Micellar Form of a Ferrocene-Containing Camphor Sulfonamide with Improved Aqueous Solubility and Tumor Curing Potential

The discovery of new anticancer drugs with а higher, more specific activity and diminished side effects than the conventional chemotherapeutic agents is a tremendous challenge to contemporary medical research and development. To achieve a pronounced efficacy, the design of antitumor agents can combi...
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Autor*in:	Maria Schröder [verfasserIn] Maria Petrova [verfasserIn] Georgi M. Dobrikov [verfasserIn] Georgy Grancharov [verfasserIn] Denitsa Momekova [verfasserIn] Petar D. Petrov [verfasserIn] Iva Ugrinova [verfasserIn]

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2023

Schlagwörter:	block copolymers polymeric micelles cancer therapy ferrocene-based drugs

Übergeordnetes Werk:	In: Pharmaceutics - MDPI AG, 2010, 15(2023), 3, p 791
Übergeordnetes Werk:	volume:15 ; year:2023 ; number:3, p 791

Links:	Link aufrufen Link aufrufen Link aufrufen Journal toc

DOI / URN:	10.3390/pharmaceutics15030791

Katalog-ID:	DOAJ087266881

Internformat


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520			\|a The discovery of new anticancer drugs with а higher, more specific activity and diminished side effects than the conventional chemotherapeutic agents is a tremendous challenge to contemporary medical research and development. To achieve a pronounced efficacy, the design of antitumor agents can combine various biologically active subunits in one molecule, which can affect different regulatory pathways in cancer cells. We recently demonstrated that a newly synthesized organometallic compound, a ferrocene-containing camphor sulfonamide (DK164), possesses promising antiproliferative activity against breast and lung cancer cells. However, it still encounters the problem of solubility in biological fluids. In this work, we describe a novel micellar form of DK164 with significantly improved solubility in aqueous medium. DK164 was embedded in biodegradable micelles based on a poly(ethylene oxide)-<i<b</i<-poly(<i<α-</i<cinnamyl-<i<ε-</i<caprolactone-<i<co-ε</i<-caprolactone)-<i<b</i<-poly(ethylene oxide) triblock copolymer (PEO<sub<113</sub<-<i<b</i<-P(CyCL<sub<3</sub<-<i<co</i<-CL<sub<46</sub<)-<i<b</i<-PEO<sub<113</sub<), and the physicochemical parameters (size, size distribution, zeta potential, encapsulation efficiency) and biological activity of the obtained system were studied. We used cytotoxicity assays and flow cytometry to determine the type of cell death, as well as immunocytochemistry to assess the influence of the encapsulated drug on the dynamics of cellular key proteins (p53 and NFkB) and the process of autophagy. According to our results, the micellar form of the organometallic ferrocene derivate (DK164-NP) exhibited several advantages compared to the free substance, such as higher metabolic stability, better cellular uptake, improved bioavailability, and long-term activity, maintaining nearly the same biological activity and anticancer properties of the drug.
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allfields	10.3390/pharmaceutics15030791 doi (DE-627)DOAJ087266881 (DE-599)DOAJ262cfa7c7cf64137b0dd1ba4daf23c67 DE-627 ger DE-627 rakwb eng RS1-441 Maria Schröder verfasserin aut Micellar Form of a Ferrocene-Containing Camphor Sulfonamide with Improved Aqueous Solubility and Tumor Curing Potential 2023 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier The discovery of new anticancer drugs with а higher, more specific activity and diminished side effects than the conventional chemotherapeutic agents is a tremendous challenge to contemporary medical research and development. To achieve a pronounced efficacy, the design of antitumor agents can combine various biologically active subunits in one molecule, which can affect different regulatory pathways in cancer cells. We recently demonstrated that a newly synthesized organometallic compound, a ferrocene-containing camphor sulfonamide (DK164), possesses promising antiproliferative activity against breast and lung cancer cells. However, it still encounters the problem of solubility in biological fluids. In this work, we describe a novel micellar form of DK164 with significantly improved solubility in aqueous medium. DK164 was embedded in biodegradable micelles based on a poly(ethylene oxide)-<i<b</i<-poly(<i<α-</i<cinnamyl-<i<ε-</i<caprolactone-<i<co-ε</i<-caprolactone)-<i<b</i<-poly(ethylene oxide) triblock copolymer (PEO<sub<113</sub<-<i<b</i<-P(CyCL<sub<3</sub<-<i<co</i<-CL<sub<46</sub<)-<i<b</i<-PEO<sub<113</sub<), and the physicochemical parameters (size, size distribution, zeta