Formulación y Optimización del Sistema Flotante de Amoxicilina para el tratamiento efectivo de la infección por Helicobacter pylori

The authors thank DST-FIST Lab (RERDS-CPR), R&D Director, for providing necessary facilities and assistance to perform this research work.Introducción: El objetivo del presente estudio fue formular y caracterizar el Sistema Flotante (FRS, siglas en Inglés) de Amoxicilina para prolongar el tiempo de residencia gástrica y liberación del fármaco para el enfoque efectivo del Helicobacter pylori. Método: Para el presente estudio se seleccionaron como factores goma guar, Monoestearato de glicerilo (GMS), carbonato de calcio. Como reacciones, se seleccionaros el período de congelación (h), el lapso de flotación (min), y el porcentaje acumulado de liberación del fármaco (CDR). Para la experimentación se seleccionaron el diseño factorial 23 con réplicas. Resultados: Se observó que la goma guar y el GMS fueron los factores principales que afectaron el período de congelación y mostraron un efecto sinérgico (positivo). Mientras que la goma guar y el carbonato de calcio mostraron un efecto positivo y el GMS mostró un efecto antagónico (negativo) en el lapso de flotación. El porcentaje CDR mostró un efecto antagónico en todos los factores. Se emplearon curvas de nivel para identificar el diseño del espacio, análisis numéricos posteriores produjeron 12 soluciones óptimas en base a la deseabilidad. El FRS mostró un mayor AUCo-t, Cmax, tmaxy t1/2 cuando se comparó con la formulación comercial, aproximadamente 2.30 cambios múltiplos y prolongación con liberación sostenida por más de 24 h que pudo deberse a una mejor congelación. Conclusiones: Se puede concluir que el sistema flotante se desarrolló satisfactoriamente por la aplicación del Diseño de Experimentos (DoE) con menores ensayos y utilizando fácilmente los excipientes disponibles para una mejor flotación, congelación y suministro constante del fármaco.Introduction: The aim of the present study was to develop and to characterize the floating raft system (FRS) of Amoxicillin to enhance gastric residence time and drug release to target Helicobacter pylori effectively. Method: In the present study, guar gum, glyceryl monostearate (GMS), calcium carbonate were selected as factors. Gelation duration (h), floating lag time (min), and % Cumulative drug release (CDR) were selected as responses. 23 factorial design with replicates was selected for experimentation. Results: It was observed that guar gum and GMS were the major factors affecting gelation duration, increase in the quantity of both guar gum and GMS increased gelation duration i.e., sustained gelation period (24 h). Floating time increased with an increase in the amount of guar gum and calcium carbonate, whereas an increase in the quantity of GMS decreased floating time. Guar gum, calcium carbonate, and GMS exhibited an antagonistic effect on % CDR. Contour plots were used to identify design space; further numerical analysis yielded 12 best solutions based on desirability. FRS exhibited greater AUCo-t, Cmax, tmax, and t1/2 when compared to marketed formulation approximately 2.30 folds enhancement and prolongation with a sustained release for greater than 24 h that might be due to better gelation. Conclusions: It can be concluded that the floating raft system was successfully developed by the Design of experiment (DoE) application with fewer trails and by utilizing easily available excipients for better floating, gelation, and sustained delivery of the drug

Apoptosis-mediated cytotoxic effect of Caralluma adscendens var. attenuata on colon (HT29) and Hepatic (HepG2) cancer cell lines

Introduction: Caralluma adscendens var. attenuata (Wight) Grav. and Mayur., a member of Apocynaceae, is a perennial stem succulent plant with wide distribution in tropics and subtropics of the world. This plant is reported for the presence of steroids, flavonoids, saponins, triterpenes, and pregnane glycosides, and is known to have antidiabetic and antiulcerogenic properties. Materials and Methods: In this study, an attempt was made to identify antioxidant capacity and cytotoxic potential of n-hexane and aqueous methanolic extracts of total stem part of C. adscendens var. attenuata. Antioxidant activity was evaluated by total phenolic content assay, total flavonoid content assay, free radical scavenging activity, and reducing ability methods. Cytotoxic activity was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT) assay and nuclear staining methods for colorectal cancer cell lines HT29 and liver cancer cell lines HepG2. Results: MTT assay method has proven that the IC50 value was 10 μg/mL for both extracts, whereas for cisplatin standard, it was 2 μg/mL. By nuclear staining, the apoptotic cells were identified as oval masses with dark cytoplasm and dense green nuclear chromatin fragments indicating the programmed cell death for both n-hexane and aqueous methanolic extracts at the same concentration (10μg/mL). Conclusion: However, aqueous methanolic extract showed prominent cytotoxic potential against both cancer cell lines