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      Formulation and in vitro characterization of rifampicin-loaded porous poly (ε-caprolactone) microspheres for sustained skeletal delivery

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          Abstract

          Purpose

          Mycobacterium tuberculosis is a serious public health problem affecting hundreds of millions of elderly people worldwide, which is difficult to be treated by traditional methods because of the peculiarity of skeletal system and liver damage caused by high-dose administration. In this research, a porous drug release system has been attempted to encapsulate rifampicin (RIF) into poly (ε-caprolactone) (PCL) microspheres to improve the efficacy and benefit of anti-tuberculosis drug in skeletal system.

          Materials and methods

          The microspheres prepared by two different methods, oil-in-oil (o/o) emulsion solvent evaporation method and oil-in-water (o/w) method, were characterized in terms of morphology, size, encapsulation efficiency, drug distribution, degradation, and crystallinity.

          Results

          The microspheres exhibited a porous structure with evenly drug distribution prepared by o/o emulsion solvent evaporation method, and their diameter ranged from 50.54 to 57.34 μm. The encapsulation efficiency was up to 61.86% when drug-loading content was only 1.51%, and showed a little decrease with the drug-loading content increasing. In vitro release studies revealed that the drug release from porous microspheres was controlled by non-Fickian diffusion, and almost 80% of the RIF were completely released after 10 days. The results of RIF-loaded microspheres on the antibacterial activity against Staphylococcus aureus proved that the porous microspheres had strong antibacterial ability. In addition, the polymer crystallinity had prominent influence on the degradation rate of microspheres regardless of the morphology.

          Conclusion

          It was an efficient way to entrap slightly water-soluble drug like RIF into PCL by o/o emulsion solvent evaporation method with uniform drug distribution. The RIF-loaded porous PCL microspheres showed the combination of good antimicrobial properties and excellent cytocompatibility, and it could generate gentle environment by PCL slow degradation.

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          Most cited references 52

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          Poly-є-caprolactone based formulations for drug delivery and tissue engineering: A review.

          Biodegradable polymer based novel drug delivery systems have provided many avenues to improve therapeutic efficacy and pharmacokinetic parameters of medicinal entities. Among synthetic biodegradable polymer, poly-є-caprolactone (PCL) is a polymer with very low glass transition temperature and melting point. Owing to its amicable nature and tailorable properties it has been trialed in almost all novel drug delivery systems and tissue engineering application in use/investigated so far. This review aims to provide an up to date of drugs incorporated in different PCL based formulations, their purpose and brief outcomes. Demonstrated PCL formulations with or without drugs, intended for drug delivery and/or tissue engineering application such as microsphere, nanoparticles, scaffolds, films, fibers, micelles etc. are categorized based on method of preparation. Copyright © 2011 Elsevier B.V. All rights reserved.
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            Surface engineered and drug releasing pre-fabricated scaffolds for tissue engineering.

             T Park,  Hyun Chung (2007)
            A wide range of polymeric scaffolds have been intensively studied for use as implantable and temporal devices in tissue engineering. Biodegradable and biocompatible scaffolds having a highly open porous structure and good mechanical strength are needed to provide an optimal microenvironment for cell proliferation, migration, and differentiation, and guidance for cellular in-growth from host tissue. A variety of natural and synthetic polymeric scaffolds can be fabricated in the form of a solid foam, nanofibrous matrix, microsphere, or hydrogel. Biodegradable porous scaffolds can be surface engineered to provide an extracellular matrix mimicking environment for better cell adhesion and tissue in-growth. Furthermore, scaffolds can be designed to release bioactive molecules, such as growth factors, DNA, or drugs, in a sustained manner to facilitate tissue regeneration. This paper reviews the current status of surface engineered and drug releasing scaffolds for tissue engineering.
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              Polycaprolactone microparticles and their biodegradation

               D.R Chen,  J.Z Bei,  S.G. Wang (2000)
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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
                2018
                31 May 2018
                : 12
                : 1533-1544
                Affiliations
                [1 ]Research Center for Nano Biomaterials, Analytical and Testing Center, Sichuan University, Chengdu, People’s Republic of China
                [2 ]Center of Bone and Trauma, The Third Affiliated Hospital of Chongqing Medical University, Chongqing, People’s Republic of China
                [3 ]National Engineering Research Center for Biomaterials, Sichuan University, Chengdu, People’s Republic of China
                Author notes
                Correspondence: Yi Zuo, Analytical and Testing Center, Sichuan University, No. 29 Wangjiang Road, Chengdu 610064, People’s Republic of China, Tel +86 288 541 8178, Fax +86 288 541 8178, Email zoae@ 123456scu.edu.cn
                Yaning Wang, National Engineering Research Center for Biomaterials, Sichuan University, No. 29 Wangjiang Road, Chengdu 610065, People’s Republic of China, Email wangyaning@ 123456scu.edu.cn
                [*]

                These authors contributed equally to this work

                Article
                dddt-12-1533
                10.2147/DDDT.S163005
                5987792
                © 2018 Mei 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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