.png){kind=icon}
.png){kind=icon}
Return
Preparation, Characterization and in vitro Pharmacological Evaluation of PLGA-Encapsulated Tofacitinib Nanoparticulate Drug Delivery Systems for the Treatment of Rheumatoid Arthritis
.png){kind=icon}
PRE
AI
W
W
L
S
S
Z
M
W
DOI：10.1142/S1793292026500724.png)
.png){kind=icon}
Original request for help.png){kind=icon}
Share.png){kind=icon}
Save
Abstract
En 中文
Tofacitinib (Tof), a JAK3 inhibitor, is clinically utilized for the treatment of moderate to severe rheumatoid arthritis (RA). However, long-term oral administration of Tof can lead to serious systemic toxicity and adverse effects. To mitigate its toxicity, this study prepared drug-loaded nanoparticles (NPs), PLGA@Tof, utilizing poly (lactic-co-glycolic acid) PLGA as the matrix. These NPs exhibited a particle size of 220nm, a zeta potential of -13.4mV, drug loading and encapsulation efficiency were 4.12% and 40.57%, and a smooth spherical morphology. In vitro studies demonstrated that these NPs achieved sustained release of Tof without inducing hemolytic effects; less than 50% Tof was released within 24h under pH 5.0 and pH 7.4 conditions. Cellular experiments revealed that the uptake rates of NPs at 1h, 2h, 4h and 8h in RAW264.7 cells were significantly higher than that of the free drug under inflammatory conditions. After 8 h of treatment with PLGA@Tof on inflammatory RAW264.7 cells, the intracellular reactive oxygen species (ROS) level was significantly lower compared to the free Tof treatment group, while the levels of TNF-alpha, IL-1 beta and IL-6 were also significantly reduced in the PLGA@Tof treatment group. These findings suggest that PLGA@Tof has the potential to be developed into a long-acting nanotherapeutic agent for systemic or localized injection in the treatment of RA.
Keywords:
Tofacitinib
PLGA
NPs
Journal
IF:
1.1
Papers:
239
Citations:
1.7K
Organization
Cited Papers