ENCAPSULATION OF PARTIALLY PURIFIED BROMELAIN FROM PINEAPPLE CORES IN ALGINATE-PECTIN BEADS AS A TARGETED ANTIPLATELET AGENT

Authors

  • HEGI ADI PRABOWO Department of Chemistry, Faculty of Mathematics and Natural Sciences, Universitas Indonesia, Depok 16424, West Java, Indonesia
  • EMIL BUDIANTO Department of Chemistry, Faculty of Mathematics and Natural Sciences, Universitas Indonesia, Depok 16424, West Java, Indonesia
  • SUMI HUDIYONO Department of Chemistry, Faculty of Mathematics and Natural Sciences, Universitas Indonesia, Depok 16424, West Java, Indonesia

DOI:

https://doi.org/10.22159/ijap.2021v13i3.41158

Keywords:

Bromelain, Alginate-pectin, In vitro release, Kinetics

Abstract

Objective: Oral administration of bromelain can decrease its bioactivity once it makes contact with stomach acid. Therefore, bromelain was loaded into alginate (Alg), pectin (Pec), and alginate-pectin (AP) beads to control its release into the intestines and avoid degradation.

Methods: Crude bromelain was purified by ammonium sulfate precipitation and the dialysis process. In vitro releases and kinetics studies of bromelain-loaded alginate-pectin beads were carried out using an acid and phosphate buffer medium. The beads were characterized using physical analysis, Fourier-Transform Infrared Spectroscopy (FTIR) analysis, and Differential Scanning Calorimetry (DSC) analysis.

Results: The dialysis fraction of bromelain has a specific activity of 67.93 U/mg, 3.05 times that of crude bromelain. That fraction was encapsulated in Alg, Pec, and AP beads with a range of encapsulation efficiency around 82.70–91.39%. Bromelain-loaded pectin and AP19 beads were chosen to study in an in vitro release based on their swelling properties and encapsulation efficiency. Bromelain-loaded AP19 beads have lower release than bromelain-loaded pectin beads in both dissolution mediums. The cumulative releases of AP19 are 9.99 and 87.81% in 0.1 N HCl and phosphate buffer medium, respectively. Bromelain-loaded P and AP beads both follow the zero-order kinetics model and the dissolution mechanism of the beads is non-Fickian with a combination of diffusion and erosion. The in vitro antiplatelet activity of dissolution aliquots (20.51 and 18.48%) is lower than its dialysis fraction (56.04%).

Conclusion: This in vitro research data shows promising potency for AP as a carrier for oral administration of bromelain as an antiplatelet agent.

Downloads

Download data is not yet available.

References

Ruan Y, Guo Y, Zheng Y, Huang Z, Sun S, Kowal P, et al. Cardiovascular disease (CVD) and associated risk factors among older adults in six low-and middle-income countries: results from SAGE wave 1. BMC Public Health 2018;18:778.

Alanon ME, Palomo I, Rodriguez L, Fuentes E, Arraez Roman D, Segura Carretero A. Antiplatelet activity of natural bioactive extracts from mango (Mangifera Indica L.) and its by-products. Antioxidants 2019;8:517.

Badimon L, Vilahur G. Coronary atherothrombotic disease: progress in antiplatelet therapy. Rev Esp Cardiol 2008;5:501–13.

Geisler T, Anders N, Paterok M, Langer H, Stellos K, Lindemann S, et al. Platelet response to clopidogrel is attenuated in diabetic patients undergoing coronary stent implantation. Diabetes Care 2007;30:372–4.

Kong Y, Xu C, He ZL, Zhou QM, Wang JB, Li ZY, et al. A novel peptide inhibitor of platelet aggregation from stiff silkworm, Bombyx batryticatus. Peptides 2014;53:70–8.

Brites MM, Ceron AA, Costa SM, Oliveira RC, Ferraz HG, Catalani LH, et al. Bromelain immobilization in cellulose triacetate nanofiber membranes from sugarcane bagasse by electrospinning technique. Enzyme Microb Technol 2020;132:109384.

Setiasih S, Prabowo HA, Budianto E, Hudiyono S. Dissolution profiles of partially purified bromelain from pineapple cores [Ananas comosus (L.) merr] encapsulated in glutaraldehyde-crosslinked chitosan. J Appl Pharm Sci 2018;8:17–24.

Setiasih S, Darwis AAC, Dzikria V, Hudiyono S. Stability test of partially purified bromelain from pineapple (Ananas comosus (L.) merr) core extract in artificial stomach fluid. IOP Conf Ser: Mater Sci Eng 2018;299:1–7.

