Toxicity evaluation of nanocarriers for the oral delivery of macromolecular drugs.
Oral administration is the most commonly used and accepted route for drug administration. However, two of the main concerns are the poor intestinal epithelium permeability and rapid degradation, which limit absorption of drugs. In this context, nanocarriers have shown great potential for oral drug delivery. Nevertheless, special importance should be given to the possible toxic effect of these nanocarriers, such as their bioaccumulation in different tissues of the body, as well as, the different physicochemical parameters influencing their properties and so their potential toxic effect. This review describes first some aspects related to the behavior of nanosystems within the gastrointestinal tract and then some aspects of nanotoxicology and its evaluation, including the most popular techniques and approaches used for in vitro and in vivo toxicity studies. It also reviews the physicochemical characteristics of polymeric nanoparticles that may influence the development of toxicological effects, and finally it summarizes the toxicity results that have been published regarding polymeric nanocarriers.
Department of Pharmacy and Pharmaceutical Technology, University of Navarra, Irunlarrea 1, 31008 Pamplona, Spain. Electronic address: pojeroje@alumni.unav.es.
P
P
Ojer
Department of Pharmacology and Toxicology, University of Navarra, Irunlarrea 1, 31008 Pamplona, Spain. Electronic address: tiglesias@alumni.unav.es.
T
T
Iglesias
Department of Pharmacology and Toxicology, University of Navarra, Irunlarrea 1, 31008 Pamplona, Spain. Electronic address: amazqueta@unav.es.
A
A
Azqueta
Department of Pharmacy and Pharmaceutical Technology, University of Navarra, Irunlarrea 1, 31008 Pamplona, Spain. Electronic address: jmirache@unav.es.
J M
JM
Irache
Department of Pharmacology and Toxicology, University of Navarra, Irunlarrea 1, 31008 Pamplona, Spain. Electronic address: acerain@unav.es.
A
A
López de Cerain
D000284:Administration, Oral; D000818:Animals; D004337:Drug Carriers / Q000737:chemistry / Q000633:toxicity*; D016503:Drug Delivery Systems; D041981:Gastrointestinal Tract / Q000378:metabolism; D006801:Humans; D046911:Macromolecular Substances / Q000008:administration & dosage / Q000493:pharmacokinetics; D053758:Nanoparticles; D011108:Polymers / Q000737:chemistry / Q000633:toxicity; D018675:Toxicity Tests / Q000379:methods
D004337:Drug Carriers; D046911:Macromolecular Substances; D011108:Polymers
Gastrointestinal tract; In vitro toxicity; In vivo toxicity; Oral administration; Polymeric nanoparticles