Polymeric micelles for delivery of poorly soluble drugs: Preparation and anticancer activity<i>in vitro</i>of paclitaxel incorporated into mixed micelles based on poly(ethylene glycol)-lipid conjugate and positively charged lipids

Wang, Junping; Mongayt, Dimitry; Torchilin, Vladimir P.

doi:10.1080/10611860400011935

Cited by 170 publications

(84 citation statements)

References 46 publications

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“…Recently, drug delivery systems have been engineered for the delivery of Ptx. [22][23][24] However, in a preliminary study, it was found that Ptx-loaded nanoparticles with amphilic copolymer as the carrier were unstable in the aqueous phase and were easy to aggregate. It was previously reported that Tet could effectively stabilize Ptx-loaded nanoparticles when it was coencapsulated with Ptx.…”

Section: Discussionmentioning

confidence: 99%

Enhanced in vitro and in vivo therapeutic efficacy of codrug-loaded nanoparticles against liver cancer

Li¹,

Xu²,

Dai³

et al. 2012

IJN

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Paclitaxel (Ptx), one of the most widely used anticancer agents, has demonstrated extraordinary activities against a variety of solid tumors. However, the therapeutic response of Ptx is often associated with severe side effects caused by its nonspecific cytotoxic effects and special solvents (Cremophor EL ® ). The current study reports the stable controlled release of Ptx/tetrandrine (Tet)-coloaded nanoparticles by amphilic methoxy poly(ethylene glycol)-poly(caprolactone) block copolymers. There were three significant findings. Firstly, Tet could effectively stabilize Ptxloaded nanoparticles with the coencapsulation of Tet and Ptx. The influence of different Ptx/Tet feeding ratios on the size and loading efficiency of the nanoparticles was also explored. Secondly, the encapsulation of Tet and Ptx into nanoparticles retains the synergistic anticancer efficiency of Tet and Ptx against mice hepatoma H22 cells. Thirdly, in the in vivo evaluation, intratumoral administration was adopted to increase the site-specific delivery. Ptx/Tet nanoparticles, when delivered intratumorally, exhibited significantly improved antitumor efficacy; moreover, they substantially increased the overall survival in an established H22-transplanted mice model. Further investigation into the anticancer mechanisms of this nanodelivery system is under active consideration as a part of this ongoing research. The results suggest that Ptx/Tet-coloaded nanoparticles could be a potential useful chemotherapeutic formulation for liver cancer therapy.

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Section: Discussionmentioning

confidence: 99%

Enhanced in vitro and in vivo therapeutic efficacy of codrug-loaded nanoparticles against liver cancer

Li¹,

Xu²,

Dai³

et al. 2012

IJN

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“…With this in mind, an attempt was made to increase the intracellular delivery and thus the anticancer activity of the micellar paclitaxel by preparing paclitaxel-containing micelles from the mixture of PEG-PE and Lipofectin lipids (LL). 217 When the cellular uptake of various fl uorescently labeled micelles in adherent BT-20 cells was studied, it was found that while both " plain " PEG-PE micelles and PEG-PE/LL micelles were endocytosed by BT-20 cells, as confi rmed by the presence of fl uorescent endosomes in cells after 2 hours of co-incubation with fl uorescently labeled micelles, in case of PEG-PE/LL micelles, endosomes became partially disrupted and their content was released into the cell cytosol. The addition of LL, facilitating the intracellular uptake and cytoplasmic release of paclitaxel-containing PEG-PE/LL micelles, resulted in a substantially increased level of cell death compared with that under the action of free paclitaxel or paclitaxel delivered using noncationic LL-free PEG-PE micelles.…”

Section: Ph-sensitive Carriersmentioning

confidence: 99%

Targeted pharmaceutical nanocarriers for cancer therapy and imaging

Torchilin

2007

AAPS J

Self Cite

673

428

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“…Such systems must load and 28 stably retain anticancer drugs and must also have a means to 29 release drugs into cells. Anticancer drug delivery systems have 30 thus far included bioconjugates (1-3), nanoparticles (4,5), 31 liposomes (6,7), polymersomes (8)(9)(10), and polymeric micelles 32 composed of amphiphilic block copolymers (11,12), but all of 33 the cited carriers are essentially spherical in shape. Long and 34 flexible Bworm-like^micelle carriers made from amphiphilic 35 block copolymers are described here in terms of formulation 36 and in vitro delivery, and the findings follow up on recent 37 studies that demonstrate surprisingly persistent circulation and 38 potent anti-tumor activity of worm-like micelles in vivo (13).…”

Section: Research Papermentioning

confidence: 99%

Micelles of Different Morphologies—Advantages of Worm-like Filomicelles of PEO-PCL in Paclitaxel Delivery

et al. 2007

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Worm-like and spherical micelles are both prepared here from the same amphiphilic diblock copolymer, poly(ethylene oxide)-b-poly (ε-caprolactone) (PEO [5 kDa]-PCL [6.5 kDa]) in order to compare loading and delivery of hydrophobic drugs. Worm-like micelles of this degradable copolymer are nanometers in crosssection and spontaneously assemble to stable lengths of microns, resembling filoviruses in some respects and thus suggesting the moniker "filomicelles". The highly flexible worm-like micelles can also be sonicated to generate kinetically stable spherical micelles composed of the same copolymer. The fission process exploits the finding that the PCL cores are fluid, rather than glassy or crystalline, and core-loading of the hydrophobic anticancer drug delivery, paclitaxel (TAX) shows that the worm-like micelles load and solubilize twice as much drug as spherical micelles. In cytotoxicity tests that compare to the clinically prevalent solubilizer, Cremophor® EL, both micellar carriers are far less toxic, and both types of TAX-loaded micelles also show 5-fold greater anticancer activity on A549 human lung cancer cells. PEO-PCL based worm-like filomicelles appear to be promising pharmaceutical nanocarriers with improved solubilization efficiency and comparable stability to spherical micelles, as well as better safety and efficacy in vitro compared to the prevalent Cremophor® EL TAX formulation. AUTHOR'S PROOFMetadata of the article that will be visualized in OnlineFirst Abstract. Worm-like and spherical micelles are both prepared here from the same amphiphilic diblock 7

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Polymeric micelles for delivery of poorly soluble drugs: Preparation and anticancer activityin vitroof paclitaxel incorporated into mixed micelles based on poly(ethylene glycol)-lipid conjugate and positively charged lipids

Cited by 170 publications

References 46 publications

Enhanced in vitro and in vivo therapeutic efficacy of codrug-loaded nanoparticles against liver cancer

Enhanced in vitro and in vivo therapeutic efficacy of codrug-loaded nanoparticles against liver cancer

Targeted pharmaceutical nanocarriers for cancer therapy and imaging

Micelles of Different Morphologies—Advantages of Worm-like Filomicelles of PEO-PCL in Paclitaxel Delivery

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