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. Author manuscript; available in PMC: 2021 Nov 10.
Published in final edited form as: J Control Release. 2020 Jul 22;327:100–116. doi: 10.1016/j.jconrel.2020.07.034

Table 3.

Some strategies of bile acid-based oral drug administration

Strategies APIs Bile acids (or derivatives) Efficacy References
Prodrug S1037 3-Diazirine-Derivatives of bile acid Increasing uptake, inhibited by taurocholate [113]
Prodrug acyclovir chenodeoxycholate 198% drug recovery [114]
Prodrug steroidal pyrazoles glycodeoxycholic acid Higher uptake with monoanionic form [115]
Prodrug gabapentin chenodeoxycholic acid Higher uptake with single charge [117]
Prodrug Asp-β-benzyl ester cholic acid Inhibition of taurocholate uptake [119]
Prodrug cytarabine ursodeoxycholic acid Relative bioavailability 209% [120]
Prodrug camptothecin deoxycholic acid 65.48% uptake inhibition by taurocholate in cell spheroids [121]
Prodrug LWMH deoxycholic acid ASBT-colocalization [92]
Electrostatic trospium chloride Glycochenodeoxycholate, taurodeoxycholate Enhanced permeation in Caco-2 [123]
Electrostatic ceftriaxone cholyethyendiaine Relative bioavailability 1300% [124]
Electrostatic LWMH deoxycholylethylamine Relative bioavailability 2500% [125]
Electrostatic EGFR2R-lytic hybrid peptide taurodeoxycholate 64% tumor volume [126]
Prodrug/Electrostatic LHT7 tetrameric deoxycholic acid/deoxycholylethylamine Relative bioavailability 916% [127]
Electrostatic ibandronate Nα-deoxycholyl-L-lysyl-methylester Relative bioavailability 430% [164]
Liposomes salmon calcitonin taurodeoxycholate Relative bioavailability 710% [165]
Liposomes insulin deoxycholic acid Relative bioavailability 143% [142]
Liposomes Exendin-4 glycocholic acid Bioavailability 19.5% to s.c. injection [143]
Bilosomes haemagglutinin antigen deoxycholic acid Higher sIgA titer [146]
Bilosomes hepatitis B surface antigen sodium deoxycholate Higher sIgA titer [147]
Bilosomes diphtheria toxoid sodium deoxycholate Higher sIgA titer [148]
Bilosomes fenofibrate sodium deoxycholate Relative bioavailability 513% [149]
SaNPs felodipine sodium taurocholate Relative bioavailability 160% [151]
SaNPs vitamin K glycocholic acid Higher drug stability/solubility [155]
SaNPs heparin-docetaxel taurocholic acid Relative bioavailability 132% [152]
SaNPs quantum Dots deoxycholic acid Jejunum/ileum accumulation [153]
SaNPs silybin sodium cholate Relative bioavailability 252% [156]
Nanoparticles rhodamine B deoxycholic acid Relative bioavailability 181% [158]