In vitro activity of Pheroid vesicles containing antibiotics against Plasmodium falciparum

Abstract

The macrolide antibiotics, erythromycin and azithromycin, have been studied for their potential antimalarial activity, but only modest activity has been demonstrated. In this study, we investigated the enhancement of the efficacy of these antibiotics in combination with a patented lipid-based drug delivery system, Pheroid technology. A chloroquine resistant strain of Plasmodium falciparum (RSA11) was incubated with the formulations for a prolonged incubation time (144 h). Drug efficacy assays were conducted by analyzing the histidine-rich protein II levels of the parasites. The effects of azithromycin and erythromycin were compared with other antibiotics and standard antimalarial drugs. The poor water soluble nature of the drugs led to the formation of micro scale Pheroid vesicles with average particle sizes of 72.76±10.73 lm for azithromycin and 100.62±29.27 lm for erythromycin. The IC 50 values of erythromycin and azithromycin alone and entrapped in Pheroid vesicles decreased statistically significant (Pp0.05). Prolonged exposure was also statistically meaningful (Pp0.05), although it seems that exposure need not exceed 96 h. Pheroid vesicles also proved successful in decreasing the IC 50 values of doxycycline, tetracycline and triclosan. Pheroid vesicles containing antibiotics could prove successful as a malaria treatment option.

Lipid-based Fe- and Zn- nanoformulation is more effective in alleviating Fe- and Zn- deficiency in maize

“…Pheroid technologyV R is a unique sub-micron-to nano-formulation that can entrap, transport, and deliver the active ingredient in an effective way in humans and plants. The Pheroid formulation is a stable structure that can be manipulated and controlled to specifically enhance the absorption of various active ingredients which can result in enhanced metabolic activity (Du Plessis et al 2012;2014;). The Pheroid system is composed of an organic carbon backbone and fatty acids that result in vesicles and sponges in the size of nano to micron, that can be manipulated to entrap hydrophilic, hydrophobic, or amphiphilic compounds for transport across numerous biological membranes (Grobler 2009).…”

Assessment of the Induction of Dormant Ring Stages in Plasmodium falciparum Parasites by Artemisone and Artemisone Entrapped in Pheroid Vesicles In Vitro

“…A Pheroid delivery system has been shown to increase the in vitro antimalarial activities of azithromycin, mefloquine, and quinine significantly (20,21). Entrapment of artemisone in Pheroid vesicles also has been shown to enhance blood artemisone concentrations in mice (22) and primates (23).…”

Formulation and evaluation of Pheroid vesicles containing mefloquine for the treatment of malaria

“…MQ was incorporated by first dissolving the drug in dl‐α‐tocopherol and then adding the appropriate amount of nitrous oxide PBS to form a Pheroid‐drug complex. This strategy has proved successful in previous studies with various antimalarial drugs …”

“…These vesicles have proved successful in increasing the bioavailability of the poorly soluble prototype antimalarial drug, artemisone, but not artemiside . We have previously shown that Pheroid vesicles are stable and have an entrapment efficiency of 67% for MQ, and proved effective in increasing the in‐vitro antimalarial efficacy of chloroquine, erythromycin, azithromycin, doxycycline and tetracycline …”