Design and Characterization of Ticagrelor‐Loaded Chitosan Biopolymer to Improve Chemical and Biological Properties of the Drug

Solubility is characterized as the sum of substance that passes into the solution to form a saturated solution at steady temperature and pressure. Solubility can be framed in terms of the maximum volume or mass of the solute that breaks up in a given volume or mass of a solvent. 2 An increase in solubility can be achieved by various methods such as Salt formation, Complexation, Micronization, 4 Solid Dispersion, altering the pH, co-solvency, co-crystals, polymeric micelles, etc. 5 A highly efficacious technique is the conversion of a crystalline drug to its amorphous form. Amorphous drugs have better solubility than crystalline drugs due to their structure, increased surface area, and better wettability. 6 The amorphous state has better solubility as it has higher entropy, enthalpy, volume, and free energy when compared to its crystalline structure. 7 TICAGRELORTicagrelor is classified as an anti-platelet aggregator, which reversibly binds to the P2Y12 receptor and acts by antagonizing the binding of adenosine phosphate to the P2Y12 receptor resulting in decreased uptake of adenosine. It is a direct-acting and immediate-release drug taken orally. Both the active drug 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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“…The proposed drug delivery system could overcome the issues related to the low solubility of the drug and be safe to use. 50,51…”

Section: Recent Advancements For Solubility Enhancement Of Ticagrelormentioning

confidence: 99%