DESIGN AND EVALUATION OF BOSENTAN CONTROLLED-RELEASE MICROCAPSULES
DOI:
https://doi.org/10.22159/ijap.2022v14i2.43730Keywords:
Bosentan, MicrocapsulesAbstract
Objective: The objective of the present work is to formulate and evaluate Bosentan controlled-release microcapsules using gum karaya and polyethylene oxide as polymers, sodium alginate and calcium chloride as encapsulating material and cross-linking agent and croscarmellose sodium as superdisintegrant.
Methods: Bosentan microcapsules were prepared by the ionic gelation method. The prepared microcapsules were characterized by flow properties such as angle of repose, compressibility index, particle size and encapsulation efficiency and drug release profiles.
Results: The prepared microcapsules were evaluated for angle of repose, compressibility index, % drug content, encapsulation efficiency and particle size. All the flow properties were within the specified IP limits. The drug content of microcapsules prepared by ionic gelation method by varying the polymeric concentration was found in the range of 121.62±0.41 to 124.99±0.51 mg. The encapsulation efficiency of Bosentan controlled-release microcapsules was found to be in the range of 59 % to 67%. Among all the formulations prepared, formulation B14 containing equal proportions (25 mg) of gum karaya and polyethylene oxide showed about 95% of drug release over a period of 12 h and were found to be suitable for extending drug release up to 16 h.
Conclusion: Bosentan controlled-release microcapsules were prepared by ionic gelation method, which is a novel formulation that is helpful in the treatment of pulmonary artery hypertension (PAH).
Downloads
References
Nath B, Nath LK, Mazumdar B, Sharma N, Sarkar M. Design and development of metformin HCl floating microcapsules using two polymers of different permeability characteristics. Int J Pharm Sci Nanotech. 2009;2(3):627-37. doi: 10.37285/ ijpsn.2009.2.3.6.
Khamanga SM, Parfitt NN, Nyamuzhiwa T, Haidula H, Walker RB. The evaluation of eudragit microcapsules manufactured by solvent evaporation using USP apparatus 1. Diss Technol. 2009;16(2):15-22. doi: 10.14227/DT160109P15.
Belgamwar VS, Kawtikwar PS, Phutane GP, Belgamwar AV. Design and evaluation of microcapsules containing ciprofloxacin hydrochloride for sustained release. Indian Drugs. 2008;45(1):553-7.
Shabaraya AR, Narayanacharyulu R. Design and evaluation of chitosan microspheres of metoprolol tartrate for sustained release. Indian J Pharm Sci. 2003;65(3):250-3.
Wieland Berghausen S, Schote U, Frey M, Schmidt F. Comparison of microencapsulation techniques for the water-soluble drugs nitenpyram and clomipramine HCl. J Control Release. 2002;85(1-3):35-43. doi: 10.1016/s0168-3659(02)00269-9, PMID 12480309.
Yamada T, Onishi H, Machida Y. Sustained release ketoprofen microparticles with ethyl cellulose and carboxymethyl ethyl cellulose. J Control Release. 2001;75(3):271-82. doi: 10.1016/s0168-3659(01)00399-6, PMID 11489315.
Bolourtchian N, Karimi K, Aboofazeli R. Preparation and characterization of ibuprofen microspheres. J Microencapsul. 2005;22(5):529-38. doi: 10.1080/02652040500161941, PMID 16361196.
Haznedar S, Dortunç B. Preparation and in vitro evaluation of eudragit microspheres containing acetazolamide. Int J Pharm. 2004;269(1):131-40. doi: 10.1016/j.ijpharm.2003.09.015. PMID 14698584.
Horoz BB, Kiliçarslan M, Yuksel N, Baykara T. Effect of different dispersing agents on the characteristics of eudragit microspheres prepared by a solvent evaporation method. J Microencapsul. 2004;21(2):191-202. doi: 10.1080/02652040310001637893, PMID 15198430.
Dong W, Bodmeier R. Encapsulation of lipophilic drugs within enteric microparticles by a novel coacervation method. Int J Pharm. 2006;326(1-2):128-38. doi: 10.1016/j.ijpharm.2006.07.013. PMID 16942845.
Hemalatha K, Lathaeswari R, Patil JS, Kamalapur MV, Marapur SC, Kadam DV. Ionotropic gelation and polyelectrolyte complexation: the novel techniques to design hydrogel particulate sustained, modulated drug delivery system. Dig J Nanometer Bios. 2010;5(1):241-8.
