FORMULATION DEVELOPMENT AND EVALUATION OF CHRONOMODULATED DRUG DELIVERY SYSTEM BY ZAFIRLUKAST
Keywords:Pulsatile formulation, Zafirlukast, Chronomodulated drug delivery system, Compression coated tablets
Objective: The main objective of the present study was to formulate and evaluate a time-controlled single-unit oral pulsatile drug delivery system containing Zafirlukast for the prevention of nocturnal asthma attacks. To provide time-scheduled drug release for Asthma disease. It is used for preventing asthmatic attacks at early morning. Pulsatile release dosage form is increasing patient compliance by reducing the dosing frequency, especially in the early morning.
Methods: Core tablets were prepared by incorporating different concentrations of natural and synthetic super disintegrants. Drug-containing core tablets (ZC1-ZC15) with different compositions of natural super disintegrants (Plantago ovata seed powder, Locust bean gum) synthetic super disintegrants (Sodium starch glycolate (SSG), Cross carmellose sodium (CCS), Crospovidone (CP)) were prepared by direct compression technique. The core tablets were subjected to pre-formulation, physicochemical and In vitro drug release studies. The fast disintegrating core tablet formulation was selected and press-coated tablets (P1-P11) were prepared with different compositions of hydrophobic polymers Eudragit RS100, Eudragit RL 100, Ethylcellulose and hydrophilic polymers Hydroxypropyl methylcellulose K4M, K100M. The optimized formulation was selected and quantified based on in vitro drug release profile in simulated gastric and intestinal fluids.
Results: The pre and post-compression parameters of tablets were also found to be within limits. Formulation ZC5 with 16 mg of Locust bean gum showed the least disintegrating time, i.e., 22.13 sec, and was selected as the best immediate release core tablet. The press-coated tablet formulation P8 having 62.5 mg Eudragit RS100 and 62.5 mg of HPMC K4M in ratio 1:1 over the core tablet ZC5 showed rapid and drug release nearly after 4 h lag time and 98.86 % up to 12 h. Accelerated stability studies of the optimized formulation P8 indicated no significant difference in release profile after 3 mo.
Conclusion: The in vitro dissolution study showed that lag time before drug release was highly affected by the coating amount level and nature of coating polymer used. Time-controlled pulsatile release tablets can be prepared using press-coating techniques.
Bussermar T, Otto L, Bodmier R. Pulsatile drug delivery system. Crit Rev Ther Drug Carrier Syst 2001;18:433–58.
Youan BC. Chronopharmaceutics: gimmick or clinically relevant approach to drug delivery. J Controlled Release 2004;98:337–53.
Chaudhari SP, Chauradhi PD, Mistry CJ, Patil MJ. The effect of core and coating composition on drug release from directly compressed time controlled-release tablets. Pharm Tech 2007;31:132–44.
MS Sokar, AS Hanafy, AH El-Kamel, SS El-Gamal. Pulsatile core-in-cup valsartan tablet formulations: in vitro evaluation. Asian J Pharm Sci 2013;8:234-43.
Shidhaye S, Dhone A, Budhkar T. Technologies in pulsatile drug delivery system. Int J Adv Pharm Biol Sci 2012;1:438-45.
Dalvadia H, Patelb J. Chronpharmaceutics, pulsatile drug delivery system as the current trend. Asian J Pharm Sci 2010;5:204-30.
Efentakis M, Koligliati S, Vlachou M. Design and evaluation of a dry coated drug delivery system with an impermeable cup, swellable top layer, and pulsatile release. Int J Pharm 2006;311:147-56.
Shweta Arora, J Ali, Alka Ahuja, Sanjula Baboota, J Qureshi. Pulsatile drug delivery systems: an approach for controlled drug delivery. Indian J Pharm Sci 2006;68:295-300.
Gaurav Thakur, Shahid Ud Din Wani, Surya Prakash Gautam. A review on recent advancement in pulsatile drug delivery systems. Int J Curr Pharm Res 2021;13:6-10.
Pasham Sowmya, Venkatesh DP, Sujit Nayek. Pulsatile drug delivery system: a formulation approach for treatment of diseases. Int J Curr Pharm Res 2020;12:16-21.
