MACROPHAGE TARGETING: A STRATEGY FOR LEISHMANIASIS SPECIFIC DELIVERY
Leishmaniasis is a vector-borne zoonotic infection caused by an obligate intra macrophage protozoan parasite â€˜Leishmaniaâ€™. Despite of a number of remedies available, leishmaniasis is still a speedy migrating and deadly infection due to the resistance of the parasite to the drugs as well as their toxicity. Hence, there is a need for targeted drug delivery system for enhancing the systematic effect of antileishmanial drugs. Although the number of antileishmanial drugs in a variety of dosage forms is available, there is an urgency to develop more efficient, cost-effective and safe therapy, which can be achieved by macrophage targeting utilizing passive (phagocytosis), and/or active (receptor mediated) strategies utilizing nano-formulations. Positive considerations of various factors like the enhanced permeation and retention (EPR) effect, size, and charge of nano-formulations can facilitate the passive targeting, and various receptors like lectin receptor, mannose receptor, mannosyl-fucosyl receptor, scavenger receptor, etc on the macrophage surface may play an important role in active drug targeting. Also, monoclonal antibody, interferonâ€™s, tufstin are other agents which have been broadly utilized for targeting.
2. Gour JK, Srivastava A, Kumar V, Bajpai S, Kumar H, Mishra M, et al. Nanomedicine and leishmaniasis: future prospects. Digest J Nanomater Biostructures 2009;4:495-9.
3. Guy RA, Belosevic M. Comparison of receptors required for entry of leishmania major amastigotes into macrophages. Infect Immun 1993;4:1553-8.
4. Rittig MH, Bogdan C. Leishmania-host-cell interaction: complexities and alternative views. Parasitol Today 2000;16:292-7.
5. Braunwald E, Fauci AS, Hauser SL. Harrisonâ€™s manual of medicine, Mcgraw-Hill, New York; 2001.
6. Chatterjee KD. Parasitology and helminthology, Chatterjee medical publishers, Calcutta; 1976
7. Prasad LS. Kala Azar. Indian J Pediatr 1999;66:539-46.
8. Moll H, Flohe S, Rollinghoff M. Dendritic cells in leishmania major-immune mice harbor persistent parasites and mediate an antigen-specific t cell immune response. Eur J Immunol 1995;25:693-9.
9. Shargel L, Yu BC. Applied biopharmaceutics and pharmacokinetics. Appleton and lange. Connecticut; 1993.
10. WHO. Model prescribing information drugs used in parasitic diseases, Geneva World health organization; 1990. p. 14-8.
11. World health organization. TDR news; 1998;34:1-7.
12. Sundar S, More DK, Singh MK, Singh VP, Sharma S, Makharia A, et al. Failure of pentavalent antimony in visceral leishmaniasis in India: report from the center of the indian epidemic. Clin Infect Dis 2000;31:1104â€“7.
13. Sundar S, Chatterjee M. Visceral leishmaniasis-current therapeutic modalities. Indian J Med Res 2006;123:345-52.
14. FreÂ´zard F, Demicheli C, Ribeiro RR. Pentavalent antimonials: New perspectives for old drugs. Molecules 2009;14:2317-6.
15. Mishra J, Saxena A, Singh S. Chemotherapy of leishmaniasis: the past, present and future. Curr Med Chem 2007;14:1153-69.
16. Fre_zard F, Martins PS, Barbosa MCM. New insights into the chemical structure and composition of the pentavalent antimonial drugs, meglumine antimoniate and sodium stibogluconate. J Inorg Biochem 2008;102:656-65.
17. Chapman JR, Hanson WL, Alving CR, Hendricks LD. Antileishmanial activity of liposome-encapsulated meglumine antimonate in the dog. Am J Vet Res 1984;45:1028-30.
