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Anti-filarial activity of novel formulations of albendazole against experimental brugian filariasis

Published online by Cambridge University Press:  02 November 2006

R. L. GAUR ,
S. DIXIT ,
M. K. SAHOO ,
M. KHANNA ,
S. SINGH  and
P. K. MURTHY
R. L. GAUR
Affiliation:
Division of Parasitology, Central Drug Research Institute, Lucknow, 226001, India
S. DIXIT
Affiliation:
Division of Parasitology, Central Drug Research Institute, Lucknow, 226001, India
M. K. SAHOO
Affiliation:
Division of Parasitology, Central Drug Research Institute, Lucknow, 226001, India
M. KHANNA
Affiliation:
Division of Pharmaceutics, Central Drug Research Institute, Lucknow, 226001, India
S. SINGH
Affiliation:
Division of Pharmaceutics, Central Drug Research Institute, Lucknow, 226001, India
P. K. MURTHY
Affiliation:
Division of Parasitology, Central Drug Research Institute, Lucknow, 226001, India
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Abstract

The study was aimed at developing better orally active albendazole (ALB) formulations. Six formulations (ALB-1 to ALB-6) were prepared and tested against Brugia malayi in Mastomys coucha and jird (Meriones unguiculatus) at 200 mg/kg, orally, for 5 consecutive days. The anti-filarial efficacy was assessed against microfilariae (mf), adult worms and female reproductive potential. Three of the 6 ALB formulations showed greatly improved female worm sterilizing potential (ALB-1: 90%; ALB-3: 63%; ALB-4: 77% of untreated control) in B. malayi – M. coucha model. Sterilization efficacy of ALB-1 was also better than that shown by pure-ALB (P<0·001) or its marketed tablet formulation, Zentel (P<0·01), while that of ALB-4 was better than pure-ALB (P<0·05). The activity of ALB-3, pure-ALB and Zentel was, however, comparable. ALB-1 also showed late microfilaricidal activity with a maximum of 78% fall in microfilarial count. In contrast, neither the pure ALB nor Zentel showed any microfilaricidal activity. In the jird – B. malayi model, ALB-1 and ALB-4 showed marginal sterilizing efficacy whereas pure ALB or Zentel were ineffective. In conclusion the anti-filarial efficacy of ALB-1 was found to be superior to pure-ALB or Zentel.

Keywords

albendazoleformulationfilariasisBrugia malayiMeriones unguiculatusMastomys coucha
Type
Research Article
Information
Parasitology , Volume 134 , Issue 4 , April 2007 , pp. 537 - 544
Copyright
© 2006 Cambridge University Press

