NICORANDIL MUCOADHESIVE MICROSPHERES: FORMULATION DEVELOPMENT, PHYSICO-CHEMICAL AND FUNCTIONAL CHARACTERIZATION

Authors

  • ANKITA V. HADKE Datta Meghe College of Pharmacy, Datta Meghe Institute of Medical Sciences (Deemed to be University), Sawangi (Meghe), Wardha, Maharashtra, India https://orcid.org/0000-0001-7163-0307
  • ANIL M. PETHE Datta Meghe College of Pharmacy, Datta Meghe Institute of Medical Sciences (Deemed to be University), Sawangi (Meghe), Wardha, Maharashtra, India https://orcid.org/0000-0002-6380-1847
  • MAHESH A. KESALKAR Institute of Pharmaceutical Education and Research, Wardha, Maharashtra, India https://orcid.org/0000-0001-7869-3247

DOI:

https://doi.org/10.22159/ijap.2023v15i2.46593

Keywords:

Nicorandil, Microspheres, Polymer, Glutaraldehyde

Abstract

Objective: The study aims to prepare and evaluate Nicorandil mucoadhesive microspheres to improve the oral physicochemical properties of nicorandil and mucoadhesion to extend the residence time at the absorption site.

Methods: Nicorandil mucoadhesive microsphere was prepared by emulsion cross-linking method using fenugreek gum, karaya gum as polymer, and glutaraldehyde as a cross-linking agent. Drug entrapment efficiency, particle size, % swelling index, mucoadhesion study, differential scanning calorimetry, powder x-ray diffraction, Fourier transform infrared spectroscopy, and in vitro dissolution studies were used to characterize the microspheres.

Results: The characterization studies indicated the formation of mucoadhesive microspheres. The nicorandil mucoadhesive microspheres particle size is130.83±0.48, entrapment efficiency 66.91±0.54, swelling index 82.69±0.40, % mucoadhesion 95.22±0.13 and in vitro drug release was found to be 89.96±0.17 % at the end of 12 h.

Conclusion: This research work successfully formed nicorandil mucoadhesive microspheres formulation using the emulsion cross-linking method. Encapsulation efficiency and other physicochemical and functional characterization of microspheres suggested the successful formation of nicorandil mucoadhesive microspheres.

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References

Ahmed LA. Nicorandil: A drug with ongoing benefits and different mechanisms in various diseased conditions. Indian J Pharmacol. 2019 Oct;51(5):296-301. doi: 10.4103/ ijp.IJP_298_19. PMID 31831918.

Roland E. Safety profile of an anti-anginal agent with potassium channel opening activity: an overview. Eur Heart J. 1993;14Suppl B:48-52. doi: 10.1093/eurheartj/14.suppl_b.48, PMID 8370373.

Vinod R. Formulation and evaluation of nicorandil sustained release matrix tablets using natural gum Mangifera indica as release modifier. Asian J Biomed PharmSci. 2013;3(18):54-60.

Patel SS, Patel MR, Patel MJ. Formulation and evaluation of microsponge-based nicorandil sustained released tablet. J Sci Res. 2017;9(3):285-96. doi: 10.3329/jsr.v9i3.31193.

Hiremath JG, Valluru R, Narhare J, Katta SA, Matad P. Pharmaceutical aspects of nicorandil. Int J Pharm Pharm Sci. 2010;2(4):24-9.

Patel SS, Patel MR, Patel MJ. Formulation and evaluation of microsponge-based nicorandil sustained released tablet. J Sci Res. 2017;9(3):285-96. doi: 10.3329/jsr.v9i3.31193.

Singh B, Garg T, Goyal AK, Rath G. Development, optimization, and characterization of polymeric electrospun nanofiber: a new attempt in sublingual delivery of nicorandil for the management of angina pectoris. Artif Cells Nanomed Biotechnol. 2016;44(6):1498-507. doi: 10.3109/21691401.2015.1052472. PMID 26134924.

Tipre DN, Vavia PR. Formulation optimization and stability study of transdermal therapeutic system of nicorandil. Pharm Dev Technol. 2002;7(3):325-32. doi: 10.1081/pdt-120005729, PMID 12229264.

Sumaiya Fathima Barveen KM, Elango K, Ramesh Kumar K, Ramprabhu RV. Development and characterization of nicorandil loaded maltodextrin based proniosomes. World J PharmSci. 2017;5(6):243-52.

Saha N, Hasan I, Nazmi M, Reza MS. Design and development of sustained release microspheres of ibuprofen by emulsification solvent evaporation method using polymeric blend. Bangla Pharma J. 2013;16(1):39-44. doi: 10.3329/bpj.v16i1.14489.

NR K. Microsphere: a brief review. AJBPS 2015;05(47):13-9. doi: 10.15272/ajbps.v5i47.713.