Chobotova K, Vernallis AB, Majid FAA. Bromelain's activity and potential as an anti-cancer agent: current evidence and perspectives. Cancer Lett 2010;290:148–56.

Auriemma G, Mencherini T, Russo P, Stigliani M, Aquino RP, Gaudio PD. Prilling for the development of multi-particulate colon drug delivery system: pectin vs pectin-alginate beads. Carbohydr Polym 2013;92:367–73.

Chung YS, Park J, Noh J, Chang ST, Kim JS, Kim J. Microencapsulation by pectin for multi-components carriers bearing both hydrophobic and hydrophilic active agents. Carbohydr Polym 2017;182:172–9.

Irfan AA, Setiasih S, Hudiyono S. Dissolution profile of partially purified bromelain from pineapple core encapsulated in alginate-guar gum with in vitro study of antiplatelet activity. IOP Conf Ser: Mat Sci Eng 2020;763:0102042.

Richards C, Oconnor N, Jose D, Barret A, Regan F. Selection and optimization of protein and carbohydrate assays for the characterization of marine biofouling. Anal Methods 2020;12:2228-36.

Sinha P, Udhumansha U, Rathnam G, Ganesh M, Jang HT. Capecitabine encapsulated chitosan succinate-sodium alginate macromolecular complex beads for colon cancer targeted delivery: in vitro evaluation. Int J Biol Macromol 2018;117:840-50.

Macdonald M, Rodriguez NM, Smith R, Hammond PT. Release of a model protein from biodegradable self-assembled films for surface delivery applications. J Controlled Release 2008;131:228–34.

Guo J, Miao Z, Wan J, Guo X. Pineapple peel bromelain extraction using gemini surfactant-based reverse micelle–Role of spacer of gemini surfactant. Sep Purif Technol 2018;190:156–64.

Bernela M, Ahuja M, Thakur R. Enhancement of anti-inflammatory activity of bromelain by its encapsulation in katira gum nanoparticles. Carbohydr Polym 2016;143:18–24.

Devi P, Rathor S, Sharma P, Sen J, Kaur H, Singh J. Development of novel gastroretentive salbutamol sulfate-loaded sodium alginate-pectin bubble beads prepared by co-axial needle air-injection method and in vivo clinical evaluation by ultrasound studies. Eur J Pharm Sci 2018;122:359–73.

Nesic A, Onjia A, Davidovic S, Dimitrijevic S, Errico ME, Santagata G, et al. Design of pectin-sodium alginate-based films for potential healthcare application: study of chemico-physical interactions between the components of films and assessment of their antimicrobial activity. Carbohydr Polym 2017;157:981–90.

Voo WP, Lee BB, Idris A, Islam A, Tey BT, Chan ES. Production of ultra-high concentration calcium alginate beads with prolonged dissolution profile. RSC Adv 2015;5:36687–95.

Abasalizadeh F, Moghaddam SV, Alizadeh E, Akbari E, Kashani E, Fazljou SMB, et al. alginate-based hydrogels as drug delivery vehicles in cancer treatment and their applications in wound dressing and 3D bioprinting. J Biol Eng 2020;14:8.

Gawkowska D, Cybulska J, Zdunek A. Structure-related gelling of pectins and linking with other natural compounds: a review. Polymers 2018;10:762.

Ganesh D, Suresh P, Rao GS. Fabrication of sodium alginate/gum ghatti IPN microbeads intercalated with kaolin nano clay for controlled release of curcumin. Int J Appl Pharm 2021;13:223-41.

Eikelboom JW, Hirsh J, Spencer FA, Baglin TP, Weitz JI. Antiplatelet drugs: antithrombotic therapy and prevention of thrombosis. 9th ed: American college of chest physicians evidence-based clinical practice guidelines. Chest 2012;141(2 Suppl):e89S-e119S.

Metzig C, Grabowska E, Eckert K, Rehse K, Maurer HR. Bromelain proteases reduce human platelet aggregation in vitro, adhesion to bovine endothelial cells and thrombus formation in rat vessels in vivo. In Vivo 1999;13:7-12.

Published

07-05-2021

How to Cite

PRABOWO, H. A., BUDIANTO, E., & HUDIYONO, S. (2021). ENCAPSULATION OF PARTIALLY PURIFIED BROMELAIN FROM PINEAPPLE CORES IN ALGINATE-PECTIN BEADS AS A TARGETED ANTIPLATELET AGENT. International Journal of Applied Pharmaceutics, 13(3), 176–182. https://doi.org/10.22159/ijap.2021v13i3.41158

Issue

Section

Original Article(s)