Ticagrelor Solubility and Dissolution Rate Enhancement Using Mesoporous Silica SBA-15
Article Sidebar
Keywords:
-
SBA-15, Ticagrelor, Solubility, Dissolution
Abstract
Ticagrelor is a triazolopyrimidine antiplatelet agent with poor water solubility. Ticagrelor was incorporated into mesoporous silica SBA15 in this study to evaluate its physical stability and improve its solubility and dissolution rate. TEOS was employed as a silica precursor and Pluronic P123 as a template to synthesize SBA-15. Ticagrelor was loaded into SBA-15 at a mass ratio of 1:1. Physicochemical characterization was conducted using nitrogen adsorption-desorption isotherm analysis, powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), fourier-transform infrared spectroscopy (FT-IR), and scanning electron microscopy (SEM). Ticagrelor solubility and dissolution were tested using distilled water as the medium. To evaluate the physical stability, Ticagrelor-SBA-15 was stored in a climatic chamber at 75% RH and 40°C for a month and analyzed using PXRD. Physicochemical characterization indicated efficient adsorption of ticagrelor into the SBA-15 pores, resulting in an amorphous form of solid material. Meanwhile, solubility and dissolution rate testing showed respective increases of 1.33 times and 1.74 times with significant differences (p<0.05) while maintaining its physical stability after storage for one month. Based on this study, it can be concluded that the incorporation of mesoporous SBA-15 significantly enhances ticagrelor’s solubility and dissolution rate while maintaining stability.
References
Adrover, M. E., M. Pedernera, M. Bonne, B. Lebeau, V. Bucala, and L. Gallo (2020). Synthesis and Characterization of Mesoporous SBA-15 and SBA-16 as Carriers to Improve Albendazole Dissolution Rate. Saudi Pharmaceutical Journal, 28(1); 15–24.
Ambrogi, V., L. Perioli, C. Pagano, F. Marmottini, M. Ricci, A. Sagnella, and C. Rossi (2012). Use of SBA-15 for Furosemide Oral Delivery Enhancement. European Journal of Pharmaceutical Sciences, 46(1–2); 43–48.
Beliatskaya, A. V., I. I. Krasnyuk, I. I. Krasnyuk, O. I. Stepanova, Z. A. Abgaryan, T. P. Kudinova, and I. S. Nesterenko (2019). Study on the Solubility of Ketoprofen From Solid Dispersions with Polyvinylpyrrolidone. Moscow University Chemistry Bulletin, 74(2); 93–99.
Bhairav, B. A., J. K. Bachhav, and R. B. Saudagar (2016). Review on Solubility Enhancement Techniques. Asian Journal of Pharmaceutical Research, 6(3); 175.
Bhalani, D. V., B. Nutan, A. Kumar, and A. K. S. Chandel (2022). Bioavailability Enhancement Techniques for Poorly Aqueous Soluble Drugs and Therapeutics. Biomedicines, 10(9); 2055.
Bolla, G., B. Sarma, and A. K. Nangia (2022). Crystal Engineering of Pharmaceutical Cocrystals in the Discovery and Development of Improved Drugs. Chemical Reviews, 122(13); 11514–11603.
Chaturvedi, K., H. S. Shah, K. Nahar, R. Dave, and K. R. Morris (2020). Contribution of Crystal Lattice Energy on the Dissolution Behavior of Eutectic Solid Dispersions. ACS Omega, 5(17); 9690–9701.
Chen, X., I. Partheniadis, I. Nikolakakis, and H. Al-Obaidi (2020). Solubility Improvement of Progesterone From Solid Dispersions Prepared by Solvent Evaporation and Co-Milling. Polymers, 12(4); 854.
Febriyenti, P. Indra, E. Zaini, F. Ismed, and H. Lucida (2020). Preparation and Characterization of Quercetin-Polyvinylpyrrolidone K-30 Spray Dried Solid Dispersion. Journal of Pharmacy & Pharmacognosy Research, 8(2); 127–134.