18. Bryceson A. Pentamidine-induced diabetes mellitus. East Afr Med J 1968;45:110-7.
19. Berman JD. Human leishmaniasis: clinical, diagnostic, and chemotherapeutic developments in the last 10 y. Clin Infect Dis 1997;24:684-703.
20. Scott JA, Davidson RN, Moody AH. Aminosidine (paromomycin) in the treatment of leishmaniasis imported into the united kingdom. Trans R Soc Trop Med Hyg 1992;86:617-9.
21. Davis AJ, Kedzierski L. Recent advances in antileishmanial drug development. Curr Opin Invest Drugs 2005;6:163-9.
22. Duclos S, Desjardins M. Subversion of a young phagosome: the survival strategies of intracellular pathogens. Cell Microbiol 2000;2:365-77.
23. Gaspar R, PreÂ´at V, Roland M. Nanoparticles of polyisohexyl-cyanoacrylate (pihca) as carriers of primaquine: formulation, physico-chemical characterization, and acute toxicity. Int J Pharm 1991;68:111-9.
24. Gaspar R, Oppredoes F, Preat V. Drug targeting with poly alkyl cyanoacrylate nanoparticles: In-vitro activity of primaquine-loaded nanoparticles against intracellular leishmania donovani. Ann Trop Med Parasitol 1992;86:41-9.
25. Rodrigues JM JR, Croft SL, Fessi H. The activity and ultrastructural localization of primaquine-loaded poly (d,l-lactide) nanoparticles in leishmania donovani infected mice. Trop Med Parasitol 1994;45:223-8.
26. Rodrigues JM JR, Fessi H, Bories C. Primaquine-loaded polylactide nanoparticles: physicochemical study and acute tolerance in mice. Int J Pharm 1995;126:253-60.
27. Shukla AK, Patra S, Dubey VK. Nanospheres are encapsulating anti-leishmanial drugs for their specific macrophage targeting, reduced toxicity, and deliberate intracellular release. Vector-Borne Zoonotic Diseases 2012;12:11.
28. Croft SL. In-vitro screens in the experimental chemotherapy of leishmaniasis and trypanosomiasis. Parasitol Today 1986;2:64-9.
29. Zhang D, Tan T, Gao L, Zhao W, Wang P. Preparation of azithromycin nanosuspensions by high-pressure homogenization and its physiochemical characterization studies. Drug Dev Ind Pharm 2007;33:569-75.
30. Gaspar R, Preat V, Oppredoes FR, Roland M. Macrophage avtivation by polymeric nanoparticles of polyalkyl-cynoacrylates: activity against intracellular leishmania donovani associated with hydrogen peroxide production. Pharm Res 1992;9:782-7.
31. Fevrier A, Ferreira ME, Fournet A. Acetogenins and other compounds from rollinia emarginate and their antiprotozoal activities. Planta Med 1999;65:47-9.
32. Matsumura Y, Maeda H. "A new concept for macromolecular therapeutics in cancer chemotherapy: mechanism of tumoritropic accumulation of proteins and the antitumor agent smancs". Cancer Res 1986;46:6387â€“92.
33. Khattab MA, Farr SJ, Taylor G, Kellaway IW. The In-vitro characterization and biodistribution of some non-ionic surfactant coated liposomes in the rabbit. J Drug Target 1995;3:39-49.
34. Proulx ME, Desormeaux A, Marquis J. Treatment of visceral leishmaniasis with sterically stabilized liposomes containing camptothecin. Antimicrob Agents Chemother 2001;45:2623-7.
35. Lakshmi V, Pandey K, Kapil A. In-vitro and in-vivo leishmanicidal activity of dysoxylum binectariferum and its fractions against leishmania donovani. Phytomedicine 2007;14:36-42.
36. Schettini DA, Ribeiro RR, Demicheli C, Rocha OGF, Melo MN, Michalick MSM, et al. Improved targeting of antimony to the bone marrow of dogs using liposomes of reduced size. Int J Pharm 2006;315:140-7.
