Bile acids and bile acid derivatives: use in drug delivery systems and as therapeutic agents.
Bile acids are biological surfactants and signaling molecules with important paracrine and endocrine functions. The enterohepatic organotropism of bile acids turns these facial amphiphiles into attractive drug delivery systems for selective drug targeting to the liver or to enhance drug bioavailability by improving intestinal absorption and metabolic stability.



Bile acid-based amphiphiles, in the form of mixed micelles, bilosomes, drug conjugates and hybrid lipid-polymer nanoparticles are critically discussed as delivery systems for anticancer drugs, antimicrobial agents and therapeutic peptides/proteins, including vaccines. Therapeutic applications of bile acid derivatives as cytotoxic and neuroprotective agents are also addressed.



Bile acids play an important role in modulating cancer therapy and novel derivatives with cytotoxic activity not restricted to the gastrointestinal tract can be expected. Selective toxicity targeting the bacterial membrane remains an attractive area of research for further development of bile acid-based bactericidal agents. On the other hand, the neuroprotective properties of some bile acids offer therapeutic potential in neurodegenerative disorders. Bile acid-based nanoparticles are also a growing research area due to the unique characteristics and tunable properties of these nanosystems. Therefore, multifaceted pharmaceutical and biomedical applications of bile salts are to be expected in the near future.
a Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy , Universidade de Lisboa , Lisbon , Portugal.
Célia
C
Faustino
a Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy , Universidade de Lisboa , Lisbon , Portugal.
Cláudia
C
Serafim
a Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy , Universidade de Lisboa , Lisbon , Portugal.|b Universidade Lusófona de Humanidades e Tecnologias, Escola de Ciências e Tecnologias da Saúde, Research Center for Biosciences and Healht Technologies (CBIOS) , Lisbon , Portugal.
Patrícia
P
Rijo
b Universidade Lusófona de Humanidades e Tecnologias, Escola de Ciências e Tecnologias da Saúde, Research Center for Biosciences and Healht Technologies (CBIOS) , Lisbon , Portugal.|c Biophysics and Biomedical Engineering Institute (IBEB), Faculty of Sciences , Universidade de Lisboa , Lisbon , Portugal.
Catarina Pinto
CP
Reis
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage; D001647:Bile Acids and Salts / Q000008:administration & dosage*; D001682:Biological Availability; D016503:Drug Delivery Systems; D006801:Humans; D007408:Intestinal Absorption; D008055:Lipids / Q000737:chemistry; D008823:Micelles; D053758:Nanoparticles; D014612:Vaccines / Q000008:administration & dosage
D000970:Antineoplastic Agents; D001647:Bile Acids and Salts; D008055:Lipids; D008823:Micelles; D014612:Vaccines
Antimicrobial agents; bile acids; bilosomes; cancer; drug delivery; micelles; nanoparticles; neuroprotection