Martin RJ, Schlegel SB. Chrono biology of Asthma. Am J Respir Crit Care Med 1998;158:1002–7.
Kulkarni PA, Jaiswal M, Jawale SB, Shirolkar SV, Kasture PV. Development and evaluation of press-coated tablets for chronopharmaceutical drug delivery using gellable and permeable polymers. Der Pharm Lett 2010;2:482-97.
Seshasayan A, Sreenivasa RB, Prasanna R, Ramana Murthy KV. Studies on the release of rifampicin from modified pulsincap technique. Indian J Pharma Sci 2001;1:337-9.
Swati C Jagdale, Vishnu M Suryawanshi, Sudhir V Pandya, Bhanudas S Kuchekar, Aniruddha R Chabukswar. Development of press-coated, floating-pulsatile drug delivery of lisinopril. Sci Pharm 2014;82:423–40.
Himabindu Peddapalli, Vasudha Bakshi, Narender Boggula. Formulation, in vitro and ex vivo characterization of mucoadhesive buccal tablets for an antihypertensive drug. Asian J Pharm Clin Res 2018;11:402-11.
Sreekanth K, Naresh G, Md Imran, Nagesh K, Hindustan Abdul Ahad. Design, development, and optimization of zafirlukast press coat tablets for pulsatile drug delivery. Int J Med Pharm Res 2014;2:834-41.
Soad A Yehia, Ahmed H Elshafeey, Aliaa ElMeshad, Hamoud A, Al-Bialey. A pharmaceutical study on different approaches for itopride hydrochloride sustainment: in vitro and in vivo evaluation. J Chem Pharm 2012;4:1398-412.
Sarada Anepu, Lohithasu Duppala, Soma Sundari M. Formulation development, characterization, and in vitro evaluation of floating matrix dosage form of Tramadol hydrochloride using various polymers. Asian J Pharm Clin Res 2017;10:281-90.
Hrishav Das Purkayastha, Bipul Nath. Formulation and evaluation of oral fast disintegrating tablet of Ibuprofen using two super disintegrants. Int J Curr Pharm Res 2017;9:92-5.
Ahmed E Aboutaleb, Sayed I Abdel-Rahman, Mahrous O Ahmed, Mahmoud A Younis. Design and evaluation of domperidone sublingual tablets. Int J Pharm Pharm Sci 2016;8:195-201.
Negar Bashardoust Josephine Leno Jenita, Parvin Zakeri Milani. Preparation, and in vitro investigation of chitosan compressed tablets for colon targeting. Adv Pharm Bull 2011;1:87–92.
Inder Kumar, Vinay Pandit. Cefpodoxime proxetil fast dissolving tablets: a comparative study. Int J Pharm Pharm Sci 2020;12:35-41.
Vishal Yadav, Prakash Jadhav, Pranali Salunkhe, Priti Nikam, Shital Matkar. Formulation and evaluation of gastroretentive tablets of antiulcer drug. Asian J Pharm Clin Res 2016;9:48-52.
Ayesha Salma Habeeb, Shahidulla SM. Formulation and in vitro evaluation of captopril floating tablets by using natural polymers. Pharm Innov 2018;7:82-9.
Poojari Anusha, Singaram Mounika, Adukondalu Devandla. Preparation and evaluation of gastroretentive floating tablets of enalapril maleate. Int J Pharm Biol Sci 2017;7:136-42.
Amrita Chakravorty, Mainak Chakraborty, Biswanath SA. Factors influencing delayed-release followed by rapid pulse release of drugs from compression coated tablets for colon targeting. Int J Pharm Pharm Sci 2016;8:330-6.
Prasanth VV, Mitesh P Modi, Sam T Mathew, Abin Abraham. Formulation, and evaluation of enteric coated time-release press coated tablets of theophylline for chronopharmacotherapy. Der Pharm Lett 2012;4:599-606.
G Ravi, P Subhash Chandra Bose, Valluru Ravi, Damineni Sarita, P Srikanth Reddy, Sandeep Kanna. Development and evaluation of oral controlled release tablets of oxybutynin using various polymers. Res J Pharm Tech 2020;13:3854-60.
