In vitro evaluation of the effectiveness and cytotoxicity of meglumine antimoniate microspheres produced by spray drying against Leishmania infantum

被引:27
作者
Pujals, G. [2 ]
Sune-Negre, J. M. [2 ]
Perez, P. [2 ]
Garcia, E. [2 ]
Portus, M. [1 ]
Tico, J. R. [2 ]
Minarro, M. [2 ]
Carrio, J. [1 ]
机构
[1] Univ Barcelona, Fac Farm, Parasitol Lab, E-08028 Barcelona, Spain
[2] Univ Barcelona, Fac Farm, Unit Pharmaceut Technol, E-08028 Barcelona, Spain
关键词
D O I
10.1007/s00436-008-0901-z
中图分类号
R38 [医学寄生虫学]; Q [生物科学];
学科分类号
07 ; 0710 ; 09 ; 100103 ;
摘要
The aim of the present study was to evaluate the in vitro activity and cytotoxicity of meglumine antimoniate microspheres produced by spray drying on Leishmania infantum and the effect of the excipients used in them. The parasite strain shows sensitivity to the meglumine antimoniate microspheres prepared. All the antimony IC50 values from encapsulated meglumine antimoniate (3.80+/-0.34 to 9.53+/-0.70 mu g SbV/ml for promastigotes assay) are considerably lower compared to the mean value of IC50 in Glucantime solution (112+/-12.74 mu g SbV/ml). Interesting IC50 values for the excipient chitosan (112.64+/-0.53 mg/ml for promastigotes and 100.81+/-26.45 mg/ml for amastigotes) were obtained (without cytotoxic activity), whereas the rest of the excipients did not show any activity. This new delivery system could offer a new pharmacological tool for the treatment of leishmaniosis that reduces the doses required, lowering toxic side effects because of meglumine antimoniate.
引用
收藏
页码:1243 / 1247
页数:5
相关论文
共 22 条
[1]   Macrophage specific drug delivery in experimental leishmaniasis [J].
Basu, MK ;
Lala, S .
CURRENT MOLECULAR MEDICINE, 2004, 4 (06) :681-689
[2]   Leishmania infantum:: Stage-specific activity of pentavalent antimony related with the assay conditions [J].
Carrió, J ;
de Colmenares, M ;
Riera, C ;
Gállego, M ;
Arboix, M ;
Portús, M .
EXPERIMENTAL PARASITOLOGY, 2000, 95 (03) :209-214
[3]   The antiviral activity of chitosan (review) [J].
Chirkov, SN .
APPLIED BIOCHEMISTRY AND MICROBIOLOGY, 2002, 38 (01) :1-8
[4]   Impact of excipients on the absorption of P-glycoprotein substrates in vitro and in vivo [J].
Cornaire, G ;
Woodley, J ;
Hermann, P ;
Cloarec, A ;
Arellano, U ;
Houin, G .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2004, 278 (01) :119-131
[5]   Oral delivery of meglumine antimoniate-β-cyclodextrin complex for treatment of leishmaniasis [J].
Demicheli, C ;
Ochoa, R ;
da Silva, JBB ;
Falcao, CAB ;
Rossi-Bergmann, B ;
de Melo, AL ;
Sinisterra, RD ;
Frézard, F .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2004, 48 (01) :100-103
[6]   In vitro and in vivo resistance of Leishmania infantum to meglumine antimoniate: A study of 37 strains collected from patients with visceral leishmaniasis [J].
FarautGambarelli, F ;
Piarroux, R ;
Deniau, M ;
Giusiano, B ;
Marty, P ;
Michel, G ;
Faugere, B ;
Dumon, H .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1997, 41 (04) :827-830
[7]   Chitosan as tear substitute: A wetting agent endowed with antimicrobial efficacy [J].
Felt, O ;
Carrel, A ;
Baehni, P ;
Buri, P ;
Gurny, R .
JOURNAL OF OCULAR PHARMACOLOGY AND THERAPEUTICS, 2000, 16 (03) :261-270
[8]   Novel methods for the encapsulation of meglumine antimoniate into liposomes [J].
Frézard, F ;
Michalick, MSM ;
Soares, CF ;
Demicheli, C .
BRAZILIAN JOURNAL OF MEDICAL AND BIOLOGICAL RESEARCH, 2000, 33 (07) :841-846
[9]   Visceral leishmaniasis: current status of control, diagnosis, and treatment, and a proposed research and development agenda [J].
Guerin, PJ ;
Olliaro, P ;
Sundar, S ;
Boelaert, M ;
Croft, SL ;
Desjeux, P ;
Wasunna, MK ;
Bryceson, ADM .
LANCET INFECTIOUS DISEASES, 2002, 2 (08) :494-501
[10]   Novel derivatives of chitosan and their antifungal activities in vitro [J].
Guo, ZY ;
Chen, R ;
Xing, RE ;
Liu, S ;
Yu, HH ;
Wang, PB ;
Li, CP ;
Li, PC .
CARBOHYDRATE RESEARCH, 2006, 341 (03) :351-354