The use of cholesterol-containing biodegradable block copolymers to exploit hydrophobic interactions for the delivery of anticancer drugs

Lee, Ashlynn L. Z.; Venkataraman, S.; Sirat, Syamilah B.M.; Gao, Shujun; Hedrick, James L.; Yang, Yi Yan

doi:10.1016/j.biomaterials.2011.11.032

Cited by 148 publications

(124 citation statements)

References 39 publications

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“…As a structural analog of paclitaxel, cabazitaxel probably has the same affinity for cholesterol, which may be another reason for the stability of cabazitaxel in the core of the micelles. 37 cytotoxicity of cabazitaxel-loaded F68-chMc micelles…”

Section: Dilution Stability Of F68-chmc Micellesmentioning

confidence: 99%

Self-assembled micelles of novel amphiphilic copolymer cholesterol-coupled F68 containing cabazitaxel as a drug delivery system

Song¹,

Tian²,

Huang³

et al. 2014

IJN

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Despite being one of the most promising amphiphilic block copolymers, use of Pluronic F68 in drug delivery is limited due to its high critical micelle concentration (CMC). In this study, we developed a novel F68 derivative, cholesterol-coupled F68 (F68-CHMC). This new derivative has a CMC of 10 μg/mL, which is 400-fold lower than that of F68. The drug-loading capacity of F68-CHMC was investigated by encapsulating cabazitaxel, a novel antitumor drug. Drug-loaded micelles were fabricated by a self-assembly method with simple dilution. The optimum particle size of the micelles was 17.5±2.1 nm, with an entrapment efficiency of 98.1% and a drug loading efficiency of 3.16%. In vitro release studies demonstrated that cabazitaxel-loaded F68-CHMC micelles had delayed and sustained-release properties. A cytotoxicity assay of S180 cells showed that blank F68-CHMC was noncytotoxic with a cell viability of nearly 100%, even at a concentration of 1,000 μg/mL. The IC 50 revealed that cabazitaxel-loaded F68-CHMC micelles were more cytotoxic than Tween 80-based cabazitaxel solution and free cabazitaxel. In vivo antitumor activity against S180 cells also indicated better tumor inhibition by the micelles (79.2%) than by Tween 80 solution (56.2%, P <0.05). Based on these results, we conclude that the F68-CHMC copolymer may be a potential nanocarrier to improve the solubility and biological activity of cabazitaxel and other hydrophobic drugs.

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Section: Dilution Stability Of F68-chmc Micellesmentioning

confidence: 99%

Self-assembled micelles of novel amphiphilic copolymer cholesterol-coupled F68 containing cabazitaxel as a drug delivery system

Song¹,

Tian²,

Huang³

et al. 2014

IJN

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“…In the past decades, polymeric micelles self-assembled from amphiphilic block copolymers in aqueous media have been widely investigated [1][2][3] and their excellent properties as drug delivery vehicles have been recognized such as the high stability in vivo, good biocompatibility, high drug loading, etc. [4,5].…”

Section: Introductionmentioning

confidence: 99%

Mesoscopic simulation studies on the formation mechanism of drug loaded polymeric micelles

Yan

Zhu

Zhou

et al. 2015

Colloids and Surfaces B: Biointerfaces

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“…For example, cholesterol has been grafted to polycarbonate to develop an anticancer drug delivery vehicle using the hydrophobic interaction of cholesterol. 5 A molecular imprinting technology has been devised to selectively separate cholesterol from its derivatives using a cholesterol-specific polymer template. 6 A poly(acrylate) hydrogel with pendant cholesterol and poly(ethylene glycol) groups has been developed to entrap lipophilic nanomaterials.…”

Section: Introductionmentioning

confidence: 99%

Impact of cholesterol grafting on molecular interactions and low temperature flexibility of polyurethanes

Chung

Kim

et al. 2015

Macromol. Res.

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A series of polyurethanes (PUs) containing grafted cholesterol (UA series) and a control series blended with free cholesterol (UB series) were prepared: the spectroscopic, thermal, tensile, shape memory, and low temperature flexibility properties of these series were compared with those of unmodified PU. For both the UA and UB series, the soft segment melting temperature (T m ) was not affected by the cholesterol content. Differential scanning calorimetry (DSC) results showed that the crystallization of the hard segment of the UA series was completely inhibited as the grafted cholesterol content increased, which were supported by dynamic mechanical analysis (DMA) results for the storage modulus. As the cholesterol content increased, the glass transition temperature (T g ) of the UA series increased and remained the same for the UB series. The tensile strength in the UA series sharply increased with the cholesterol content, unlike that of the UB series. The strain at break in the UA series remained the same as the cholesterol content increased, whereas that of the UB series decreased significantly. As the cholesterol content increased, the shape recovery of the UA series remained above 90% at 45 o C and sharply increased at 0 o C. Finally, the UA series containing grafted cholesterol demonstrated excellent low temperature flexibilities compared to the UB series and unmodified PU.

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The use of cholesterol-containing biodegradable block copolymers to exploit hydrophobic interactions for the delivery of anticancer drugs

Cited by 148 publications

References 39 publications

Self-assembled micelles of novel amphiphilic copolymer cholesterol-coupled F68 containing cabazitaxel as a drug delivery system

Self-assembled micelles of novel amphiphilic copolymer cholesterol-coupled F68 containing cabazitaxel as a drug delivery system

Mesoscopic simulation studies on the formation mechanism of drug loaded polymeric micelles

Impact of cholesterol grafting on molecular interactions and low temperature flexibility of polyurethanes

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