Micellar Delivery System for Dequalinium—A Lipophilic Cationic Drug with Anticarcinoma Activity

Weissig, Volkmar; Lizano, Carmen; Torchilin, Vladimir P.

doi:10.3109/08982109809035542

Cited by 40 publications

(16 citation statements)

References 7 publications

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“…Unfortunately, the authors also did not hypothesize any constraints a phospholipid bilayer membrane might impose on the accommodation of the bola amphilic dequalinium cation. As demonstrated already in 1998, the stable incorporation of dequalinium into liposomes made of phosphatidylcholine and/or phosphatidyserine does not seem to be possible based on a very limited ability of dequalinium to mix with phospholipids (93). However, a variety of in vitro and in vivo assays including cytochrome C release, Bid cleavage, and caspase 8 and 3 activation suggest an enhanced pro-apoptotic activity of daunorubicin / amlodipine incorporated into dequaliniumcontaining liposomes (92), and the authors concluded in their 2010 paper that "mitochondria-specifically targeting drug-loaded liposomes would provide a new strategy for treating resistant cancers" (92).…”

Section: Targeting Cancer Cell Mitochondriamentioning

confidence: 93%

From Serendipity to Mitochondria-Targeted Nanocarriers

Weissig

2011

Pharm Res

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This review illustrates how a random observation at the laboratory bench has helped pave the way towards the development of organelle-targeted pharmaceutical nanocarriers. A fortuitous discovery in the mid 1990s involving the self-assembly of a molecule, known to accumulate inside mitochondria, has lead to the development of subcellular nanocarriers suited for the selective delivery of biologically active molecules to mitochondria inside living mammalian cells. Applications for mitochondria-specific drug and DNA delivery are described, the current state-of-the-art of mitochondrial drug targeting technology is reviewed, and its future perspectives are discussed.

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Section: Targeting Cancer Cell Mitochondriamentioning

confidence: 93%

From Serendipity to Mitochondria-Targeted Nanocarriers

Weissig

2011

Pharm Res

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“…A wide variety of polymer particulate carriers has been devised for protecting biologically active molecules against inactivation by the organism and for controlling drug release in body fluids. The advantages of polymeric colloidal delivery systems are easy control of particle size, good structural stability and stability during long-term storage, solubilization of hydrophobic drugs and ability to deliver drugs showing low interactions with biocomponents such as proteins and cells (6,7).…”

Section: Introductionmentioning

confidence: 99%

Amphiphilic poly-N-vinylpyrrolidone nanoparticles as carriers for non-steroidal anti-inflammatory drugs: Characterization and in vitro controlled release of indomethacin

Tsatsakis¹

2010

Int J Mol Med

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Abstract. Novel amphiphilic poly-N-vinylpyrrolidone derivatives with different molecular weight of hydrophilic PVP fragment and one secondary di-n-alkyl terminal hydrophobic fragment of different length were synthesized to compare their inclination for formation of nano-scaled micelle-like aggregates in aqueous media with previously studied primary n-alkyl terminated poly-N-vinylpyrrolidones. The behavior of amphiphilies in water solutions was studied and critical aggregation concentration values for prepared polymer samples were determined by fluorescence spectroscopy and compared with those for primary n-alkyl derivatives. Polymeric micelle-like particles with or without encapsulated drug were prepared using dialysis or solvent evaporation techniques. Indomethacin was incorporated into hydrophobic inner core of these nanoparticles as a typical model drug. Dynamic light-scattering studies determined that the average size of particles formed was from 90 nm up to 600 nm with monodisperse size distribution and the nanoparticle size slightly increased with the amount of indomethacin encapsulated into inner core of the particles. In vitro release experiments carried out at different medium pH values using indomethacin-loaded nanoparticles exhibited slow and steady drug release into the medium.

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“…We have reported some data on stable and long-circulating polymeric micelles formed by PEG-PE conjugates (Trubetskoy and Torchilin 1996). Such micelles can be loaded with a variety of poorly soluble drugs including paclitaxel (Weissig et al 1998a and are capable of delivering their load even into poorly permeable tumors in mice with a higher efficiency than other long-circulating carriers (Weissig et al 1998b.…”

Section: Introductionmentioning

confidence: 99%

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

Wang

Mongayt

Torchilin

2005

Journal of Drug Targeting

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170

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Paclitaxel-loaded mixed polymeric micelles consisting of poly(ethylene glycol)-distearoyl phosphoethanolamine conjugates (PEG-PE), solid triglycerides (ST), and cationic Lipofectin® lipids (LL) have been prepared. Micelles with the optimized composition (PEG-PE/ST/LL/paclitaxel = 12/12/2/1 by weight) had an average micelle size of about 100 nm, and zeta-potential of about 26 mV. Micelles were stable and did not release paclitaxel when stored at 4°C in the darkness (just 2.9% of paclitaxel have been lost after 4 months with the particle size remaining unchanged). The release of paclitaxel from such micelles at room temperature was also insignificant. However, at 37°C, approx. 16% of paclitaxel was released from PEG-PE/ST/LL/paclitaxel micelles in 72 h, probably, because of phase transition in the ST-containing micelle core. In vitro anticancer effects of PEG-PE/ ST/LL/paclitaxel and control micelles were evaluated using human mammary adenocarcinoma (BT-20) and human ovarian carcinoma (A2780) cell lines. Paclitaxel in PEG-PE/ST/LL micelles demonstrated the maximum anti-cancer activity. Cellular uptake of fluorescently-labeled paclitaxelcontaining micelles by BT-20 cells was investigated using a fluorescence microscopy. It seems that PEG-PE/ST/LL micelles, unlike micelles without the LL component, could escape from endosomes and enter the cytoplasm of BT-20 cancer cells thus increasing the anticancer efficiency of the micellar paclitaxel.

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Micellar Delivery System for Dequalinium—A Lipophilic Cationic Drug with Anticarcinoma Activity

Cited by 40 publications

References 7 publications

From Serendipity to Mitochondria-Targeted Nanocarriers

From Serendipity to Mitochondria-Targeted Nanocarriers

Amphiphilic poly-N-vinylpyrrolidone nanoparticles as carriers for non-steroidal anti-inflammatory drugs: Characterization and in vitro controlled release of indomethacin

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

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