving sublingual films of terbutaline sulfate: formulation and in vitro/in vivo evaluation. Mol Pharm 2013;10:2942-7.

Chowdary YA, Soumya M, Madhubabu M, Aparna K, Himabindu P. A review of fast-dissolving drug delivery systems-a pioneering drug delivery technology. Bull Envpharmacol Life Sci 2012;1:8-20.

Mahajan A, Chhabra N, Agarwal G. Formulation and characterization of fast dissolving buccal film: a review. Pharm Sin 2011;3:152-65.

Honey G, Parshuram R, Vikas R, Ashok KT. Orally disintegration systems: innovations in formulation and technology. Recent Pat Drug Delivery Formul 2008;2:258-74.

Mashru R, Sutariya V, Sankalia M, Parikh P. Development and evaluation of fast-dissolving film of salbutamol sulphate. Drug Dev Ind Pharm 2005;31:25–34.

Yellanki SK, Jagtap S, Masareddy R. Dissofilm: a novel approach for delivery of phenobarbital; design and characterization. J Young Pharm 2011;3:181–8.