SB Thirumalesh Naik, Kambham Venkateswarlu, KB Chandrasekhar. Formulation and in vitro evaluation of orodispersible tablets of olanzapine for the improvement of dissolution rate. J Chem Pharm 2016;8:177-81.
Ghosh T, Karki VS, Ghosh A, Kumar A, Hullatti. A novel core-coat chronotherapeutic technique for effective delivery of antihypertensive drug. Int J Appl Pharm 2018;10:92-9.
K Kavitha, RAM Jainaf Nachiya. Formulation and evaluation of furosemide tablets as gastro retentive dosage forms using various polymers. Int J Sci Res 2019;8:11-6.
Upendra Kulkarni, NG Raghavendra Rao, Basawaraj S Patil. Fabrication and evaluation of fast dissolving tablets of tizanidine hydrochloride by solid dispersion technique. Int J Pharm Sci Rev Res 2011;6:88-93.
Garima Joshi, Abhinesh Kumar, Krutika Sawant. Enhanced bioavailability and intestinal uptake of Gemcitabine HCl-loaded PLGA nanoparticles after oral delivery. Eur J Pharm Sci 2014;60:80-9.
Montella S, Maglione M, De Stefano S. Update on leukotriene receptor antagonists in preschool children wheezing disorders. Ital J Pediatr 2012;38:2-9.
Esmat Zien El-Deen, Mamdouh Ghorab, Shadeed Gadand Heba Yassin. Effect of different polymers on the release of diclofenac sodium controlled release drug delivery system. Res Rev J Pharm Pharm Sci 2015;4:11-21.
Poreddy Srikanth Reddy, V Alagarsamy, P Subhah Chandra Bose, Damineni Sarita, V Sruthi. Development and evaluation of indapamide effervescent floating tablets using different HPMC grade polymers. Int J Pharm Sci Rev Res 2019;57:122-9.
P Gopalakrishna, B Ramarao, G Chiranjeevi, Ramya Sri S. In vitro evaluation of gastro retentive floating drug delivery system for nitrendipine bilayer tablets. Int J Pharm Chem Res 2016;2:63-72.
Karan Malik, Gurpreet Arora, Inderbir Singh. Locust bean gum as super disintegrant–formulation and evaluation of nimesulide orodispersible tablets. Polimeryw Med 2011;41:17-28.
R Krishna Kumari, P Bharathi, CH Saritha Reddy. Formulation, in vitro drug release, and stability studies of clopidogrel rapidly disintegrating tablets.
Asian J Res Pharm Sci Biotechnol 2013;1:40-54.
Anupam K Sachan, Ankita Gupta, Lovi Nigam, Ranjana Sharma, Sudhir S Gangwar. Design and characterization of solid dispersion-based fast dissolving tablet of cetirizine hydrochloride. MIT Int J Pharm Sci 2015;1:37–44.
N Kanaka Durga Devi, B Sai Mrudula, A Prameela Rani. Chronomodulated drug delivery system of montelukast sodium. Der Pharm Lett 2010;2:316-29.
Sapna N Makhija, Pradeep R Vavia. Once-daily sustained-release tablets of venlafaxine, a novel antidepressant. Eur J Pharm Biopharm 2002;54:9-15.
Katayoun Derakhshandeh, Marzieh Soleymani. Formulation and in vitro evaluation of nifedipine controlled release tablet: influence of a combination of hydrophilic and hydrophobic matrix forms. Asian J Pharm 2010;4:185-93.
Anisa Amalia, Yudi Srifiana, Amalia Anwar. Physical properties and rate of diffusion transethosome curcumin using a combination of tween 60 and span 60 as surfactant. Int J Appl Pharm 2021;13:66-70.
Sandhya Rajendra Shenoy, Pritam Jain, Madhur Kulkarni. Development and evaluation of chronomodulated delivery system of metoclopramide hydrochloride. Int J Appl Pharm 2016;8:38-42.
Srividya Ramreddy, Prabhakar Kandadi, Kishan Veerabrahma. Formulation and pharmacokinetics of diclofenac lipid nanoemulsions for parenteral application. PDA J Pharm Sci Technol 2012;66:28-37.