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Eplerenone sublingual dissolving film: preparation and evaluation

Year 2024, Volume: 28 Issue: 5, 1768 - 1776, 28.06.2025

Abstract

Eplerenone is a medication used to manage hypertension and chronic heart failure by inhibiting aldosterone receptors. This study's objective is to prepare sublingual dissolving films containing Eplerenone, to enhance patient adherence, avoid first-pass metabolism, and minimize the need for repeated dosing. To achieve this goal, eight different formulations were prepared using a solvent-casting method. The study examined how various formulation factors influenced the physical and mechanical characteristics of the films, as well as their drug-release behavior. Notably, the results showed that the Eplerenone oral film, which included a combination of hydroxypropyl methylcellulose (HPMC E5) and polyvinyl alcohol (PVA), exhibited the fastest disintegration time, dissolving within just 27 seconds. Furthermore, formula F3, containing 25 mg of HPMC E5, 25 mg of PVA, and 30% glycerin, demonstrated a remarkable drug release rate of 72.4% within a 2-minute period with satisfactory mechanical properties. To summarize, this investigation successfully developed sublingual dissolving films for Eplerenone to improve patient adherence and decrease the necessity for frequent dosing. These films disintegrate rapidly and provide effective drug release, offering a patient-friendly alternative for managing conditions such as hypertension and chronic heart failure.

References

  • [1] Patel VF, Liu F, Brown MB. Advances in oral transmucosal drug delivery. J Control Rel. 2011;153(2):106-116. https://doi.org/10.1016/j.jconrel.2011.01.027.
  • [2] Abd-Alhammid SN, Saleeh HH. Formulation and evaluation of flurbiprofen oral film. Iraqi J Pharm Sci. 2014;23(1):53-59.https://doi.org/10.31351/vol23iss1pp53-59
  • [3] Al-Mogherah AI, Ibrahim MA, Hassan MA. Optimization and evaluation of venlafaxine hydrochloride fast dissolving oral films. Saudi Pharm J. 2020;28(11):1374-1382. https://doi.org/10.1016/j.jsps.2020.09.001
  • [4] Rajab NA, Jassim ZE, Hameed AM. Preparation and characterization of lacidipine as an oral fast dissolving film. J Pharm Res. 2018;12(3):321.
  • [5] Allam A, Fetih G. Sublingual fast dissolving niosomal films for enhanced bioavailability and prolonged effect of metoprolol tartrate. Drug Des Devel Ther. 2016;10:2421-2433. https://doi.org/10.2147%2FDDDT.S113775.
  • [6] Seferovic PM, Pelliccia F, Zivkovic I, Ristic A, Lalic N, Seferovic J, Simeunovic D, Milinkovic I, Rosano G. Mineralocorticoid receptor antagonists, a class beyond spironolactone--Focus on the special pharmacologic properties of eplerenone. Int J Cardiol. 2015 Dec 1;200:3-7. https://doi.org/10.1016/j.ijcard.2015.02.096
  • [7] Yassin GE, Khalifa MK. Development of eplerenone nano sono-crystals using factorial design: enhanced solubility and dissolution rate via anti solvent crystallization technique. Drug Dev Ind Pharm. 2022;48(12):683-693. https://doi.org/10.1080/03639045.2022.2160985
  • [8] Khames A. Formulation and characterization of eplerenone nanoemulsion liquisolids, an oral delivery system with higher release rate and improved bioavailability. Pharmaceutics. 2019;11(1):40. https://doi.org/10.3390/pharmaceutics11010040
  • [9] Bamberg K, Johansson U, Edman K, William-Olsson L, Myhre S, Gunnarsson A, Geschwindner S, Aagaard A, Björnson Granqvist A, Jaisser F, Huang Y, Granberg KL, Jansson-Löfmark R, Hartleib-Geschwindner J. Preclinical pharmacology of AZD9977: A novel mineralocorticoid receptor modulator separating organ protection from effects on electrolyte excretion. PLoS One. 2018;13(2):e0193380. https://doi.org/10.1371/journal.pone.0193380
  • [10] Rao PBB, Rao AL, Kumar KR, Sowmya K, Rao SK. Formulation and evaluation of eplerenone matrix tablets using Aloe Vera, Guar Gum and Povidone K-30. Pharm J Sri Lanka. 2018;8(1):49-60. http://dx.doi.org/10.4038/pjsl.v8i1.24
  • [11] Paarakh MP, Jose PA, Setty C, Peterchristoper G. Release kinetics–concepts and applications. Int J Pharm Res Technol (IJPRT). 2018;8(1):12-20. https://doi.org/10.31838/ijprt/08.01.02
  • [12] Khan MA, Ansari MM, Arif ST, Raza A, Choi HI, Lim CW, Noh HY, Noh JS, Akram S, Nawaz HA, Ammad M, Alamro AA, Alghamdi AA, Kim JK, Zeb A. Eplerenone nanocrystals engineered by controlled crystallization for enhanced oral bioavailability. Drug Deliv. 2021;28(1):2510-2524. https://doi.org/10.1080/10717544.2021.2008051.
  • [13] Alhagiesa AW, Ghareeb MM. The formulation and characterization of nimodipine nanoparticles for the enhancement of solubility and dissolution rate. Iraqi J Pharm Sci. 2021;30(2):143-152. https://doi.org/10.31351/vol30iss2pp143-152.
  • [14] Sasikala L, Rao VK, Gangadhara R, Reddy MR, Rani TS. Formulation, Characterization and evaluation of eplerenone drug loaded nanoparticles. J Pharm Sci Res. 2022;14(8):873-882.
  • [15] Kadhim ZJ, Rajab NA. Formulation and characterization of glibenclamide nanoparticles as an oral film. Int J Drug Deliv Technol. 2022;12(1):387-394. http://dx.doi.org/10.25258/ijddt.12.1.70
  • [16] Wadher K, Umekar M, Sheikh G, Younus M, Sapate R, Fatima N. Formulation and characterization of pediatric paracetamol oral mouth dissolving film. Int J Res Pharm Sci. 2017;8(3):397-402.
  • [17] Radhi ZA, Ghareeb MM. Preparation and evaluation of extended release ocular inserts of rebamipide for local effect using casting technique. Iraqi J Pharm Sci. 2018;28:24-36. https://doi.org/10.31351/vol28iss1pp24-36
  • [18] Pratiwi G, Susanti S, Shiyan S. Application of factorial design for optimization of PVC-HPMC polymers in matrix film ibuprofen patch-transdermal drug delivery system. Indones J Chemom Pharm Anal. 2021;1(1):1122. http://dx.doi.org/10.22146/ijcpa.486
  • [19] Abbas IK, Rajab NA, Hussein AA. Formulation and in-vitro evaluation of darifenacin hydrobromide as buccal films. Iraqi J Pharm Sci. 2019;28(2):83-94. https://doi.org/10.31351/vol28iss2pp83-94
  • [20] Desai PB. Design and evaluation of fast dissolving film of domperidone. Int Res J Pharm. 2012(9):134-145.
  • [21] Khalil YI. Preparation and characterization of montelukast sodium (SMLT) as a dual sustained release buccal strips. Iraqi J Pharm Sci. 2015;24(2):61-71.https://doi.org/10.31351/vol24iss2pp61-71.
  • [22] Wadetwar RN, Ali F, Kanojiya P. Formulation and evaluation of fast dissolving sublingual film of paroxetine hydrochloride for treatment of depression. Asian J Pharm Clin Res. 2019;12(10):126–132. http://dx.doi.org/10.22159/ajpcr.2019.v12i10.34690
  • [23] Bhattarai M, Gupta AK. Fast dissolving oral films: A novel trend to oral drug delivery system. Update Dent College J. 2016;2:58-68. http://dx.doi.org/10.3126/stcj.v2i1.14802
  • [24] Rani KC, Parfati N, Aryani NLD, Winantari AN, Fitriani EW, Pradana AT, Nawatila R, Putranti AR, Irine F, Angelica F, Yohanes C, Avanti C. Development, evaluation, and molecular docking of oral dissolving film of atenolol. Pharmaceutics. 2021;13(10):1727. https://doi.org/10.3390/pharmaceutics13101727
  • [25] Bhupinder B, Sarita J. Formulation and evaluation of fast dissolving sublingual films of rizatriptan benzoate. Int J Drug Dev Res. 2012;4(1):133-143.
  • [26] Thonte S, Pentewar R, Bhusnure O, Gholve S, Giram P, Khadkutkar V. Formulation and evaluation of oral fast dissolving film of levosalbutamol sulphate. World J Pharm Res. 2017;6(7):1298-1318.
  • [27] Alobaidy RAR, Rajab NA. Preparation and in-vitro evaluation of darifenacin HBr as nanoparticles prepared as nanosuspension. Int J Drug Deliv Technol. 2021;12(2):1-7.
  • [28] Al-Hassani HR, Al-Khedairy EB. Formulation and in-vitro evaluation of meloxicam solid dispersion using natural polymers. Iraqi J Pharm Sci. 2021;30(1):169-178. https://doi.org/10.31351/vol30iss1pp169-178
There are 28 citations in total.