Fitriani, L., H. Azizah, U. Hasanah, and E. Zaini (2023). Enhancement of Curcumin Solubility and Dissolution by Adsorption in Mesoporous SBA-15. International Journal of Applied Pharmaceutics, 15(Special Issue 1); 61–67.
Hasanah, U., S. Wikarsa, and S. Asyarie (2021). Various Chloride Salt Addition in Mesoporous Material (SBA-15) Synthesis and Potential as Carrier for Dissolution Enhancer. In Proceedings of the 2nd International Conference on Contemporary Science and Clinical Pharmacy 2021 (ICCSCP 2021), volume 40. pages 343–349.
Hong, S., S. Shen, D. C. T. Tan, W. K. Ng, X. Liu, L. S. O. Chia, and R. Gokhale (2016). High Drug Load, Stable, Manufacturable and Bioavailable Fenofibrate Formulations in Mesoporous Silica: A Comparison of Spray Drying Versus Solvent Impregnation Methods. Drug Delivery, 23(1); 316–327.
Juneja, S., K. Gupta, and S. Kaushal (2013). Ticagrelor: An Emerging Oral Antiplatelet Agent. Journal of Pharmacology and Pharmacotherapeutics, 4(1); 78–80.
Kim, S. J., H. K. Lee, Y. G. Na, K. H. Bang, H. J. Lee, M. Wang, and C. W. Cho (2019). A Novel Composition of Ticagrelor by Solid Dispersion Technique for Increasing Solubility and Intestinal Permeability. International Journal of Pharmaceutics, 555; 11–18.
Letchmanan, K., S.-C. Shen, W. K. Ng, and R. B. H. Tan (2017). Dissolution and Physicochemical Stability Enhancement of Artemisinin and Mefloquine Co-Formulation via Nano-Confinement with Mesoporous SBA-15. Colloids and Surfaces B: Biointerfaces, 155; 560–568.
Lutfiyah, D. S., L. Fitriani, M. Taher, and E. Zaini (2022). Crystal Engineering Approach in Physicochemical Properties Modifications of Phytochemical. Science and Technology Indonesia, 7(3); 353–371.
McCarthy, C. A., R. J. Ahern, R. Dontireddy, K. B. Ryan, and A. M. Crean (2016). Mesoporous Silica Formulation Strategies for Drug Dissolution Enhancement: A Review. Expert Opinion on Drug Delivery, 13(1); 93–108.
Pote, S. V., K. Bavaskar, and A. Jain (2022). Solubility Enhancement of Poorly Soluble Drug by Using Different Techniques. Research Journal of Pharmaceutical Dosage Forms and Technology, 14(4); 315–323.
Shane, N. L. J., A. H. Chamle, A. Vasantharaju, A. Pai, G. Pai, and M. B. Sathyanarayana (2017). Fabrication and Solid State Characterization of Ticagrelor Co-Crystals with Improved Solubility and Dissolution. International Journal of Pharmaceutical Quality Assurance, 8(1); 1–8.
Shen, S. C., W. K. Ng, L. Chia, Y. C. Dong, and R. B. H. Tan (2010). Stabilized Amorphous State of Ibuprofen by Co-Spray Drying with Mesoporous SBA-15 to Enhance Dissolution Properties. Journal of Pharmaceutical Sciences, 99(4); 1997–2007.
Speybroeck, M. V., V. Barillaro, T. Do, R. Mellaerts, J. Martens, J. V. Humbeeck, and P. Augustijns (2009). Ordered Mesoporous Silica Material SBA-15: A Broad-Spectrum Formulation Platform for Poorly Soluble Drugs. Journal of Pharmaceutical Sciences, 98(8); 2648–2658.
Srivastava, A., M. A. Khan, S. Bedi, and U. Bhandari (2022). A Review on Different Solubility Enhancement Techniques of Ticagrelor. International Journal of Pharmaceutical Investigation, 13(1); 01–06.
Thahir, R., A. W. Wahid, N. La Nafie, and I. Raya (2019). Synthesis of Mesoporous Silica SBA-15 through Surfactant Set-Up and Hydrothermal Process. Rasayan Journal of Chemistry, 12(3); 1117–1126.
