Self-assembled nanospheres as a novel delivery system for taxol: A molecular hydrogel with nanosphere morphology

Key Laboratory of Bioactive Materials, Ministry of Education, College of Life Sciences, Nankai University, Tianjin 300071, PR China.
Chemical Communications (Impact Factor: 6.83). 03/2011; 47(15):4439-41. DOI: 10.1039/c1cc10506j
Source: PubMed


Here we reported on the first example of a Folic acid-based molecular hydrogel with nanosphere morphology as a delivery system for Taxol.

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    • "Our group has reported several molecular hydrogelators of taxol derivatives [21] [22]. During the preparation of aqueous solutions of taxol derivatives, we occasionally found that taxol derivatives would undergo an ester bond hydrolysis process to release the original taxol molecule, thus leading to the formation of molecular hydrogels. "
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    ABSTRACT: Molecular hydrogels have big potential for local delivery and sustained release of therapeutic agents. In this paper, we reported on a molecular hydrogel mainly formed by the widely used anti-cancer drug of taxol. The hydrogel was formed by an ester bond hydrolysis process from a taxol derivative (Taxol-SA-GSSG, 1) and could be administrated into solid tumors to dramatically hinder their growths and prevent their metastasis. Besides the improved anti-cancer effect compared to the clinically used intravenous (i.v.) injection of Taxol(®), the concentration of taxol in blood was low due to the local administration of taxol hydrogels, which greatly enhanced the dosage tolerance of mice to taxol and might reduce side effects of taxol during chemotherapy. Our observations suggested that the hydrogel mainly composed of taxol would have great potential for its practical applications.
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    ABSTRACT: The integration of nucleobase, amino acid, and glycoside into a single molecule results in a novel class of supramolecular hydrogelators, which not only exhibit biocompatibility and biostability but also facilitate the entry of nucleic acids into cytosol and nuclei of cells. This work illustrates a simple way to generate an unprecedented molecular architecture from the basic biological building blocks for the development of sophisticated soft nanomaterials, including supramolecular hydrogels.
    Full-text · Article · Sep 2011 · Journal of the American Chemical Society
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    ABSTRACT: The relationship between thermodynamic dissolution parameters (enthalpy and entropy) and gelation ability was examined for two different classes of compounds in three different solvent systems. In total, 11 dipeptides and 19 pyridines were synthesized and screened for gelation in aqueous and organic solvents, respectively. The dissolution parameters were determined from the variable-temperature solubilities using the van't Hoff equation. These studies revealed that the majority of gelators had higher dissolution enthalpies and entropies compared to nongelators, consistent with the notion that gelators have stronger intermolecular interactions and more order in the solid state. The dissolution parameters were also found to be solvent-dependent, suggesting that solvent-solute interactions are also important in gelation. Overall, these results indicate that converting nongelators into gelators is attainable when structural modifications or a change in solvent lead to increases in the dissolution parameters.
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