Rai A, Malviya RK, Patidar D. Formulation development and evaluation of gastro retentive delivery system (microspheres) using natural polymer. J Drug Deliv Ther. 2019 Jul 15;9(4):496-503.

Sahu VK, Sharma N, Sahu PK, Saraf SA. Formulation and evaluation of floating-mucoadhesive microspheres of novel natural polysaccharide for site specific delivery of ranitidine hydrochloride. Int J App Pharm. 2017;9(3):15-9. doi: 10.22159/ijap.2017v9i3.16137.

Marina K, Ansu J, Prabhakara P, Girish SN. Mucoadhesive microspheres of famotidine for gastro retentive drug delivery. Int J Drug Dev Res. 2012;4:59-64.

Telange DR, Denge R, Patil AT, Umekar MJ, Gupta SV, Dave VS. Pentaerythritol as an excipient/solid dispersion carrier for improved solubility and permeability of ursodeoxycholic acid. J Excip Food Chem. 2018 Sep;9(3):80-95.

Hemant KSY, Singh MN, Shivakumar HG. Chitosan/sodium tripolyphosphate cross-linked microspheres for the treatment of gastric ulcer. Pharm Lett. 2010;2:106-13.

Hari PR, Chandy T, Sharma CP. Chitosan/calcium alginate microcapsules for intestinal delivery of nitrofurantoin. J Microencapsul. 1996;13(3):319-29. doi: 10.3109/ 02652049609026019, PMID 8860687.

Dinarvand R, Rahmani E, Farbod E. Gelatin microspheres for the controlled release of all–trans-retinoic acid topical formulation and drug delivery evaluation. Iran J Pharm Res. 2010;2:47-50.

Patel K, Patel M, Ajmera A, Patel P, Rathod K. Formulation and evaluation of nicorandil microspheres. Int J Pharm Pharm Sci. 2013;5(2):593-7.

Teymouri Rad RT, Mortazavi SA, Vatanara A, Dadashzadeh S. Enhanced dissolution rate of tadalafil nanoparticles prepared by sonoprecipitation technique: optimization and physicochemical investigation. Iran J Pharm Res. 2017;16(4):1335-48. PMID 29721025, PMCID PMC5843297.

Deshmukh M, Mohite S. Formulation and characterization of olanzapine-loaded mucoadhesive microspheres. Asian J Pharm Clin Res. 2017;10(4):249-55. doi: 10.22159/ajpcr.2017.v10i4.16659.27.

Rastogi R, Sultana Y, Aqil M, Ali A, Kumar S, Chuttani K. Alginate microspheres of isoniazid for oral sustained drug delivery. Int J Pharm. 2007;334(1-2):71-7. doi: 10.1016/j.ijpharm.2006.10.024, PMID 17113732.

Yeo Y, Park K. Control of encapsulation efficiency and initial burst in polymeric microparticle systems. Arch Pharm Res. 2004;27(1):1-12. doi: 10.1007/BF02980037, PMID 14969330.

Rajinikanth PS, Sankar C, Mishra B. Sodium alginate microspheres of metoprolol tartrate for intranasal systemic delivery: development and evaluation. Drug Deliv. 2003;10(1):21-8. doi: 10.1080/713840323, PMID 12554360.

Sharma N, Kulkarni GT, Sharma A, Bhatnagar A, Kumar N. Natural mucoadhesive microspheres of Abelmoschus esculentus polysaccharide as a new carrier for nasal drug delivery. J Microencapsul. 2013;30(6):589-98. doi: 10.3109/02652048.2013.764941, PMID 23379506.

Nayak AK, Pal D, Pradhan J, Hasnain MS. Fenugreek seed mucilage-alginate mucoadhesive beads of metformin HCl: Design, optimization and evaluation. Int J Biol Macromol. 2013 Mar;54:144-54. doi: 10.1016/j.ijbiomac.2012.12.008, PMID 23246901.

Lal C, Garg R, Gupta GD. Formulation and optimization by applying 32 full factorial design of mucoadhesive microspheres of nifedipine. Asian J Pharm Clin Res. 2019;12(6):321-7.

Adimoolam S, Phonhaxa S. Trigonella-foenum graecum l. seed mucilage-based mucoadhesive microspheres of diclofenac sodium. JAPLR. 2018 Mar;7(2):114-9. doi: 10.15406/japlr.2018.07.00210.

Biswal B, Parmar H, Nayak J. Design development and evaluation of buccal tablet containing nicorandil as a model drug. Asian J Pharm Clin Res. 2014;8(2):102-6.

Published

07-03-2023

How to Cite

HADKE, A. V., PETHE, A. M., & KESALKAR, M. A. (2023). NICORANDIL MUCOADHESIVE MICROSPHERES: FORMULATION DEVELOPMENT, PHYSICO-CHEMICAL AND FUNCTIONAL CHARACTERIZATION. International Journal of Applied Pharmaceutics, 15(2), 123–130. https://doi.org/10.22159/ijap.2023v15i2.46593

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