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Drug Delivery Systems: Water Soluble Taxol 2‘-Poly(ethylene glycol) Ester ProdrugsDesign and in Vivo Effectiveness
Abstract
Water soluble 2'-taxol poly(ethylene glycol) (PEG) esters have been synthesized and shown to function in vitro as prodrugs. However, in vivo experiments clearly establish that in order for these prodrugs to behave in a predictable fashion, the molecular weight of PEG must be of such magnitude so as to maintain a t1/2(circulation) > t1/2(hydrolysis). When PEG derivatives of molecular weight approximately 40 kDa were employed with paclitaxel, ca. 4% by weight of paclitaxel was carried by the water soluble prodrug form, and equivalent in vivo toxicity and increased life expectancy in the P388-treated mouse was observed. An effective method for prescreening prodrugs was found to be the acute murine lethality, which reflects the equivalency of the solubilized transport form and the native drug.
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Citations
Cited by
Micellar Nanocarriers: Pharmaceutical Perspectives
Torchilin, V. P. (2006) · Pharmaceutical Research · doi:10.1007/s11095-006-9132-0 · Cited by 1,910
Effective drug delivery by PEGylated drug conjugates
Greenwald, R. B., Choe, Y. H., McGuire, J., & Conover, C. D. (2003) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(02)00180-1 · Cited by 869
Self-citationIn vivo evaluation of polymeric micellar paclitaxel formulation: toxicity and efficacy
Kim, S. C., Kim, D. W., Shim, Y. H., Bang, J. S., Oh, H. S., Kim, S. W., & Seo, M. H. (2001) · Journal of Controlled Release · doi:10.1016/s0168-3659(01)00275-9 · Cited by 734
Lessons Learned from Marketed and Investigational Prodrugs
Ettmayer, P., Amidon, G. L., Clement, B., & Testa, B. (2004) · Journal of Medicinal Chemistry · doi:10.1021/jm0303812 · Cited by 384
Mourtas, S., Lazar, A. N., Markoutsa, E., Duyckaerts, C., & Antimisiaris, S. G. (2014) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2014.04.050 · Cited by 263
Metadata
- Authors
- Greenwald, R. B., Gilbert, C. W., Pendri, A., Conover, C. D., Xia, J., & Martinez, A.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 1996-01-01
- Volume
- 39
- Issue
- 2
- Pages
- 424-431
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2012625044
- Cited by
- 223
- References
- 0
- FWCI
- 6.54
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: Drug Delivery Systems: Water Soluble Taxol 2‘-Poly(ethylene glycol) Ester ProdrugsDesign and in Vivo Effectiveness. https://app.cochat.ai/papers/10.1021/jm950475e
- The paper
- Greenwald, R. B., Gilbert, C. W., Pendri, A., Conover, C. D., Xia, J., & Martinez, A. (1996). Drug Delivery Systems: Water Soluble Taxol 2‘-Poly(ethylene glycol) Ester ProdrugsDesign and in Vivo Effectiveness. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm950475e
Data sources
Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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