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References

REFERENCES

Addiss, D. G., Beach, M. J., Streit, T. G., Lutwick, S., Leconte, F. H., Lafontant, J. G., Hightower, A. W. and Lammie, P. J. ( 1997). Randomised placebo-controlled comparison of ivermectin and albendazole alone and in combination for Wuchereria bancrofti microfilaraemia in Haitian children. Lancet 350, 480–484.CrossRefGoogle Scholar
Bartoloni, A., Gulglielmetti, P., Cancrini, G., Gamboa, H., Roselli, M., Nicoletti, A. and Paradisi, F. ( 1993). Comparative efficacy of a single 400 mg dose of albendazole or mebendazole in the treatment of nematode infections in children. Tropical and Geographical Medicine 45, 114–116.Google Scholar
Beach, M. J., Streit, T. G., Addiss, D. G., Prospere, R., Roberts, M. and Lammie, P. J. ( 1999). Assessment of combined ivermectin and albendazole for treatment of intestinal helminth and Wuchereria bancrofti infections in Haitian school children. American Journal of Tropical Medicine and Hygiene 60, 479–486.CrossRefGoogle Scholar
Chatterjee, R. K., Fatma, N., Murthy, P. K., Sinha, P., Kulshreshtha, D. K. and Dhawan, B. N. ( 1992). Macrofilaricidal activity of the stem bark of Streblus asper and its major active constituents. Drug Development and Research 26, 67–78.CrossRefGoogle Scholar
Chen, T. T. ( 1964). Demonstration of macrofilaricidal action of hetrazan, antimony and arsenic preparation in man. Chinese Medical Journal 83, 625–640.Google Scholar
Chiou, W. L. and Riegelman, S. ( 1969). Preparation and dissolution characteristics of several fast-release solid dispersions of griseofulvin. Journal of Pharmacological Sciences 58, 1505–1510.CrossRefGoogle Scholar
Chiou, W. L. and Riegelman, S. ( 1971). Increased dissolution rates of water-insoluble glycosides and steroids via solid dispersions in polyethylene glycol 6000. Journal of Pharmacological Sciences 60, 1569–1571.CrossRefGoogle Scholar
Critchley, J., Addiss, D., Ejere, H., Gamble, C., Garner, P. and Gelband, H. ( 2005). Albendazole for the control and elimination of lymphatic filariasis: systematic review. Tropical Medicine and International Health 10, 818–825.CrossRefGoogle Scholar
Denham, D. A., Liron, D. A. and Brandt, E. ( 1978). The anthelmintic effect of albendazole on Brugia pahangi. Journal of Helminthology 54, 199–200.Google Scholar
Dreyer, G., Coutinho, A., Miranda, D., Noroes, J., Rizzo, J. A., Galdino, E., Rocha, A., Medeiros, Z., Andrade, L. D., Santos, A., Figueredo-Silva, J. and Ottensen, E. A. ( 1995). Treatment of bancroftian filariasis in Recife, Brazil: a two-year comparative study of the efficacy of single treatments with ivermectin or diethylcabamazine. Transaction of Royal Society of Tropical Medicine and Hygiene 89, 98–102.CrossRefGoogle Scholar
Dunyo, S. K., Nkrumah, F. K. and Simonsen, P. ( 1999). A study on the provocative day test effect of ivermectin and albendazole on nocturnal periodic Wuchereria bancrofti microfilaraemia. Transactions of the Royal Society of Tropical Medicine and Hygiene 93, 608–610.CrossRefGoogle Scholar
Dunyo, S. K., Nkrumah, F. K. and Simonsen, P. E. ( 2000). A randomized double blind placebo controlled field trial of ivermectin and albendazole alone and its combination for the treatment of lymphatic filariasis in Ghana. Transactions of the Royal Society of Tropical Medicine and Hygiene 94, 205–211.CrossRefGoogle Scholar
Edeson, J. F. B. and Laing, A. B. G. ( 1959). Studies on filariasis in Malaya. The effect of diethylcarbamazine on Brugia malayi and Brugia pahangi in domestic cats. Annals of Tropical Medicine and Parasitology 53, 394–399.Google Scholar
El Setouhy, M., Reda, M. R., Ramzy, R. M., Ahmed, E. S., Kandil, A. M., Hussain, O., Farid, H. A., Helmy, H. and Weil, G. J. ( 2004). A randomized clinical trial comparing single- and multi-dose combination therapy with diethylcarbamazine and albendazole for treatment of bancroftian filariasis. American Journal of Tropical Medicine and Hygiene 70, 191–196.Google Scholar
Estal, J. L., Alvarez, A. I., Vilaverde, C., Justel, A. and Prieto, I. G. ( 1994). Increased systemic bioavailability of albendazole in patients with brain cysticercosis. Journal of Clinical Pharmacology 32, 28–31.Google Scholar
Evans, D. B., Gelband, H. and Vlassoff, C. ( 1993). Social and economic factor and the control of lymphatic filariasis: a review. Acta Tropica 53, 1–26.CrossRefGoogle Scholar
Gyapong, J. O., Kumaraswami, V., Biswas, G. and Ottesen, E. A. ( 2005). Treatment strategies underpinning the global programme to eliminate lymphatic filariasis. Expert Opinions in Pharmacotherapy 6, 179–200.CrossRefGoogle Scholar
Horton, J. ( 2000). Albendazole: a review of anthelmintic efficacy and safety in human. Parasitology (Suppl.) 121, S113–S132.CrossRefGoogle Scholar
International Filariasis Review Group ( 2004). Albendazole for lymphatic filariasis. Cochrane Database of Systematic Reviews 1, CD003753.CrossRef
Kohri, N., Yamayoshi, Y., Iseki, K., Sato, N., Todo, S. and Miyazaki, K. ( 1998). Effect of gastric pH on the bioavailability of albendazole. Pharmaceutics and Pharmacological Communications 4, 267–270.Google Scholar