potential, encapsulation efficiency) and biological activity of the obtained system were studied. We used cytotoxicity assays and flow cytometry to determine the type of cell death, as well as immunocytochemistry to assess the influence of the encapsulated drug on the dynamics of cellular key proteins (p53 and NFkB) and the process of autophagy. According to our results, the micellar form of the organometallic ferrocene derivate (DK164-NP) exhibited several advantages compared to the free substance, such as higher metabolic stability, better cellular uptake, improved bioavailability, and long-term activity, maintaining nearly the same biological activity and anticancer properties of the drug. block copolymers polymeric micelles cancer therapy ferrocene-based drugs Pharmacy and materia medica Maria Petrova verfasserin aut Georgi M. Dobrikov verfasserin aut Georgy Grancharov verfasserin aut Denitsa Momekova verfasserin aut Petar D. Petrov verfasserin aut Iva Ugrinova verfasserin aut In Pharmaceutics MDPI AG, 2010 15(2023), 3, p 791 (DE-627)614096529 (DE-600)2527217-2 19994923 nnns volume:15 year:2023 number:3, p 791 https://doi.org/10.3390/pharmaceutics15030791 kostenfrei https://doaj.org/article/262cfa7c7cf64137b0dd1ba4daf23c67 kostenfrei https://www.mdpi.com/1999-4923/15/3/791 kostenfrei https://doaj.org/toc/1999-4923 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 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_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 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 15 2023 3, p 791
spelling	10.3390/pharmaceutics15030791 doi (DE-627)DOAJ087266881 (DE-599)DOAJ262cfa7c7cf64137b0dd1ba4daf23c67 DE-627 ger DE-627 rakwb eng RS1-441 Maria Schröder verfasserin aut Micellar Form of a Ferrocene-Containing Camphor Sulfonamide with Improved Aqueous Solubility and Tumor Curing Potential 2023 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier The discovery of new anticancer drugs with а higher, more specific activity and diminished side effects than the conventional chemotherapeutic agents is a tremendous challenge to contemporary medical research and development. To achieve a pronounced efficacy, the design of antitumor agents can combine various biologically active subunits in one molecule, which can affect different regulatory pathways in cancer cells. We recently demonstrated that a newly synthesized organometallic compound, a ferrocene-containing camphor sulfonamide (DK164), possesses promising antiproliferative activity against breast and lung cancer cells. However, it still encounters the problem of solubility in biological fluids. In this work, we describe a novel micellar form of DK164 with significantly improved solubility in aqueous medium. DK164 was embedded in biodegradable micelles based on a poly(ethylene oxide)-<i<b</i<-poly(<i<α-</i<cinnamyl-<i<ε-</i<caprolactone-<i<co-ε</i<-caprolactone)-<i<b</i<-poly(ethylene oxide) triblock copolymer (PEO<sub<113</sub<-<i<b</i<-P(CyCL<sub<3</sub<-<i<co</i<-CL<sub<46</sub<)-<i<b</i<-PEO<sub<113</sub<), and the physicochemical parameters (size, size distribution, zeta potential, encapsulation efficiency) and biological activity of the obtained system were studied. We used cytotoxicity assays and flow cytometry to determine the type of cell death, as well as immunocytochemistry to assess the influence of the encapsulated drug on the dynamics of cellular key proteins (p53 and NFkB) and the process of autophagy. According to our results, the micellar form of the organometallic ferrocene derivate (DK164-NP) exhibited several advantages compared to the free substance, such as higher metabolic stability, better cellular uptake, improved bioavailability, and long-term activity, maintaining nearly the same biological activity and anticancer properties of the drug. block copolymers polymeric micelles cancer therapy ferrocene-based drugs Pharmacy and materia medica Maria Petrova verfasserin aut Georgi M. Dobrikov verfasserin aut Georgy Grancharov verfasserin aut Denitsa Momekova verfasserin aut Petar D. Petrov verfasserin aut Iva Ugrinova verfasserin aut In Pharmaceutics MDPI AG, 2010 15(2023), 3, p 791 (DE-627)614096529 (DE-600)2527217-2 19994923 nnns volume:15 year:2023 number:3, p 791 https://doi.org/10.3390/pharmaceutics15030791 kostenfrei https://doaj.org/article/262cfa7c7cf64137b0dd1ba4daf23c67 kostenfrei https://www.mdpi.com/1999-4923/15/3/791 kostenfrei https://doaj.org/toc/1999-4923 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 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_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 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 15 2023 3, p 791