Yuliandra, Y., L. Fitriani, R. Kurniawan, F. Yasardi, and E. Zaini (2020). Solid Dispersions of Famotidine: Physicochemical Properties and In Vivo Comparative Study on the Inhibition of Hyperacidity. ChemistrySelect, 5(29); 9218–9225.
Zaini, E., D. Riska, M. D. Oktavia, F. Ismed, and L. Fitriani (2020). Improving Dissolution Rate of Piperine by Multicomponent Crystal Formation with Saccharin. Research Journal of Pharmacy and Technology, 13(4); 1926–1930.
Ambrogi, V., L. Perioli, C. Pagano, F. Marmottini, M. Ricci, A. Sagnella, and C. Rossi (2012). Use of SBA-15 for Furosemide Oral Delivery Enhancement. European Journal of Pharmaceutical Sciences, 46(1–2); 43–48.
Beliatskaya, A. V., I. I. Krasnyuk, I. I. Krasnyuk, O. I. Stepanova, Z. A. Abgaryan, T. P. Kudinova, and I. S. Nesterenko (2019). Study on the Solubility of Ketoprofen From Solid Dispersions with Polyvinylpyrrolidone. Moscow University Chemistry Bulletin, 74(2); 93–99.
Bhairav, B. A., J. K. Bachhav, and R. B. Saudagar (2016). Review on Solubility Enhancement Techniques. Asian Journal of Pharmaceutical Research, 6(3); 175.
Bhalani, D. V., B. Nutan, A. Kumar, and A. K. S. Chandel (2022). Bioavailability Enhancement Techniques for Poorly Aqueous Soluble Drugs and Therapeutics. Biomedicines, 10(9); 2055.
Bolla, G., B. Sarma, and A. K. Nangia (2022). Crystal Engineering of Pharmaceutical Cocrystals in the Discovery and Development of Improved Drugs. Chemical Reviews, 122(13); 11514–11603.
Chaturvedi, K., H. S. Shah, K. Nahar, R. Dave, and K. R. Morris (2020). Contribution of Crystal Lattice Energy on the Dissolution Behavior of Eutectic Solid Dispersions. ACS Omega, 5(17); 9690–9701.
Chen, X., I. Partheniadis, I. Nikolakakis, and H. Al-Obaidi (2020). Solubility Improvement of Progesterone From Solid Dispersions Prepared by Solvent Evaporation and Co-Milling. Polymers, 12(4); 854.
Febriyenti, P. Indra, E. Zaini, F. Ismed, and H. Lucida (2020). Preparation and Characterization of Quercetin-Polyvinylpyrrolidone K-30 Spray Dried Solid Dispersion. Journal of Pharmacy & Pharmacognosy Research, 8(2); 127–134.
Fitriani, L., H. Azizah, U. Hasanah, and E. Zaini (2023). Enhancement of Curcumin Solubility and Dissolution by Adsorption in Mesoporous SBA-15. International Journal of Applied Pharmaceutics, 15(Special Issue 1); 61–67.
Hasanah, U., S. Wikarsa, and S. Asyarie (2021). Various Chloride Salt Addition in Mesoporous Material (SBA-15) Synthesis and Potential as Carrier for Dissolution Enhancer. In Proceedings of the 2nd International Conference on Contemporary Science and Clinical Pharmacy 2021 (ICCSCP 2021), volume 40. pages 343–349.
Hong, S., S. Shen, D. C. T. Tan, W. K. Ng, X. Liu, L. S. O. Chia, and R. Gokhale (2016). High Drug Load, Stable, Manufacturable and Bioavailable Fenofibrate Formulations in Mesoporous Silica: A Comparison of Spray Drying Versus Solvent Impregnation Methods. Drug Delivery, 23(1); 316–327.
Juneja, S., K. Gupta, and S. Kaushal (2013). Ticagrelor: An Emerging Oral Antiplatelet Agent. Journal of Pharmacology and Pharmacotherapeutics, 4(1); 78–80.
