Pregnancy in the 20th century involves women of many age groups from early teens to the fourth or fifth decade. Modern medicine and in vitro fertilization techniques have increased options for pregnancy and childbirth. Pregnancy is a dynamic state, and medical concerns may involve disorders of the fetus and mother requiring medications and special nutrients. Therefore, different techniques have been developed to evaluate the placental transfer of drugs and nutrients using tissues and cells derived from human placenta. These include (a) isolated tissues and cells to study placental transport, (b) primary and malignant trophoblast cell cultures and (c) biophysical methods for studying placental transport. Also, convenient study models have been developed to evaluate placental transfer of safe drugs in pregnant women. Some of the drugs studied by these techniques and models include (a) anesthetics and pain medications used during delivery, (b) antibiotics and anti-bacterials used to cure infections, (c) drugs abused by pregnant women and (d) nutrients required for proper fetal growth. Placental transfer and exchange mechanisms are complicated processes, and in vitro models reflect only partially the equilibria that exist among mother, placenta and fetus. The perfused cotyledon model is elegant and simple but gives only restricted information. Isolated placental tissues give useful information about the pharmacological effects of drugs. Metabolic studies using human placental models provide information on the metabolism of a drug during placental transfer and accumulation of the drug or its metabolite in the placenta or fetal circulation. Several studies on the transplacental passage of drugs exist but many questions regarding the transfer of drugs between the maternal and fetal circulations and clearance of drugs from fetal circulation have yet to be answered. This article reviews in vitro and in vivo methods for evaluation of transplacental transport of drugs and their current effectiveness to obtain clinically useful data.