Study of erythrocytes as a novel drug carrier for the delivery of artemether

Resealed erythrocytes have been explored in various dimensions of drug delivery, owing to their high biocompatibility and inability to initiate immune response. The present research was designed to evaluate the drug delivery potential of erythrocytes by loading a hydrophobic anti-malarial drug, Artemether. Three different loading techniques were applied to achieve maximum optimized drug loading. A HPLC method was validated for drug quantification in erythrocytes. The relatively high loading was achieved using hypotonic treatment was 31.39% as compared to other two methods. These, drug loaded erythrocytes were characterized for membrane integrity via ESR showing higher ESR values for drug loaded cells as compared to normal cells. Moreover, microscopic evaluation was done to observe morphological changes in erythrocytes after successful loading which showed swollen cells with slight rough surface as compared to smooth surface of normal cells. Drug release was studied for 8 h which showed more than 80% release within 3-7 h from erythrocytes treated with different hypotonic methods. Overall, the study revealed a potential application of erythrocytes in delivery of hydrophobic drugs using hypotonic treatment as compared to other methods.

The Neurotoxic Effects of Artemether on the Cytoarchitecture of the Trapezoid Nuclei of Adult Male Wistar Rats (Rattus novegicus) / Efectos Neurotóxicos del Artemeter sobre la Citoarquitectura del Núcleo Trapezoide en Ratas Machos Adultas Wistar (Rattus novegicus)

In Man, artemether is given at 160mg/kg/bodyweight for three days in the treatment of malarial. This study investigated the effects of corresponding 1.23/mg/kg/bodyweight of artemether for a period of seven days on the trapezoid nuclei and the behavioural functions on day 7 after drug administration in rats. This study observed no gross or morphological differences between the two groups of animals (control and experimental groups) on day 7 at the completion of experimental procedure. A significant statistical increase in average body weight was observed in the control groups C1 (which received only standard diet and water) and C2 (which received 1.23mg/kg/bodyweight of normal saline intramuscularly in addition to standard diet and water) from 140- + 19.65g on day 1 to 146 + 19.90g on Day 1 and 151 + 12.0g on Day 1 to 156.2 + 12.2g on Day 7 respectively. There was a non-statistically significant apparent reduction in body weight in the experimental group E, (which received intramuscular injection of 1.23mg/kg/bodyweight of artemether) from 160 + 9.0g on Day 1 to 157.4 + 8.0g on Day 7. The assessment of brainstem nuclei showed patchychromatic appearance of neurons of the trapezoid nuclei in the experimental group as against the normal vesicular appearance of neurons of the trapezoid nuclei in the Control Group C. The rats in the control groups CI and C2 displayed normal balance and co-ordination, while rats in the experimental group E, showed abnormalities of balance and co-ordination. Using t-test analysis technique at 95% confidence interval i.e t < 0.05 and P - value = 2.26, no significant difference was observed between the average brain weight in the control groups C1 and C2 and the experimental group E.

En el Hombre, el artemeter es dado en el tratamiento de la malaria en dosis de 160 mg/kg de peso, por tres días. Este estudio abordó los efectos de un tratamiento con artemeter, durante 7 días (en dosis de 1,23 mg/kg de peso) sobre el núcleo trapezoide de ratas y las funciones de conducta, en el día 7 después de la administración de la droga. No se observaron ni macro ni diferencias morfológicas entre dos grupos de animales (grupos control y experimental) en el día 7 de la completación del procedimiento. Un incremento estadísticamente significativo en el promedio del peso del cuerpo fue encontrado en el grupo control C1 (el que recibió solamente una dieta standard y agua) y C2 (que recibió 1,23 mg/kg de peso de solución salina intramuscular agregada a la dieta y al agua) que fue desde 140± 19,65 g y 146 ± 19,9 g en el día 1, respectivamente y de 151 ± 12 g y de 156,2 ± 12,2 g en el día 7, respectivamente. No hubo una reducción aparente estadísticamente significativa en el peso del cuerpo del grupo experimental (el cual recibió inyección intramuscular de 1,23 mg/kg de peso de artemeter), la que fue desde 160 ± 9 g en el día 1 y de 157,4 ± 8, en el día 7. La evaluación de núcleos del tronco encefálico mostró apariencia cromática irregular de las neuronas del núcleo trapezoide en el grupo experimental contrariamente a la apariencia vesicular normal de las neuronas de este núcleo en el grupo control. Las ratas de los grupos controles C1 y C2 presentaron un normal balanceo y coordinación, mientras que las ratas del grupo experimental, mostraron anormalidades de balanceo y coordinación. Usando el test t con 95% de intervalo de confianza, p 0,05 y con un valor p=2,26, no se observaron diferencias estadísticamente significativas entre el promedio de los grupos C1 y C2 y del grupo experimental.