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      Polymeric Nanocarriers for the Delivery of Antimalarials

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          Abstract

          Malaria is an infectious disease caused by a protozoan parasite which is transmitted by female Anopheles mosquitoes around tropical and sub-tropical regions. Half of the world’s population is at risk of being infected by malaria. This mainly includes children, pregnant women and people living with chronic diseases. The main factor that has contributed to the spread of this disease is the increase in the number of drug-resistant parasites. To overcome drug resistance, researchers have developed drug delivery systems from biodegradable polymers for the loading of antimalarials. The drug delivery systems were characterized by distinct features such as good biocompatibility, high percentage drug encapsulation, reduced drug toxicity and targeted drug delivery. In this review article, we highlight the various types of drug delivery systems developed from polymeric nanocarriers used for the delivery of antimalarials.

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          Most cited references66

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          Stealth liposomes: review of the basic science, rationale, and clinical applications, existing and potential

          Among several promising new drug-delivery systems, liposomes represent an advanced technology to deliver active molecules to the site of action, and at present several formulations are in clinical use. Research on liposome technology has progressed from conventional vesicles (“first-generation liposomes”) to “second-generation liposomes”, in which long-circulating liposomes are obtained by modulating the lipid composition, size, and charge of the vesicle. Liposomes with modified surfaces have also been developed using several molecules, such as glycolipids or sialic acid. A significant step in the development of long-circulating liposomes came with inclusion of the synthetic polymer poly-(ethylene glycol) (PEG) in liposome composition. The presence of PEG on the surface of the liposomal carrier has been shown to extend blood-circulation time while reducing mononuclear phagocyte system uptake (stealth liposomes). This technology has resulted in a large number of liposome formulations encapsulating active molecules, with high target efficiency and activity. Further, by synthetic modification of the terminal PEG molecule, stealth liposomes can be actively targeted with monoclonal antibodies or ligands. This review focuses on stealth technology and summarizes pre-clinical and clinical data relating to the principal liposome formulations; it also discusses emerging trends of this promising technology.
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            Progress of drug-loaded polymeric micelles into clinical studies.

            Targeting tumors with long-circulating nano-scaled carriers is a promising strategy for systemic cancer treatment. Compared with free small therapeutic agents, nanocarriers can selectively accumulate in solid tumors through the enhanced permeability and retention (EPR) effect, which is characterized by leaky blood vessels and impaired lymphatic drainage in tumor tissues, and achieve superior therapeutic efficacy, while reducing side effects. In this way, drug-loaded polymeric micelles, i.e. self-assemblies of amphiphilic block copolymers consisting of a hydrophobic core as a drug reservoir and a poly(ethylene glycol) (PEG) hydrophilic shell, have demonstrated outstanding features as tumor-targeted nanocarriers with high translational potential, and several micelle formulations are currently under clinical evaluation. This review summarizes recent efforts in the development of these polymeric micelles and their performance in human studies, as well as our recent progress in polymeric micelles for the delivery of nucleic acids and imaging. Copyright © 2014 Elsevier B.V. All rights reserved.
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              Poor-quality antimalarial drugs in southeast Asia and sub-Saharan Africa.

              Poor-quality antimalarial drugs lead to drug resistance and inadequate treatment, which pose an urgent threat to vulnerable populations and jeopardise progress and investments in combating malaria. Emergence of artemisinin resistance or tolerance in Plasmodium falciparum on the Thailand-Cambodia border makes protection of the effectiveness of the drug supply imperative. We reviewed published and unpublished studies reporting chemical analyses and assessments of packaging of antimalarial drugs. Of 1437 samples of drugs in five classes from seven countries in southeast Asia, 497 (35%) failed chemical analysis, 423 (46%) of 919 failed packaging analysis, and 450 (36%) of 1260 were classified as falsified. In 21 surveys of drugs from six classes from 21 countries in sub-Saharan Africa, 796 (35%) of 2297 failed chemical analysis, 28 (36%) of 77 failed packaging analysis, and 79 (20%) of 389 were classified as falsified. Data were insufficient to identify the frequency of substandard (products resulting from poor manufacturing) antimalarial drugs, and packaging analysis data were scarce. Concurrent interventions and a multifaceted approach are needed to define and eliminate criminal production, distribution, and poor manufacturing of antimalarial drugs. Empowering of national medicine regulatory authorities to protect the global drug supply is more important than ever. Copyright © 2012 Elsevier Ltd. All rights reserved.
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                Author and article information

                Contributors
                Role: Academic Editor
                Journal
                Molecules
                Molecules
                molecules
                Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry
                MDPI
                1420-3049
                02 October 2018
                October 2018
                : 23
                : 10
                : 2527
                Affiliations
                Department of Chemistry, University of Fort Hare, Alice Campus, Eastern Cape 5700, South Africa; 201103519@ 123456ufh.ac.za
                Author notes
                [* ]Correspondence: baderibigbe@ 123456ufh.ac.za ; Tel.: +27-(0)-40-602-2266
                Article
                molecules-23-02527
                10.3390/molecules23102527
                6222303
                30279405
                14231dba-a791-4807-b336-a58899acc24c
                © 2018 by the authors.

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

                History
                : 13 August 2018
                : 26 September 2018
                Categories
                Review

                biodegradable polymers,antimalarials,drug resistance,drug delivery

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