Kumaraswami, V., Ottesen, E. A., Vijayasekaran, S., Devi, U., Swaminathan, M., Aziz, M. A., Sharma, G. R., Prabhakar, R. and Tripathi, S. P. ( 1988). Ivermectin for the treatment of Wuchereria bancrofti filariasis. Efficacy and adverse reactions. Journal of the American Association 259, 3150–3153.CrossRefGoogle Scholar
Lammler, G. and Wolf, E. ( 1977). Chemoprophylaktische Wirksamkeit filarizie der Verbindungen bei der Litomosoides carinii-Infektion der Mastomys natalensis. Tropenmedizin und Parasitologie 28, 205–225.Google Scholar
Lange, H., Eggers, R. and Bircher, J. ( 1988). Increased systemic availability of albendazole when taken with a fatty meal. European Journal of Clinical Pharmacology 34, 315–317.CrossRefGoogle Scholar
Malllick, S. ( 2004). The solid-state amorphization of poorly water-soluble drugs. Indian Journal of Pharmacological Sciences 66, 729–734.Google Scholar
Malllick, S., Sahoo, A., and Mitra, S. S. ( 2003). Preparation, physiochemical characterization and drug release studies of albendazole solid dispersions. Bolletino Chimico Farmaceutico 142, 180–186.Google Scholar
Marriner, S. E, Morris, D. L., Dickson, B. and Bogan, J. A. ( 1986). Pharmacokinetics of albendazole in man. European Journal of Clinical Pharmacology 30, 705–708.CrossRefGoogle Scholar
Murthy, P. K., Murthy, P. S. R., Tyagi, K. and Chatterjee, R. K. ( 1997). Fate of implanted infective larvae of Brugia malayi in the peritoneal cavity of Mastomys natalensis and Meriones unguiculatus. Folia Parasitologica 44, 302–304.Google Scholar
Murthy, P. K., Tyagi, K. and Chatterjee, R. K. ( 1992). Brugia malayi in Mastomys natalensis: efficacy of mebendazole in combination with Freund's complete adjuvant. Folia Parasitologica 39, 51–59.Google Scholar
Murthy, P. K., Tyagi, K., Roychowdhury, T. K. and Sen, A. B. ( 1983). Susceptibility of Mastomys natalensis (GRA strain) to a subperiodic strain of human Brugia malayi. Indian Journal of Medical Research 77, 623–630.Google Scholar
Noroes, J., Dreyer, G., Santos, A., Mendes, V. G., Medeiros, Z. and Addiss, D. ( 1997). Assessment of the efficacy of diethylcarbamazine on adult Wuchereria bancrofti in vivo. Transactions of the Royal Society of Tropical Medicine and Hygiene 91, 78–81.CrossRefGoogle Scholar
Ottesen, E. A. ( 1992). Infection and disease in lymphatic filariasis: an immunologic perspective. Parasitology 104, S71–S79.CrossRefGoogle Scholar
Ottesen, E. A., Duke, B. O. L., Karam, M. and Behbehani, K. ( 1997). Strategies and tools for the control and elimination of lymphatic filariasis. Bulletin of the World Health Organization 75, 491–503.Google Scholar
Ottesen, E. A., Ismail, M. M. and Horton, J. ( 1999). The role of albendazole in programmes to eliminate lymphatic filariasis. Parasitology Today 15, 382–386.CrossRefGoogle Scholar
Ottessen, E. A. and Ramachandran, C. P. ( 1995). Lymphatic filarial infection and disease, control strategies. Parasitology Today 11, 129–131.CrossRefGoogle Scholar
Sadanaga, A., Hayashi, Y., Tanaka, H., Nogami, S. and Shirasaka, A. ( 1984). Evaluation of transplantation method of Brugia malayi into the jird, Meriones unguiculatus, for testing macrofilaricides. Japnese Journal of Experimental Medicine 54, 275–277.Google Scholar
Tanaka, H., Takaoka, M., Matsuda, H. and Hayashi, Y. ( 1981). Effect of diethylcarbamazine on microfilariae of Brugia malayi in the jird, Meriones unguiculatus. Japnese Journal of Experimental Medicine 51, 195–196.Google Scholar
Tisch, D. J., Michael, E. and Kazura, J. W. ( 2005). Mass chemotherapy options to control lymphatic filariasis: a systematic review. Lancet Infectious Diseases 5, 514–523.CrossRefGoogle Scholar
Tracy, J. W. and Webster, L. T. Jr. ( 2001). Drugs used in the chemotherapy of helminthiasis. In Goodman and Gilman's The Pharmacological Basis of Therapeutics ( ed. Harman, J. G., Limbird, L. E. and Gilman, A. G.), 10th Edn, pp. 1131–1133. McGraw-Hill, International Edition, New York.
Tripathi, R. P., Tiwari, V. K., Misra-Bhattacharya, S., Tyagi, K., Srivastava, V. M. L. and Murthy, P. K. ( 2003). 7-O-[4-methyl piperazine-1-(2-acetyl)]-2H-1-benzopyran-2-one: a novel antifilarial lead compound. Acta Tropica 87, 215–224.CrossRefGoogle Scholar
Turner, L. H. ( 1959). Studies on filariasis in Malaya: treatment of Wuchereria malayi filariasis with diethylcarbamazine in single daily doses. Transactions of the Royal Society of Tropical Medicine and Hygiene 53, 180–188.Google Scholar
Tyagi, K., Murthy, P. K., Chatterjee, R. K. and Sen, A. B. ( 1986). Chemotherapeutic response of Brugia malayi to antifilarials in Mastomys natalensis. Indian Journal of Parasitology 10, 195–207.Google Scholar
Vanden Bossche, H. ( 1981). A look at the mode of action of some old and new antifilarial compounds. Annales de la Société Belge de Medicine Tropicale 61, 287–296.Google Scholar
Welling, P. G. ( 1977). Influence of food and diet on gastrointenstinal drug absorption: a review. Journal of Pharmacokinetics and Biopharmacy 5, 291–334.CrossRefGoogle Scholar
Wilson, T. ( 1950). Hetrazan in the treatment of filariasis due to Wuchereria malayi. Transactions of the Royal Society of Tropical Medicine and Hygiene 44, 49–66.CrossRefGoogle Scholar