Core-cross-linked polymeric micelles as paclitaxel carriers
Shuai, XT; Merdan, T; Schaper, AK; Xi, F; Kissel, T
AbstractCross-linkable di- and triblock copolymers of poly(c-caprolactone) (PCL) and monomethoxyl poly(ethylene glycol) (MPEG) were synthesized. These amphiphilic copolymers self-assembled into nanoscale micelles capable of encapsulating hydrophobic paclitaxel in their hydrophobic cores in aqueous solutions. To further enhance their thermodynamic stability, the micelles were cross-linked by radical polymerization of the double bonds introduced into the PCL blocks. Reaction conditions were found to significantly affect both the cross-linking efficiency and the micelle size. The encapsulation of paclitaxel into the micelles was confirmed by the proton nuclear magnetic resonance (H-1 NMR) spectroscopy. Encouragingly, paclitaxel-loading efficiency of micelles was enhanced significantly upon micelle core-cross-linking. Both the micelle size and the drug loading efficiency increased markedly with increasing the PCL block lengths, no matter if the micelles were core-crosslinked or not. However, paclitaxel-loading did not obviously affect the micelle size or size distribution. The cross-linked micelles exhibited a significantly enhanced thermodynamic stability against dilution with aqueous solvents. The efficient cellular uptake of paclitaxel loaded in the nanomicelles was demonstrated by confocal laser scanning microscopy (CLSM) imaging. This new biodegradable nanoscale carrier system merits further investigations for parenteral drug delivery.
Indexed BySCI
WOS IDWOS:000221563300002
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Cited Times:274[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Corresponding AuthorKissel, T
Affiliation1.Univ Marburg, Dept Pharmaceut & Biopharm, D-35032 Marburg, Germany
2.Univ Marburg, Dept Geosci, D-35032 Marburg, Germany
3.Univ Marburg, Ctr Mat Sci, D-35032 Marburg, Germany
4.Chinese Acad Sci, Inst Chem, Beijing 100080, Peoples R China
Recommended Citation
GB/T 7714
Shuai, XT,Merdan, T,Schaper, AK,et al. Core-cross-linked polymeric micelles as paclitaxel carriers[J]. BIOCONJUGATE CHEMISTRY,2004,15(3):441-448.
APA Shuai, XT,Merdan, T,Schaper, AK,Xi, F,&Kissel, T.(2004).Core-cross-linked polymeric micelles as paclitaxel carriers.BIOCONJUGATE CHEMISTRY,15(3),441-448.
MLA Shuai, XT,et al."Core-cross-linked polymeric micelles as paclitaxel carriers".BIOCONJUGATE CHEMISTRY 15.3(2004):441-448.
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