Fig. 2: Nanoformulation of TFV ProTides.

Nanoformulations were synthesized by high-pressure homogenization using poloxamer 407 (P407) as the excipient for NM1TFV/NM2TFV, or P407 and PEG 3350 as excipients for NTAF. a Formulation stability at 25 °C (up to 110 days) was measured by particle hydrodynamic diameter (size), polydispersity index (PDI), and zeta potential as determined by dynamic light scattering (DLS). Data were independently reproduced three times. b Cell viability was assessed in MDM by MTT assay 8 h after NM1TFV, NM2TFV, or TAF treatment over a range of concentrations (1–200 µM). Results were normalized to untreated control cells. All results are shown as the mean ± SEM of four replicates. c IC₅₀ of M1TFV, M2TFV, and their nanoformulations in MDM was investigated at a range of concentrations (0.00005–5,000 nM) and determined by HIV-1 reverse transcriptase (RT) activity after viral challenge with HIV-1_ADA at an MOI of 0.1. Data were normalized and expressed as a percentage of HIV-1 infected vehicle control ± SEM; n = 4 biological replicates. Experiments b, c were repeated independently two times with equivalent results.