Formulation and antisickling activity of the effervescent granules of Cissus populnea Guill et. Perr (Vitaceae) root on deoxygenated drepanocytes Formulation et activité antifalciforme des granules effervescents de la racine de Cissus populnea Guill et. Perr (Vitaceae) sur drépanocytes désoxygénés
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Abstract
Background: Ethanol extracts of Cissus populnea have been documented to possess antisickling activities, useful in the management of Sickle Cell Anaemia (SCA). However, it is necessary to develop the extracts into acceptable dosage forms with further potentials for drug development.
Objectives: This present study investigated the in-vitro evaluation of the antisickling activities of the crude ethanol extract and effervescent granules of Cissus populnea roots.
Methods: Cissus populnea root was dried at 37±0.5oC, powdered, extracted in 80 % ethanol (72 h.), filtered, concentrated, freeze-dried and prepared as effervescent granules (CPG) formulations 1, 2 and 3 with varying percentages of sodium bicarbonate, citric and tartaric acids, while the crude extract was formulation 4. CPG were characterized using density measurements (Bulk and Tapped Densities), Hausner's ratio [HR], Carr's Index [CI]) and angle of repose as assessment criteria, while antisickling properties were evaluated using inhibitory and reversal activities of sodium metabisulphite-induced sickling of hemoglobin erythrocytes. Para-hydroxybenzoic acid (PHBA) and phosphate-buffered saline solutions served as controls.
Results: Bulk and tapped densities ranked formulations 1(1.37±0.03) >3(1.18±0.13) >2(1.13±0.11)>4(1.07±0.07), and 3(1.69±0.03)>1(1.68±0.02) >2(1.51±0.07) >4(1.31±0.13) respectively. The HR and CI had a reverse relationship with the crude extract granules having the highest HR (1.03±0.53) and lowest CI (18.32±0.03) values. Angle of repose ranked formulations 4(39.18±0.11)>3(34.18±0.28)>2(31.03±0.27)>1(29.13±0.17). Formulations 3 and 4 showed the highest antisickling (72.0 % and 68.0%) and reversal activities (57.0 % and 59.0 %) comparable to PHBA (64 % inhibitory and 56.0 % reversal activities)
Conclusion: CPG showed better flow and antisickling properties than those of the crude extract, and may play important roles in the management of SCA.
FRENCH
Contexte: Il a été démontré que les extraits d'éthanol de Cissus populnea possèdent des activités antifalciformes, utiles dans la gestion de l'anémie falciforme. Cependant, il est nécessaire de développer les extraits sous des formes posologiques acceptables, avec d'autres potentiels pour le développement de médicaments.
Objectifs: Cette étude a examiné l'évaluation in vitro des activités antifalciformes de l'extrait d'éthanol brut et des granules effervescents de racines de Cissus populnea.
Méthode: La racine de Cissus populnea a été séchée à 37±0,5oC, réduite en poudre, extraite dans de l'éthanol à 80% (72 h), filtrée, concentrée, lyophilisée et préparée sous forme de granulés effervescents (CPG) formulations 1, 2 et 3 avec des pourcentages variables de bicarbonate de sodium, d'acides citrique et tartrique, tandis que l'extrait brut constituait la formulation 4. Les CPG ont été caractérisés à l'aide de mesures de densité (densités apparentes et tassées), du rapport de Hausner [HR], de l'indice de Carr [IC]) et de l'angle de repos comme critères d'évaluation, tandis que les propriétés antifalciformes ont été évaluées à l'aide des activités d'inhibition et d'inversion de la falciformation des érythrocytes de l'hémoglobine induite par le métabisulfite de sodium. L'acide para-
hydroxybenzoïque (PHBA) et les solutions salines tamponnées au phosphate ont servi de témoins.
Résultats: Les densités apparentes et tassées ont classé les formulations 1(1,37±0,03) >3(1,18±0,13) >2(1,13±0,11) >4(1,07±0,07), et 3(1,69±0,03)>1(1,68±0,02) >2(1,51±0,07) >4(1,31±0,13) respectivement. Le HR et le CI avaient une relation inverse avec les granulés d'extrait brut ayant les valeurs HR les plus élevées (1,03±0,53) et CI les plus basses (18,32±0,03). L'angle de repos a classé les formulations 4(39.18±0.11)>3(34.18±0.28)>2(31.03±0.27)>1(29.13±0.17). Les formulations 3 et 4 ont montré les activités antifalciformes les plus élevées (72,0% et 68,0%) et d'inversion (57,0 % et 59,0 %), comparables à celles du PHBA (64 % d'activité inhibitrice et 56,0 % d'activité d'inversion).
Conclusion: Le CPG a montré de meilleures propriétés d'écoulement et antifalciformes que celles de l'extrait brut et peut jouer un rôle important dans la gestion de l'anémie falciforme.
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