Therapeutic efficacy of novel microcrystalline formulations of albendazole (ABZ) in the

acute stage of infection with Trichinella spiralis (Ts), in mice with different susceptibility to
the parasite

SAIC

AUTORES: Valeria Marizza1, Ana V. Codina1,2, Josefina Priotti3,4, María D. Vasconi1,5

Darío Leonardi3,4, María C. Lamas3,4, Lucila I. Hinrichsen1,2

ÁREA TEMÁTICA:

1
Instituto de Genética Experimental, Facultad de Ciencias Médicas, UNR
2
CIC-UNR
3
Depto. de Farmacia, Facultad de Ciencias Bioquímicas y Farmacéuticas, UNR
4
IQUIR-CONICET
5
Área Parasitología, Facultad de Ciencias Bioquímicas y Farmacéuticas, UNR

Keywords: Albendazole – microcrystal formulations – Trichinella spiralis – in vivo assay –

enteral stage

ABZ, the preferred therapeutic agent to treat trichinellosis, has a very low and erratic
bioavailability, which limits its oral absorption and increases its therapeutic failure. To
modify that property, microcrystalline ABZ formulations were developed by a bottom-up
methodology, using stabilizing polymers. After physicochemical and in vitro assays,
hydroxyethyl-cellulose (S4A) and chitosan (S10A) based formulations were selected as those
which most probably improve ABZ in vivo efficiency. This work aimed to compare the in
vivo antiparasitic effectiveness of ABZ, S4A, and S10A in the acute stage of Ts infection, in
two mouse lines differing in susceptibility to the parasite. CBi+ (susceptible) and CBi/L
(resistant) adult mice of both sexes were infected orally with 2 Ts larvae/g bw and treated
with ABZ, S4A, or S10A (30 mg ABZ/kg bw) on days 5, 6 and 7 post-infection (p-i), or non-
treated, controls. Half the animals were sacrificed two days after the last administration to
estimate intestinal parasitic load (number of adult parasites recovered, nAP) and Ts females
fecundity (Ff). The remaining animals were sacrificed 37 days p-i to assess the effect of the
treatment on muscular worm burden (MWB, number of parasites/g of tissue). nAP from
treated mice did not differ significantly from controls. Ff could only be determined in Ts
females recovered from control mice since female parasites found in treated mice were dead
or with an altered morphology. In both lines MWB was significantly lower in treated animals
(CBi+, ♂ P=0.0002, ♀ P=0.02; CBi/L, ♂ P=0.01, ♀ P=0.0001,). These results indicate that
ABZ, S4A, and S10A were effective when administered in the acute stage of the infection.
No significant differences were observed among the treatments. The alteration of the female
internal morphology, caused by the treatments, would lead to a modification in Ff with the
consequent reduction of muscle encysted larvae.