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Nanosuspensions for the formulation of aphidicolin to improve drug targeting effects against leishmania infected macrophages.

Abstract：

:A series of labdans and their derivatives have been identified as novel potential antileishmanial drugs using an in vitro test system against extracellular promastigotes and intracellular amastigotes of Leishmania donovani in murine macrophages (Kayser, O., Kiderlen, A.F., 1998. In vitro activity of leishmanicidal labdanes and related compounds. Proceedings of the Ninth International Congress of Parasitology, Monduzi Editore, Bologna, 925-929). Of these compounds, aphidicolin, a tetradecanhydro-3,9-dihydroxy-4,11b-dimethyl-8, 11a-methano-11aH-cyclo-hepta[a]naphthalin-4,9-dimethanol+ ++ (Fig. 1), was shown to be highly active at concentrations in the microgram range (EC(50) = 0.16 microg/ml). To improve drug targeting effects aphidicolin was formulated as nanosuspension and retested for its enhanced activity (EC(50) = 0.003 microg/ml).

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Kayser O

doi

10.1016/s0378-5173(99)00434-2

keywords:

subject

Has Abstract

pub_date

2000-03-10 00:00:00

pages

253-6

issue

2

eissn

0378-5173

issn

1873-3476

pii

S0378517399004342

journal_volume

196

pub_type

杂志文章

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