Enhanced Antitumor Activity of Lidocaine Nanoparticles Encapsulated by a Self-Assembling Peptide
Although local anesthetics (LAs) such as lidocaine have been traditionally used for pain relief, their antitumor activity has attracted more and more attentions in recent years. However, since nearly all LAs used in clinic are in their hydrochloride forms with small molecular weight and high water-s...
Ausführliche Beschreibung
Autor*in: |
Yang Yang [verfasserIn] Jiaxiao Sun [verfasserIn] Fei Peng [verfasserIn] Haibei Liu [verfasserIn] Guoyan Zhao [verfasserIn] Junjie Chen [verfasserIn] Wensheng Zhang [verfasserIn] Feng Qiu [verfasserIn] |
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Format: |
E-Artikel |
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Sprache: |
Englisch |
Erschienen: |
2022 |
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Schlagwörter: |
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Übergeordnetes Werk: |
In: Frontiers in Pharmacology - Frontiers Media S.A., 2010, 13(2022) |
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Übergeordnetes Werk: |
volume:13 ; year:2022 |
Links: |
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DOI / URN: |
10.3389/fphar.2022.770892 |
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Katalog-ID: |
DOAJ025345826 |
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10.3389/fphar.2022.770892 doi (DE-627)DOAJ025345826 (DE-599)DOAJ25e3bb600aeb4deb8fdb1f756f6a557a DE-627 ger DE-627 rakwb eng RM1-950 Yang Yang verfasserin aut Enhanced Antitumor Activity of Lidocaine Nanoparticles Encapsulated by a Self-Assembling Peptide 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Although local anesthetics (LAs) such as lidocaine have been traditionally used for pain relief, their antitumor activity has attracted more and more attentions in recent years. However, since nearly all LAs used in clinic are in their hydrochloride forms with small molecular weight and high water-solubility, their fast absorption and clearance greatly limit their antitumor activity in vivo. To better exploit the antitumor activity of LAs, lidocaine nanoparticles (LNPs) are prepared by using a self-assembling peptide to encapsulate the hydrophobic base form of lidocaine. In cultured A375 human melanoma cells, the LNPs show much higher cellular uptake level than the clinic formulation of lidocaine hydrochloride, which leads to enhanced efficacy in inhibiting the proliferation, migration and invasion of the cells, as well as in inducing cell apoptosis. Compared with lidocaine hydrochloride, LNPs can also significantly slow down the release rate of lidocaine. In nude mice, LNPs can effectively inhibit the development of solid tumors from seeded A375 cells and prevent the recurrence of tumors after surgical excision. These results indicate that by using self-assembling peptide to fabricate nanoparticle formulations of local anesthetics, their antitumor activity can be significantly enhanced, suggesting a potential postoperative treatment to prevent tumor recurrence after surgical excision. lidocaine antitumor activity self-assembling peptide local anesthetics nanoparticles tumor recurrence Therapeutics. Pharmacology Yang Yang verfasserin aut Jiaxiao Sun verfasserin aut Fei Peng verfasserin aut Fei Peng verfasserin aut Haibei Liu verfasserin aut Haibei Liu verfasserin aut Guoyan Zhao verfasserin aut Guoyan Zhao verfasserin aut Junjie Chen verfasserin aut Wensheng Zhang verfasserin aut Wensheng Zhang verfasserin aut Feng Qiu verfasserin aut Feng Qiu verfasserin aut In Frontiers in Pharmacology Frontiers Media S.A., 2010 13(2022) (DE-627)642889392 (DE-600)2587355-6 16639812 nnns volume:13 year:2022 https://doi.org/10.3389/fphar.2022.770892 kostenfrei https://doaj.org/article/25e3bb600aeb4deb8fdb1f756f6a557a kostenfrei https://www.frontiersin.org/articles/10.3389/fphar.2022.770892/full kostenfrei https://doaj.org/toc/1663-9812 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2003 GBV_ILN_2014 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 13 2022 |
