Formulation and evaluation of floating tablets of Aegle marmelos (bael) fruit extract for sustained release

Author

Ashwin Roshan Raj.M , Atchaya . M ,Balaji.P ,Bharath .V , S.Hemavathy , Dr. J. Karthi , Dr. S. Swarnalatha


Abstract

 Background: The fruit pulp of Aegle marmelos (bael) protects the gastric mucosa in several animal models, but a conventional tablet of the extract would leave the stomach quickly and give the mucosa only a brief exposure. A floating, sustained-release tablet could hold the extract in the stomach for longer.

Objective: To formulate effervescent floating matrix tablets of bael fruit extract with sodium alginate as the release-controlling polymer, and to characterise their buoyancy, swelling and release behaviour.

Methods: Dried fruit pulp was defatted with n-hexane and extracted with ethanol in a Soxhlet apparatus. Five formulations (F1–F5) were prepared by wet granulation. The extract, PVP K30, citric acid and lubricants were kept constant, while sodium alginate was raised from 1.5 to 2.4 g per batch, with microcrystalline cellulose reduced correspondingly and sodium bicarbonate raised slightly (1.2 to 1.4 g). Blends and tablets were assessed for flow, hardness, friability, drug content, floating behaviour, swelling and in vitro release. Drug–excipient compatibility was examined by FTIR spectroscopy.

Results: All blends flowed well (angle of repose 24.3–28.9°; Carr's index 11.9–14.6%), and the tablets were mechanically sound (hardness 4.2–4.6 kg/cm²; friability 0.84–0.96%; drug content 97.4–99.8%). Floating lag time followed a U-shaped trend, falling from 2.50 min (F1) to 1.20 min (F3) and rising again to 5.56 min (F4) and 12.00 min (F5). Every tablet floated for more than 8 h, and F3 for more than 12 h. F3 also showed the greatest swelling (102% at 8 h) and the highest release (93.6% at 12 h), with no initial burst. Release from F3 was best described by the Korsmeyer–Peppas model (n = 0.822), which indicates anomalous (non-Fickian) transport. FTIR gave no evidence of extract–excipient interaction.

Conclusion: A moderate alginate level (F3) gave the best balance of rapid buoyancy, matrix integrity and 12-h release, which supports bael extract as a candidate for gastroretentive delivery. Marker-based standardisation, stability testing and in vivo gastric retention studies are still required.


Keywords

Aegle marmelos; bael; gastroretentive drug delivery; floating tablets; sodium alginate; sustained release; Korsmeyer–Peppas model



