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.
Pinto
Luciana M A
LM
Departamento de Bioquímica, Instituto de Biologia, Universidade Estadual de Campinas (UNICAMP), Campinas, São Paulo, Brazil.
Pereira
Renata
R
de Paula
Eneida
E
de Nucci
Gilberto
G
Santana
Maria Helena A
MH
Donato
José L
JL
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