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      Soluplus-Mediated Diosgenin Amorphous Solid Dispersion with High Solubility and High Stability: Development, Characterization and Oral Bioavailability

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          Abstract

          Background and Purpose

          The traditional Chinese medicine, diosgenin (Dio), has attracted increasing attention because it possesses various therapeutic effects, including anti-tumor, anti-infective and anti-allergic properties. However, the commercial application of Dio is limited by its extremely low aqueous solubility and inferior bioavailability in vivo. Soluplus, a novel excipient, has great solubilization and capacity of crystallization inhibition. The purpose of this study was to prepare Soluplus-mediated Dio amorphous solid dispersions (ASDs) to improve its solubility, bioavailability and stability.

          Methods

          The crystallization inhibition studies were firstly carried out to select excipients using a solvent shift method. According to solubility and dissolution results, the preparation methods and the ratios of drug to excipient were further optimized. The interaction between Dio and Soluplus was characterized by differential scanning calorimetry (DSC), fourier transform infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), powder X-ray diffraction (PXRD) and molecular docking. The pharmacokinetic study was conducted to explore the potential of Dio ASDs for oral administration. Furthermore, the long-term stability of Dio ASDs was also investigated.

          Results

          Soluplus was preliminarily selected from various excipients because of its potential to improve solubility and stability. The optimized ASDs significantly improved the aqueous solubility of Dio due to its amorphization and the molecular interactions between Dio and Soluplus, as evidenced by dissolution test in vitro, DSC, FT-IR spectroscopy, SEM, PXRD and molecular docking technique. Furthermore, pharmacokinetic studies in rats revealed that the bioavailability of Dio from ASDs was improved about 5 times. In addition, Dio ASDs were stable when stored at 40°C and 75% humidity for 6 months.

          Conclusion

          These results indicated that Dio ASDs, with its high solubility, high bioavailability and high stability, would open a promising way in pharmaceutical applications.

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          Most cited references 55

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          Coexistence of passive and carrier-mediated processes in drug transport.

          The permeability of biological membranes is one of the most important determinants of the pharmacokinetic processes of a drug. Although it is often accepted that many drug substances are transported across biological membranes by passive transcellular diffusion, a recent hypothesis speculated that carrier-mediated mechanisms might account for the majority of membrane drug transport processes in biological systems. Based on evidence of the physicochemical characteristics and of in vitro and in vivo findings for marketed drugs, as well as results from real-life discovery and development projects, we present the view that both passive transcellular processes and carrier-mediated processes coexist and contribute to drug transport activities across biological membranes.
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            Amorphous solid dispersions: Rational selection of a manufacturing process

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              Biological ingredient analysis of traditional Chinese medicine preparation based on high-throughput sequencing: the story for Liuwei Dihuang Wan

              Although Traditional Chinese Medicine (TCM) preparations have long history with successful applications, the scientific and systematic quality assessment of TCM preparations mainly focuses on chemical constituents and is far from comprehensive. There are currently only few primitive studies on assessment of biological ingredients in TCM preparations. Here, we have proposed a method, M-TCM, for biological assessment of the quality of TCM preparations based on high-throughput sequencing and metagenomic analysis. We have tested this method on Liuwei Dihuang Wan (LDW), a TCM whose ingredients have been well-defined. Our results have shown that firstly, this method could determine the biological ingredients of LDW preparations. Secondly, the quality and stability of LDW varies significantly among different manufacturers. Thirdly, the overall quality of LDW samples is significantly affected by their biological contaminations. This novel strategy has the potential to achieve comprehensive ingredient profiling of TCM preparations.
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                Author and article information

                Journal
                Drug Des Devel Ther
                Drug Des Devel Ther
                DDDT
                dddt
                Drug Design, Development and Therapy
                Dove
                1177-8881
                27 July 2020
                2020
                : 14
                : 2959-2975
                Affiliations
                [1 ]Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University , Shenyang 110016, People’s Republic of China
                [2 ]Hebei Province Key Laboratory of Research and Development for Chinese Medicine, Chengde Medical University , Chengde, Hebei 067000, People’s Republic of China
                [3 ]Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University , Shenyang 110016, People’s Republic of China
                Author notes
                Correspondence: Cui-zhe Liu 103 Wenhua Road, Shenyang110016, People’s Republic of ChinaTel +86-0314-2291142 Email liucuizhexy@163.com
                Jian Wang Hebei Province Key Laboratory of Research and Development for Chinese Medicine, Chengde Medical University ,Chengde, Hebei067000, People’s Republic of ChinaTel +86-13604051904 Email jianwang@email.com
                Article
                253405
                10.2147/DDDT.S253405
                7396739
                © 2020 Liu 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: 14, Tables: 2, References: 57, Pages: 17
                Funding
                Funded by: the Key Discipline Construction Projects of Higher School, Science and Technology Research Youth Fund Project of National Natural Science Foundation of China
                Funded by: Hebei Province Natural Science Foundation of China
                Funded by: Science and Technology Research Youth Fund Project of Higher School in Hebei Province
                Funded by: Program for Innovative Talents of Higher Education of Liaoning
                This study was financially supported by the Key Discipline Construction Projects of Higher School, Science and Technology Research Youth Fund Project of National Natural Science Foundation of China (No.81703736), Hebei Province Natural Science Foundation of China (No. H2018406038), Science and Technology Research Youth Fund Project of Higher School in Hebei Province (No. QN2015127), and Program for Innovative Talents of Higher Education of Liaoning (2012520005).
                Categories
                Original Research

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