Arch Pharm Res
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Comparative Study
Formulation and evaluation of an alternative triglyceride-free propofol microemulsion.
A new triglyceride-free propofol microemulsion for intravenous injection was formulated using nonionic surfactants, poloxamers and polyethylene glycol 660 hydroxystearate. The aim of this investigation was to evaluate the formulation for storage stability, antimicrobial activity, toxicity and preclinical efficacy. The results were compared to the characteristics obtained for the most commonly used formulation of propofol (Diprivan®). ⋯ In preclinical studies, the efficacy and pharmacokinetic profile of the microemulsion were similar to those of Diprivan®. Nevertheless, the administration of the microemulsion caused considerably low histamine release compared to the macroemulsion. Based on these results, the newly developed microemulsion of propofol appeared to have several advantages and, thus, could be an alternative to the fat macroemulsions of propofol.
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Piceid (5,4'-dihydroxystilbene-3-O-β-D-glucopyranoside) is one of the stilbenes found in Polygonum cuspidatum. Previous studies have shown that this compound has little effect on tyrosinase inhibition when compared with other stilbenes in a cell-free tyrosinase assay. Furthermore, its role for melanogenesis in melanocytes is relatively unknown. ⋯ Interestingly, the effects of piceid on hypopigmentation and inhibition of tyrosinase activity were better than those of arbutin, which is well known to inhibit melanin formation in melanocytes. In addition, piceid suppressed the mRNA and protein expression of the aforementioned enzymes and transcriptional factor in a concentration-dependent manner. In this regards, our results showed that piceid represents a safe and new candidate for a skin-lightening agent.