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Although local anesthetics (LAs) such as lidocaine have been traditionally used for pain relief, their antitumor activity has attracted more and more attentions in recent years. However, since nearly all LAs used in clinic are in their hydrochloride forms with small molecular weight and high water-solubility, their fast absorption and clearance greatly limit their antitumor activity in vivo. To better exploit the antitumor activity of LAs, lidocaine nanoparticles (LNPs) are prepared by using a self-assembling peptide to encapsulate the hydrophobic base form of lidocaine. In cultured A375 human melanoma cells, the LNPs show much higher cellular uptake level than the clinic formulation of lidocaine hydrochloride, which leads to enhanced efficacy in inhibiting the proliferation, migration and invasion of the cells, as well as in inducing cell apoptosis. Compared with lidocaine hydrochloride, LNPs can also significantly slow down the release rate of lidocaine. In nude mice, LNPs can effectively inhibit the development of solid tumors from seeded A375 cells and prevent the recurrence of tumors after surgical excision. These results indicate that by using self-assembling peptide to fabricate nanoparticle formulations of local anesthetics, their antitumor activity can be significantly enhanced, suggesting a potential postoperative treatment to prevent tumor recurrence after surgical excision. |
abstractGer |
Although local anesthetics (LAs) such as lidocaine have been traditionally used for pain relief, their antitumor activity has attracted more and more attentions in recent years. However, since nearly all LAs used in clinic are in their hydrochloride forms with small molecular weight and high water-solubility, their fast absorption and clearance greatly limit their antitumor activity in vivo. To better exploit the antitumor activity of LAs, lidocaine nanoparticles (LNPs) are prepared by using a self-assembling peptide to encapsulate the hydrophobic base form of lidocaine. In cultured A375 human melanoma cells, the LNPs show much higher cellular uptake level than the clinic formulation of lidocaine hydrochloride, which leads to enhanced efficacy in inhibiting the proliferation, migration and invasion of the cells, as well as in inducing cell apoptosis. Compared with lidocaine hydrochloride, LNPs can also significantly slow down the release rate of lidocaine. In nude mice, LNPs can effectively inhibit the development of solid tumors from seeded A375 cells and prevent the recurrence of tumors after surgical excision. These results indicate that by using self-assembling peptide to fabricate nanoparticle formulations of local anesthetics, their antitumor activity can be significantly enhanced, suggesting a potential postoperative treatment to prevent tumor recurrence after surgical excision. |
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Although local anesthetics (LAs) such as lidocaine have been traditionally used for pain relief, their antitumor activity has attracted more and more attentions in recent years. However, since nearly all LAs used in clinic are in their hydrochloride forms with small molecular weight and high water-solubility, their fast absorption and clearance greatly limit their antitumor activity in vivo. To better exploit the antitumor activity of LAs, lidocaine nanoparticles (LNPs) are prepared by using a self-assembling peptide to encapsulate the hydrophobic base form of lidocaine. In cultured A375 human melanoma cells, the LNPs show much higher cellular uptake level than the clinic formulation of lidocaine hydrochloride, which leads to enhanced efficacy in inhibiting the proliferation, migration and invasion of the cells, as well as in inducing cell apoptosis. Compared with lidocaine hydrochloride, LNPs can also significantly slow down the release rate of lidocaine. In nude mice, LNPs can effectively inhibit the development of solid tumors from seeded A375 cells and prevent the recurrence of tumors after surgical excision. These results indicate that by using self-assembling peptide to fabricate nanoparticle formulations of local anesthetics, their antitumor activity can be significantly enhanced, suggesting a potential postoperative treatment to prevent tumor recurrence after surgical excision. |
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However, since nearly all LAs used in clinic are in their hydrochloride forms with small molecular weight and high water-solubility, their fast absorption and clearance greatly limit their antitumor activity in vivo. To better exploit the antitumor activity of LAs, lidocaine nanoparticles (LNPs) are prepared by using a self-assembling peptide to encapsulate the hydrophobic base form of lidocaine. In cultured A375 human melanoma cells, the LNPs show much higher cellular uptake level than the clinic formulation of lidocaine hydrochloride, which leads to enhanced efficacy in inhibiting the proliferation, migration and invasion of the cells, as well as in inducing cell apoptosis. Compared with lidocaine hydrochloride, LNPs can also significantly slow down the release rate of lidocaine. In nude mice, LNPs can effectively inhibit the development of solid tumors from seeded A375 cells and prevent the recurrence of tumors after surgical excision. 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