IMPROVED ORAL DELIVERY OF AGOMELATIN FROM MALTODEXTRIN BASED PRONIOSOME POWDERS
Pradeep Kumar, Yennamaneni
2017
J. Global Trends Pharm Sci
unpublished
Key words: Proniosome Maltodextrin Agomelatine The current research was designed to improve the oral delivery of agomelatine by loading into maltodextrin based proniosome powders. proniosome powders proved to be the potential carriers for efficient oral delivery of lipophilic or amphiphilic drugs. These 'proniosomes' minimize problems of niosome physical stability such as aggregation, fusion and leaking, and provide additional convenience in transportation, distribution, storage, and dosing.
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... proniosome powders were fabricated by various ratios of span 60 and cholesterol and evaluated for micromeritic properties and the results indicates adequate micrometric properties. The formulation containing equimolar ratio of span 60 and cholesterol showed smaller vesicle size, high surface charge and entrapment efficiency. The formation of niosomes and surface morphology of optimized proniosome formulation was evaluated by optical and scanning electron microscopy, FT-IR, differential scanning calorimetry, and powder X-ray diffraction studies performed to understand the solid state properties of the drug reveal the absence of chemical interaction, drug transformation from crystalline to amorphous and molecular state. The drug release performance in vitro carried out in both simulated gastric and intestinal fluid demonstrate improved dissolution characteristics compared to pure drug. INTRODUCTION: Agomelatine is a melatonin receptor agonist MT1 and MT2 and a 5-HT2C receptor antagonist. Agomelatine resynchronises circadian rhythms in animal models of delayed sleep phase syndrome. By antagonizing 5-HT2C receptors, it increases noradrenaline and dopamine release specifically in the frontal cortex. Therefore, it is sometimes classified as a norepinephrine-dopamine disinhibitor. It has no influence on the extracellular levels of serotonin. Agomelatine has shown an antidepressant-like effect in animal models of depression as well as in models with circadian rhythm desynchronisation and in models related to stress and anxiety. In humans, agomelatine has positive phase shifting properties; it induces a phase advance of sleep,
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