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Efficacy of camptothecin and polymer-conjugated camptothecin in tumor spheroids and solid tumors.
J Biomater Sci Polym Ed. 2007; 18(10):1283-99.JB

Abstract

Camptothecin (CPT) is an anti-cancer drug with low solubility in aqueous solutions, which limits its efficacy during chemotherapy. To bypass this problem, CPT was conjugated to poly(ethylene glycol) (PEG) to make CPT more hydrophilic: CM-PEG-CPT (carboxylmethylpoly(ethlyene glycol)-camptothecin), CM-PEG-GLY-CPT (carboxylmethyl-poly(ethlyene glycol)-glycine-camptothecin) and CM-PEG-SAR-CPT (carboxylmethyl-poly(ethlyene glycol)-sarcosine camptothecin) were synthesized. These conjugates differed in the amino-acid linker, which altered the hydrolysis rate of CPT from CPT-PEG. We tested the hypothesis that CPT conjugates were more effective than unconjugated CPT in effectiveness upon direct delivery to solid tumors using two systems: in vitro tumor spheroids suspended in collagen gels and in vivo solid tumors in rats. CPT was effective in spheroids, but not in flank tumors. However, when CPT was conjugated, there was improvement in the treatment of spheroids and, to a lesser extent, tumors in rats. There was no difference in therapeutic effects among the various conjugates. We conclude that conjugation of CPT to PEG enhances CPT solubility and improves effectiveness of delivery to tumors.

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Authors+Show Affiliations

Ying V
School of Veterinary Medicine, Cornell University, C2-502 Clinical Programs Center Ithaca, NY 14853, USA.
Haverstick K
No affiliation info available
Page RL
No affiliation info available
Saltzman WM
No affiliation info available

MeSH

AnimalsAntineoplastic AgentsCamptothecinCollagenCollagenasesDrug Delivery SystemsDrug Screening Assays, AntitumorFemaleNeoplasmsPolyethylene GlycolsPolymersRatsRats, Inbred F344SolubilitySpheroids, CellularTumor Cells, Cultured

Pub Type(s)

Journal Article

Language

eng

PubMed ID

17939886

Citation

Ying, Victoria, et al. "Efficacy of Camptothecin and Polymer-conjugated Camptothecin in Tumor Spheroids and Solid Tumors." Journal of Biomaterials Science. Polymer Edition, vol. 18, no. 10, 2007, pp. 1283-99.
Ying V, Haverstick K, Page RL, et al. Efficacy of camptothecin and polymer-conjugated camptothecin in tumor spheroids and solid tumors. J Biomater Sci Polym Ed. 2007;18(10):1283-99.
Ying, V., Haverstick, K., Page, R. L., & Saltzman, W. M. (2007). Efficacy of camptothecin and polymer-conjugated camptothecin in tumor spheroids and solid tumors. Journal of Biomaterials Science. Polymer Edition, 18(10), 1283-99.
Ying V, et al. Efficacy of Camptothecin and Polymer-conjugated Camptothecin in Tumor Spheroids and Solid Tumors. J Biomater Sci Polym Ed. 2007;18(10):1283-99. PubMed PMID: 17939886.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Efficacy of camptothecin and polymer-conjugated camptothecin in tumor spheroids and solid tumors. AU - Ying,Victoria, AU - Haverstick,Kraig, AU - Page,Rodney L, AU - Saltzman,W Mark, PY - 2007/10/18/pubmed PY - 2008/1/3/medline PY - 2007/10/18/entrez SP - 1283 EP - 99 JF - Journal of biomaterials science. Polymer edition JO - J Biomater Sci Polym Ed VL - 18 IS - 10 N2 - Camptothecin (CPT) is an anti-cancer drug with low solubility in aqueous solutions, which limits its efficacy during chemotherapy. To bypass this problem, CPT was conjugated to poly(ethylene glycol) (PEG) to make CPT more hydrophilic: CM-PEG-CPT (carboxylmethylpoly(ethlyene glycol)-camptothecin), CM-PEG-GLY-CPT (carboxylmethyl-poly(ethlyene glycol)-glycine-camptothecin) and CM-PEG-SAR-CPT (carboxylmethyl-poly(ethlyene glycol)-sarcosine camptothecin) were synthesized. These conjugates differed in the amino-acid linker, which altered the hydrolysis rate of CPT from CPT-PEG. We tested the hypothesis that CPT conjugates were more effective than unconjugated CPT in effectiveness upon direct delivery to solid tumors using two systems: in vitro tumor spheroids suspended in collagen gels and in vivo solid tumors in rats. CPT was effective in spheroids, but not in flank tumors. However, when CPT was conjugated, there was improvement in the treatment of spheroids and, to a lesser extent, tumors in rats. There was no difference in therapeutic effects among the various conjugates. We conclude that conjugation of CPT to PEG enhances CPT solubility and improves effectiveness of delivery to tumors. SN - 0920-5063 UR - https://www.unboundmedicine.com/medline/citation/17939886/Efficacy_of_camptothecin_and_polymer_conjugated_camptothecin_in_tumor_spheroids_and_solid_tumors_ L2 - https://www.tandfonline.com/doi/full/10.1163/156856207782177918 DB - PRIME DP - Unbound Medicine ER -