Jang, Yura Ko, Min Kyung Park, Ye Eun Hong, Jung Wan Lee, In-Hyun Chung, Hye Jin Chung, Hesson 2024-01-19T21:04:47Z 2024-01-19T21:04:47Z 2021-09-05 2018-12 1773-2247 https://pubs.kist.re.kr/handle/201004/120611 DHP107 is a novel lipid-based oral paclitaxel formulation for the treatment of various cancers. In the present study, to increase the treatment effect of DHP107, we aimed to improve this formulation. We optimized the paclitaxel content in DHP107 formulation, evaluated its antitumor activity, and compared its activity with that of the intravenous paclitaxel formulation, Taxol (R), in various mouse cancer models. The oral bioavailability of paclitaxel increased dose-dependently up to 50 mg/kg. However, the paclitaxel absorption from the DHP107 formulations containing >= 1.5% (w/v) paclitaxel decreased with the increase in DHP107 dose as paclitaxel was crystallized when exposed to water. Therefore, the optimized DHP107 formulation containing 1% (w/v) paclitaxel was selected, and it exhibited similar antitumor activity as Taxol (R). However, the DHP107 showed a better survival rate with low toxicity than that of Taxol (R). The concentration of paclitaxel in the tumor tissues of mice in the DHP107 was also higher than that in Taxol (R). The optimized DHP107 formulation might reduce the possible toxic effects of the formulation, with antitumor activities similar to those of intravenous paclitaxel Taxol (R), by enhancing the distribution to tumor tissues. Furthermore, it might be beneficial to use DHP107 for patients with hypersensitivity reactions to intravenous Taxol (R). English ELSEVIER SCIENCE BV DRUG-DELIVERY-SYSTEM IN-VIVO EVALUATION TISSUE DISTRIBUTION BODY-TEMPERATURE MOUSE MODEL EFFICACY ABSORPTION PHARMACOKINETICS NANOPARTICLES HYPOTHERMIA Effect of paclitaxel content in the DHP107 oral formulation on oral bioavailability and antitumor activity Article 10.1016/j.jddst.2018.09.014 1 JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY, v.48, pp.183 - 192 JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY 48 183 192 scie scopus 000451008000022 2-s2.0-85054165991 Pharmacology & Pharmacy Pharmacology & Pharmacy Article DRUG-DELIVERY-SYSTEM IN-VIVO EVALUATION TISSUE DISTRIBUTION BODY-TEMPERATURE MOUSE MODEL EFFICACY ABSORPTION PHARMACOKINETICS NANOPARTICLES HYPOTHERMIA Paclitaxel Oral formulation DHP107 Formulation optimization Antitumor activity Tumor distribution