37. Das S, Khan W, Mohsin S, Kumar N. Miltefosine loaded albumin microparticles for the treatment of visceral leishmaniasis: formulation development and in vitro evaluation. Polymer Adv Technol 2010;22:172-9.
38. Nahar M, Dubey V, Mishra D, Mishra PK, Dube A, Jain NK. In vitro evaluation of surface functionalized gelatin nanoparticles for macrophage targeting in the therapy of visceral leishmaniasis. J Drug Targeting 2010;18:93-105.
39. Singh P, Gupta A, Jaiswal A, Dube A, Mishra S, Chaurasia MK. Design and development of amphotericin b bearing polycaprolactone microparticles for macrophage targeting. J Biomed Nanotechnol 2011;7:50-1.
40. Dey T, Anam K, Afrin F. Antileishmanial activities of stearyl amine-bearing liposomes. Antimicrob Agents Chemother 2000;44:1739-42.
41. Alving CR, Steck EA, Chapman WL. Therapy of leishmaniasis: superior efficacies of liposome encapsulated drugs (antimonial compounds/phospholipids/model membranes/parasites). Proc Natl Acad Sci 1978;75:2959-63.
42. Banerjee G, Nandi G, Mahato SB. Drug delivery system: targeting of pentamidines to specific sites using sugar grafted liposomes. J Antimicrob Chemother 1996;38:145-50.
43. Veerareddy PR, Vobalaboina V, Nahid A. Formulation and evaluation of oil-in-water emulsions of piperine in visceral leishmaniasis. Pharmazie 2004;59:194-7.
44. Ahsan F, Rivas IP, Khan MA, Torres Suarez AI. Targeting to macrophages: role of physicochemical properties of particulate carriers-liposomes and microspheres on the phagocytosis by macrophages. J Controlled Release 2002;79:29-40.
45. Papagiannaros A, Bories C, Demetzos C. Antileishmanial and trypanocidal activities of new miltefosine liposomal formulations. Biomed Pharmacother 2005;59:545-50.
46. Cauchetier E, Paul M, Rivollet D. Therapeutic evaluation of free and liposome-encapsulated atovaquone in the treatment of murine leishmaniasis. Int J Parasitol 2000;30:777-83.
47. Mullen AB, Carter KC, Baillie AJ. Comparison of the efficacies of various formulations of amphotericin b against murine visceral leishmaniasis. Antimicrob Agents Chemother 1997;41:2089-92.
48. Carter KC, Baillie AJ, Mullen AB. The cured immune phenotype achieved by treatment of visceral leishmaniasis in the balb/c mouse with a nonionic surfactant vesicular formulation of sodium stibogluconate does not protect against reinfection. Clin Diagn Lab Immunol 1999;6:61-5.
49. Hunter CA, Dolan TF, Coombs GH. Vesicular systems (niosomes and liposomes) for delivery of sodium stibogluconate in experimental murine visceral leishmaniasis. J Pharm Pharmacol 1988;40:161-5.
50. Mullen AB, Baillie AJ, Carter KC. Visceral leishmaniasis in the balb/c mouse: a comparison of the efficacy of a nonionic surfactant formulation of sodium stibogluconate with those of three proprietary formulations of amphotericin B. Antimicrob Agent Chemother 1998;42:2722-5.
51. Nieto J, Alvar J, Mullen AB. Pharmacokinetics, toxicities and efficacies of sodium stibogluconate formulations after intravenous administration in animals. Antimicrob Agents Chemother 2003;47:2781-7.
52. Baillie AJ, Coombs GH, Dolan TF. Biodegradable microspheres: polyacrylate starch microparticles as a delivery system for the antileishmanial drug, sodium stibogluconate. J Pharm Pharmacol 1987;39:832-5.
53. Ordonez GL, Espada FR, Dea MA. In vitro effect of new formulations of amphotericin B on amastigote and promastigote forms of leishmania infantum. Int J Antimicrob Agents 2007;30:325-9.
