• Title/Summary/Keyword: micellar solubilizer

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THE TOXICITY OF ACEPOROL 460 AS A NOVEL HIGH LOADING CAPACITY SOLUBILIZER OF PACLITAXEL

  • Kim, Yeo-Woon;Kim, Ja-Young;Cho, Min-Jung;Song, Hye-Weon;Lee, Min-Jae;Kim, Jong-Jae;Lee, Mi-Suk;Sheen, Yhun-Yhong
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2002.11b
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    • pp.160-160
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    • 2002
  • Previously, we reported a novel polymeric micellar solubilizer, Aceporol 330, that showed relatively low toxic effects when it was compared with that of Cremophor EL which is currently being used for paclitaxel. In this study, we have developed a new micellar solubilizer, Aceporol 460, that has 3-4 times higher lading capacity for paclitaxel than Aceporol 330.(omitted)

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The toxicity of Aceporol 460 as a novel high loading capacity solubilizer of paclitaxel

  • Kim, Yeo-Woon;Kim, Ja-Young;Cho, Min-Jung;Song, Hye-Weon;Lee, Min-Jae;Kim, Jong-Jae;Lee, Mi-Suk;Sheen, Yhun-Yhong
    • Proceedings of the Korea Society of Environmental Toocicology Conference
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    • 2002.10a
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    • pp.172-172
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    • 2002
  • Previously, we reported a novel polymeric micellar solubilizer, Aceporol 330, that showed relatively low toxic effects when it was compared with that of Cremophor EL which is currently being used for paclitaxel. In this study, we have developed a new micellar solubilizer, Aceporol 460, that has 3-4 times higher loding capacity for paclitaxel than Aceporol 330. The single-dose and the repeated-dose toxicity of Aceporol 460 were evaluated in ICR mice. For single dose toxicity test, male and female mice were randomly assigned to one of five study groups to receive, and injected intravenously with dosages of 0, 3, 4mL Cremophor EL/kgbody weight, and 3, 4mL Aceporol 460/kg body weight, respectively. In both male and female mice, LD50 for Aceporol 460 can not he determined even at the maximal administrable dosage, 4mL/kg due to the high viscosity of chemical and there was no significant change in body weight, hematological and serum biochemical analysis, organ weight, and histopathological examination compared with that of Cremophor EL. For the repeated dose toxicity test, male and female mice were given the dosage of 0, 1.6mL Cremophor EL/kgbody weight/day, and 1.6mL Aceporol 460/kg body weight/day for 2 weeks. Results of repeated dose toxicity tests for 2 weeks suggested that Aceporol 460 treated group show no significant toxicological findings with body weight, hematological and serum biochemical analysis, organ weight, urinalysis, and ophthalmoscopic and histopathological examination compared with that of Cremophor EL. These results indicate that Aceporol 460 have higher paclitaxeL-loading capacity than Aceporol 330 and less toxic effects than Cremophor EL in male and female mice.

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Tissue Distribution of Novel Polymeric Micellar Paclitaxel in Mice

  • Kim, Hye-Jin;Kang, Min-Kyung;Kim, Kil-Soo
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.413.3-414
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    • 2002
  • Paclitaxel is a diterpenoid isolated from Taxus brevifolia and is an active anticancer drug for the treatment of ovarian cancer, breast cancer and Kaposi's sarcoma. Due to its low solubility in water, it is dissolved in Cremophor EL(polyethoxylated castor oil) and ethanol, which cause serious side effects including hypersensitivity. BLK460 was developed as a novel polymeric micellar paclitaxel formulation containing Aceporol460 as solubilizer (omitted)

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The toxicity of Aceporol 460 as a novel high loading capacity solubilizer of paclitaxel

  • Kim, Yeo-Woon;Kim, Ja-Young;Cho, Min-Jung;Song, Hae-Won;Lee, Min-Jae;Kim, Jong-Jae;Lee, Mi-Suk;Sheen, Yhun-Yhong
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.287.3-288
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    • 2002
  • Previously. we reported a novel polymeric micellar solubilizeI'. Aceporol 330. that showed relatively low toxic effects when it was compared with that of Cremophor EL which is currently being used for paclitaxel. In this study. we have developed a new micellar solubilizeI, Aceporol 460. that has 3-4 times higher loding capacity for paclitaxel than Aceporol 330. The single-dose and the repeated-dose toxicity of Aceporol 460 were evaluated in ICR mice. (omitted)

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THE ACUTE TOXICITY TEST OF A NOVEL MICELLAR SOLUBILIZER FOR USE WITH INJECTABLE ANTICANCER AGENTS

  • Kim, Y.W.;Min, K.N.;Pan, S.R.;Ok, K.E.;Lee, M.J.;Kim, J.J.;Sheen, Y.Y.
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2001.05a
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    • pp.130-130
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    • 2001
  • The commercially available paclitaxel product, Taxol$\circledR$ is currently formulated in a vehicle containing approximately a 1:1 v/v mixture of polyoxyethylated castor oil (Cremophor EL) and ethanol. Cremophor EL, a commonly used surfactant for lipophilic compounds, has been associated with many issues, such as adverse effects particularly following rapid administration, stability with the possibility for drug precipitation upon dilution, and filtering requirements.(omitted)

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