Inhibiting efflux with novel non-ionic surfactants: Rational design based on vitamin E TPGS

Enhanced toxicity and cellular uptake of methotrexate-conjugated nanoparticles in folate receptor-positive cancer cells by decorating with folic acid-conjugated d -α-tocopheryl polyethylene glycol 1000 succinate

“…Additionally, TPGS showed inhibitory activity to P-glycoprotein and potent antitumor activity [6,16]. As a consequence, the concomitant administration of TPGS and anticancer drugs, such as doxorubicin, vinblastine and paclitaxel, provided the synergistic effect on cancer cells [17][18][19]. Nevertheless, a few studies have reported the development of the targeted nanoparticles using FOL-conjugated TPGS (TPGS-FOL) as a targeting moiety [5,20].…”

Nanoemulsion liquid preconcentrates for raloxifene hydrochloride: optimization and in vivo appraisal

“…[35][36][37][38][39][40][41][42] In this novel method, the potential of the elaborated nanocarriers to increase RLX delivery to endocrine target organs (uterus, ovaries and fallopian tubes) was assessed in female Wistar rats weighing 190 ± 20 g. Rats were obtained from Vacsera (Cairo, Egypt). Experiments were performed in accordance with the European Community guidelines for the use of experimental animals and were approved by the institutional ethics committee.…”

“…Some surfactants were categorized as "generally recognized as safe" bioactive excipients due to lymphotropic character (Tween 80) or inhibitory effects on P-gp and metabolic enzymes (Cremophor RH40 and Cremophor EL). 36 In this context, a competitive-type inhibition between Cremophor EL and RLX was recognized at the level of the active site of the UGT enzyme, therefore, Cremophor EL competitively inhibited formation of RLX metabolites. In addition, Tween 80 was reported to inhibit RLX metabolism via a mixed-competition mechanism.…”

The Ameliorated Pharmacokinetics of VP-16 in Wistar Rats: A Possible Role of P-Glycoprotein Inhibition by Pharmaceutical Excipients

“…Consequently, more attention is now being paid to pharmaceutical excipients as efflux pump inhibitors in improving oral drug delivery [3][4][5]. Several pharmaceutical excipients are emerging as different classes of P-gp inhibitors owing to many advantages including that they are safe, not being absorbed from the gut and pharmaceutically acceptable [6,7]. The chemosensitizing effects of such excipients were first proved when combined with the active P-gp substrate molecule [8].…”