DHP23002 as a next generation oral paclitaxel formulation for pancreatic cancer therapy

• DOI: 10.1371/journal.pone.0225095
• Publication Date: 2019-11-19T13:25:53Z
• Authors: Eunseo Jang; Minhee Son; Junhee Jang; In-Hyun Lee; Sol Kim; Taejun Kwon; Yong-hyun Jeon; Woo-Suk Koh; Kil-Soo Kim; Sang Kyoon Kim
• Keywords: Paclitaxel; Science; Drug Compounding; Q; R; Administration, Oral; Mice, Nude; Fluorescence; 3. Good health; Pancreatic Neoplasms; 03 medical and health sciences; 0302 clinical medicine; Tubulin; Cell Line, Tumor; Medicine; Animals; Humans; Female; Research Article

Objective This study aimed to develop a new oral paclitaxel formulation (DHP23002) and evaluate its absorption antitumor effects in pancreatic tumor mouse model. Methods To investigate the of DHP23002, newly developed lipid-based orally active formulation, pharmacokinetic was conducted mice (62.5 125 mg/kg). Moreover, effect DHP23002 cancer treatment, drug administered female athymic nude at 0 (vehicle), 25, 62.5, mg/kg on alternate days; efficacy agent compared with intravenous Taxol® injections 10 once per week. After 3 weeks administration, growth belonging each group further monitored for 4 after discontinuing medication. examine accumulation tissue, amount tumor/blood quantified using liquid chromatography quadruple-TOF mass spectrometry. Results In study, showed negligible absorption, whereas high rate dependent dosage, bioavailability approximately 40% dose 62.5 mg/kg. efficacy-related studies, administration or days superior inhibitory 80%, 92%, 97% xenograft model, respectively, 7 weeks. Paclitaxel tumors persisted >24 h mice, when doses DHP23002. Conclusion Oral chemotherapy excellent animals owing strong activity demonstrates that is largely distributed persists prolonged period site administration.