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      Engineering of Naproxen Loaded Polymer Hybrid Enteric Microspheres for Modified Release Tablets: Development, Characterization, in silico Modelling and in vivo Evaluation

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          Naproxen (NP) is a non-steroidal anti-inflammatory drug with poor aqueous solubility and low oral bioavailability, which may lead to therapeutic failure. NP causes crucial GIT irritation, bleeding, and peptic and duodenal ulcers.

          Purpose of the study

          This study aimed to engineer and characterize polymer hybrid enteric microspheres using an integrated (experimental and molecular modelling) approach with further development to solid dosage form with modified drug release kinetics and improved bioavailability.

          Materials and methods

          NP loaded polymer hybrid enteric microspheres (PHE-Ms) were fabricated by using a modified solvent evaporation technique coupled with molecular modelling (MM) approach. The PHE-Ms were characterized by particle size, distribution, morphology, crystallinity, EE, drug-polymer compatibility, and DSC. The optimized NP loaded PHE-Ms were further subjected to downstream procedures including tablet dosage form development, stability studies and comparative in vitro-in vivo evaluation.


          The hydrophobic polymer EUD-L100 and hydrophilic polymer HPMC-E5 delayed and modified drug release at intestinal pH while imparting retardation of NP release at gastric pH to diminish the gastric side effects. The crystallinity of the NP loaded PHE-Ms was established through DSC and P (XRD). The particle size for the developed formulations of PEH-Ms (M1-M5) was in the range from 29.06 ±7.3–74.31 ± 17.7 μm with Span index values of 0.491–0.69, respectively. The produced NP hybrid microspheres demonstrated retarded drug release at pH 1.2 and improved dissolution at pH 6.8. The in vitro drug release patterns were fitted to various release kinetic models and the best-followed model was the Higuchi model with a release exponent “n” value > 0.5. Stability studies at different storage conditions confirmed stability of the NP loaded PHE-Ms based tablets ( P<0.05). The molecular modelling (MM) study resulted in adequate binding energy of co-polymer complex SLS-Eudragit-HPMC-Naproxen (−3.9 kcal/mol). In contrast to the NP (unprocessed) and marketed formulations, a significant increase in the C max of PHE-MT1 (44.41±4.43) was observed.


          The current study concludes that developing NP loaded PHE-Ms based tablets could effectively reduce GIT consequences with restored therapeutic effects. The modified release pattern could improve the dissolution rate and enhancement of oral bioavailability. The MM study strengthens the polymer-drug relationship in microspheres.

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          Most cited references 49

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          A simple equation for description of solute release II. Fickian and anomalous release from swellable devices

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            Small-molecule library screening by docking with PyRx.

            Virtual molecular screening is used to dock small-molecule libraries to a macromolecule in order to find lead compounds with desired biological function. This in silico method is well known for its application in computer-aided drug design. This chapter describes how to perform small-molecule virtual screening by docking with PyRx, which is open-source software with an intuitive user interface that runs on all major operating systems (Linux, Windows, and Mac OS). Specific steps for using PyRx, as well as considerations for data preparation, docking, and data analysis, are also described.
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              Microencapsulation techniques, factors influencing encapsulation efficiency.

              Microencapsulation is one of the quality preservation techniques of sensitive substances and a method for production of materials with new valuable properties. Microencapsulation is a process of enclosing micron-sized particles in a polymeric shell. There are different techniques available for the encapsulation of drug entities. The encapsulation efficiency of the microparticle or microsphere or microcapsule depends upon different factors like concentration of the polymer, solubility of polymer in solvent, rate of solvent removal, solubility of organic solvent in water, etc. The present article provides a literature review of different microencapsulation techniques and different factors influencing the encapsulation efficiency of the microencapsulation technique.

                Author and article information

                Drug Des Devel Ther
                Drug Des Devel Ther
                Drug Design, Development and Therapy
                07 January 2020
                : 14
                : 27-41
                [1 ]Department of Pharmacy, University of Malakand , Chakdara, Khyber Pakhtunkhwa 18800, Pakistan
                [2 ]Discipline of Pharmaceutical Sciences, School of Health Sciences, University of KwaZulu-Natal , Durban 4000, South Africa
                [3 ]Division of Molecular Pharmaceutics and Drug Delivery, College of Pharmacy, The University of Texas at Austin , Austin, TX, USA
                [4 ]Department of Pharmacy, Sarhad University of Science and Information Technology , Peshawar, Khyber Pakhtunkhwa, Pakistan
                [5 ]Medicinal, Aromatic & Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University , Riyadh 11451, Saudi Arabia
                [6 ]Central Laboratory, College of Pharmacy, King Saud University , Riyadh 11451, Saudi Arabia
                [7 ]Department of Pharmaceutics and Pharmaceutical Technology, College of Pharmacy, University of Sharjah , Sharjah 27272, United Arab Emirates
                [8 ]Department of Pharmacy, COMSATS University Islamabad , Abbottabad 22060, Pakistan
                [9 ]School of Pharmacy, Monash University Malaysia , Bandar Sunway, Subang Jaya 47500, Malaysia
                Author notes
                Correspondence: Shahzeb Khan Department of Pharmacy, University of Malakand , Dir Lower KPK, Pakistan Email shahzeb_333@hotmail.com
                © 2020 Hameed 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: 9, Tables: 7, References: 54, Pages: 15
                Original Research


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