54. Sanchez-brunete JA, Dea MA, Rama S. Treatment of experimental visceral leishmaniasis with amphotericin b in stable albumin microspheres. Antimicrob Agents Chemother 2004;48:3246-52.
55. Kunjachan S, Gupta S, Dwivedi AK, Dube A, Chourasia MK. Chitosan-based macrophage-mediated drug targeting for the treatment of experimental visceral leishmaniasis. Informa Health Care 2011;28:301-10.
56. Venier-julienne MC, Vouldoukis I, Monjour L. In vitro study of the anti-leishmanial activity of biodegradable nanoparticles. J Drug Target 1995;3:23-9.
57. Durand R, Paul M, Rivollet D. Activity of pentamidine loaded methacrylate nanoparticles against leishmania infantum in a mouse model. Int J Parasitol 1997;27:1361-7.
58. Rodrigues JM, Croft SL, Fessi H. The activity and ultrastructural localization of primaquine-loaded poly (d, llactide) nanoparticles in leishmania donovani infected mice. Trop Med Parasitol 1994;45:223-8.
59. Kayser O, Olbrich C, Yardley V. Formulation of amphotericin B as nanosuspension for oral administration. Int J Pharm 2003;254:73-5.
60. Kayser O. Nanosuspensions for the formulation of aphidicolin to improve drug targeting effects against leishmania-infected macrophages. Int J Pharm 2000;196:253-6.
61. Veerareddy PR, Vobalaboina V, Ali N. Antileishmanial activity, pharmacokinetics and tissue distribution studies of mannose-grafted amphotericin B lipid nanospheres. J Drug Target 2009;17:140-7.
62. Gupta S, Moulik SP, Lala S. Designing and testing of an effective oil-in-water microemulsion drug delivery system for in vivo application. Drug delivery 2005;12:267-73.
63. Cortadellas O. Initial and long-term efficacy of a lipid emulsion of amphotericin B desoxycholate in the management of canine leishmaniasis. J Vet Intern Med 2003;17:808-12.
64. Lamothe J. Activity of amphotericin B in lipid emulsion in the initial treatment of canine leishmaniasis. J Small Anim Pract 2001;42:170-5.
65. Gupta S, Vyas SP. Development and characterization of amphotericin B bearing emulsomes for passive and active macrophage targeting. J Drug Target 2007;15:206-17.
66. Carter KC, Mullen AB, Sundar S. Efficacies of vesicular and free sodium stibogluconate formulations against clinical isolates of leishmania donovani. Antimicrob Agents Chemother 2001;45:3555-9.
67. Garnier T, Brown MB, Lawrence MJ. In-vitro and in vivo studies on a topical formulation of sitamaquine dihydrochloride for cutaneous leishmaniasis. J Pharm Pharmacol 2006;58:1043-54.
68. Roberts WL, Hariprashad J, Rainey PM. Pentavalent antimony-mannan conjugate therapy of experimental visceral leishmaniasis. Am J Trop Med Hyg 1996;55:444-6.
69. Golenser J, Frankenburg S, Ehrenfreund T. Efficacious treatment of experimental leishmaniasis with amphotericin b-arabinogalactan water-soluble derivatives. Antimicrob Agents Chemother 1999;43:2209-14.
70. Nan A, Croft SL, Yardley V, Ghandehari H. Targetable water-soluble polymer-drug conjugates for the treatment of visceral leishmaniasis. J Controlled Release 2004;94:115-27.
71. Alexander J, Russell DG. The interaction of leishmania species with macrophages. Adv Parasitol 1992;31:175-254.
72. Mosser DM, Vlassara H, Edelson PJ, Cerami A. Leishmania promastigotes are recognized by the macrophage receptor for advanced glycosylation end products. J Exp Med 1987;165:140-5.
