85 research outputs found

    ENHANCEMENT OF STABILITY, RELEASE AND IN VITRO DIGESTIBILITY OF MULBERRY STEM EXTRACT USING MICROEMULSIONS

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    Objective: This study was aimed to develop oral microemulsions and to evaluate their ability to enhance stability, release and intestinal digestion of mulberry stem extract (MSE).Methods: The pseudoternary phase diagrams were constructed using caprylic/capric triglyceride (oil), PEG-8 caprylic/capric glycerides (S), polyglyceryl-3 diisostearate (CoS) and an aqueous phase. The effects of S/CoS (Km) ratio and a cosolvent, i.e. polyethene glycol 400 or propylene glycol (PG), were investigated. The optimized formulations were selected and incorporated with MSE. Then, they were then subjected to stability, release and lipolysis studies. The control solution consisted of 50% PG and 50% water.Results: The formation and characteristics of the microemulsions were influenced by Km and cosolvents. The two optimized formulations (F3 and F4) consisted of 10% oil, 70% S/CoS mixture and 20% aqueous phase were chosen. The Km ratios of F3 and F4 were 4:1 and 3:1. The aqueous phase of F3 and F4 was water and water mixed with PG, respectively. These formulations could improve the stability of MSE better than the control solution. The accumulated release of MSE from F3, F4 and the control solution reached 100% while that of unformulated crude extract reached only 70% after 6 h. The lipolysis study showed that MSE incorporated in both F3 and F4 was digested more than double the percentage compared to that of MSE incorporated in the control solution.Conclusion: MSE was successfully developed in microemulsions. They are shown to be promising vehicles for oral delivery of MSE. Further animal trials are suggested

    Neuropharmacology of morphine-3-glucuronide (M3G)

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    Measurement of intracellular Ca2+ in cultured rat embryonic hippocampal neurons using a fluorescence microplate reader: Potential application to biomolecular screening

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    Introduction: Fluorescence microplate readers for the measurement of cytosolic free Ca ([Ca]) are used as a drug screening tool, particularly for immortal cell lines. However, wider application of this methodological approach to more differentiated cells such as neurons would also be useful for the screening of compounds that modulate synaptic transmission. Such an approach has the potential to identify lead compounds for the development of novel drugs for the treatment of epilepsy, pathological pain states, Parkinson's disease, or other neurological disorders. Methods: In this paper, we describe the development of a microplate reader assay for the assessment of [Ca] in a primary culture of rat hippocampal neurons maintained in Neurobasal medium using the fluorescent calcium indicator, fluo-3. Results: The assay was appropriate for the screening of glutamate receptor agonists and antagonists. Furthermore, lowering the extracellular Mg concentration ([Mg] ) produced consistent oscillations in neuronal [Ca ] detected using the fluorescence microplate reader. These oscillations were inhibited by the GABA agonist, baclofen, and the NMDA receptor antagonist, LY274614. Discussion: Our results indicate that assessment of the inhibitory effects of agents on spontaneous [Ca ] oscillations in neurons may be useful for the identification of agents that act on targets for which specific screening methods are not currently available, or those which act via a previously unknown pathway to inhibit synaptic transmission. This technique also has the potential to increase the productivity of experiments designed to characterize changes in [Ca] (including calcium oscillations) in cultured neurons
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