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      Aceclofenac nanocrystals with enhanced in vitro, in vivo performance: formulation optimization, characterization, analgesic and acute toxicity studies

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          Abstract

          This study was aimed to enhance the dissolution rate, oral bioavailability and analgesic potential of the aceclofenac (AC) in the form of nanosuspension using cost-effective simple precipitation–ultrasonication approach. The nanocrystals were produced using the optimum conditions investigated for AC. The minimum particle size (PS) and polydispersity index was found to be 112±2.01 nm and 0.165, respectively, using hydroxypropyl methylcellulose (1%, w/w), polyvinylpyrrolidone K30 (1%, w/w) and sodium lauryl sulfate (0.12%, w/w). The characterization of AC was performed using zeta sizer, scanning electron microscopy, transmission electron microscopy, powder X-ray diffraction and differential scanning calorimetry. The saturation solubility of the AC nanocrystals was substantially increased 2.6- and 4.5-fold compared to its unprocessed active pharmaceutical ingredient in stabilizer solution and unprocessed drug. Similarly, the dissolution rate of the AC nanocrystals was substantially enhanced compared to its other counterpart. The results showed that >88% of AC nanocrystals were dissolved in first 10 min compared to unprocessed AC (8.38%), microsuspension (66.65%) and its marketed tablets (17.65%). The in vivo studies of the produced stabilized nanosuspension demonstrated that the C max were 4.98- and 2.80-fold while area under curve from time of administration to 24 h (AUC 0→24 h) were found 3.88- and 2.10-fold greater when compared with unprocessed drug and its marketed formulation, respectively. The improved antinociceptive activity of AC nanocrystals was shown at much lower doses as compared to unprocessed drug, which is purely because of nanonization which may be attributed to improved solubility and dissolution rate of AC, ultimately resulting in its faster rate of absorption.

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          Most cited references 34

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          Physical and chemical stability of drug nanoparticles.

          As nano-sizing is becoming a more common approach for pharmaceutical product development, researchers are taking advantage of the unique inherent properties of nanoparticles for a wide variety of applications. This article reviews the physical and chemical stability of drug nanoparticles, including their mechanisms and corresponding characterization techniques. A few common strategies to overcome stability issues are also discussed. Published by Elsevier B.V.
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            Nanocrystal technology, drug delivery and clinical applications

            Nanotechnology will affect our lives tremendously over the next decade in very different fields, including medicine and pharmacy. Transfer of materials into the nanodimension changes their physical properties which were used in pharmaceutics to develop a new innovative formulation principle for poorly soluble drugs: the drug nanocrystals. The drug nanocrystals do not belong to the future; the first products are already on the market. The industrially relevant production technologies, pearl milling and high pressure homogenization, are reviewed. The physics behind the drug nanocrystals and changes of their physical properties are discussed. The marketed products are presented and the special physical effects of nanocrystals explained which are utilized in each market product. Examples of products in the development pipelines (clinical phases) are presented and the benefits for in vivo administration of drug nanocrystals are summarized in an overview.
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              Effect of light and temperature on zeta potential and physical stability in solid lipid nanoparticle (SLN™) dispersions

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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
                2017
                23 August 2017
                : 11
                : 2443-2452
                Affiliations
                [1 ]Department of Pharmacy, University of Malakand, Chakdara
                [2 ]Department of Pharmacy, Sarhad University of Science and Information Technology Peshawar, Khyber Pakhtunkhwa, Pakistan
                [3 ]Faculty of Pharmacy, Department of Pharmaceutics, Universiti Teknologi, Mara, Selangor, Malaysia
                [4 ]Department of Pharmacognosy and Medicinal, Aromatic and Poisonous Plants Research Center, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
                [5 ]Phytochemistry Department, National Research Center, Dokki, Giza, Egypt
                [6 ]Department of Chemical Engineering, College of Engineering, Al-Muzahmeiah Branch, King Saud University, Riyadh, Saudi Arabia
                Author notes
                Correspondence: Shahzeb Khan; Abdul Sadiq, Department of Pharmacy, University of Malakand, Dir (Lower), Chakdara 23050, KPK, Pakistan, Tel +92 34 5949 2869; +92 33 2504 6485, Email shahzeb_333@ 123456hotmail.com ; sadiquom@ 123456yahoo.com
                Article
                dddt-11-2443
                10.2147/DDDT.S140626
                5574597
                © 2017 Rahim 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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                Original Research

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