A Review on Different Solubility Enhancement Techniques of Ticagrelor

  • Abhishek Srivastava Formulation Research and Development-Orals, Sun Pharmaceutical Industries Ltd., Gurugram, Haryana, INDIA.
  • Mohammad Ahmad Khan Department of Pharmacology, School of Pharmaceutical Education and Research Jamia Hamdard, New Delhi, INDIA
  • Simrata Bedi Formulation Research and Development-Orals, Sun Pharmaceutical Industries Ltd., Gurugram, Haryana, INDIA
  • Uma Bhandari Department of Pharmacology, School of Pharmaceutical Education and Research Jamia Hamdard, New Delhi, INDIA.
Keywords: Ticagrelor, Bioavailability, Antiplatelet drug, Solubility enhancement, P2Y12 receptor, BCS classification

Abstract

Ticagrelor is a BCS class IV drug that inhibits platelet action by reversibly binding to the P2Y12 receptor. One of the major challenges faced by the class IV (low solubility, low permeability) drug is the lower dissolution rate leading to low bioavailability. The bioavailability of the marketed formulation of ticagrelor is approximately 36%. Researchers have come up with various techniques to improve the BCS class II and IV drug formulations as an integral part of the development of the pharmaceutical sciences. An increase in solubility can be achieved by various methods such as Salt formation, Complexation, Micronization, Solid Dispersion, altering the pH, Co-solvency, co-crystals, polymeric micelles, etc. A highly efficacious technique is converting a crystalline drug to its amorphous form. An extensive literature search was conducted using various databases like science direct, Taylor and Francis, Springer to extract relevant articles. Keywords like “Ticagrelor”, “low permeability”, “P2Y12 receptor inhibitor” were used for the literature search. Relevant articles were screened and referred for further study. This article discusses the techniques employed to increase the solubility of ticagrelor, thus highlighting the research conducted and reported. The increase in bioavailability of ticagrelor could be seen when formulated as nanoparticles, co-crystals, ticagrelor loaded self-micro emulsifying and nano emulsifying drug delivery system, solid dispersion, etc. the conversion of the crystalline drug into amorphous drug is a highly recommended approach to increase the solubility of ticagrelor which can be seen in cases of co-crystals and solid dispersion formulation.

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Structure of Ticagrelor.
Published
2022-12-16
How to Cite
1.
Srivastava A, Khan MA, Bedi S, Bhandari U. A Review on Different Solubility Enhancement Techniques of Ticagrelor. ijpi [Internet]. 16Dec.2022 [cited 27Jan.2023];13(1):1-. Available from: https://jpionline.org/index.php/ijpi/article/view/1574