Preparation, Controlled Drug Release, and Cell Viability Evaluation of Tenofovir Alafenamide‐Loaded Chitosan Nanoparticles

Abstract

Tenofovir alafenamide (TAF) is used as a hepatitis B virus (HBV) nucleotide reverse transcriptase inhibitor for the treatment of chronic HBV infection. However, the use of TAF suffers from its poor solubility and low bioavailability. Therefore, this study prepared and characterized chitosan nanoparticles (CHS NPs) loaded with TAF. Morphological findings demonstrated that CHS NPs are roughly spherical and homogeneous in shape. Besides, TAF‐loaded CHS NPs displayed the hydrodynamic diameter, zeta potential, and PDI of approximately 340 nm, 48.9 mV, and 0.65, respectively. The encapsulation efficiency is at about 50%, and TAF is released about 93% at the end of 80 hours at pH 7.4. In addition, human hepatocellular carcinoma cells (HepG2) are used for cell viability studies and it is observed that TAF‐loaded CHS NPs has 1.24 times less viable cells as compared to the control. Collectively, TAF‐loaded CHS NPs could be used as an efficient formulation for the treatment of chronic HBV infection.

Fabrication of PEGylated Chitosan Nanoparticles Containing Tenofovir Alafenamide: Synthesis and Characterization

“…However, none of the peaks of TAF appear in the FTIR of the drug-loaded nanoparticles. Similar results were reported by Ulu et al in their study where they proposed that the absence of peaks of TAF suggests that the drug was fully encapsulated within the nanoparticles and no possible interaction of the drug with the components of the nanoparticles was observed, which is why only the peaks of PEGylated chitosan nanoparticles were observed and the peaks of TAF were masked within the nanoparticle structure [ 29 ].…”

“…In the XRD diffractogram, the synthesized polymer had an amorphous nature, and the SEM results were authenticated with XRD where distinct or sharp peaks were observed. Ulu et al developed simple and drug-loaded chitosan nanoparticles and reported that the nanoparticles were roughly spherical in shape and evenly distributed [ 29 ]. The spherical shape of the nanoparticles was due to the tendency of chitosan molecules to fuse with each other with extensive hydrogen bonds in the structure [ 32 ].…”

“…The current results correlate with previous studies where similar results were reported [ 33 , 34 ]. Additionally, Ulu et al also reported that TAF loaded in nanoparticles did not change the morphology of fabricated nanoparticles [ 29 ]. The PEGylation of chitosan and drug-loaded PEGylated nanoparticles was performed, and the results of the FTIR and SEM analyses authenticated the successful synthesis of the polymer and nanoparticles.…”

“…The %EE of TAF loaded in PEGylated chitosan nanoparticles was calculated to be ~90% and ~15%. Ulu et al aimed to develop TAF loaded in simple chitosan nanoparticles and found an EE of approximately 50% [ 29 ]. In another study, Shailender et al found an EE of 48.2%, but they prepared nanoparticles of chitosan loaded with a drug that was similar to that used in the current project [ 35 ].…”

“…The particle size of the drug-loaded PEGylated chitosan was analyzed, and the observed particle size distribution was 219.4 nm with a PDI of 0.369 ( Figure 10 ), which indicated the stability of the nanoparticles ( Figure 11 ). Ulu et al checked the hydrodynamic diameters of drug-unloaded and drug-loaded nanoparticles and found average particle sizes of 200 to 340 nm [ 29 ]. The increase in the average particle size of nanoparticles might be due to drug incorporation between the chitosan network [ 32 ].…”