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References


  1. Garg R, Gupta GD. Progress in controlled gastroretentive delivery systems. Trop J Pharm Res. 2008;7(3):1055–66.
  2. Streubel A, Siepmann J, Bodmeier R. Gastroretentive drug delivery systems. Expert Opin Drug Deliv. 2006;3(2):217–33.
  3. Arora S, Ali J, Ahuja A, Khar RK, Baboota S. Floating drug delivery systems: a review. AAPS PharmSciTech. 2005;6(3):E372–90.
  4. Vrettos NN, Roberts CJ, Zhu Z. Gastroretentive technologies in tandem with controlled-release strategies: a potent answer to oral drug bioavailability and patient compliance implications. Pharmaceutics. 2021;13(10):1591.
  5. Rowe RC, Sheskey PJ, Quinn ME, editors. Handbook of Pharmaceutical Excipients. 6th ed. London: Pharmaceutical Press; 2009.
  6. Choi BY, Park HJ, Hwang SJ, Park JB. Preparation of alginate beads for floating drug delivery system: effects of CO2gas-forming agents. Int J Pharm. 2002;239(1–2):81–91. doi:10.1016/S0378-5173(02)00054-6.
  7. Jadach B, Świetlik W, Froelich A. Sodium alginate as a pharmaceutical excipient: novel applications of a well-known polymer. J Pharm Sci. 2022;111(5):1250–61. doi:10.1016/j.xphs.2021.12.024.
  8. Liew CV, Chan LW, Ching AL, Heng PW. Evaluation of sodium alginate as drug release modifier in matrix tablets. Int J Pharm. 2006;309(1–2):25–37. doi:10.1016/j.ijpharm.2005.10.040.
  9. Baliga MS, Bhat HP, Joseph N, Fazal F. Phytochemistry and medicinal uses of the bael fruit (Aegle marmelosCorrea): a concise review. Food Res Int. 2011;44(7):1768–75. doi:10.1016/j.foodres.2011.02.008.
  10. Hazra SK, Sarkar T, Salauddin M, Sheikh HI, Pati S, Chakraborty R. Characterization of phytochemicals, minerals and in vitro medicinal activities of bael (Aegle marmelosL.) pulp and differently dried edible leathers. Heliyon. 2020;6(11):e05382.
  11. Tiwari R, Mishra S, Danaboina G, Jadaun GPS, Kalaivani M, Kalaiselvan V, et al. Comprehensive chemo-profiling of coumarins enriched extract derived from Aegle marmelos(L.) Correa fruit pulp, as an anti-diabetic and anti-inflammatory agent. Saudi Pharm J. 2023;31(9):101708.
  12. Ramakrishna YG, Savithri K, Kist M, Niranjali Devaraj S. Aegle marmelosfruit extract attenuates Helicobacter pylorilipopolysaccharide induced oxidative stress in Sprague Dawley rats. BMC Complement Altern Med. 2015;15:375.
  13. Das SK, Roy C. The protective role of Aegle marmeloson aspirin-induced gastro-duodenal ulceration in albino rat model: a possible involvement of antioxidants. Saudi J Gastroenterol. 2012;18(3):188–94.
  14. Ghatule RR, Gautam MK, Goel S, Singh A, Joshi VK, Goel RK. Protective effects of Aegle marmelosfruit pulp on 2,4,6-trinitrobenzene sulfonic acid-induced experimental colitis. Pharmacogn Mag. 2014;10(Suppl 3):S147–52.
  15. Tyagi L, Sharma N, Sharma A, Ahmad S. Evaluation of synergistic antiulcer activity of Aegle marmelosand Ocimum sanctumin ulcer induced Wistar rats. Panacea J Pharm Pharm Sci. 2019;8(2):01–09.
  16. Aswatha Ram HN, Lachake P, Kaushik U, Shreedhara CS. Formulation and evaluation of floating tablets of liquorice extract. Pharmacogn Res. 2010;2(5):304–8.
  17. Nathe RB, Gosavi RD, Bhamare V. Aegle marmelos(anti-ulcer activity). Int J Novel Res Dev. 2023;8(1):c391–7.
  18. Venthodika A, Chhikara N, Mann S, Garg MK, Sofi SA, Panghal A. Bioactive compounds of Aegle marmelosL., medicinal values and its food applications: a critical review. Phytother Res. 2021;35(4):1887–907. doi:10.1002/ptr.6934.
  19. Sahoo L, Nayak Y, Mohanty SK. Exploring the phytochemical constituents of Aegle marmelos(bael) and their therapeutic potential against chronic diseases. Int J Basic Clin Pharmacol. 2025;14(2):316–23.
  20. Shetty A, Fernandes L, Shambhavi D, Mahadev M, Dubey A. Phytochemical and pharmacological profile of Aegle marmelos(L.) Correa: a comprehensive review of therapeutic potential, mechanisms of action, and translational relevance. J Appl Pharm Sci. 2026;16(2):6–18.
  21. World Flora Online. Aegle marmelos(L.) Corrêa [Internet]. 2026 [cited 2026 Jul 3]. Available from: http://www.worldfloraonline.org/taxon/wfo-0000521533
  22. World Health Organization. Quality control methods for medicinal plant materials. Geneva: WHO; 1998.
  23. Kokate CK, Purohit AP, Gokhale SB. Pharmacognosy. 49th ed. Pune: Nirali Prakashan; 2015.
  24. Lachman L, Lieberman HA, Kanig JL. The Theory and Practice of Industrial Pharmacy. 3rd ed. Mumbai: Varghese Publishing House; 1987.
  25. Prajapati ST, Patel LD, Patel DM. Studies on formulation and in vitro evaluation of floating matrix tablets of domperidone. Indian J Pharm Sci. 2009;71(1):19–23. doi:10.4103/0250-474X.51944.
  26. Carr RL. Evaluating flow properties of solids. Chem Eng. 1965;72:163–8.
  27. Aulton ME, Taylor KMG. Aulton's Pharmaceutics: The Design and Manufacture of Medicines. 4th ed. Edinburgh: Churchill Livingstone Elsevier; 2013.
  28. Indian Pharmacopoeia. Ghaziabad: Indian Pharmacopoeia Commission, Ministry of Health and Family Welfare, Government of India; 2018.
  29. Higuchi T. Mechanism of sustained-action medication: theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci. 1963;52(12):1145–9.
  30. Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm. 1983;15(1):25–35.
  31. Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol Pharm. 2010;67(3):217–23.
  32. Ritger PL, Peppas NA. A simple equation for description of solute release I. Fickian and non-Fickian release from non-swellable devices in the form of slabs, spheres, cylinders or discs. J Control Release. 1987;5(1):23–36. doi:10.1016/0168-3659(87)90034-4.
  33. Ritger PL, Peppas NA. A simple equation for description of solute release II. Fickian and anomalous release from swellable devices. J Control Release. 1987;5(1):37–42. doi:10.1016/0168-3659(87)90035-6.
  34. Siepmann J, Peppas NA. Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). Adv Drug Deliv Rev. 2001;48(2–3):139–57.
  35. Costa P, Sousa Lobo JM. Modeling and comparison of dissolution profiles. Eur J Pharm Sci. 2001;13(2):123–33. doi:10.1016/S0928-0987(01)00095-1.
  36. Nigusse B, Gebre-Mariam T, Belete A. Design, development and optimization of sustained release floating, bioadhesive and swellable matrix tablet of ranitidine hydrochloride. PLoS One. 2021;16(6):e0253391.
  37. Senjoti FG, Mahmood S, Jaffri JM, Mandal UK. Design and in-vitro evaluation of sustained release floating tablets of metformin HCl based on effervescence and swelling. Iran J Pharm Res. 2016;15(1):53–70.

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