The effect of the Pheroid delivery system on thein vitrometabolism andin vivopharmacokinetics of artemisone

Abstract

The in vivo results obtained in this study indicate that the Pheroid delivery system improves the PK profile of artemisone. The in vitro results indicate that microsomal metabolism of artemisone is inhibited by the Pheroid delivery system.

In vitro anti-cancer effects of artemisone nano-vesicular formulations on melanoma cells

“…One previous attempt to entrap artemisone with lipophilic vesicles known as Pheroids resulted in formation of micrometer sized vesicles (4-34 m) with little or no information available on the entrapment efficiency [27,28]. In general, drug entrapment depends upon the nature of the matrix material and whether the drug is lipophilic or hydrophilic.…”

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). We investigated the effect of a Pheroid formulation on the antimalarial activity of artemisone and on dormancy in vitro.…”

“…The active M1 metabolite is formed via dehydrogenation in the thiomorpholine-dioxide moiety of artemisone (5,6). The artemisone-entrapped Pheroid vesicles (AMS-Phe) were prepared by adding 30 mM artemisone to a pro-Pheroid formulation (i.e., oil phase only) containing 4.9% polyethylene glycol 400 (PEG-400) instead of 20%, vitamin F ethyl ester, PEGylated ricinoleic acid (Kolliphor), and ␣-tocopherol as previously described (23). This oil phase was saturated with nitrous oxide.…”

“…No growing parasites were observed in the mefloquine-treated cultures during the 30-day follow-up period. Although artemisone entrapped in Pheroid vesicles increased in vivo drug concentrations in blood (22,23), it is unlikely that this Pheroid delivery system will prevent recrudescence.…”

A toxicity profile of the Pheroid® technology in rodents

“…Morphological conformation was determined by confocal laser scanning electron microscopy (CLSM, Nikon D-eclipse C1 confocal scanning microscope, United States) as per the method outlined by Slabbert et al, . The self-emulsifying formulation was prepared for physical characterization by mixing it with a 0.1 N hydrochloric acid diluent, to simulate the acidic environment of the stomach [27,28]. The presence of bacterial endotoxins in the raw materials was determined using the point-of-use Endosafe®-PTS™ System (Charles River Laboratories, United States).…”