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      Advances of Nano-Structured Extended-Release Local Anesthetics

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          Abstract

          Extended-release local anesthetics (LAs) have drawn increasing attention with their promising role in improving analgesia and reducing adverse events of LAs. Nano-structured carriers such as liposomes and polymersomes optimally meet the demands of/for extended-release, and have been utilized in drug delivery over decades and showed satisfactory results with extended-release. Based on mature technology of liposomes, EXPAREL, the first approved liposomal LA loaded with bupivacaine, has seen its success in an extended-release form. At the same time, polymersomes has advances over liposomes with complementary profiles, which inspires the emergence of hybrid carriers. This article summarized the recent research successes on nano-structured extended-release LAs, of which liposomal and polymeric are mainstream systems. Furthermore, with continual optimization, drug delivery systems carry properties beyond simple transportation, such as specificity and responsiveness. In the near future, we may achieve targeted delivery and controlled-release properties to satisfy various analgesic requirements.

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          30-99% of administered nanoparticles will accumulate and sequester in the liver after administration into the body. This results in reduced delivery to the targeted diseased tissue and potentially leads to increased toxicity at the hepatic cellular level. This review article focuses on the inter- and intra-cellular interaction between nanoparticles and hepatic cells, the elimination mechanism of nanoparticles through the hepatobiliary system, and current strategies to manipulate liver sequestration. The ability to solve the "nanoparticle-liver" interaction is critical to the clinical translation of nanotechnology for diagnosing and treating cancer, diabetes, cardiovascular disorders, and other diseases.
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            The mechanisms of drug release in poly(lactic-co-glycolic acid)-based drug delivery systems--a review.

            Poly(D,L-lactic-co-glycolic acid) (PLGA) is the most frequently used biodegradable polymer in the controlled release of encapsulated drugs. Understanding the release mechanisms, as well as which factors that affect drug release, is important in order to be able to modify drug release. Drug release from PLGA-based drug delivery systems is however complex. This review focuses on release mechanisms, and provides a survey and analysis of the processes determining the release rate, which may be helpful in elucidating this complex picture. The term release mechanism and the various techniques that have been used to study release mechanisms are discussed. The physico-chemical processes that influence the rate of drug release and the various mechanisms of drug release that have been reported in the literature are analyzed in this review, and practical examples are given. The complexity of drug release from PLGA-based drug delivery systems can make the generalization of results and predictions of drug release difficult. However, this complexity also provides many possible ways of solving problems and modifying drug release. Basic, generally applicable and mechanistic research provides pieces of the puzzle, which is useful in the development of controlled-release pharmaceuticals. Copyright © 2011 Elsevier B.V. All rights reserved.
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                Author and article information

                Contributors
                garypumch@163.com
                machao@ibms.cams.cn
                Journal
                Nanoscale Res Lett
                Nanoscale Res Lett
                Nanoscale Research Letters
                Springer US (New York )
                1931-7573
                1556-276X
                16 January 2020
                16 January 2020
                2020
                : 15
                : 13
                Affiliations
                [1 ]ISNI 0000 0001 0662 3178, GRID grid.12527.33, Department of Anesthesiology, Peking Union Medical College Hospital, , Chinese Academy of Medical Sciences, ; Beijing, 100730 China
                [2 ]ISNI 0000 0001 0662 3178, GRID grid.12527.33, Joint Laboratory of Anesthesia and Pain, , Peking Union Medical College, ; Beijing, 100730 China
                [3 ]ISNI 0000 0001 0662 3178, GRID grid.12527.33, Department of Human Anatomy, Histology and Embryology, , Institute of Basic Medical Sciences, Chinese Academy of Medical Sciences, School of Basic Medicine, Peking Union Medical College, ; Beijing, 100005 China
                Author information
                http://orcid.org/0000-0003-1346-6961
                Article
                3241
                10.1186/s11671-019-3241-2
                6965527
                31950284
                ac0d062c-de34-45c3-90b1-69a991e87b9d
                © The Author(s). 2020

                Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License ( http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made.

                History
                : 2 July 2019
                : 26 December 2019
                Funding
                Funded by: FundRef http://dx.doi.org/10.13039/501100001809, National Natural Science Foundation of China;
                Award ID: NSFC #81771205, #91632113
                Award Recipient :
                Funded by: the Natural Science Foundation and Major Basic Research Program of Shanghai
                Award ID: 16JC1420500, 16JC1420502
                Award Recipient :
                Funded by: the CAMS Innovation Fund for Medical Sciences
                Award ID: CIFMS #2017-I2M-3-008
                Award Recipient :
                Categories
                Nano Review
                Custom metadata
                © The Author(s) 2020

                Nanomaterials
                extended-release,local anesthetics,nano-scale,liposomes,polymersome,hybrid
                Nanomaterials
                extended-release, local anesthetics, nano-scale, liposomes, polymersome, hybrid

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