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Tytuł:
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In vitro and in vivo delivery of gliclazide loaded mPEG-PCL micelles and its kinetic release and solubility study.
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Autorzy:
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Danafar H; a Zanjan Pharmaceutical Nanotechnology Research Center, Zanjan University of Medical Sciences , Zanjan , Iran.; b Department of Pharmaceutical Nanotechnology , School of Pharmacy, Zanjan University of Medical Sciences , Zanjan , Iran.
Jaberizadeh H; b Department of Pharmaceutical Nanotechnology , School of Pharmacy, Zanjan University of Medical Sciences , Zanjan , Iran.
Andalib S; c Department of Pharmacology and Toxicology , School of Pharmacy, Zanjan University of Medical Sciences , Zanjan , Iran.
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Źródło:
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Artificial cells, nanomedicine, and biotechnology [Artif Cells Nanomed Biotechnol] 2018 Dec; Vol. 46 (8), pp. 1625-1636. Date of Electronic Publication: 2017 Nov 03.
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Typ publikacji:
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Journal Article
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Język:
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English
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Imprint Name(s):
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Publication: 2015- : Abingdon, Oxford : Taylor & Francis
Original Publication: London : Informa Healthcare, [2013]-
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MeSH Terms:
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Gliclazide*/pharmacokinetics
Gliclazide*/pharmacology
Diabetes Mellitus, Experimental/*drug therapy
Animals ; Delayed-Action Preparations/pharmacokinetics ; Delayed-Action Preparations/pharmacology ; Diabetes Mellitus, Experimental/metabolism ; Diabetes Mellitus, Experimental/pathology ; Male ; Micelles ; Rats ; Rats, Wistar ; Solubility
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Contributed Indexing:
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Keywords: Copolymer; gliclazide; micelles; sustained release
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Substance Nomenclature:
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0 (Delayed-Action Preparations)
0 (Micelles)
G4PX8C4HKV (Gliclazide)
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Entry Date(s):
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Date Created: 20171104 Date Completed: 20190220 Latest Revision: 20190320
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Update Code:
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20240104
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DOI:
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10.1080/21691401.2017.1386191
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PMID:
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29099241
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In this study, drug delivery system of gliclazide, a poorly soluble drug, was developed and evaluated in vitro and in vivo. We synthesized five series of mPEG-PCL di block copolymers. The structure of the copolymers was characterized by 1 H-NMR, Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and gel permeation chromatography (GPC) techniques. In this study, gliclazide was encapsulated within micelles through a single-step nano-precipitation method, leading to formation of gliclazide/mPEG-PCL micelles. The resulting micelles were characterized further by various techniques such as DLS and AFM. The serum glucose lowering effect of gliclazide micelles was studied in streptozotocin-diabetic rats and were compared with the gliclazide treated rats. The results showed that the zeta potential of micelles was about -14.9 mV and the average size was 83.12 nm. Gliclazide was encapsulated into mPEG-PCL micelles with loading capacity of 21.05 ± 0.14% and entrapment efficiency of 94.11 ± 0.12%. In vivo testing of the gliclazide micelles in diabetic rats demonstrated a significant antidiabetic effect of gliclazide micelles after the 7 day that lasted for 21 days when compared with gliclazide powder. The results suggest that gliclazide micelles are a valuable system for the sustained delivery of gliclazide.
Erratum in: Artif Cells Nanomed Biotechnol. 2019 Dec;47(1):2240. (PMID: 31172801)
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