Details

Primary Language English
Subjects Pharmaceutical Delivery Technologies
Journal Section Articles
Authors

Hawraa K. Khafeef 0009-0006-3642-5221

Nawal A. Rajab 0000-0003-1812-2244

Publication Date June 28, 2025
Submission Date October 12, 2023
Acceptance Date October 21, 2023
Published in Issue Year 2024 Volume: 28 Issue: 5

Cite

APA Khafeef, H. K., & Rajab, N. A. (2025). Eplerenone sublingual dissolving film: preparation and evaluation. Journal of Research in Pharmacy, 28(5), 1768-1776.
AMA Khafeef HK, Rajab NA. Eplerenone sublingual dissolving film: preparation and evaluation. J. Res. Pharm. July 2025;28(5):1768-1776.
Chicago Khafeef, Hawraa K., and Nawal A. Rajab. “Eplerenone Sublingual Dissolving Film: Preparation and Evaluation”. Journal of Research in Pharmacy 28, no. 5 (July 2025): 1768-76.
EndNote Khafeef HK, Rajab NA (July 1, 2025) Eplerenone sublingual dissolving film: preparation and evaluation. Journal of Research in Pharmacy 28 5 1768–1776.
IEEE H. K. Khafeef and N. A. Rajab, “Eplerenone sublingual dissolving film: preparation and evaluation”, J. Res. Pharm., vol. 28, no. 5, pp. 1768–1776, 2025.
ISNAD Khafeef, Hawraa K. - Rajab, Nawal A. “Eplerenone Sublingual Dissolving Film: Preparation and Evaluation”. Journal of Research in Pharmacy 28/5 (July 2025), 1768-1776.
JAMA Khafeef HK, Rajab NA. Eplerenone sublingual dissolving film: preparation and evaluation. J. Res. Pharm. 2025;28:1768–1776.
MLA Khafeef, Hawraa K. and Nawal A. Rajab. “Eplerenone Sublingual Dissolving Film: Preparation and Evaluation”. Journal of Research in Pharmacy, vol. 28, no. 5, 2025, pp. 1768-76.
Vancouver Khafeef HK, Rajab NA. Eplerenone sublingual dissolving film: preparation and evaluation. J. Res. Pharm. 2025;28(5):1768-76.