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      A Solid Ultra Fine Self-Nanoemulsifying Drug Delivery System (S-SNEDDS) of Deferasirox for Improved Solubility: Optimization, Characterization, and In Vitro Cytotoxicity Studies

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          Abstract

          The research work was designed to develop a solid self-nanoemulsifying drug delivery system (S-SNEDDS) of deferasirox (DFX). According to the solubility studies of DFX in different components, Peceol, Kolliphor EL, and Transcutol were selected as excipients. Pseudo-ternary phase diagrams were constructed, and then SNEDDS formation assessment studies and solubility of DFX in selected SNEDDSs formulations were performed. DFX loaded SNEDDS were prepared and characterized. The optimum DFX-SNEDDS formulations were developed. The relative safety of the optimized SNEDDS formulation was examined in a human immortalized myelogenous leukemia cell line, K562 cells, using the MTT cell viability test. Cytotoxicity studies revealed more cell viability (71.44%) of DFX loaded SNEDDS compared to pure DFX (3.99%) at 40 μM. The selected DFX-SNEDDS formulation was converted into S-SNEDDS by adsorbing into porous carriers, in order to study its dissolution behavior. The in vitro drug release studies indicated that DFX release (Q5%) from S-SNEDDS solidified with Neusilin UFL2 was significantly higher (93.6 ± 0.7% within 5 min) compared with the marketed product (81.65 ± 2.10%). The overall results indicated that the S-SNEDDS formulation of DFX could have the potential to enhance the solubility of DFX, which would in turn have the potential to improve its oral bioavailability as a safe novel delivery system.

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          Most cited references46

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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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            Self-nanoemulsifying drug delivery system (SNEDDS) of the poorly water-soluble grapefruit flavonoid Naringenin: design, characterization, in vitro and in vivo evaluation.

            Naringenin (NRG), predominant flavanone in grapefruits, possesses anti-inflammatory, anti-carcinogenic, hepato-protective and anti-lipid peroxidation effects. Slow dissolution after oral ingestion due to its poor solubility in water, as well as low bioavailability following oral administration, restricts its therapeutic application. The study is an attempt to improve the solubility and bioavailability of NRG by employing self-nanoemulsifying drug delivery technique. Preliminary screening was carried out to select oil, surfactant and co-surfactant, based on solubilization and emulsification efficiency of the components. Pseudo ternary phase diagrams were constructed to identify the area of nanoemulsification. The developed self-nanoemulsifying drug delivery systems (SNEDDS) were evaluated in term of goluble size, globule size distribution, zeta potential, and surface morphology of nanoemulsions so obtained. The TEM analysis proves that nanoemulsion shows a droplet size less than 50 nm. Freeze thaw cycling and centrifugation studies were carried out to confirm the stability of the developed SNEDDS. In vitro drug release from SNEDDS was significantly higher (p < 0.005) than pure drug. Furthermore, area under the drug concentration time-curve (AUC(0-24)) of NRG from SNEDDS formulation revealed a significant increase (p < 0.005) in NRG absorption compared to NRG alone. The increase in drug release and bioavailability as compared to drug suspension from SNEDDS formulation may be attributed to the nanosized droplets and enhanced solubility of NRG in the SNEDDS.
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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.
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                Author and article information

                Journal
                Pharmaceuticals (Basel)
                Pharmaceuticals (Basel)
                pharmaceuticals
                Pharmaceuticals
                MDPI
                1424-8247
                24 July 2020
                August 2020
                : 13
                : 8
                : 162
                Affiliations
                [1 ]Department of Pharmaceutical Technology, Faculty of Pharmacy, Near East University, Nicosia 99010, Cyprus; alaasami2489@ 123456gmail.com (A.A.); yildiz.ozalp@ 123456neu.edu.tr (Y.Ö.)
                [2 ]Department of Pharmaceutical Sciences, Faculty of Pharmacy, Jerash University, Jerash 26150, Jordan
                [3 ]Department of Pharmaceutical Technology, Istanbul University, Faculty of Pharmacy, Istanbul 34116, Turkey; bmesut@ 123456istanbul.edu.tr (B.M.); yozsoy@ 123456istanbul.edu.tr (Y.Ö.)
                [4 ]Department of Medical Genetics, Faculty of Medicine, Near East University, Nicosia 99010, Cyprus; nedime.serakinci@ 123456neu.edu.tr
                [5 ]Department of Molecular Biology and Genetics, Faculty of Art and Sciences Near East University, Nicosia 99010, Cyprus
                Author notes
                [* ]Correspondence: sgungor@ 123456istanbul.edu.tr ; Tel.: +90-212-440-00-00 (ext. 13493)
                Author information
                https://orcid.org/0000-0001-7928-1666
                https://orcid.org/0000-0003-2838-1688
                https://orcid.org/0000-0002-1884-0839
                Article
                pharmaceuticals-13-00162
                10.3390/ph13080162
                7465256
                32722238
                f1178a6b-d945-439f-95c6-4b7bf005b3a1
                © 2020 by the authors.

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

                History
                : 18 June 2020
                : 21 July 2020
                Categories
                Article

                deferasirox,snedds,solid snedds,solid carriers,enhancement solubility,oral delivery

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