Development and Characterization of Novel Chitosan-Coated Curcumin Nanophytosomes for Treating Drug-Resistant Malaria.

This study aimed at enhancing the efficacy of curcumin (CR) by formulating and coating it with chitosan. In silico molecular docking studies revealed that CR exhibited almost similar and low binding energies when compared to artemisinin, indicating high stability at the target site. It can be confirmed that CR is effective in treating and reducing Plasmodium falciparum parasites. Fourier transform infrared studies confirmed that there was a shift and disappearance of some drug peaks in the formulation which revealed complexation with phospholipids. The F2EXT3-developed formulation exhibited greater solubility (24.31 ± 3.47 µg/mL) when compared to pure CR (7.99 ± 1.95 µg/mL). Proton nuclear magnetic resonance studies confirmed the formation of Curcumin-phospholipid hydrogen bonding in F2EXT3. The in vitro drug release studies revealed that the developed formulation F2EXT3 exhibited better drug release at 71.98% at 48 h; this might be due to the effective entrapment efficiency of the drug inside the phospholipid, presence of polyethylene glycol 4000 and chitosan further assisted in sustained release of the drug. Scanning electron microscopy studies revealed that optimized F2EXT3 CR nanophytosomes were nearly spherical with narrow size distribution and smooth surface. The zeta potential of the F2EXT3 showed -3.5 mV. Stability studies revealed that the formulation remained stable even after 6 months. It was observed from the hemin assay that CR and F2EXT3 exhibited (50 µg/mL curcumin) exhibited IC50 values of 47 ± 2.45 and 22 ± 1.58 µM, respectively. Further in vivo antimalarial activity on resistant and sensitive strains needs to be performed to evaluate the efficacy of the developed formulation.

Development and Optimization of Amoxicillin Floating Raft System to effectively treat Helicobacter pylori infection / Formulación y Optimización del Sistema Flotante de Amoxicilina para el tratamiento efectivo de la infección por Helicobacter pylori

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

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