73. Mosser DM, Edelson PJ. The third component of complement (c3) is responsible for the intracellular survival of leishmania major. Nature 1987;327:329-31.
74. Ilgoutz SC, Mcconville MJ. Function and assembly of the leishmania surface coat. Int J Parasitol 2001;31:899-908.
75. Kansa S, Tandon R, Dwivedi P. Development of nanocapsules bearing doxorubicin for macrophage targeting through h the phosphatidylserine ligand: a system for intervention in visceral leishmaniasis J Antimicrob Chemother 2012;67:2650-60.
76. Roy P, Das S, Auddy RG, Mukherjee A. Biological targeting and drug delivery in control of leishmaniasis. J Cell Anim Biol 2012;6:6:73-87.
77. Mitra M, Mandal AK, Chatterjee TK, Das N. Targeting of mannosylated liposome incorporated benzyl derivative of penicillium nigricans derived compound mt81 to reticuloendothelial systems for the treatment of visceral leishmaniasis. J Drug Target 2005;13:285-93.
78. Barratt G, Tenu JP, Yapo A, Peti JF. Preparation and characterization of liposomes containing mannosylated phospholipids capable of targeting drugs to macrophages. Biochim Biophys Acta 1986;862:153-64.
79. Muller CD, Schuber F. Neo-mannosylated liposomes: synthesis and interaction with mouse kupffer cells and resident peritoneal macrophages. Biochim Biophys Acta 1989;986:97-105.
80. Harashima H, Kiwada H. Liposomal targeting and drug delivery: kinetic consideration. Adv Drug Delivery Rev 1996;19:425.
81. Fiani ML, Beitz J, Turvy D, Blum JS, Stahl PD. Regulation of mannose receptor synthesis and turnover in mouse j774 macrophages. J Leukoc Biol 1998;64:85â€“91.
82. Datta N, Mukherjee S, Das L, Das P. Targeting of immunostimulatory DNA cures experimental visceral leishmaniasis through nitric oxide up-regulation and Tâ€„cell activation. Eur J Immunol 2003;33:1508â€“18.
83. Kole L, Das L, Das PK. Synergistic effect of interferon-g and mannosylated liposome incorporated doxorubicin in the therapy of experimental visceral leishmaniasis. J Infect Dis 1999;180:811-20.
84. Amselem S, Yogev A, Zawoznik E. Emulsomes, a novel drug delivery Technology. Proc Int Symp Controlled Release Bioact Mater 1994;21:1368-9.
85. Amselem S, Friedman D. Solid fat nanoemulsions. Us5662932; 1997.
86. Negre E, Michael I, Chance, Hanboula SY, Monsigny M, Roche AC, et al. Antileishmanial drug targeting through glycosylated polymers specifically internalized by macrophage membrane lectins. Antimicrob Agents Chemother 1992;36:2228-32.
87. Arkar K, Sarkar HS, Kole L. Receptor-mediated endocytosis of fucosylated neoglycoprotein by macrophages. Mol Cell Biochem 1996;156:109-16.
88. Chakraborty P, Bhaduri AN, Das PK. Neoglycoproteins as carriers for receptor-mediated drug targeting in the treatment of experimental visceral leishmaniasisâ€. J Eukaryotic Microbiol 1990;37:358-64.
89. Schottelius J. Neoglycoproteins as tools for the detection of carbohydrate-specific receptors on the cell surface of Leishmania. Parasitol Res 1991;78:309-15.
90. Sarkar K, Das PK. Rotective effect of neoglycoprotein-conjugated muramyl dipeptide against leishmania donovani infection: the role of cytokinesâ€ J Immunonol 1997;158:5357-65.
91. Tempone AG, Perez D, That S, Vilanrinho AL, Mortara RA, Andrade HF. Targeting Leishmania (L.) chagasi amastigotes through macrophage scavenger receptor: the use of drugs entrapped in liposomes containing phosphatidylserine. J Antimicrob Chemother 2004;54:60-8.
