• NINING NINING Faculty of Pharmacy and Science, Universitas Muhammadiyah Prof. DR. HAMKA, Jakarta, Indonesia 13460
  • YUDI SRIFIANA Faculty of Pharmacy and Science, Universitas Muhammadiyah Prof. DR. HAMKA, Jakarta, Indonesia 13460
  • ELY MALINDA FADLIANTY Faculty of Pharmacy and Science, Universitas Muhammadiyah Prof. DR. HAMKA, Jakarta, Indonesia 13460


Objective: Allicin, a natural organosulfur compound, is the main garlic ingredient, which has extensive pharmacological activities. Its unstable under acidic conditions due to alliinase's inactivation causes the need for preparations that delayed-release in the stomach to maximize allicin absorption. This study aimed to prepare and characterize the enteric-coated microsphere of phytosome loading allicin-rich extract to protect it from gastric acid.

Methods: The allicin-rich extract phytosome (ArE-Ps) was prepared and evaluated for characteristics. Microsphere was made in three formulas with different molar ratios of ArE-Ps and Eudragit L30D-55 (1:1; 1:1.5 and 1:2) by spray dry. The three microspheres compared to particle size, entrapment efficiency, and dissolution test in acid and 7.4 pH medium.

Results: Optimized ArE-Ps has a size of 251.6 nm, polydispersity index 0.466, zeta potential 34.11, entrapment efficiency of 62.62 %, and specific gravity of 1,005 g/ml. The surface topography of the three formulas shows an almost spherical shape with concave surfaces. The particle size of the microsphere ranges from 215±6.27 nm to 548.8±10.15 nm. Entrapment efficiency increases with an increasing number of polymers with a maximum value of 65.44 % at F3. The results dissolution test in vitro showed no drug release in acidic medium, and drug release occurred at a 7.4 pH medium. Drug release of three microsphere formulations followed the Korsmeyer-Peppas model with a k value of 12.7088±0.1769; 17.9322±1.5621; and 12.958±1.2677; respectively.

Conclusion: Based on these results, the polymer's increase in three microsphere formulations can affect characteristics and retain drug release under acidic conditions.

Keywords: Enteric-coated, Delayed-release, Phytosome, Allicin-rich extract, Characterization


1. Morales Gonzalez JA, Madrigal Bujaidar E, Sanchez Gutierrez M, Izquierdo Vega JA, Carmen Valadez Vega M Del, Alvarez Gonzalez I, et al. Garlic (Allium sativum L.): a brief review of its antigenotoxic effects. Foods 2019;8:1–17.
2. Sharifi Rad J, Silva NCC, Jantwal A, Bhatt ID, Sharopov F, Cho WC, et al. Therapeutic potential of allicin-rich garlic preparations: emphasis on clinical evidence toward upcoming drugs formulation. Appl Sci 2019;9:1–16.
3. Khorshed Alam M, Obydul Hoq M, Shahab Uddin M. Medicinal plant allium sativum. J Med Plants Stud 2016;4:72–9.
4. Viswanathan V, Phadatare A, Mukne A. Antimycobacterial and antibacterial activity of allium sativum bulbs. Indian J Pharm Sci 2014;76:256–61.
5. Garcia Trejo EMA, Arellano Buendia AS, Arguello Garcia R, Loredo Mendoza ML, Garcia Arroyo FE, Arellano Mendoza MG, et al. Effects of allicin on hypertension and cardiac function in chronic kidney disease. Oxid Med Cell Longev 2016. DOI:10.1155/2016/3850402.
6. Phadatare AG, Viswanathan V, Mukne A. Novel strategies for optimized delivery of select components of allium sativum. Pharmacognosy Res 2014;6:334–40.
7. Guler E, Demir B, Guler B, Demirkol DO, Timur S. Biofu nctionalized nanomaterials for targeting cancer cells [Internet]. Nanostructures for Cancer Therapy. Elsevier Inc; 2017. p. 51–86.
8. Almajdoub SS. Polymer coating of an optimized nano lipid carrier system of harpagophytum procumbens extract for oral delivery [Master's thesis, University of the Western Cape]. Institutional Repository at the University of the Western Cape; 2017.
9. Lawson LD, Gardner CD. Composition, stability, and bioavailability of garlic products used in a clinical trial. J Agric Food Chem 2005;53:6254–61.
10. Lawson LD, Hunsaker SM. Allicin bioavailability and bioequivalence from garlic supplements and garlic foods. Nutrients 2018;10:4–6.
11. Halimi M, Alishahi M, Abbaspour MR, Ghorbanpoor M, Tabandeh MR. Efficacy of a Eudragit L30D-55-encapsulated oral vaccine containing inactivated bacteria (Lactococcusgarvieae/ Streptococcus iniae) in rainbow trout (Oncorhynchus mykiss). Fish Shellfish Immunol 2018;81:430–7.
12. Rahman MA, Ali J. Development and in vitro evaluation of enteric-coated multiparticulate system for resistant tuberculosis. Indian J Pharm Sci 2008;70:477–81.
13. Raffin RP, Jornada DS, Re MI, Pohlmann AR, Guterres SS. Sodium pantoprazole-loaded enteric microparticles prepared by spray drying: effect of the scale of production and process validation. Int J Pharm 2006;324:10–8.
14. Pyar H, Peh KK. Enteric coating of granules containing the probiotic lactobacillus acidophilus. Acta Pharm 2014; 64:247–56.
15. Anwar E, Farhana N. Formulation and evaluation of phytosome-loaded maltodextrin-gum arabic microsphere system for delivery of camellia sinensis extract. J Young Pharm 2018;10:s56–62.
16. Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol Pharm Drug Res 2010;67:217–23.
17. Unagolla JM, Jayasuriya AC. Drug transport mechanisms and in vitro release kinetics of vancomycin encapsulated chitosan-alginate polyelectrolyte microparticles as a controlled drug delivery system. Eur J Pharm Sci 2018;114:199–209.
18. Phan ADT, Netzel G, Chhim P, Netzel ME, Sultanbawa Y. Phytochemical characteristics and antimicrobial activity of Australian grown garlic (Allium sativum L.) cultivars. Foods 2019;8:358.
19. Saraf S, Khan J, Alexander A, Ajazuddin, Saraf S. Recent advances and future prospects of phyto-phospholipid complexation technique for improving pharmacokinetic profile of plant actives. J Controlled Release 2013;168:50–60.
20. Srifiana Y, Surini S, Yanuar A. Encapsulation of ketoprofen with coaservation and spray drying methods using pregelatinized cassava starch phtlate as a film-forming excipient. J Ilmu Kefarmasian Indones 2014;12:162–9.
21. Nijdam JJ, Langrish TAG. The effect of surface composition on the functional properties of milk powders. J Food Eng 2006;77:919–25.
22. Nining N, Suwandi SN, Wikarsa S. Rosella flower (Hibiscus sabdariffa L.) extract drying through microencapsulation of spray drying method with maltodextrin. Farmasains 2017;4:65–71.
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