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Antimicrobial Agents and Chemotherapy, January 2004, p. 100-103, Vol. 48, No. 1
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.1.100-103.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.

Oral Delivery of Meglumine Antimoniate-ß-Cyclodextrin Complex for Treatment of Leishmaniasis

Departamento de Química, ICEX,¹ Departamento de Parasitology, ICB,³ Departamento de Fisiologia e Biofísica, ICB, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, MG,⁴ Instituto de Biofisica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, 21.949-900 Rio de Janeiro, RJ, Brazil²

Received 8 August 2003/ Returned for modification 23 September 2003/ Accepted 6 October 2003

The need for daily parenteral administration represents one of the most serious limitations in the clinical use of pentavalent antimonials against leishmaniasis. In this work, we investigated the ability of ß-cyclodextrin to enhance the oral absorption of antimony and to promote the oral efficacy of meglumine antimoniate against experimental cutaneous leishmaniasis. The occurrence of interactions between ß-cyclodextrin and meglumine antimoniate was demonstrated through the changes induced in the spin lattice relaxation times of protons in both compounds. When free and complexed meglumine antimoniate were given orally to Swiss mice, plasma antimony levels were found to be about three times higher for the meglumine antimoniate-ß-cyclodextrin complex than for the free drug. Antileishmanial efficacy was evaluated in BALB/c mice experimentally infected with Leishmania amazonensis. Animals treated daily with the complex (32 mg of Sb/kg of body weight) by the oral route developed significantly smaller lesions than those treated with meglumine antimoniate (120 mg of Sb/kg) and control animals (treated with saline). The effectiveness of the complex given orally was equivalent to that of meglumine antimoniate given intraperitoneally at a twofold-higher antimony dose. The antileishmanial efficacy of the complex was confirmed by the significantly lower parasite load in the lesions of treated animals than in saline-treated controls. This work reports for the first time the effectiveness of an oral formulation for pentavalent antimonials.

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