Fig. 3.

Screening and selection of prodrug candidates for subsequent in vivo studies. (a) Association of bexarotene (BEX) and its prodrugs selected for in vivo studies with human chylomicrons (CM) mean ± SD, n = 5). (b) Half-lives of active drug release from prodrugs of bexarotene (BEX) selected for in vivo studies in rat plasma and fasted state simulated intestinal fluid (FaSSIF) with added esterase activity (20 IU/mL) (mean ± SD, n = 3). BEX was not released from prodrug 13. Full screening of all tested prodrugs including association with natural CM, artificial CM-like emulsion and stability in simulated intestinal fluid and plasma is shown in Supplementary Material (Fig. S1 and S3). *, p < .05.