allfields_unstemmed	10.3390/pharmaceutics15030791 doi (DE-627)DOAJ087266881 (DE-599)DOAJ262cfa7c7cf64137b0dd1ba4daf23c67 DE-627 ger DE-627 rakwb eng RS1-441 Maria Schröder verfasserin aut Micellar Form of a Ferrocene-Containing Camphor Sulfonamide with Improved Aqueous Solubility and Tumor Curing Potential 2023 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier The discovery of new anticancer drugs with а higher, more specific activity and diminished side effects than the conventional chemotherapeutic agents is a tremendous challenge to contemporary medical research and development. To achieve a pronounced efficacy, the design of antitumor agents can combine various biologically active subunits in one molecule, which can affect different regulatory pathways in cancer cells. We recently demonstrated that a newly synthesized organometallic compound, a ferrocene-containing camphor sulfonamide (DK164), possesses promising antiproliferative activity against breast and lung cancer cells. However, it still encounters the problem of solubility in biological fluids. In this work, we describe a novel micellar form of DK164 with significantly improved solubility in aqueous medium. DK164 was embedded in biodegradable micelles based on a poly(ethylene oxide)-<i<b</i<-poly(<i<α-</i<cinnamyl-<i<ε-</i<caprolactone-<i<co-ε</i<-caprolactone)-<i<b</i<-poly(ethylene oxide) triblock copolymer (PEO<sub<113</sub<-<i<b</i<-P(CyCL<sub<3</sub<-<i<co</i<-CL<sub<46</sub<)-<i<b</i<-PEO<sub<113</sub<), and the physicochemical parameters (size, size distribution, zeta potential, encapsulation efficiency) and biological activity of the obtained system were studied. We used cytotoxicity assays and flow cytometry to determine the type of cell death, as well as immunocytochemistry to assess the influence of the encapsulated drug on the dynamics of cellular key proteins (p53 and NFkB) and the process of autophagy. According to our results, the micellar form of the organometallic ferrocene derivate (DK164-NP) exhibited several advantages compared to the free substance, such as higher metabolic stability, better cellular uptake, improved bioavailability, and long-term activity, maintaining nearly the same biological activity and anticancer properties of the drug. block copolymers polymeric micelles cancer therapy ferrocene-based drugs Pharmacy and materia medica Maria Petrova verfasserin aut Georgi M. Dobrikov verfasserin aut Georgy Grancharov verfasserin aut Denitsa Momekova verfasserin aut Petar D. Petrov verfasserin aut Iva Ugrinova verfasserin aut In Pharmaceutics MDPI AG, 2010 15(2023), 3, p 791 (DE-627)614096529 (DE-600)2527217-2 19994923 nnns volume:15 year:2023 number:3, p 791 https://doi.org/10.3390/pharmaceutics15030791 kostenfrei https://doaj.org/article/262cfa7c7cf64137b0dd1ba4daf23c67 kostenfrei https://www.mdpi.com/1999-4923/15/3/791 kostenfrei https://doaj.org/toc/1999-4923 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 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_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 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 15 2023 3, p 791
allfieldsGer	10.3390/pharmaceutics15030791 doi (DE-627)DOAJ087266881 (DE-599)DOAJ262cfa7c7cf64137b0dd1ba4daf23c67 DE-627 ger DE-627 rakwb eng RS1-441 Maria Schröder verfasserin aut Micellar Form of a Ferrocene-Containing Camphor Sulfonamide with Improved Aqueous Solubility and Tumor Curing Potential 2023 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier The discovery of new anticancer drugs with а higher, more specific activity and diminished side effects than the conventional chemotherapeutic agents is a tremendous challenge to contemporary medical research and development. To achieve a pronounced efficacy, the design of antitumor agents can combine various biologically active subunits in one molecule, which can affect different regulatory pathways in cancer cells. We recently demonstrated that a newly synthesized organometallic compound, a ferrocene-containing camphor sulfonamide (DK164), possesses promising antiproliferative activity against breast and lung cancer cells. However, it still encounters the problem of solubility in biological fluids. In this work, we describe a novel micellar form of DK164 with significantly improved solubility in aqueous medium. DK164 was embedded in biodegradable micelles based on a poly(ethylene oxide)-<i<b</i<-poly(<i<α-</i<cinnamyl-<i<ε-</i<caprolactone-<i<co-ε</i<-caprolactone)-<i<b</i<-poly(ethylene oxide) triblock copolymer (PEO<sub<113</sub<-<i<b</i<-P(CyCL<sub<3</sub<-<i<co</i<-CL<sub<46</sub<)-<i<b</i<-PEO<sub<113</sub<), and the physicochemical parameters (size, size distribution, zeta potential, encapsulation efficiency) and biological activity of the obtained system were studied. We used cytotoxicity assays and flow cytometry to determine the type of cell death, as well as immunocytochemistry to assess the influence of the encapsulated drug on the dynamics of cellular key proteins (p53 and NFkB) and the process of autophagy. According to our results, the micellar form of the organometallic ferrocene derivate (DK164-NP) exhibited several advantages compared to the free substance, such as higher metabolic stability, better cellular uptake, improved bioavailability, and long-term activity, maintaining nearly the same biological activity and anticancer properties of the drug. block copolymers polymeric micelles cancer therapy ferrocene-based drugs Pharmacy and materia medica Maria Petrova verfasserin aut Georgi M. Dobrikov verfasserin aut Georgy Grancharov verfasserin aut Denitsa Momekova verfasserin aut Petar D. Petrov verfasserin aut Iva Ugrinova verfasserin aut In Pharmaceutics MDPI AG, 2010 15(2023), 3, p 791 (DE-627)614096529 (DE-600)2527217-2 19994923 nnns volume:15 year:2023 number:3, p 791 https://doi.org/10.3390/pharmaceutics15030791 kostenfrei https://doaj.org/article/262cfa7c7cf64137b0dd1ba4daf23c67 kostenfrei https://www.mdpi.com/1999-4923/15/3/791 kostenfrei https://doaj.org/toc/1999-4923 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 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_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 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 15 2023 3, p 791
allfieldsSound	10.3390/pharmaceutics15030791 doi (DE-627)DOAJ087266881 (DE-599)DOAJ262cfa7c7cf64137b0dd1ba4daf23c67 DE-627 ger DE-627 rakwb eng RS1-441 Maria Schröder verfasserin aut Micellar Form of a Ferrocene-Containing Camphor Sulfonamide with Improved Aqueous Solubility and Tumor Curing Potential 2023 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier The discovery of new anticancer drugs with а higher, more specific activity and diminished side effects than the conventional chemotherapeutic agents is a tremendous challenge to contemporary medical research and development. To achieve a pronounced efficacy, the design of antitumor agents can combine various biologically active subunits in one molecule, which can affect different regulatory pathways in cancer cells. We recently demonstrated that a newly synthesized organometallic compound, a ferrocene-containing camphor sulfonamide (DK164), possesses promising antiproliferative activity against breast and lung cancer cells. However, it still encounters the problem of solubility in biological fluids. In this work, we describe a novel micellar form of DK164 with significantly improved solubility in aqueous medium. DK164 was embedded in biodegradable micelles based on a poly(ethylene oxide)-<i<b</i<-poly(<i<α-</i<cinnamyl-<i<ε-</i<caprolactone-<i<co-ε</i<-caprolactone)-<i<b</i<-poly(ethylene oxide) triblock copolymer (PEO<sub<113</sub<-<i<b</i<-P(CyCL<sub<3</sub<-<i<co</i<-CL<sub<46</sub<)-<i<b</i<-PEO<sub<113</sub<), and the physicochemical parameters (size, size distribution, zeta potential, encapsulation efficiency) and biological activity of the obtained system were studied. We used cytotoxicity assays and flow cytometry to determine the type of cell death, as well as immunocytochemistry to assess the influence of the encapsulated drug on the dynamics of cellular key proteins (p53 and NFkB) and the process of autophagy. According to our results, the micellar form of the organometallic ferrocene derivate (DK164-NP) exhibited several advantages compared to the free substance, such as higher metabolic stability, better cellular uptake, improved bioavailability, and long-term activity, maintaining nearly the same biological activity and anticancer properties of the drug. block copolymers polymeric micelles cancer therapy ferrocene-based drugs Pharmacy and materia medica Maria Petrova verfasserin aut Georgi M. Dobrikov verfasserin aut Georgy Grancharov verfasserin aut Denitsa Momekova verfasserin aut Petar D. Petrov verfasserin aut Iva Ugrinova verfasserin aut In Pharmaceutics MDPI AG, 2010 15(2023), 3, p 791 (DE-627)614096529 (DE-600)2527217-2 19994923 nnns volume:15 year:2023 number:3, p 791 https://doi.org/10.3390/pharmaceutics15030791 kostenfrei https://doaj.org/article/262cfa7c7cf64137b0dd1ba4daf23c67 kostenfrei https://www.mdpi.com/1999-4923/15/3/791 kostenfrei https://doaj.org/toc/1999-4923 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 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_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 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 15 2023 3, p 791
language	English
source	In Pharmaceutics 15(2023), 3, p 791 volume:15 year:2023 number:3, p 791
sourceStr	In Pharmaceutics 15(2023), 3, p 791 volume:15 year:2023 number:3, p 791
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topic_facet	block copolymers polymeric micelles cancer therapy ferrocene-based drugs Pharmacy and materia medica
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container_title	Pharmaceutics
authorswithroles_txt_mv	Maria Schröder @@aut@@ Maria Petrova @@aut@@ Georgi M. Dobrikov @@aut@@ Georgy Grancharov @@aut@@ Denitsa Momekova @@aut@@ Petar D. Petrov @@aut@@ Iva Ugrinova @@aut@@
publishDateDaySort_date	2023-01-01T00:00:00Z
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author	Maria Schröder
spellingShingle	Maria Schröder misc RS1-441 misc block copolymers misc polymeric micelles misc cancer therapy misc ferrocene-based drugs misc Pharmacy and materia medica Micellar Form of a Ferrocene-Containing Camphor Sulfonamide with Improved Aqueous Solubility and Tumor Curing Potential
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topic_title	RS1-441 Micellar Form of a Ferrocene-Containing Camphor Sulfonamide with Improved Aqueous Solubility and Tumor Curing Potential block copolymers polymeric micelles cancer therapy ferrocene-based drugs
topic	misc RS1-441 misc block copolymers misc polymeric micelles misc cancer therapy misc ferrocene-based drugs misc Pharmacy and materia medica
topic_unstemmed	misc RS1-441 misc block copolymers misc polymeric micelles misc cancer therapy misc ferrocene-based drugs misc Pharmacy and materia medica
topic_browse	misc RS1-441 misc block copolymers misc polymeric micelles misc cancer therapy misc ferrocene-based drugs misc Pharmacy and materia medica
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title	Micellar Form of a Ferrocene-Containing Camphor Sulfonamide with Improved Aqueous Solubility and Tumor Curing Potential
ctrlnum	(DE-627)DOAJ087266881 (DE-599)DOAJ262cfa7c7cf64137b0dd1ba4daf23c67
title_full	Micellar Form of a Ferrocene-Containing Camphor Sulfonamide with Improved Aqueous Solubility and Tumor Curing Potential
author_sort	Maria Schröder
journal	Pharmaceutics
journalStr	Pharmaceutics
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author_browse	Maria Schröder Maria Petrova Georgi M. Dobrikov Georgy Grancharov Denitsa Momekova Petar D. Petrov Iva Ugrinova
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author-letter	Maria Schröder
doi_str_mv	10.3390/pharmaceutics15030791
author2-role	verfasserin
title_sort	micellar form of a ferrocene-containing camphor sulfonamide with improved aqueous solubility and tumor curing potential
callnumber	RS1-441
title_auth	Micellar Form of a Ferrocene-Containing Camphor Sulfonamide with Improved Aqueous Solubility and Tumor Curing Potential
abstract	The discovery of new anticancer drugs with а higher, more specific activity and diminished side effects than the conventional chemotherapeutic agents is a tremendous challenge to contemporary medical research and development. To achieve a pronounced efficacy, the design of antitumor agents can combine various biologically active subunits in one molecule, which can affect different regulatory pathways in cancer cells. We recently demonstrated that a newly synthesized organometallic compound, a ferrocene-containing camphor sulfonamide (DK164), possesses promising antiproliferative activity against breast and lung cancer cells. However, it still encounters the problem of solubility in biological fluids. In this work, we describe a novel micellar form of DK164 with significantly improved solubility in aqueous medium. DK164 was embedded in biodegradable micelles based on a poly(ethylene oxide)-<i<b</i<-poly(<i<α-</i<cinnamyl-<i<ε-</i<caprolactone-<i<co-ε</i<-caprolactone)-<i<b</i<-poly(ethylene oxide) triblock copolymer (PEO<sub<113</sub<-<i<b</i<-P(CyCL<sub<3</sub<-<i<co</i<-CL<sub<46</sub<)-<i<b</i<-PEO<sub<113</sub<), and the physicochemical parameters (size, size distribution, zeta potential, encapsulation efficiency) and biological activity of the obtained system were studied. We used cytotoxicity assays and flow cytometry to determine the type of cell death, as well as immunocytochemistry to assess the influence of the encapsulated drug on the dynamics of cellular key proteins (p53 and NFkB) and the process of autophagy. According to our results, the micellar form of the organometallic ferrocene derivate (DK164-NP) exhibited several advantages compared to the free substance, such as higher metabolic stability, better cellular uptake, improved bioavailability, and long-term activity, maintaining nearly the same biological activity and anticancer properties of the drug.
