MICROENCAPSULATION BISOPROLOL FUMARATE WITH EUDRAGIT E PO BY SOLVENT EVAPORATION METHOD

AZHOMA GUMALA; FEBRIYENTI; FITHRIANI ARMIN; ZAHRAH YULINDRA

doi:10.22159/ijap.2024.v16s1.19

Authors

AZHOMA GUMALA Pharmaceutics Department, Faculty of Pharmacy, Universitas Andalas, Padang, Indonesia https://orcid.org/0000-0001-7168-6861
FEBRIYENTI Pharmaceutics Department, Faculty of Pharmacy, Universitas Andalas, Padang, Indonesia
FITHRIANI ARMIN Pharmaceutical Chemistry Department, Faculty of Pharmacy, Universitas Andalas, Padang, Indonesia
ZAHRAH YULINDRA Pharmaceutics Department, Faculty of Pharmacy, Universitas Andalas, Padang, Indonesia

DOI:

https://doi.org/10.22159/ijap.2024.v16s1.19

Keywords:

Bisoprolol fumarate, Eudragit E PO, Microencapsulation, Solvent evaporation

Abstract

Objective: This study aimed to develop and optimize the microcapsule formula of bisoprolol fumarate-Eudragit EPO by double-emulsion solvent evaporation.

Methods: The preparation of bisoprolol fumarate-Eudragit EPO microcapsule was done in three different ratios 1: 3 (F1), 1: 4 (F2), and 1: 5 (F3), followed by characterization of each of the microcapsule formula using Fourier transform infrared, scanning electron microscopy, particle size analyzer. Further analysis included investigation of the drug loading, entrapment efficiency, solubility in pH 6.8, and the difference among dissolution profiles of each microcapsule using one-way ANOVA.

Results: Infra-red spectrum showed no chemical interaction between bisoprolol fumarate and Eudragit E PO in microcapsules. The morphology and structure of F1 microcapsule was irregular spheres, while F2 and F3 were regular spheres. The average particle distribution of microcapsules was 24.765±0,236 μm (F1), 28.245±0,252 μm (F2), and 40.634±0,218 μm (F3). The drug loading was 7.691±0,087 % (F1), 8.922±0,056 % (F2), and 9.012±0,133% (F3). The encapsulation efficiency was 4.980 % (F1), 5.857%(F2), and 6,285 %(F3). The average amount of bisoprolol fumarate released in pH 6.8 was 2.113±0,289 % (F1), 1.954±0,015 % (F2), and 1.619±0,020 % (F3). The dissolution profile between each formula was statistically different (p value= 0,000).

Conclusion: As the low value of drug loading and encapsulation efficiency in each formula, we concluded that the microencapsulation formula with Eudragit EPO by solvent evaporation method is not effective to entrap bisoprolol fumarate.

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References

Telrandhe R. Formulation and evaluation of oral fast dissolving film of bisoprolol fumarate formulation and evaluation of oral fast dissolving film of bisoprolol fumarate. J Pharm Investig. 2018;6(2):105-15.

Charoo NA, Shamsher AAA, Lian LY, Abrahamsson B, Cristofoletti R, Groot DW. Biowaiver monograph for immediate-release solid oral dosage forms: bisoprolol fumarate. J Pharm Sci. 2014;103(2):378-91. doi: 10.1002/jps.23817, PMID 24382794.

Panainte AD, Gafitanu C, Stoleriu I, Tartau LM, Popescu M, Lisa G. New modified release tablets of bisoprolol fumarate for the treatment of hypertension: characterization and in vitro evaluation. J Drug Deliv Sci Technol. 2019;50:402-9. doi: 10.1016/j.jddst.2018.11.011.

Sudhamani. Development of fast dissolving tablets of bisoprolol fumarate and statistical optimization. Erode College of Pharmacy and Research Institute; 2012.

Chiappetta DA, Carcaboso AM, Bregni C, Rubio M, Bramuglia G, Sosnik A. Indinavir-loaded pH-sensitive microparticles for taste masking: toward extemporaneous pediatric anti-HIV/AIDS liquid formulations with improved patient compliance. AAPS PharmSciTech. 2009;10(1):1-6. doi: 10.1208/s12249-008-9168-z.

Sandile MK, Natalie P, Tsitsi N, Hendrina H, Roderick BW. The evaluation of eudragit microcapsules using USP apparatus 1. Diss Technol. 2009;5:15-22.

Yi EJ, Kim JY, Rhee YS, Kim SH, Lee HJ, Park CW. Preparation of sildenafil citrate microcapsules and in vitro/in vivo evaluation of taste masking efficiency. Int J Pharm. 2014;466(1-2):286-95. doi: 10.1016/j.ijpharm.2014.03.001, PMID 24607218.

Shahinaz AM, Mohammed EA, Shaza WS. Development and validation of uv spectrophotometric method for determination of bisoprolol fumarate in bulk and pharmaceutical dosage forms. Mediterranean Journal of Chemistry. 2017;6(5):196-9.

Rizky F. Mikroenkapsulasi lansoprazole dengan penyalut Eudragit rs po menggunakan metode emulsifikasi penguapan pelarut. Univeritas Andalas. 2016.

Leon L, Herbert AL, Joseph LK. The theory and practice of pharmaceutical industry. 3rd ed. Lea & Febiger; 1987. p. 412-6.

Sahoo SK, Mallick AA, Barik BB, Senapati PC. Formulation and in vitro evaluation of eudragit® microspheres of stavudine. Trop J Pharm Res 2005;4(1):369-75. doi: 10.4314/tjpr.v4i1.14622.

Bogataj M, Mrhar A, Kristl A, Kozjek F. Preparation and evaluation of eudragit e microspheres containing bacampicillin. Drug Dev Ind Pharm. 1989;15(14-16):2295-313. doi: 10.3109/03639048909052532.

Georgieva YG, Kassarova MK, Kokova VK, Apostolova EA, Pilicheva BP. Taste masking of enalapril maleate by microencapsulation in Eudragit EPO® microparticles. Pharmazie. 2020;75(2):61-9. doi: 10.1691/ph.2020.9123, PMID 32213236.

Ruan G, Feng SS. Preparation and characterization of poly(lactic acid)–poly(ethylene glycol)–poly(lactic acid) (PLA–PEG–PLA) microspheres for controlled release of paclitaxel. Biomaterials. 2003;24(27):5037-44. doi: 10.1016/s0142-9612(03)00419-8, PMID 14559017.

Park SJ, Kim SH. Preparation and characterization of biodegradable poly(l-lactide)/poly(ethylene glycol) microcapsules containing erythromycin by emulsion solvent evaporation technique. J Colloid Interface Sci. 2004;271(2):336-41. doi: 10.1016/j.jcis.2003.08.067, PMID 14972610.