92. Mukhopadhyay A, Basu SK. Scavenger receptor-mediated drug delivery: a versatile approach for modulation of macrophage metabolism. Proc Natl Acad Sci India 2002;B68:4:361-70.
93. Solaro R, Chiellini F, Battisti A. Targeted delivery of protein drugs by nanocarriers. Materials 2010;3:1928-80.
94. Mukherjee S, Das L, Kole L. Targeting of parasite-specific immuno- liposome-encapsulated doxorubicin in the treatment of experimental visceral leishmaniasis. J Infect Dis 2004;189:1024-34.
95. Dasgupta D, Chakraborty P, Basu MK. Ligation of fc receptor of macrophages Stimulates protein kinase c and anti-leishmanial activity. Mol Cell Biochem 2000;209:1-8.
96. Kumara R, Sahoo GC, Pandeya K, Dasa VNR, Ansaria Y, Ranaa S, et al. PLGA-PEG Encapsulated sitamaquine nanoparticles drug delivery system against Leishmania donovani. Am J Sci Ind Res 2014;3:85-90.
97. Kole L, Das AL, Das PK. Synergistic effect of interferon-g and mannosylated liposome-incorporated doxorubicin in the therapy of experimental visceral leishmaniasis. J Infect Dis 1999;180:811â€“20.
98. Najjar VA. Biological and biochemical characteristics of the tetrapeptide tuftsin, Thr-lys-pro-arg. Adv Exp Med Biol 1979;121:131-47.
99. Fridkin M, Gottlieb P. Tuftsin, thr-lys-pro-arg. Anatomy of an immunologically active peptide. Mol Cell Biochem 1981;41:73-97.
100. Nishioka K, Constantopoulos A, Satoh PS. The characteristics, isolation, and synthesis of the phagocytosis stimulating peptide tuftsin. Biochem Biophys Res Commun 1972;47:172-9.
101. Fridkin M, Stabinsky Y, Zakuth V, Spirer Z. Tuftsin and some analogs: synthesis and interaction with human polymorphonuclear leukocytes. Biochim Biophys Acta 1977;496:203-11.
102. Bar-shavit Z, Stabinsky Y, Fridkin M, Goldman R. Tuftsin-macrophage interaction: specific binding and augmentation of phagocytosis. J Cell Physiol 1979;100:55-62.
103. Gupta CM, Haq W. Tuftsin-bearing liposomes as antibiotic carriers in the treatment of macrophage infections. Methods Enzymol 2005;391:291-304.
104. Guru PY, Agarwal AK, Singha UK. Drug targeting in leishmania donovani infections using tuftsin-bearing liposomes as drug vehicles. Febs Lett 1989;254:204-8.
105. Agrawal AK, Agrawal A, Pal A. Superior chemotherapeutic efficacy of Amphotericin b in tuftsin-bearing liposomes against leishmania donovani infection in hamsters. J Drug Target 2002;10:41-5.
106. Schettini DA, Costa Val Ap, Souza LF. Pharmacokinetic and parasitological evaluation of the bone marrow of dogs with visceral leishmaniasis submitted to multiple dose treatment with liposome-encapsulated meglumine antimoniate. Braz J Med Biol Res 2005;38:1879-83.
107. Brajtburg J, Bolard J. Carrier effects on biological activity of amphotericin B. Clin Microbiol Rev 1996;9:512-31.
108. Nicoletti S, Seifert K, Gilbert IH. N-(2-hydroxypropyl)meth acrylamideâ€“amphotericin b (hpmaâ€“amb) copolymer conjugates as antileishmanial agents. Int J Antimicrob Agents 2009;33:441-8.
109. Koczan G, Ghose AC, Mookerjee A, Hudecz F. Methotrexate conjugate with branched polypeptide influences leishmania donovani infection in-vitro and in experimental animals. Bioconjug Chem 2002;13:518-24.