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

Abstract

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.

Chitosan as a Functional Carrier for the Local Delivery Anti-Inflammatory Systems Containing Scutellariae baicalensis radix Extract

“…It can be used in pharmaceutical excipients or drug carriers [ 4 ], wound-healing materials [ 5 ], and as a scaffold for tissue engineering [ 6 ]. Chitosan is often used in pharmaceutical technology as an ingredient controlling and delaying the release of both synthetic [ 7 , 8 , 9 ] and natural ingredients [ 10 , 11 ].…”

Physicochemical Characterization of Nanobiocomposites

“…Similarly, Shahid et al used XRD to predict the type of interaction within Ticagrelorloaded chitosan-based NPs [46]. Ahmad et al reported the use of XRD to study the crystallite structure within starch-based NPs prepared using mild alkali hydrolysis and an ultra-sonication process.…”

“…The presence of specific chemical groups on the surface of the NBCs will also enable further functionalization by antibodies or by enzymes [41]. These properties greatly affect drug targeting resulting in site-specific drug delivery, for example, in tumor treatment [46].…”

“…Many published data have reported the use of zeta potential in NBCs characterization. The following are examples: cellulose NBCs [86], glucose-conjugated chitosan [48], starch [44], pectin [43], chitosan [7,46], lecithin/chitosan phthalate and Phenyl succinate [79], etc.…”

Design of Chitosan-Coated, Quercetin-Loaded PLGA Nanoparticles for Enhanced PSMA-Specific Activity on LnCap Prostate Cancer Cells

“…It has a strong positive charge in solution, which can increase cancer cell uptake through interactions with the negatively charged cell membrane [ 15 ]. There are also several studies on chitosan nanoparticle systems that demonstrate its ability to release its payload more efficiently at an acidic pH [ 16 , 17 , 18 ], which is relevant for cancer treatment as the tumor microenvironment is reported to lie in the acidic pH range of 5.6–6.8 [ 19 , 20 ].…”