Influence of liposomal local anesthetics on platelet aggregation in vitro.
We assessed the effect of local anesthetics (LA) from different families such as esters (benzocaine), linear aminoamides (lidocaine) and cyclic aminoamides (bupivacaine) on the platelet aggregation induced by ADP. Liposomal formulations of the three LA, prepared with egg phosphatidylcholine:cholesterol alpha-tocopherol, were also tested. The three LA were able to inhibit platelet aggregation induced by ADP, in the following order: bupivacaine > lidocaine > benzocaine. After encapsulation into liposomes the inhibitory effect increased for all anesthetics studied, showing that aggregation tests could be used to assess the toxicity of new drug formulations.
Departamento de Bioquímica, Instituto de Biologia, Universidade Estadual de Campinas (UNICAMP), Campinas, São Paulo, Brazil.
Luciana M A
LM
Pinto
Renata
R
Pereira
Eneida
E
de Paula
Gilberto
G
de Nucci
Maria Helena A
MH
Santana
José L
JL
Donato
D000244:Adenosine Diphosphate / Q000037:antagonists & inhibitors / Q000494:pharmacology; D000779:Anesthetics, Local / Q000494:pharmacology*; D001566:Benzocaine / Q000494:pharmacology; D001792:Blood Platelets / Q000378:metabolism*; D002045:Bupivacaine / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D016503:Drug Delivery Systems; D006801:Humans; D008012:Lidocaine / Q000494:pharmacology; D008081:Liposomes; D010974:Platelet Aggregation / Q000187:drug effects* / Q000502:physiology
D000779:Anesthetics, Local; D008081:Liposomes; D000244:Adenosine Diphosphate; D008012:Lidocaine; D001566:Benzocaine; D002045:Bupivacaine