Amphotericin B eye drops as a lipidic emulsion

Treatment of ocular mycosis is based on painful instillation of Fungizone(R) eye drops. The purpose of the study was to develop and to evaluate an Amphotericin B eye drop (AmB) as a better tolerated lipidic emulsion. A concentrated alkaline solution of AmB was mixed with Intralipid(R) 20%, then neutralized and buffered. The eye drop tolerance and pharmacokinetics were evaluated compared with eye drops in Fungizone(R) aqueous solution. The tolerance of the AmB lipidic emulsion was better than those observed with a magistral preparation of Fungizone(R) eye drops (P < 0.0005). The average corneal concentrations obtained with the Fungizone(R) and emulsion eye drops were 501 +/- 208 and 274 +/- 106 ng/g, respectively (P = 0.039). The average AmB concentrations in the aqueous humour were 490 +/- 180 and 300 +/- 260 ng/ml, respectively, for the Fungizone(R) and emulsion eye drops (NS). The plasmatic concentrations measured, lower than 20 ng/ml, were too weak to be toxic.