Current study aimed to build a dendrimer for tuberculosis treatment that was loaded with pyrazinamide. The medication pyrazinamide was loaded onto a PEGylated poly(propylene-imine) dendrimer. When it comes to tailored drug delivery, dendrimers are highly suitable. Investigations into improving the drug loading capacity are being conducted on the free dendrimer, and the synthesized pyrazinamide-loaded dendrimer. According to multiple studies, the core Ethylene Diamine (EDA)-PPI dendrimers of the ethylene diamine initiator can be effectively modified by PEGylation. This effort increases therapeutic value and minimizes changes in plasma concentration by carrying out drug transportation at a controlled rate. The therapeutic intervention for tuberculosis patients is enhanced by this feature. A pyrazinamide drug-loaded dendrimer was prepared in separate batches with varying concentrations; the optimal formulation was chosen and administered to a rabbit, with the plasma concentration compared to that of the pure drug. Various pharmacokinetic parameters were calculated and the optimized formulation showed excellence in the pharmacokinetic parameters. © 2024 Elsevier B.V., All rights reserved.