Kim, S. J., H. K. Lee, Y. G. Na, K. H. Bang, H. J. Lee, M. Wang, and C. W. Cho (2019). A Novel Composition of Ticagrelor by Solid Dispersion Technique for Increasing Solubility and Intestinal Permeability. International Journal of Pharmaceutics, 555; 11–18.
Letchmanan, K., S.-C. Shen, W. K. Ng, and R. B. H. Tan (2017). Dissolution and Physicochemical Stability Enhancement of Artemisinin and Mefloquine Co-Formulation via Nano-Confinement with Mesoporous SBA-15. Colloids and Surfaces B: Biointerfaces, 155; 560–568.
Lutfiyah, D. S., L. Fitriani, M. Taher, and E. Zaini (2022). Crystal Engineering Approach in Physicochemical Properties Modifications of Phytochemical. Science and Technology Indonesia, 7(3); 353–371.
McCarthy, C. A., R. J. Ahern, R. Dontireddy, K. B. Ryan, and A. M. Crean (2016). Mesoporous Silica Formulation Strategies for Drug Dissolution Enhancement: A Review. Expert Opinion on Drug Delivery, 13(1); 93–108.
Pote, S. V., K. Bavaskar, and A. Jain (2022). Solubility Enhancement of Poorly Soluble Drug by Using Different Techniques. Research Journal of Pharmaceutical Dosage Forms and Technology, 14(4); 315–323.
Shane, N. L. J., A. H. Chamle, A. Vasantharaju, A. Pai, G. Pai, and M. B. Sathyanarayana (2017). Fabrication and Solid State Characterization of Ticagrelor Co-Crystals with Improved Solubility and Dissolution. International Journal of Pharmaceutical Quality Assurance, 8(1); 1–8.
Shen, S. C., W. K. Ng, L. Chia, Y. C. Dong, and R. B. H. Tan (2010). Stabilized Amorphous State of Ibuprofen by Co-Spray Drying with Mesoporous SBA-15 to Enhance Dissolution Properties. Journal of Pharmaceutical Sciences, 99(4); 1997–2007.
Speybroeck, M. V., V. Barillaro, T. Do, R. Mellaerts, J. Martens, J. V. Humbeeck, and P. Augustijns (2009). Ordered Mesoporous Silica Material SBA-15: A Broad-Spectrum Formulation Platform for Poorly Soluble Drugs. Journal of Pharmaceutical Sciences, 98(8); 2648–2658.
Srivastava, A., M. A. Khan, S. Bedi, and U. Bhandari (2022). A Review on Different Solubility Enhancement Techniques of Ticagrelor. International Journal of Pharmaceutical Investigation, 13(1); 01–06.
Thahir, R., A. W. Wahid, N. La Nafie, and I. Raya (2019). Synthesis of Mesoporous Silica SBA-15 through Surfactant Set-Up and Hydrothermal Process. Rasayan Journal of Chemistry, 12(3); 1117–1126.
Yuliandra, Y., L. Fitriani, R. Kurniawan, F. Yasardi, and E. Zaini (2020). Solid Dispersions of Famotidine: Physicochemical Properties and In Vivo Comparative Study on the Inhibition of Hyperacidity. ChemistrySelect, 5(29); 9218–9225.
Zaini, E., D. Riska, M. D. Oktavia, F. Ismed, and L. Fitriani (2020). Improving Dissolution Rate of Piperine by Multicomponent Crystal Formation with Saccharin. Research Journal of Pharmacy and Technology, 13(4); 1926–1930.
Authors
Hasanah, U., Rizky, F. ., Mohd Amin, M. C. I. ., & Zaini, E. (2025). Ticagrelor Solubility and Dissolution Rate Enhancement Using Mesoporous Silica SBA-15 . Science and Technology Indonesia, 10(2), 598–604. https://doi.org/10.26554/sti.2025.10.2.598-604
This work is licensed under a Creative Commons Attribution 4.0 International License.