Suganeswari M, Senthil Kumar V, Anto SM. Formulation and evaluation of metoclopramide hydrochloride microbeads by ionotropic gelation method. Int J Pharm Biol Arch. 2011;2(3);162:921-8. DOI. doi: 10.37022/wjcmpr. vi.
Bonello B, Renard S, Mancini J, Hubert S, Habib G, Fraisse A. Life span of patients with Eisenmenger syndrome is not superior to that of patients with other causes of pulmonary hypertension. Cardiovasc Diagn Ther. 2014;4(5):341-9. doi: 10.3978/j.issn.2223-3652.2014.10.03. PMID 25414820.
Kuang HY, Wu YH, Yi QJ, Tian J, Wu C, Shou WN, Lu TW. The efficiency of endothelin receptor antagonist bosentan for pulmonary arterial hypertension associated with congenital heart disease: a systematic review and meta-analysis. Medicine. 2018;97(10):e0075. doi: 10.1097/MD.0000000000010075, PMID 29517668.
Iswandana R, Putri KSS, Dwiputra R, Yanuari T, Sari SP, Djajadisastra J. Raditya iswandana, kurnia sari setio putri, randika dwiputra, tryas yanuari, santi purna sari, joshita djajadisastra. Int J Appl Pharm. 2017;9(5):109-15. doi: 10.22159/ijap.2017v9i5.20842.
Rao KV, Venkatchalam VV. Sustained-release mucoadhesive microcapsules of ramipril by ionic gelation technique: formulation design, optimization and characterization. Int J Pharm Pharm Sci. 2017;9(2):128-41. doi: 10.22159/ijpps.2017v9i2.12660.
Samran S, Dalimunthe D, Dalimunthe D, Dalimunthe D. The formulation of dry curcuma (Curcuma Xanthorrhiza Roxb.) extract microcapsules by spray wet microencapsulation techniques. Asian J Pharm Clin Res 2018;11(3). doi: 10.22159/ajpcr.2018.v11i3.22608.
Mosab A. Approaches to achieve an oral controlled release drug delivery system using polymers: a recent review. Int J Pharm Pharm Sci. 2015;7(7):16-21.
priya SN, N-aga Jyothi A, Poojitha J, Santhosh A, Rama Rao N. A comprehensive review on hydrogels. Int J Curr Pharm Res. 2016;8(1):19-23.
Vidyadhara S, Babu JR, Balakrishna T, Trilochani P, Kumar MP. Design and evaluation of controlled release losartan potassium microcapsules. J Pharm Res. 2013;6(4):470-5. doi: 10.1016/j.jopr.2013.04.015.
Sadhana S, Ashok S, Suhas V, Nityanand Z. Formulation and in vitro characterization of acyclovir floating matrix tablets: a factorial design study. J Appl Pharm Sci. 2013;3(5):65-74. doi: 10.7324/JAPS.2013.3513.
Sree PA, Pradeep RT, Praveen KM, Shrutika C. Formulation of regioselective floating matrix tablets of dextromethorphan using gas-forming technique and evaluation. Int J Pharm Sci Res. 2013;4(10):3976-91. doi: 10.13040/IJPSR.0975-8232.4(10).3976-91.
Sirisha VNL, Eswariah MC, Rao AS. Formulation and evaluation of karaya gum microspheres of cromolyn sodium: treatment of ulcerative colitis. Int Res J Pharm. 2017;8(10):182-8. doi: 10.7897/2230-8407.0810205.
Maliha K, Shahid MD. Formulation and in vitro evaluations of floating microspheres of bosentan. Int J Res Pharm Nano Sci. 2017;6(3):134-46.
Ashok KA, Balakrishna T, Rajiv J, Murthy TEGK, Anil KA, Sudheer B. Formulation and evaluation of mucoadhesive microcapsules of metformin HCl with Gum karaya. Int J Pharm Pharm Sci. 2011;3(3):150-5.
Published
How to Cite
Issue
Section
Copyright (c) 2022 HARSHA KOREDDI, VIDYADHARA SURYADEVARA, BALAKRISHNA TALAMANCHI, RAMU ANNE
This work is licensed under a Creative Commons Attribution 4.0 International License.
