Pyrrolidone-modified PAMAM dendrimers enhance anti-inflammatory potential of indomethacin in vitro

Michał Gorzkiewicz; Anna Janaszewska; Mario Ficker; Søren W. Svenningsen; Jørn B. Christensen; Barbara Klajnert-Maculewicz

doi:10.1016/j.colsurfb.2019.06.056

Pyrrolidone-modified PAMAM dendrimers enhance anti-inflammatory potential of indomethacin in vitro

Michał Gorzkiewicz, Anna Janaszewska, Mario Ficker, Søren W. Svenningsen, Jørn B. Christensen, Barbara Klajnert-Maculewicz

4 Citations (Scopus)

Abstract

The therapeutic effect of indomethacin, a water-insoluble non-steroidal anti-inflammatory drug, requires its efficient transport through cellular membranes and accumulation inside the target cells. The application of dendritic polymers has been proposed for the improvement of the drug's solubility and intracellular delivery. In this study we evaluated the anti-inflammatory potential of novel, highly-biocompatible 4-carbomethoxypyrrolidone-coated PAMAM dendrimers loaded with indomethacin. Our results indicate that complexation with dendrimers do not hamper the inhibitory action of indomethacin towards cyclooxygenases. Drug-dendrimer formulations exhibited improved anti-inflammatory activity in in vitro-cultured cellular models, showing enhanced inhibition of prostaglandin secretion and significantly decreased expression of NF-κB marker genes compared to free drug.

Original language	English
Journal	Colloids and Surfaces B: Biointerfaces
Volume	181
Pages (from-to)	959-962
ISSN	0927-7765
DOIs	https://doi.org/10.1016/j.colsurfb.2019.06.056
Publication status	Published - 1 Sept 2019

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title = "Pyrrolidone-modified PAMAM dendrimers enhance anti-inflammatory potential of indomethacin in vitro",

abstract = "The therapeutic effect of indomethacin, a water-insoluble non-steroidal anti-inflammatory drug, requires its efficient transport through cellular membranes and accumulation inside the target cells. The application of dendritic polymers has been proposed for the improvement of the drug's solubility and intracellular delivery. In this study we evaluated the anti-inflammatory potential of novel, highly-biocompatible 4-carbomethoxypyrrolidone-coated PAMAM dendrimers loaded with indomethacin. Our results indicate that complexation with dendrimers do not hamper the inhibitory action of indomethacin towards cyclooxygenases. Drug-dendrimer formulations exhibited improved anti-inflammatory activity in in vitro-cultured cellular models, showing enhanced inhibition of prostaglandin secretion and significantly decreased expression of NF-κB marker genes compared to free drug.",

author = "Micha{\l} Gorzkiewicz and Anna Janaszewska and Mario Ficker and Svenningsen, {S{\o}ren W.} and Christensen, {J{\o}rn B.} and Barbara Klajnert-Maculewicz",

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doi = "10.1016/j.colsurfb.2019.06.056",

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TY - JOUR

T1 - Pyrrolidone-modified PAMAM dendrimers enhance anti-inflammatory potential of indomethacin in vitro

AU - Gorzkiewicz, Michał

AU - Janaszewska, Anna

AU - Ficker, Mario

AU - Svenningsen, Søren W.

AU - Christensen, Jørn B.

AU - Klajnert-Maculewicz, Barbara

PY - 2019/9/1

Y1 - 2019/9/1

N2 - The therapeutic effect of indomethacin, a water-insoluble non-steroidal anti-inflammatory drug, requires its efficient transport through cellular membranes and accumulation inside the target cells. The application of dendritic polymers has been proposed for the improvement of the drug's solubility and intracellular delivery. In this study we evaluated the anti-inflammatory potential of novel, highly-biocompatible 4-carbomethoxypyrrolidone-coated PAMAM dendrimers loaded with indomethacin. Our results indicate that complexation with dendrimers do not hamper the inhibitory action of indomethacin towards cyclooxygenases. Drug-dendrimer formulations exhibited improved anti-inflammatory activity in in vitro-cultured cellular models, showing enhanced inhibition of prostaglandin secretion and significantly decreased expression of NF-κB marker genes compared to free drug.

AB - The therapeutic effect of indomethacin, a water-insoluble non-steroidal anti-inflammatory drug, requires its efficient transport through cellular membranes and accumulation inside the target cells. The application of dendritic polymers has been proposed for the improvement of the drug's solubility and intracellular delivery. In this study we evaluated the anti-inflammatory potential of novel, highly-biocompatible 4-carbomethoxypyrrolidone-coated PAMAM dendrimers loaded with indomethacin. Our results indicate that complexation with dendrimers do not hamper the inhibitory action of indomethacin towards cyclooxygenases. Drug-dendrimer formulations exhibited improved anti-inflammatory activity in in vitro-cultured cellular models, showing enhanced inhibition of prostaglandin secretion and significantly decreased expression of NF-κB marker genes compared to free drug.

U2 - 10.1016/j.colsurfb.2019.06.056

DO - 10.1016/j.colsurfb.2019.06.056

M3 - Journal article

C2 - 31382346

SN - 0927-7765

VL - 181

SP - 959

EP - 962

JO - Colloids and Surfaces B: Biointerfaces

JF - Colloids and Surfaces B: Biointerfaces

ER -

Pyrrolidone-modified PAMAM dendrimers enhance anti-inflammatory potential of indomethacin in vitro

Abstract

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