دورية أكاديمية
Synthesis and colloidal characterization of folic acid-modified PEG-b-PCL Micelles for methotrexate delivery.
العنوان: | Synthesis and colloidal characterization of folic acid-modified PEG-b-PCL Micelles for methotrexate delivery. |
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المؤلفون: | Brandt JV; Department of Physical Chemistry, Institute of Chemistry, São Paulo State University (UNESP), Araraquara, SP, 14801-970, Brazil. Electronic address: joao.brandt@gmail.com., Piazza RD; Department of Physical Chemistry, Institute of Chemistry, São Paulo State University (UNESP), Araraquara, SP, 14801-970, Brazil., Dos Santos CC; Department of Physical Chemistry, Institute of Chemistry, São Paulo State University (UNESP), Araraquara, SP, 14801-970, Brazil., Vega-Chacón J; Department of Physical Chemistry, Institute of Chemistry, São Paulo State University (UNESP), Araraquara, SP, 14801-970, Brazil., Amantéa BE; Department of Physical Chemistry, Institute of Chemistry, São Paulo State University (UNESP), Araraquara, SP, 14801-970, Brazil., Pinto GC; Department of Physical Chemistry, Institute of Chemistry, São Paulo State University (UNESP), Araraquara, SP, 14801-970, Brazil., Magnani M; Department of Physical Chemistry, Institute of Chemistry, São Paulo State University (UNESP), Araraquara, SP, 14801-970, Brazil., Piva HL; Department of Chemistry, Center of Nanotechnology and Tissue Engineering -Photobiology and Photomedicine Research Group, Faculty of Philosophy, Science and Letters of Ribeirão Preto, University of São Paulo (USP), 14040-901, Ribeirão Preto, SP, Brazil., Tedesco AC; Department of Chemistry, Center of Nanotechnology and Tissue Engineering -Photobiology and Photomedicine Research Group, Faculty of Philosophy, Science and Letters of Ribeirão Preto, University of São Paulo (USP), 14040-901, Ribeirão Preto, SP, Brazil., Primo FL; Department of Bioprocess and Biotechnology, School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara, SP, 14801-903, Brazil., Jafelicci M Junior; Department of Physical Chemistry, Institute of Chemistry, São Paulo State University (UNESP), Araraquara, SP, 14801-970, Brazil., Marques RFC; Department of Physical Chemistry, Institute of Chemistry, São Paulo State University (UNESP), Araraquara, SP, 14801-970, Brazil. |
المصدر: | Colloids and surfaces. B, Biointerfaces [Colloids Surf B Biointerfaces] 2019 May 01; Vol. 177, pp. 228-234. Date of Electronic Publication: 2019 Feb 06. |
نوع المنشور: | Journal Article |
اللغة: | English |
بيانات الدورية: | Publisher: Elsevier Country of Publication: Netherlands NLM ID: 9315133 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1873-4367 (Electronic) Linking ISSN: 09277765 NLM ISO Abbreviation: Colloids Surf B Biointerfaces Subsets: MEDLINE |
أسماء مطبوعة: | Original Publication: Amsterdam ; New York : Elsevier, c1993- |
مواضيع طبية MeSH: | Drug Delivery Systems*, Folic Acid/*chemistry , Lactones/*chemistry , Methotrexate/*chemistry , Polyethylene Glycols/*chemistry, Animals ; Cell Survival ; Cells, Cultured ; Colloids/chemical synthesis ; Colloids/chemistry ; Hydrogen-Ion Concentration ; Hydrophobic and Hydrophilic Interactions ; Lactones/chemical synthesis ; Mice ; Micelles ; Molecular Structure ; NIH 3T3 Cells ; Particle Size ; Polyethylene Glycols/chemical synthesis ; Surface Properties |
مستخلص: | Hydrophobic drugs, such as methotrexate, are not easily delivered into the human body. Therefore, the use of amphiphilic nanoplatforms to the transport of these drugs through the bloodstream is a challenge. While the hydrophobic region interacts with the drug, the hydrophilic outer layer enhances its bioavailability and circulation time. Poly (ethylene glycol)-block-poly(ε-caprolactone) PEG-b-PCL micelles are biodegradable and biocompatible, allowing its use as a nanocarrier for drug delivery systems. The stealth property of PEG that composes the outer layer of nanoplatforms, makes the micelle unperceivable to phagocytic cells, increasing the circulation time in the human body. In addition, folic acid functionalization enables micelle selectively targeting to cancer cells, improving treatment efficiency and reducing side effects. In this work, PEG-b-PCL copolymer was synthesized by ring opening polymerization (ROP) of the ε-caprolactone with Poly(ethylene glycol) as a macroinitiator and tin(II) 2-ethyl hexanoate as a catalyst. Functionalization of such micelles with folic acid occurred through the modification of the PEG terminal group. The surface modification of the copolymer micelles resulted in higher critical micellar concentration (CMC), increasing approximately 100 times. The synthesis of the copolymers resulted in molecular weight around 3000 g mol -1 with low polydispersity. The polymer micelles have a hydrodynamic diameter in the range of 100-200 nm and the functionalized sample doesn't show aggregation in the considered pH range. High incorporation efficiency was obtained with a minimum percentage of 85%. The drug release profile and linearization from the Peppas model confirmed the interaction of methotrexate with the hydrophobic segment of the copolymer and its release mechanism by relaxation and/or degradation of the chains, making PEG-b-PCL micelles suitable candidates for hydrophobic drug delivery systems. (Copyright © 2019 Elsevier B.V. All rights reserved.) |
فهرسة مساهمة: | Keywords: Copolymer micelles; Methotrexate; PEG-b-PCL; Targeted drug delivery |
المشرفين على المادة: | 0 (Colloids) 0 (Lactones) 0 (Micelles) 0 (poly(ethylene glycol)-block-poly(epsilon-caprolactone)) 3WJQ0SDW1A (Polyethylene Glycols) 935E97BOY8 (Folic Acid) YL5FZ2Y5U1 (Methotrexate) |
تواريخ الأحداث: | Date Created: 20190213 Date Completed: 20190909 Latest Revision: 20190909 |
رمز التحديث: | 20231215 |
DOI: | 10.1016/j.colsurfb.2019.02.008 |
PMID: | 30753959 |
قاعدة البيانات: | MEDLINE |
تدمد: | 1873-4367 |
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DOI: | 10.1016/j.colsurfb.2019.02.008 |