Dataset Information

The Impact of Polymer Size and Cleavability on the Intravenous Pharmacokinetics of PEG-Based Hyperbranched Polymers in Rats.

ABSTRACT: A better understanding of the impact of molecular size and linkers is important for PEG-based hyperbranched polymers (HBPs) intended as tailored drug delivery vehicles. This study aimed to evaluate the effects of crosslinker chemistry (cleavable disulphide versus non-cleavable ethylene glycol methacrylate (EGDMA) linkers) and molecular weight within the expected size range for efficient renal elimination (22 vs. 48 kDa) on the intravenous pharmacokinetic and biodistribution properties of ⁸⁹Zr-labelled HBPs in rats. All HBPs showed similar plasma pharmacokinetics over 72 h, despite differences in linker chemistry and size. A larger proportion of HBP with the cleavable linker was eliminated via the urine and faeces compared to a similar-sized HBP with the non-cleavable linker, while size had no impact on the proportion of the dose excreted. The higher molecular weight HBPs accumulated in organs of the mononuclear phagocyte system (liver and spleen) more avidly than the smaller HBP. These results suggest that HBPs within the 22 to 48 kDa size range show no differences in plasma pharmacokinetics, but distinct patterns of organ biodistribution and elimination are evident.

SUBMITTER: Marasini N

PROVIDER: S-EPMC7762536 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature

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The Impact of Polymer Size and Cleavability on the Intravenous Pharmacokinetics of PEG-Based Hyperbranched Polymers in Rats.

Marasini Nirmal N Fu Changkui C Fletcher Nicholas L NL Subasic Christopher C Er Gerald G Mardon Karine K Thurecht Kristofer J KJ Whittaker Andrew K AK Kaminskas Lisa M LM

Nanomaterials (Basel, Switzerland) 20201208 12

A better understanding of the impact of molecular size and linkers is important for PEG-based hyperbranched polymers (HBPs) intended as tailored drug delivery vehicles. This study aimed to evaluate the effects of crosslinker chemistry (cleavable disulphide versus non-cleavable ethylene glycol methacrylate (EGDMA) linkers) and molecular weight within the expected size range for efficient renal elimination (22 vs. 48 kDa) on the intravenous pharmacokinetic and biodistribution properties of <sup>89 ...[more]

PMID: 33302413

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Project description:A new series of hyperbranched polymers consisting of fluorene-alt-carbazole as the branches and the three-dimensional-structured spiro[3.3]heptane-2,6-dispirofluorene (SDF) as the core were designed and synthesized by one-pot Suzuki coupling polycondensation. A phosphor group with broad full width at half maximum (FWHM) bis(1-phenyl-isoquinoline)(acetylacetonato)iridium(iii) (Ir(Brpiq)2acac, 0.08 mol%) as the red-light emitting unit and bis(2-(4-bromophenyl)-1-[6-(9-carbazolyl)hexyl]-imidazole)(2-(5-(4-fluorinated phenyl)-1,3,4-triazole)pyridine)iridium(iii) ((CzhBrPI)2Ir(fpptz)) as the green-light emitting unit were introduced into the backbones to obtain sunlight-style white-light emission by adjusting the feeding ratios of (CzhBrPI)2Ir(fpptz) (0.08 to 0.32 mol%). The results indicate the synthesized polymers show high thermal stabilities and good amorphous film morphology because of the hyperbranched structures. Besides, the lowest unoccupied molecular orbital (LUMO) levels of polymers were reduced and the electron injection was improved because of excellent electron-transporting ability of the triazole unit in the green group. The hyperbranched structures can effectively suppress the polymers' chain distortion and aggregation, and promote the incomplete Förster resonance energy transfer (FRET) efficiency from fluorene-alt-carbazole segments to Ir complex units. As a result, the devices with hyperbranched polymer light-emitting layers realize white light emission, and the optimized device also exhibits good electroluminescent (EL) performance with Commission Internationale de l'Eclairage (CIE) coordinates at (0.32, 0.31), a maximum luminance of 9054 cd m-2, a maximum current efficiency of 3.59 cd A-1 and a maximum Color Rendering Index (CRI) of 91. The hyperbranched polymers based on fluorene-alt-carbazole branches and a SDF core and high-efficiency phosphor groups with broad full width at half maximum are attractive candidates for sunlight-style white polymer light-emitting device.

Dataset Information

The Impact of Polymer Size and Cleavability on the Intravenous Pharmacokinetics of PEG-Based Hyperbranched Polymers in Rats.

Publications

The Impact of Polymer Size and Cleavability on the Intravenous Pharmacokinetics of PEG-Based Hyperbranched Polymers in Rats.

Similar Datasets

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