Synthesis and evaluation of chitosan based controlled release nanoparticles for the delivery of ticagrelor

Designed Monomers and Polymers

Qurat-ul-ain Shoaib¹  Nadia Shamshad Malik²  Rizwana Kausar³  Ayesha Rashid⁴  Muhammad Zaman⁵  Nariman Shahid⁶  Alia Erum⁶  Umaira Rehman⁶  Ume Ruqia Tulain⁶ 

[1] Akhtar Saeed College of Pharmaceutical Sciences;Capital University of Science and Technology;ILM College of Pharmaceutical Sciences;The Women University Multan;University of Central Punjab;University of Sargodha;

关键词: nanoparticles;    chitosan;    ticagrelor;    hydrophobic;    hydrophilic;    ionic gelation;    bioavailability;   

DOI  :  10.1080/15685551.2022.2054117

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown