Distribution of <sup>111</sup> in‐bleomycin complex in small cell lung cancer cells by autoradiography

Hou, De‐Yan; Maruyama, Yosh

doi:10.1002/jso.2930490206

Cited by 13 publications

(4 citation statements)

References 20 publications

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“…In easily forms a complex with bleomycin ( 111 In-BLMC) [111,112], and it has been observed to be a tumourtargeting agent in head-and-neck squamous cell carcinoma and glioma patients, thus being a useful diagnostic tracer [113][114][115][116]. In an autoradiography study by Hou and Maruyama, 78% of 111 In-BLMC was localised in the nucleus and nuclear membrane of human small cell lung cancer cells [117,118]. 111 In-BLMC induced more chromosome aberrations than BLMC [118,119].…”

Section: In-bleomycin 111mentioning

confidence: 99%

“…In an autoradiography study by Hou and Maruyama, 78% of 111 In-BLMC was localised in the nucleus and nuclear membrane of human small cell lung cancer cells [117,118]. 111 In-BLMC induced more chromosome aberrations than BLMC [118,119]. The cytotoxicity of 111 In-BLMC has been demonstrated in human small cell lung cancer and head-and-neck carcinoma cell lines [120][121][122].…”

Section: In-bleomycin 111mentioning

confidence: 99%

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Targeting the Nucleus: An Overview of Auger-Electron Radionuclide Therapy

Cornelissen¹,

Vallis

2010

CDDT

108

104

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The review presented here lays out the present state of the art in the field of radionuclide therapies specifically targeted against the nucleus of cancer cells, focussing on the use of Auger-electron-emitters. Nuclear localisation of radionuclides increases DNA damage and cell kill, and, in the case of Auger-electron therapy, is deemed necessary for therapeutic effect. Several strategies will be discussed to direct radionuclides to the nucleoplasm, even to specific protein targets within the nucleus. An overview is given of the applications of Auger-electron-emitting radionuclide therapy targeting the nucleus. Finally, a few suggestions are made as how radioimmunotherapy with nuclear targets can be improved, and the challenges that might be met, such as how to perform accurate dosimetry measurements, are examined.

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Section: In-bleomycin 111mentioning

confidence: 99%

Section: In-bleomycin 111mentioning

confidence: 99%

Targeting the Nucleus: An Overview of Auger-Electron Radionuclide Therapy

Cornelissen¹,

Vallis

2010

CDDT

108

104

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“…Tumours were palpable after 12-14 days and were used after reaching a volume of approximately 8 cm 3 (longest dimension: 2.5 cm). Bleomycin (Blenoxane, Mead Johnson, Princeton, NJ) was labelled with 111 In by mixing 1 mCi (0.1 ml) of 111 InCl (Nycomed Amersham, Amersham, England) with 0.4 ml bleomycin solution (10 mg = 15 units bleomycin, per ml normal saline, acidified with cHCl to pH 1-3), letting the mixture stand for 1 h at room temperature with occasional mixing, and adding another 0.5 ml bleomycin solution and 1.0 ml acidified normal saline to the mixture [49][50][51]. Labelling efficiency was approximately 97% as determined by thin layer chromatography on silica gel (liquid phase: equal volumes of MeOH and 10% aqueous ammonium acetate; Rf approximately 0.7).…”

Section: In-bleomycin Pharmacokineticsmentioning

confidence: 99%

Enhancement of therapeutic drug and DNA delivery into cells by electroporation*

Rabussay¹,

Dev²,

Fewell³

et al. 2003

J. Phys. D: Appl. Phys.

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The effectiveness of potentially powerful therapeutics, including DNA, is often limited by their inability to permeate the cell membrane efficiently. Electroporation (EP) also referred to as `electropermeabilization' of the outer cell membrane renders this barrier temporarily permeable by inducing `pores' across the lipid bilayer. For in vivo EP, the drug or DNA is delivered into the interstitial space of the target tissue by conventional means, followed by local EP. EP pulses of micro- to millisecond duration and field strengths of 100–1500 V cm−1 generally enhance the delivery of certain chemotherapeutic drugs by three to four orders of magnitude and intracellular delivery of DNA several hundred-fold. We have used EP in clinical studies for human cancer therapy and in animals for gene therapy and DNA vaccination. Late stage squamous cell carcinomas of the head and neck were treated with intratumoural injection of bleomycin and subsequent EP. Of the 69 tumours treated, 25% disappeared completely and another 32% were reduced in volume by more than half. Residence time of bleomycin in electroporated tumours was significantly greater than in non-electroporated lesions. Histological findings and gene expression patterns after bleomycin-EP treatment indicated rapid apoptosis of the majority of tumour cells. In animals, we demonstrated the usefulness of EP for enhanced DNA delivery by achieving normalization of blood clotting times in haemophilic dogs, and by substantially increasing transgene expression in smooth muscle cells of arterial walls using a novel porous balloon EP catheter. Finally, we have found in animal experiments that the immune response to DNA vaccines can be dramatically enhanced and accelerated by EP and co-injection of micron-sized particles. We conclude that EP represents an effective, economical and safe approach to enhance the intracellular delivery, and thus potency, of important drugs and genes for therapeutic purposes. The safety and pharmaco-economic profile of EP compares favourably with other drug and DNA delivery methods.

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Section: In-bleomycin Pharmacokineticsmentioning

confidence: 99%

Nikolai Sergeevich Dikanskii (on his sixtieth birthday)

Balakin¹,

Барков²,

Dimov³

et al. 2001

Phys.-Usp.

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The effectiveness of potentially powerful therapeutics, including DNA, is often limited by their inability to permeate the cell membrane efficiently. Electroporation (EP) also referred to as 'electropermeabilization' of the outer cell membrane renders this barrier temporarily permeable by inducing 'pores' across the lipid bilayer. For in vivo EP, the drug or DNA is delivered into the interstitial space of the target tissue by conventional means, followed by local EP. EP pulses of micro-to millisecond duration and field strengths of 100-1500 V cm −1 generally enhance the delivery of certain chemotherapeutic drugs by three to four orders of magnitude and intracellular delivery of DNA several hundred-fold. We have used EP in clinical studies for human cancer therapy and in animals for gene therapy and DNA vaccination. Late stage squamous cell carcinomas of the head and neck were treated with intratumoural injection of bleomycin and subsequent EP. Of the 69 tumours treated, 25% disappeared completely and another 32% were reduced in volume by more than half. Residence time of bleomycin in electroporated tumours was significantly greater than in non-electroporated lesions. Histological findings and gene expression patterns after bleomycin-EP treatment indicated rapid apoptosis of the majority of tumour cells. In animals, we demonstrated the usefulness of EP for enhanced DNA delivery by achieving normalization of blood clotting times in haemophilic dogs, and by substantially increasing transgene expression in smooth muscle cells of arterial walls using a novel porous balloon EP catheter. Finally, we have found in animal experiments that the immune response to DNA vaccines can be dramatically enhanced and accelerated by EP and co-injection of micron-sized particles. We conclude that EP represents an effective, economical and safe approach to enhance the intracellular delivery, and thus potency, of important drugs and genes for therapeutic purposes. The safety and pharmaco-economic profile of EP compares favourably with other drug and DNA delivery methods.

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Distribution of ¹¹¹ in‐bleomycin complex in small cell lung cancer cells by autoradiography

Cited by 13 publications

References 20 publications

Targeting the Nucleus: An Overview of Auger-Electron Radionuclide Therapy

Targeting the Nucleus: An Overview of Auger-Electron Radionuclide Therapy

Enhancement of therapeutic drug and DNA delivery into cells by electroporation*

Nikolai Sergeevich Dikanskii (on his sixtieth birthday)

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Distribution of 111 in‐bleomycin complex in small cell lung cancer cells by autoradiography

Cited by 13 publications

References 20 publications

Targeting the Nucleus: An Overview of Auger-Electron Radionuclide Therapy

Targeting the Nucleus: An Overview of Auger-Electron Radionuclide Therapy

Enhancement of therapeutic drug and DNA delivery into cells by electroporation*

Nikolai Sergeevich Dikanskii (on his sixtieth birthday)

Contact Info

Product

Resources

About

Distribution of ¹¹¹ in‐bleomycin complex in small cell lung cancer cells by autoradiography