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Tytuł:
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Molecular mechanism of high capacity-high release transdermal drug delivery patch with carboxyl acrylate polymer: Roles of ion-ion repulsion and hydrogen bond.
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Autorzy:
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Yang D; Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning, 110016, China.
Liu C; Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning, 110016, China.
Quan P; Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning, 110016, China.
Fang L; Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning, 110016, China. Electronic address: .
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Źródło:
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International journal of pharmaceutics [Int J Pharm] 2020 Jul 30; Vol. 585, pp. 119376. Date of Electronic Publication: 2020 May 23.
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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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Original Publication: Amsterdam, Elsevier/North-Holland Biomedical Press.
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MeSH Terms:
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Hydrogen Bonding*
Transdermal Patch*
Acrylates/*chemistry
Anti-Inflammatory Agents, Non-Steroidal/*pharmacokinetics
Skin Absorption/*physiology
Animals ; Chemistry, Pharmaceutical ; Drug Liberation ; Excipients/chemistry ; Male ; Photoelectron Spectroscopy ; Rats ; Rats, Wistar ; Skin/metabolism ; Spectroscopy, Fourier Transform Infrared ; Spectrum Analysis, Raman ; Technology, Pharmaceutical
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Contributed Indexing:
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Keywords: Carboxyl polyacrylate polymer; High drug release; High loading capacity; Hydrogen bond; Ion-ion repulsion; Transdermal patch
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Substance Nomenclature:
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0 (Acrylates)
0 (Anti-Inflammatory Agents, Non-Steroidal)
0 (Excipients)
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Entry Date(s):
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Date Created: 20200527 Date Completed: 20210303 Latest Revision: 20210303
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Update Code:
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20240105
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DOI:
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10.1016/j.ijpharm.2020.119376
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PMID:
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32454131
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In this study, a high capacity-high release transdermal patch was conducted with COOH polyacrylate polymer (PA-1) and non-steroidal anti-inflammatory drugs (NSAIDs), which were characterized using miscibility study, in vitro drug release, drug skin absorption studies in vitro and in vivo. And ibuprofen with the highest cargo loading capacity was chosen as a model drug to investigate innovative molecular mechanism, which was proposed based on ion-ion repulsion and hydrogen bond by FT-IR, Raman, 13 C NMR and X-ray photoelectron spectroscopy (XPS). Drug loading and skin absorption in PA-1 was improved up to 2.4 and 2.5 times, respectively. The hydrogen bond formed between drug (COOH) and PA-1 (COOH) was weaken by repulsive interaction using FT-IR and Raman spectra, and molecular mobility of PA-1 was elevated by dielectric spectroscopy. And COO - was confirmed as molecular basis of repulsion in PA-1 through new peak appearance (α-carbon of COOH: 77.22 ppm) of 13 C NMR and 9% increased carbonyl content in XPS spectra. It was further confirmed by enhanced conductivity of PA-1 with dielectric spectroscopy, EPR spectra, four-point probe method and molecular modeling by appearance of COO - . In conclusion, our results revealed that ion-ion repulsion decreased hydrogen bonding to construct a high capacity-high release patch.
Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2020. Published by Elsevier B.V.)
