Construction and characterization of a novel Tenofovir-loaded PEGylated niosome conjugated with TAT peptide for evaluation of its cytotoxicity and anti-HIV effects

In recent years, nanocarriers have become potent drug delivery system candidates, especially in anti-HIV therapies. Meanwhile, using cell-penetrating peptides such as TAT for improvement of cellular transportation has been widely noticed. In the current study, a novel PEGylated niosomal formulation (PEG-NI) loaded with an anti-HIV drug (Tenofovir) has been prepared by using thin-film hydration method based on cholesterol and Span 60 surfactant. Then, the TAT peptide was incorporated into optimized PEGylated niosome. Further morphological and in vitro studies were performed by TAT conjugated (TAT-NI1) and PEGylated niosomes. The average size, polydispersity index and encapsulation efficiency of Tenofovir-loaded TAT-NI1 were 208 ± 9.004 nm, 0.39 ± 0.008 and 75 ± 2.516%, respectively. The cytotoxicity effects of TAT-NI1 and PEG-NI niosomes were analyzed by MTT assay in comparison with Tenofovir. The IC50 of PEG-NI, empty PEG-NI, TAT-NI1, free Tenofovir and TAT peptide were 65.41, 37.04, 41.02, 43.07, and 37.12, respectively. Furthermore, the inhibitory effects of samples against the HIV infected HeLa cells were evaluated. The results displayed a higher cytotoxicity, lower anti-Scr HIV effect and improved Tenofovir release profile for TAT-NI1 in comparison with PEG-NI. Overall, this study revealed that PEGylation is a superior alternative rather than TAT conjugation in anti-HIV drug delivery systems.