Key result
Chitosan-based ticagrelor nanoparticles demonstrate prolonged in vitro release across acidic and neutral mediums.
Why the study?
Ticagrelor is a BCS class IV drug with low oral bioavailability of about 36%, prompting the development of a controlled release mucoadhesive nanoparticle formulation to enhance its bioavailability.
Does a chitosan-based nanoparticle formulation of ticagrelor improve its in vitro solubility and controlled release profile?
Does a chitosan-based nanoparticle formulation of ticagrelor improve its in vitro solubility and controlled release profile?
Chitosan-based nanoparticles can effectively encapsulate ticagrelor to provide controlled release and potentially enhance its oral bioavailability.
Supports preclinical ticagrelor nanoparticle development; leaves open human bioavailability or outcome benefits.
The aim of this contemporary work was to formulate a controlled release mucoadhesive nanoparticle formulation for enhancing the oral bioavailability of Ticagrelor (TG), a BCS class IV drug, having low oral bioavailability of about 36%. The nanoparticles can act as efficient carriers for hydrophobic drugs, due to having high surface area and hence can improve their aqueous solubility due to their hydrophilic nature. The nanoparticles (NPs) of TG were formulated using chitosan (CH) as polymer and sodium tripolyphosphate (TPP) as cross-linker, by ionic gelation technique with varying concentrations of polymer with respect to TG and TPP. Characterization of prepared nanoparticles was carried out to assess zeta potential, size, shape, entrapment efficiency (EE) and loading capacity (LC), using zeta sizer, surface morphology and chemical compatibility analysis. Drug release was observed using UV-Spectrophotometer. By increasing concentration of CH the desired size of particles (106.9 nm), zeta potential (22.6 mv) and poly dispersity index (0.364) was achieved. In vitro profiles showed a controlled and prolonged release of TG in both lower pH-1.2 and neutral pH-7.4 mediums, with effective protection of entrapped TG in simulated gastric conditions. X-ray diffraction patterns (XRD) showed the crystalline nature of formed NPs. Hence, this effort showed that hydrophobic drugs can be effectively encapsulated in nanoparticulate systems to enhance their solubility and stability, ultimately improving their bioavailability and effectiveness with better patient compliance by reducing dosing frequencies as well.
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Shahid et al. (2022) studied this question. Chitosan-based controlled release nanoparticles for ticagrelor was evaluated on Particle size, zeta potential, poly dispersity index, and in vitro drug release. Chitosan-based nanoparticles of ticagrelor achieved a particle size of 106.9 nm and zeta potential of 22.6 mV, showing controlled and prolonged in vitro release in both acidic and neutral mediums.
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