Conjugated Chitosan as a Novel Platform for Oral Delivery of Paclitaxel
- Authors
- Lee, E[Lee, Eunhye]; Lee, J[Lee, Jinju]; Lee, IH[Lee, In-Hyun]; Yu, M[Yu, Mikyung]; Kim, H[Kim, Hyungjun]; Chae, SY[Chae, Su Young]; Jon, S[Jon, Sangyong]
- Issue Date
- 23-Oct-2008
- Publisher
- AMER CHEMICAL SOC
- Citation
- JOURNAL OF MEDICINAL CHEMISTRY, v.51, no.20, pp.6442 - 6449
- Indexed
- SCIE
SCOPUS
- Journal Title
- JOURNAL OF MEDICINAL CHEMISTRY
- Volume
- 51
- Number
- 20
- Start Page
- 6442
- End Page
- 6449
- URI
- https://scholarworks.bwise.kr/skku/handle/2021.sw.skku/80418
- DOI
- 10.1021/jm800767c
- ISSN
- 0022-2623
- Abstract
- A new platform for oral delivery of paclitaxel (PTX) was developed through chemical conjugation of PTX to a low molecular weight chitosan (LMWC). The LMWC-PTX conjugate contained similar to 12 wt % PTX and showed greatly enhanced water solubility (> 1 mg/mL) as compared to native PTX. The conjugate showed comparable IC(50) values to that of the parent PTX against human cancer cell lines. The pharmacokinetic data revealed similar to 42% of bioavailability after oral administration of 5 mg PTX/kg of the conjugate. When the conjugate (10 mg/kg based on PTX content) was administered orally to mice bearing xenograft or allograft tumors, the conjugate-treated group showed significant inhibition of tumor growth, which was comparable to that seen with PTX of the clinically available injected form, formulated in cremophor EL/ethanol (iv) but with much lower toxicity. Tracking I(125)-labeled conjugate showed that LMWC-PTX was likely to be absorbed mainly from the ileum and reach the blood as the intact conjugate.
- Files in This Item
- There are no files associated with this item.
- Appears in
Collections - Pharmacy > Department of Pharmacy > 1. Journal Articles
![qrcode](https://api.qrserver.com/v1/create-qr-code/?size=55x55&data=https://scholarworks.bwise.kr/skku/handle/2021.sw.skku/80418)
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.