ArticleMolecular pharmaceutics
Synthesis and in vivo antitumor efficacy of PEGylated poly(l-lysine) dendrimer-camptothecin conjugates.
Article in Molecular pharmaceutics. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 151 citations in OpenAlex.
- Review
- A Celastrol Drug Delivery System Based on PEG Derivatives: The Structural Effects of Nanocarriers.Molecules (Basel, Switzerland) · 2023Article
- Chemical Approaches to Synthetic Drug Delivery Systems for Systemic Applications.Angewandte Chemie (International ed. in English) · 2022Review
- Nanoparticles from Gantrez-based conjugates for the oral delivery of camptothecin.International journal of pharmaceutics: X · 2021Article
- Endometrial membrane organoids from human embryonic stem cell combined with the 3D Matrigel for endometrium regeneration in asherman syndrome.Bioactive materials · 2021Article
- Article
- RNA Nanotechnology to Solubilize Hydrophobic Antitumor Drug for Targeted Delivery.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2019Article
- Self-Assembly and Enzyme Responsiveness of Amphiphilic Linear-Dendritic Block Copolymers Based on Poly(Polymers · 2019Article
- Drug-Conjugated Dendrimer Hydrogel Enables Sustained Drug Release via a Self-Cleaving Mechanism.Molecular pharmaceutics · 2019Article
- Synthesis and Antiproliferative Activities of Conjugates of Paclitaxel and Camptothecin with a Cyclic Cell-Penetrating Peptide.Molecules (Basel, Switzerland) · 2019Article
- Molecular dynamics simulation of coarse-grained poly(L-lysine) dendrimers.Journal of molecular modeling · 2016Article
- Brain Delivery of Drug and MRI Contrast Agent: Detection and Quantitative Determination of Brain Deposition of CPT-Glu Using LC-MS/MS and Gd-DTPA Using Magnetic Resonance Imaging.Molecular pharmaceutics · 2016Article
- Sunflower Polymers for Folate-Mediated Drug Delivery.Biomacromolecules · 2016Article
- Recent advances in targeted drug delivery approaches using dendritic polymers.Biomaterials science · 2015Article
- Enhanced bioactivity of internally functionalized cationic dendrimers with PEG cores.Biomacromolecules · 2012Article
- Transepithelial transport and toxicity of PAMAM dendrimers: implications for oral drug delivery.Advanced drug delivery reviews · 2012Review
- In vitro and in vivo antitumor activity of a novel pH-activated polymeric drug delivery system for doxorubicin.PloS one · 2012Article
- Designing dendrimers for drug delivery and imaging: pharmacokinetic considerations.Pharmaceutical research · 2011Review
- G3.5 PAMAM dendrimers enhance transepithelial transport of SN38 while minimizing gastrointestinal toxicity.Journal of controlled release : official journal of the Controlled Release Society · 2011Article
- Chemotherapeutic evaluation of a synthetic tubulysin analogue-dendrimer conjugate in c26 tumor bearing mice.ChemMedChem · 2011Article
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6 authors at 2 institutions in 1 country.
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Abstract
Polymer conjugates of camptothecin (CPT) have been pursued as a solution to the difficulties present in treating cancers with CPT and its derivatives. Covalent attachment of CPT to a polymer can improve solubility, increase blood circulation time, enhance tumor uptake, and significantly improve efficacy of the drug. In this report, we describe a novel polymer conjugate of CPT using a core-functionalized, symmetrically PEGylated poly(l-lysine) (PLL) dendrimer. The PEGylated dendrimer consisted of a lysine dendrimer functionalized with aspartic acid, which was used as an attachment site for poly(ethylene glycol) (PEG) and CPT. The final conjugate had a molecular weight of 40 kDa and was loaded with 4-6 wt % CPT. Polymer-bound CPT was shown to have a long blood circulation half-life of 30.9 +/- 8.8 h and a tumor uptake of 4.2 +/- 2.3% of the injected dose/g of tissue, compared to free CPT in which less than 1% was retained in the blood after 30 min and had a tumor accumulation of 0.29 +/- 0.04% of the injected dose/g of tissue. The PEGylated PLL-CPT showed superior efficacy in murine (C26) and human colon carcinoma (HT-29) tumor models when compared with no treatment or treatment with irinotecan. In the C26 tumor model, treatment resulted in significantly prolonged survival (P < 0.05) for all mice treated with a single injection of PEGylated PLL-CPT. In the HT-29 tumor model, all mice treated with multiple injections of a low dose survived to the end of the study, with three mice of eight surviving tumor-free.
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