Skip to main content
. 2021 Jul 20;13(7):1103. doi: 10.3390/pharmaceutics13071103

Table 5.

Polymeric nanoparticles with P-gp inhibitory effects.

Drug
(P-gp Substrate)		 Polymer Major Outcome Reference
PTX Poly(methyl vinyl ether-co-maleic anhydride), PEGs
  • -

    Ex vivo permeability studies: increases in Papp (1.8-fold for uncoated and 3.3–7.3-fold for PEG-coated NPs).

  • -

    In vivo pharmacokinetic study in rats: increases in absolute oral bioavailability (1.7–7.7-fold) compared with uncoated NPs.

 [188]
Tacrolimus CD-PVM/MA amphiphilic copolymer
  • -

    In vivo pharmacokinetic study in rats: increase in bioavailability (9.51-fold) and Cmax (11.54-fold) compared with drug solution.

 [104]
Rapamycin PLGA
  • -

    Everted gut sac: NPs increased permeability 5-fold after co-encapsulated piperine.

  • -

    In vivo pharmacokinetic study in rats: increases in bioavailability (3.5 and 4.8-fold for NPs without and with piperine co-encapsulation, respectively) compared with drug suspension.

 [189]
Rapamycin TPGS, lecithin, zein
  • -

    Caco-2 cell: increase cellular uptake.

  • -

    Caco-2 cell monolayers: increase in Papp (1.39-fold) and decrease in ER (from 1.47 to 1.02).

  • -

    SPIP: increases in Ka and Peff in all segments of rat intestine.

  • -

    In vivo pharmacokinetic study in rats: increases in bioavailability (2.64-fold) and Cmax (2.04-fold) compared with drug solution.

 [190]
Epirubicin PLGA, PEG, mannosamine
  • -

    Caco-2 cell: increases in cellular uptake and Papp (2.45-fold for EPI-PNPs and 3.17-fold for EPI-MNPs) compared with drug solution.

  • -

    SPIP: increases in Papp (5.23-fold for EPI-PNPs and 5.93-fold for EPI-MNPs) compared with drug solution.

  • -

    In vivo pharmacokinetic study in rats: increases in bioavailability (4.7-fold for EPI-PNPs and 5.57-fold for EPI-MNPs) compared with drug solution.

  • -

    In vivo antitumor: comparable tumor suppression effect among intravenous epirubicin and two oral NPs.

 [191]
Etoposide PLGA
  • -

    In vivo pharmacokinetic study in rats: etoposide–quercetin co-loaded NPs increased bioavailability 2.4 and 3.84-fold compared with etoposide-loaded NPs and Etosid®, respectively.

 [192]
Doxorubicin Enoxaparin sodium, PLGA
  • -

    SPIP: increases in Ka and Papp compared with drug solution.

  • -

    Caco-2 cells: increase in drug uptake.

  • -

    In vivo pharmacokinetic study in rats: increases in Cmax (5.23-fold), bioavailability (3.63-fold), and t1/2 (2.47-fold) compared with drug solution.

 [193]
Gemcitabine TMC-CSKSSDYQC peptide conjugates
  • -

    Ex vivo permeation: increases in Papp (1.92 and 4.44-fold) compared with TMC-NPs and drug solution, respectively.

  • -

    In vivo pharmacokinetic study in rats: increases in absolute bioavailability (60.14%) compared with TMC-NPs (54.03%) and drug solution (9.86%).

  • -

    In vivo antitumor efficacy: decreases in tumor growth rate (5.1 and 3.3-fold) compared with non-treated and drug solution groups.

 [46]
Docetaxel PLGA, PEI-FA, PEI-BO
  • -

    Everted gut sac: increase in Papp (6-fold) compared with drug solution.

  • -

    Caco-2 cells: increase in drug uptake.

  • -

    In vivo pharmacokinetic study in rats: increases in bioavailability (6.8, 4.65, and 2.78-fold for FA/BO-PLGA-NPs, BO-PLGA-NPs, and PLGA-NPs, respectively) compared drug solution.

 [195]

PLGA: polyglycolic acid copolymers, CD-PVM/MA: poly(methyl vinyl ether-co-maleic anhydride)-graft-hydroxypropyl-β-cyclodextrin amphiphilic copolymer, TMC: trimethyl chitosan, PEI polyethylenimine, FA: folic acid, BO: borneol.