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Enhanced anticryptococcal activity of chloroquine in phosphatidylserine-containing liposomes in a murine model
Masood A Khan1, Rukhsana Jabeen, T H Nasti
1Interdisciplinary Biotechnology Unit, Aligarh Muslim University, Aligarh-202002, India. alammasood1@rediffmail.com
Objectives:
The anticryptococcal activity of chloroquine was assessed after incorporation in phosphatidylserine (PS)-containing negatively charged liposomes in a murine model.
Methods:
In the present study, we investigated the antifungal activity of chloroquine entrapped in PS liposomes against Cryptococcus neoformans in the macrophage cell line J 774 and in a murine model. Mice were treated with free as well as liposomal formulations of chloroquine before and after challenging with C. neoformans infection. The anticryptococcal activity of chloroquine was also evaluated in combination with fluconazole in the treatment of systemic murine cryptococcosis. The efficacy of chloroquine treatment was assessed by continued survival as well as by colony forming units (cfu) in liver and brain of treated mice.
Results:
Chloroquine entrapped in PS liposomes shows increased activity against C. neoformans infection both in in vitro and in vivo studies. Moreover, the antifungal activity of fluconazole increases when used in combination with liposomal chloroquine. Chloroquine in PS liposomes was found to be more effective in comparison with the same dose of free chloroquine or chloroquine entrapped in neutral liposomes.
Conclusions:
The enhanced anticryptococcal activity of chloroquine in PS liposomes seems to be due to uptake of drug-containing PS liposomes by macrophages. It can be assumed that liposome-mediated delivery of chloroquine to macrophages results in an unfavourable (alkaline) environment for the growth of C. neoformans inside macrophages.
Insights
Chloroquine in phosphatidylserine (PS) liposomes enhances antifungal activity against Cryptococcus neoformans. This liposomal formulation improves drug delivery to macrophages, increasing efficacy in treating cryptococcosis.
Area of Science:
- Mycology
- Pharmacology
- Nanomedicine
Background:
- Cryptococcus neoformans is a fungal pathogen causing cryptococcosis.
- Chloroquine has shown anticryptococcal activity.
- Liposomes are potential drug delivery systems.
Purpose of the Study:
- To evaluate chloroquine incorporated in phosphatidylserine (PS)-containing liposomes for anticryptococcal activity.
- To assess the efficacy of liposomal chloroquine in a murine model of cryptococcosis.
- To investigate the combination therapy of liposomal chloroquine with fluconazole.
Main Methods:
- Chloroquine was encapsulated in PS liposomes.
- Antifungal activity was tested in vitro using J 774 macrophage cell line and in vivo in a murine model.
- Mice were treated with free or liposomal chloroquine before and after infection.
- Efficacy was measured by survival rates and colony-forming units (cfu) in organs.
- Combination therapy with fluconazole was also evaluated.
Main Results:
- Chloroquine in PS liposomes demonstrated enhanced anticryptococcal activity in vitro and in vivo.
- Liposomal chloroquine was more effective than free chloroquine or chloroquine in neutral liposomes.
- Combination of fluconazole with liposomal chloroquine showed increased antifungal efficacy.
- Improved survival and reduced cfu in liver and brain were observed with liposomal chloroquine.
Conclusions:
- PS liposomes enhance the anticryptococcal activity of chloroquine.
- Liposome-mediated delivery of chloroquine to macrophages is likely responsible for the enhanced efficacy.
- This delivery mechanism creates an alkaline environment within macrophages, unfavorable for C. neoformans growth.
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