This paper describes design and evaluation of parenteral lecithin-based nanoemulsions intended for brain delivery of risperidone, a poorly water-soluble psychopharmacological drug. The nanoemulsions were prepared through cold/hot high pressure homogenization and characterized regarding droplet size, polydispersity, surface charge, morphology, drug-vehicle interactions, and physical stability. To estimate the simultaneous influence of nanoemulsion formulation and preparation parameters--co-emulsifier type, aqueous phase type, homogenization temperature--on the critical quality attributes of developed nanoemulsions, a general factorial experimental design was applied. From the established design space and stability data, promising risperidone-loaded nanoemulsions (mean size about 160 nm, size distribution <0.15, zeta potential around -50 mV), containing sodium oleate in the aqueous phase and polysorbate 80, poloxamer 188 or Solutol(®) HS15 as co-emulsifier, were produced by hot homogenization and their ability to improve risperidone delivery to the brain was assessed in rats. Pharmacokinetic study demonstrated erratic brain profiles of risperidone following intraperitoneal administration in selected nanoemulsions, most probably due to their different droplet surface properties (different composition of the stabilizing layer). Namely, polysorbate 80-costabilized nanoemulsion showed increased (1.4-7.4-fold higher) risperidone brain availability compared to other nanoemulsions and drug solution, suggesting this nanoemulsion as a promising carrier worth exploring further for brain targeting.
Due to the lack of skin irritation and skin barrier impairment along with the marked hydration effect, it could be said that the in-vestigated actives incorporated into alkyl polyglucoside emulsi-fier-stabilized creams may be safely applied as ingredients for "tailor-made" cosmetic moisturizers intended for normal and dry skin care, whereas olive oil squalene could be used for the treatment of irritated or sensitive skin as well. [Projekat Ministarstva nauke Republike Srbije, br. TR34031]
Alkyl polyglucosides (APGs) are a perfect amphiphilic structure, with excellent surface activity and solubility feature. The aim of this study is to develop a simple system, with a relatively low emulsifier content, composed of materials mainly naturally based and with no additional fatty alcohol. Hydroxystearyl alcohol and Hydroxystearyl glucoside, prepared with Jojoba and Hazelnut oil, medium chain triglycerides with or without Xylitylglucoside and Anhydroxylitol and Xylitol, have been investigated by using microscopy, rheology, thermal analysis, pH and conductimetry. Cyclic stress and in vivo skin irritation tests were also conducted. The investigated natural APG emulsifier has a capacity to form simple and stable emulsions of desirable rheological profile with improved hydration potential and to renew damaged skin, thus it can be safely applied as stabilizer in cosmetic and prospective pharmaceutical cream-bases.
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