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      Development, Characterization, and in-vivo Pharmacokinetic Study of Lamotrigine Solid Self-Nanoemulsifying Drug Delivery System

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          This study aimed to prepare solid self-nanoemulsified drug delivery system (S-SNEDDS) of lamotrigine (LMG) for enhancing its dissolution and oral bioavailability (BA).


          Nineteen liquid SNEDDS were prepared (R1-R19) using D-optimal design with different ratios of oil, surfactant (S), and cosurfactant (Cos). The formulations were characterized regarding robustness to dilution, droplet size, thermodynamic stability testing, self-emulsification time, in-vitro release in 0.1 N HCl and phosphate buffer (PB; pH 6.8). Design Expert ® 11 software was used to select the optimum formulations. Eight S-SNEDDS were prepared (S1-S8) using 2 3 factorial design, and characterized by differential scanning calorimetry (DSC), powder x-ray diffraction (PXRD), and scanning electron microscopy (SEM). The optimum formulation was chosen regarding in-vitro drug released in 0.1 N HCl and PB, compared to pure LMG and commercial tablet (Lamictal ®). The BA of LMG from the optimized S-SNEDDS formulation was evaluated in rabbits compared to pure LMG and Lamictal ®.


          The optimized S-SNEDDS was S2, consisting of R9 adsorbed on Aeroperl ® 300 in a ratio of 1:1, with the best results regarding in-vitro drug released in 0.1 N HCl at 15 min (100%) compared to pure LMG (73.40%) and Lamictal ® (79.43%), and in-vitro drug released in PB at 45 min (100%) compared to pure LMG (30.46%) and Lamictal ® (92.08%). DSC, PXRD, and SEM indicated that LMG was molecularly dispersed within the solid nano-system. The BA of S2 was increased 2.03 and 1.605 folds compared to pure LMG, and Lamictal ®, respectively.


          S2 is a promising S-SNEDDS formulation. It can be a potential carrier for improving dissolution, and BA of LMG.

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          Most cited references 72

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          Modeling and comparison of dissolution profiles.

          Over recent years, drug release/dissolution from solid pharmaceutical dosage forms has been the subject of intense and profitable scientific developments. Whenever a new solid dosage form is developed or produced, it is necessary to ensure that drug dissolution occurs in an appropriate manner. The pharmaceutical industry and the registration authorities do focus, nowadays, on drug dissolution studies. The quantitative analysis of the values obtained in dissolution/release tests is easier when mathematical formulas that express the dissolution results as a function of some of the dosage forms characteristics are used. In some cases, these mathematic models are derived from the theoretical analysis of the occurring process. In most of the cases the theoretical concept does not exist and some empirical equations have proved to be more appropriate. Drug dissolution from solid dosage forms has been described by kinetic models in which the dissolved amount of drug (Q) is a function of the test time, t or Q=f(t). Some analytical definitions of the Q(t) function are commonly used, such as zero order, first order, Hixson-Crowell, Weibull, Higuchi, Baker-Lonsdale, Korsmeyer-Peppas and Hopfenberg models. Other release parameters, such as dissolution time (tx%), assay time (tx min), dissolution efficacy (ED), difference factor (f1), similarity factor (f2) and Rescigno index (xi1 and xi2) can be used to characterize drug dissolution/release profiles.
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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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              Development of solid self-emulsifying drug delivery systems: preparation techniques and dosage forms.

              Approximately 40% of new chemical entities exhibit poor aqueous solubility and present a major challenge to modern drug delivery system, because of their low bioavailability. Self-emulsifying drug delivery systems (SEDDS) are usually used to improve the bioavailability of hydrophobic drugs. Conventional SEDDS, however, are mostly prepared in a liquid form, which can produce some disadvantages. Accordingly, solid SEDDS (S-SEDDS), prepared by solidification of liquid/semisolid self-emulsifying (SE) ingredients into powders, have gained popularity. This article gives an overview of the recent advances in the study of S-SEDDS, especially the related solidification techniques and the development of solid SE dosage forms. Finally, the existing problems and the possible future research directions in this field are pointed out.

                Author and article information

                Drug Des Devel Ther
                Drug Des Devel Ther
                Drug Design, Development and Therapy
                19 October 2020
                : 14
                : 4343-4362
                [1 ]Department of Industrial Pharmacy, Faculty of Pharmacy, Misr University for Science and Technology , 6th of October City, Giza, Egypt
                [2 ]Department of Pharmaceutics, Faculty of Pharmacy, Misr University for Science and Technology , 6th of October City, Giza, Egypt
                [3 ]Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University , Cairo, Egypt
                [4 ]Department of Pharmaceutics, Faculty of Pharmacy, Kuwait University , Kuwait City, Kuwait
                Author notes
                Correspondence: Marian Sobhy Azer Department of Pharmaceutics, Faculty of Pharmacy, Misr University for Science and Technology , 6th of October City, Giza, EgyptTel +2 010 050 529 83 Email drmariansobhy@hotmail.com
                Mohamed El-Nabarawi Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University , Kasr El-Aini Street, Cairo11562, EgyptTel +2 010 014 244 39 Email nabrwima@hotmail.com
                © 2020 Abdelmonem 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. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms ( https://www.dovepress.com/terms.php).

                Page count
                Figures: 8, Tables: 15, References: 75, Pages: 20
                Original Research


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