Key result
A novel pH-sensitive nanocomposite hydrogel formulation of Ticagrelor demonstrated controlled drug release and enhanced in vivo bioavailability compared to pure Ticagrelor.
Why the study?
Ticagrelor is used to treat patients with acute coronary syndrome, but its inadequate oral bioavailability due to poor solubility and low permeability limits its effectiveness.
Does a pH-sensitive nanocomposite hydrogel formulation of ticagrelor improve oral bioavailability compared to pure ticagrelor?
Does a pH-sensitive nanocomposite hydrogel formulation of ticagrelor improve oral bioavailability compared to pure ticagrelor?
A novel pH-responsive nanocomposite hydrogel formulation of ticagrelor significantly enhances its oral bioavailability compared to pure ticagrelor in vivo.
Answers are grounded in this paper and cite their sources.
Could improve ticagrelor adherence via controlled release; warrants larger outcome trials before clinical adoption.
BACKGROUND: Ticagrelor (TG), an antiplatelet drug is employed to treat patients with acute coronary syndrome, but its inadequate oral bioavailability due to poor solubility and low permeability restricts its effectiveness. PURPOSE: This contemporary work was aimed to design a novel pH-sensitive nanocomposite hydrogel (NCH) formulation incorporating thiolated chitosan (TCH) based nanoparticles (NPs) of Ticagrelor (TG), to enhance its oral bioavailability for effectively inhibiting platelet aggregation. METHODS: NCHs were prepared by free radical polymerization technique, using variable concentrations of chitosan (CH) as biodegradable polymer, acrylic acid (AA) as a monomer, N,N-methylene bisacrylamide (MBAA) as cross-linker, and potassium persulphate (KPS) as initiator. RESULTS: The optimum hydrogel formulation was selected for fabricating NCHs, considering porosity, sol-gel fraction, swelling studies, drug loading capacity, and TG's in vitro release as determining factors. Outcomes of the studies have shown that the extent of hydrogel swelling and drug release was comparatively greater at higher pH (7.4). Moreover, an amplifying trend was observed for drug loading and hydrogel swelling by increasing AA content, while it declined by increasing MBAA. The NCHs were evaluated by various physicochemical techniques and the selected formulation was subjected to in vivo bioavailability studies, confirming enhancement of bioavailability as indicated by prolonged half-life and multifold increase in area under the curve (AUC) as compared to pure TG. CONCLUSION: The results suggest that NCHs demonstrated a pH-responsive, controlled behavior along with enhanced bioavailability. Thus NCHs can be effectively utilized as efficient delivery systems for oral delivery of TG to reduce the risk of myocardial infarction.
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Shahid et al. (2021) studied Acute coronary syndrome. pH-sensitive nanocomposite hydrogel (NCH) formulation of Ticagrelor vs. Pure Ticagrelor was evaluated on Bioavailability (half-life and area under the curve). A novel pH-sensitive nanocomposite hydrogel formulation of Ticagrelor demonstrated controlled drug release and enhanced in vivo bioavailability compared to pure Ticagrelor.
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