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      Design and optimization of self-nanoemulsifying drug delivery systems for improved bioavailability of cyclovirobuxine D

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          Abstract

          Background

          The main purpose of this research was to design a self-nanoemulsifying drug delivery system (SNEDDS) for improving the bioavailability of cyclovirobuxine D as a poorly water-soluble drug.

          Materials and methods

          Solubility trials, emulsifying studies, and pseudo-ternary phase diagrams were used to screen the SNEDDS formulations. The optimized drug-loaded SNEDDS was prepared at a mass ratio of 3:24:38:38 for cyclovirobuxine D, oleic acid, Solutol SH15, and propylene glycol, respectively. The optimized formulation was characterized in terms of physicochemical and pharmacokinetic parameters compared with marketed cyclovirobuxine D tablets.

          Results

          The optimized cyclovirobuxine-D-loaded SNEDDS was spontaneously dispersed to form a nanoemulsion with a globule size of 64.80±3.58 nm, which exhibited significant improvement of drug solubility, rapid absorption rate, and enhanced area under the curve, together with increased permeation and decreased efflux. Fortunately, there was a nonsignificant cytotoxic effect toward Caco-2 cells. The relative bioavailability of SNEDDS was 200.22% in comparison with market tablets, in rabbits.

          Conclusion

          SNEDDS could be a potential candidate for an oral dosage form of cyclovirobuxine D with improved bioavailability.

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          Most cited references 39

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          Self-nanoemulsifying drug delivery systems: formulation insights, applications and advances.

          There has been a resurgence of interest in nanoemulsions for various pharmaceutical applications since low-energy emulsification methods, such as spontaneous or self-nanoemulsification, have been described. Self-nanoemulsifying drug delivery systems (SNEDDS) are anhydrous homogenous liquid mixtures consisting of oil, surfactant, drug and coemulsifier or solubilizer, which spontaneously form oil-in-water nanoemulsion of approximately 200 nm or less in size upon dilution with water under gentle stirring. The physicochemical properties, drug solubilization capacity and physiological fate considerably govern the selection of the SNEDDS components. The composition of the SNEDDS can be optimized with the help of phase diagrams, whereas statistical experimental design can be used to further optimize SNEDDS. SNEDDS can improve oral bioavailability of hydrophobic drugs by several mechanisms. The conversion of liquid SNEDDS to solid oral dosage forms or solid SNEDDS has also been achieved by researchers. Solid SNEDDS can offer better patient compliance and minimize problems associated with capsules filled with liquid SNEDDS.
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            Enhanced oral bioavailability of dexibuprofen by a novel solid self-emulsifying drug delivery system (SEDDS).

            The main objective of this study was to prepare a solid form of lipid-based self-emulsifying drug delivery system (SEDDS) by spray drying liquid SEDDS with an inert solid carrier Aerosil 200 to improve the oral bioavailability of poorly water-soluble drug dexibuprofen. The liquid SEDDS was a system that consisted of dexibuprofen, Labrasol, Capryol 90 and Labrafil M 1944 CS. The particle size analysis revealed no difference in the z-average particle diameter of the reconstituted emulsion between liquid and solid SEDDS. The solid SEDDS was characterized by SEM, DSC and XRD studies. In vivo results of solid SEDDS and dexibuprofen powder in rats at the dose of 10mg/kg showed that the initial plasma concentrations of drug in solid SEDDS were significantly higher than those of dexibuprofen powder (P<0.05). The solid SEDDS gave significantly higher AUC and Cmax than did dexibuprofen powder (P<0.05). In particular, the AUC of solid SEDDS was about twofold higher than that of dexibuprofen powder. Our results suggested that this solid SEDDS could be used as an effective oral solid dosage form to improve the bioavailability of poorly water-soluble drug dexibuprofen.
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              SNEDDS containing bioenhancers for improvement of dissolution and oral absorption of lacidipine. I: development and optimization.

              The aim of this study was to develop and optimize SNEDDS formulations containing surfactants reported to be bioenhancers for improvement of dissolution and oral absorption of lacidipine (LCDP). Preliminary screening was carried out to select proper components combination. D-optimal mixture experimental design was applied to optimize a SNEDDS that contains a minimum amount of surfactant, a maximum amount of lipid, and possesses enhanced emulsification and dissolution rates. Three formulation variables; the oil phase X(1) (a mixture of Labrafil/Capmul), the surfactant X(2) (a mixture of Cremophor/Tween 80) and the co-surfactant X(3), were included in the design. The systems were assessed for droplet size, light absorbance, optical clarity, drug release and emulsification efficiency. Following optimization, the values of formulation components (X(1), X(2), and X(3)) were 34.20%, 40.41% and 25.39%, respectively. There is a good correlation between light absorbance and droplet size analysis of diluted SNEDDS (R(2)=0.883). Transmission electron microscopy demonstrated spherical droplet morphology. The stability of the optimized formulation was retained after storage at 40 degrees C/75% RH for three months. The optimized formulation of LCDP showed a significant increase in dissolution rate compared to the drug suspension under the same conditions. Our results proposed that the optimized SNEDDS formulation, containing bioenhancing surfactants, could be promising to improve oral absorption of LCDP. Copyright (c) 2010 Elsevier B.V. All rights reserved.
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                Author and article information

                Journal
                Drug Des Devel Ther
                Drug Des Devel Ther
                Drug Design, Development and Therapy
                Drug Design, Development and Therapy
                Dove Medical Press
                1177-8881
                2016
                28 June 2016
                : 10
                : 2049-2060
                Affiliations
                [1 ]Nanjing University of Chinese Medicine, Nanjing, Jiangsu
                [2 ]Huangshan University, Huangshan, Anhui
                [3 ]Third Clinical Medical College, Nanjing University of Chinese Medicine, Nanjing, Jiangsu
                [4 ]Anhui University of Chinese Medicine, Hefei, Anhui, People’s Republic of China
                Author notes
                Correspondence: Xiao-bin Jia, Third Clinical Medical College, Nanjing University of Chinese Medicine, No 100, Shizi Street, Hongshan Road, Qixia Dist, Nanjing, 210028, Jiangsu, People’s Republic of China, Tel +86 25 8563 7809, Email jxiaobin2005@ 123456hotmail.com
                Article
                dddt-10-2049
                10.2147/DDDT.S106356
                4933569
                27418807
                © 2016 Ke et al. This work is published and licensed by Dove Medical Press Limited

                The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License ( http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.

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