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      The Effects of Primary Unconjugated Bile Acids on Nanoencapsulated Pharmaceutical Formulation of Hydrophilic Drugs: Pharmacological Implications


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          In a recent study, in our laboratory, primary unconjugated bile acids, commonly found in humans, chenodeoxycholic acid (CDCA), have been shown to improve stability of nanoencapsulated lipophilic drugs and improve their release profile after oral administration likely via electrokinetic stabilisation. Hence, this study aimed to examine the effects of CDCA on exerting similar effects on hydrophilic drugs.


          Various CDCA-based formulations were produced for the orally administered hydrophilic drug, metformin. Analyses of these formulations included electrokinetic potentials, topography, drug and CDCA formulation contents, nano size distribution, heat-induced deformation and outer-core expansion indices, release profiles, shell-resistance ratio, and thermal and chemical indices. With the drug’s main target being pancreatic beta-cells, the formulations’ effects on cell viability, functions and inflammatory profiles were also investigated.

          Results and Conclusions

          CDCA-based metformin formulations exhibited improved stability and release profiles via thermal, chemical and electrokinetic effects, which were formulation-dependent suggesting potential applications of CDCA in the oral targeted delivery of hydrophilic drugs.

          Most cited references61

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          Targeting bile-acid signalling for metabolic diseases.

          Bile acids are increasingly being appreciated as complex metabolic integrators and signalling factors and not just as lipid solubilizers and simple regulators of bile-acid homeostasis. It is therefore not surprising that a number of bile-acid-activated signalling pathways have become attractive therapeutic targets for metabolic disorders. Here, we review how the signalling functions of bile acids can be exploited in the development of drugs for obesity, type 2 diabetes, hypertriglyceridaemia and atherosclerosis, as well as other associated chronic diseases such as non-alcoholic steatohepatitis.
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            Bile acids: Chemistry, physiology, and pathophysiology

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              Eudragit: a technology evaluation.

              Eudragit is the brand name for a diverse range of polymethacrylate-based copolymers. It includes anionic, cationic, and neutral copolymers based on methacrylic acid and methacrylic/acrylic esters or their derivatives.

                Author and article information

                Drug Des Devel Ther
                Drug Des Devel Ther
                Drug Design, Development and Therapy
                23 October 2021
                : 15
                : 4423-4434
                [1 ]The Biotechnology and Drug Development Research Laboratory, Curtin Medical School & Curtin Health Innovation Research Institute, Curtin University , Bentley, Perth, 6102, WA, Australia
                [2 ]Hearing Therapeutics, Ear Science Institute Australia, Queen Elizabeth II Medical Centre , Nedlands, Perth, 6009, WA, Australia
                [3 ]Fiona Stanley Hospital , Perth, WA, Australia
                [4 ]Curtin Medical School & Curtin Health Innovation Research Institute, Curtin University , Perth, WA, Australia
                [5 ]Department of Pharmacology, Toxicology and Clinical Pharmacology, Faculty of Medicine, University of Novi Sad , Novi Sad, 21101, Serbia
                Author notes
                Correspondence: Hani Al-Salami Hearing Therapeutics, Biotechnology and Pharmaceutical Sciences, Curtin University , Bentley, Perth, 6102, WA, Australia Tel +61 8 9266 9816 Fax + 61 8 9266 2769 Email hani.al-salami@curtin.edu.au
                Author information
                © 2021 Mooranian 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).

                : 08 July 2021
                : 10 August 2021
                Page count
                Figures: 5, Tables: 1, References: 70, Pages: 12
                Funded by: Beijing Nat-Med Biotechnology Co. Ltd;
                Funded by: European Union Horizon 2020 research project;
                Funded by: Curtin Faculty ORS-WAHAI Consortium and the Australian National Health and Medical Research;
                H Al-Salami has been and is currently receiving funding from Beijing Nat-Med Biotechnology Co. Ltd. The work is partially supported by the European Union Horizon 2020 research project and innovation program under the Marie Skłodowska-Curie Grant Agreement No 872370. Curtin Faculty ORS-WAHAI Consortium and the Australian National Health and Medical Research (APP9000597).
                Original Research

                Pharmacology & Pharmaceutical medicine
                microencapsulation,diabetes mellitus,glyceryl monooleate,eudragit,chenodeoxycholic acid


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