abstractGer	The discovery of new anticancer drugs with а higher, more specific activity and diminished side effects than the conventional chemotherapeutic agents is a tremendous challenge to contemporary medical research and development. To achieve a pronounced efficacy, the design of antitumor agents can combine various biologically active subunits in one molecule, which can affect different regulatory pathways in cancer cells. We recently demonstrated that a newly synthesized organometallic compound, a ferrocene-containing camphor sulfonamide (DK164), possesses promising antiproliferative activity against breast and lung cancer cells. However, it still encounters the problem of solubility in biological fluids. In this work, we describe a novel micellar form of DK164 with significantly improved solubility in aqueous medium. DK164 was embedded in biodegradable micelles based on a poly(ethylene oxide)-<i<b</i<-poly(<i<α-</i<cinnamyl-<i<ε-</i<caprolactone-<i<co-ε</i<-caprolactone)-<i<b</i<-poly(ethylene oxide) triblock copolymer (PEO<sub<113</sub<-<i<b</i<-P(CyCL<sub<3</sub<-<i<co</i<-CL<sub<46</sub<)-<i<b</i<-PEO<sub<113</sub<), and the physicochemical parameters (size, size distribution, zeta potential, encapsulation efficiency) and biological activity of the obtained system were studied. We used cytotoxicity assays and flow cytometry to determine the type of cell death, as well as immunocytochemistry to assess the influence of the encapsulated drug on the dynamics of cellular key proteins (p53 and NFkB) and the process of autophagy. According to our results, the micellar form of the organometallic ferrocene derivate (DK164-NP) exhibited several advantages compared to the free substance, such as higher metabolic stability, better cellular uptake, improved bioavailability, and long-term activity, maintaining nearly the same biological activity and anticancer properties of the drug.
abstract_unstemmed	The discovery of new anticancer drugs with а higher, more specific activity and diminished side effects than the conventional chemotherapeutic agents is a tremendous challenge to contemporary medical research and development. To achieve a pronounced efficacy, the design of antitumor agents can combine various biologically active subunits in one molecule, which can affect different regulatory pathways in cancer cells. We recently demonstrated that a newly synthesized organometallic compound, a ferrocene-containing camphor sulfonamide (DK164), possesses promising antiproliferative activity against breast and lung cancer cells. However, it still encounters the problem of solubility in biological fluids. In this work, we describe a novel micellar form of DK164 with significantly improved solubility in aqueous medium. DK164 was embedded in biodegradable micelles based on a poly(ethylene oxide)-<i<b</i<-poly(<i<α-</i<cinnamyl-<i<ε-</i<caprolactone-<i<co-ε</i<-caprolactone)-<i<b</i<-poly(ethylene oxide) triblock copolymer (PEO<sub<113</sub<-<i<b</i<-P(CyCL<sub<3</sub<-<i<co</i<-CL<sub<46</sub<)-<i<b</i<-PEO<sub<113</sub<), and the physicochemical parameters (size, size distribution, zeta potential, encapsulation efficiency) and biological activity of the obtained system were studied. We used cytotoxicity assays and flow cytometry to determine the type of cell death, as well as immunocytochemistry to assess the influence of the encapsulated drug on the dynamics of cellular key proteins (p53 and NFkB) and the process of autophagy. According to our results, the micellar form of the organometallic ferrocene derivate (DK164-NP) exhibited several advantages compared to the free substance, such as higher metabolic stability, better cellular uptake, improved bioavailability, and long-term activity, maintaining nearly the same biological activity and anticancer properties of the drug.
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container_issue	3, p 791
title_short	Micellar Form of a Ferrocene-Containing Camphor Sulfonamide with Improved Aqueous Solubility and Tumor Curing Potential
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up_date	2024-07-04T00:57:16.939Z
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