BIOMAT Database Logo BIOMAT Database Logo

Anthracycline antibiotics non-covalently incorporated into the block copolymer micelles: in vivo evaluation of anti-cancer activity. 1996

E V Batrakova, and T Y Dorodnych, and E Y Klinskii, and E N Kliushnenkova, and O B Shemchukova, and O N Goncharova, and S A Arjakov, and V Y Alakhov, and A V Kabanov
Moscow Institute of Biotechnology, Inc., and Russian Research Center of Molecular Diagnostics and Therapy.

The chemosensitising effects of poly(ethylene oxide)-poly(propylene oxide)-poly-(ethylene oxide) (PEO-PPO-PEO) block copolymers (Pluronic) in multidrug-resistant cancer cells has been described recently (Alakhov VY, Moskaleva EY, Batrakova EV, Kabanov AV 1996, Biocon. Chem., 7, 209). This paper presents initial studies on in vivo evaluation of Pluronic copolymers in the treatment of cancer. The anti-tumour activity of epirubicin (EPI) and doxorubicin (DOX), solubilised in micelles of Pluronic L61, P85 and F108, was investigated using murine leukaemia P388 and daunorubicin-sensitive Sp2/0 and -resistant Sp2/0(DNR) myeloma cells grown subcutaneously (s.c.). The study revealed that the lifespan of the animals and inhibition of tumour growth were considerably increased in mice treated with drug/copolymer compositions compared with animals treated with the free drugs. The anti-tumour activity of the drug/copolymer compositions depends on the concentration of the copolymer and its hydrophobicity, as determined by the ratio of the lengths of hydrophilic PEO and hydrophobic PPO segments. The data suggest that higher activity is associated with more hydrophobic copolymers. In particular, a significant increase in lifespan (T/C> 150%) and tumour growth inhibition (> 90%) was observed in animals with Sp2/0 tumours with EPI/P85 and DOX/L61 compositions. The effective doses of these compositions caused inhibition of Sp2/0 tumour growth and complete disappearance of tumour in 33-50% of animals. Future studies will focus on the evaluation of the activity of Pluronic-based compositions against human drug-resistant tumours.

UI MeSH Term Description Entries
D007941 Leukemia P388 An experimental lymphocytic leukemia originally induced in DBA/2 mice by painting with methylcholanthrene. P388D(1) Leukemia,P388, Leukemia
D008297 Male Males
D008807 Mice, Inbred BALB C An inbred strain of mouse that is widely used in IMMUNOLOGY studies and cancer research. BALB C Mice, Inbred,BALB C Mouse, Inbred,Inbred BALB C Mice,Inbred BALB C Mouse,Mice, BALB C,Mouse, BALB C,Mouse, Inbred BALB C,BALB C Mice,BALB C Mouse
D008810 Mice, Inbred C57BL One of the first INBRED MOUSE STRAINS to be sequenced. This strain is commonly used as genetic background for transgenic mouse models. Refractory to many tumors, this strain is also preferred model for studying role of genetic variations in development of diseases. Mice, C57BL,Mouse, C57BL,Mouse, Inbred C57BL,C57BL Mice,C57BL Mice, Inbred,C57BL Mouse,C57BL Mouse, Inbred,Inbred C57BL Mice,Inbred C57BL Mouse
D008823 Micelles Particles consisting of aggregates of molecules held loosely together by secondary bonds. The surface of micelles are usually comprised of amphiphatic compounds that are oriented in a way that minimizes the energy of interaction between the micelle and its environment. Liquids that contain large numbers of suspended micelles are referred to as EMULSIONS. Micelle
D009101 Multiple Myeloma A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY. Myeloma, Plasma-Cell,Kahler Disease,Myeloma, Multiple,Myeloma-Multiple,Myelomatosis,Plasma Cell Myeloma,Cell Myeloma, Plasma,Cell Myelomas, Plasma,Disease, Kahler,Multiple Myelomas,Myeloma Multiple,Myeloma, Plasma Cell,Myeloma-Multiples,Myelomas, Multiple,Myelomas, Plasma Cell,Myelomas, Plasma-Cell,Myelomatoses,Plasma Cell Myelomas,Plasma-Cell Myeloma,Plasma-Cell Myelomas
D009368 Neoplasm Transplantation Experimental transplantation of neoplasms in laboratory animals for research purposes. Transplantation, Neoplasm,Neoplasm Transplantations,Transplantations, Neoplasm
D011060 Poloxalene A copolymer of polyethylene and polypropylene ether glycol. It is a non-ionic polyol surface-active agent used medically as a fecal softener and in cattle for prevention of bloat. Oxyethylene Oxypropylene Polymer,Polyoxyethylene Polyoxypropylene Polyoxyethylene Polymer,Bloat Guard,Poloxalene 2930,Proxanol,SK&F-18667,Tergitol,Therabloat,Oxypropylene Polymer, Oxyethylene,Polymer, Oxyethylene Oxypropylene,SK&F 18667,SK&F18667
D002626 Chemistry, Pharmaceutical Chemistry dealing with the composition and preparation of agents having PHARMACOLOGIC ACTIONS or diagnostic use. Medicinal Chemistry,Chemistry, Pharmaceutic,Pharmaceutic Chemistry,Pharmaceutical Chemistry,Chemistry, Medicinal
D002627 Chemistry, Physical The study of CHEMICAL PHENOMENA and processes in terms of the underlying PHYSICAL PHENOMENA and processes. Physical Chemistry,Chemistries, Physical,Physical Chemistries

Related Publications

E V Batrakova, and T Y Dorodnych, and E Y Klinskii, and E N Kliushnenkova, and O B Shemchukova, and O N Goncharova, and S A Arjakov, and V Y Alakhov, and A V Kabanov
in vitro biological evaluation of folate-functionalized block copolymer micelles for selective anti-cancer drug delivery.
July 2008, Macromolecular bioscience,
E V Batrakova, and T Y Dorodnych, and E Y Klinskii, and E N Kliushnenkova, and O B Shemchukova, and O N Goncharova, and S A Arjakov, and V Y Alakhov, and A V Kabanov
Anti-cancer activity of anthracycline antibiotics and DNA condensation.
August 1990, Anti-cancer drug design,
E V Batrakova, and T Y Dorodnych, and E Y Klinskii, and E N Kliushnenkova, and O B Shemchukova, and O N Goncharova, and S A Arjakov, and V Y Alakhov, and A V Kabanov
Silicon Tetrapyrazinoporphyrazine Derivatives-Incorporated Carbohydrate-Based Block Copolymer Micelles for Photodynamic Therapy.
March 2021, ACS applied bio materials,
E V Batrakova, and T Y Dorodnych, and E Y Klinskii, and E N Kliushnenkova, and O B Shemchukova, and O N Goncharova, and S A Arjakov, and V Y Alakhov, and A V Kabanov
A supramolecularly assisted transformation of block-copolymer micelles into nanotubes.
January 2009, Angewandte Chemie (International ed. in English),
E V Batrakova, and T Y Dorodnych, and E Y Klinskii, and E N Kliushnenkova, and O B Shemchukova, and O N Goncharova, and S A Arjakov, and V Y Alakhov, and A V Kabanov
The challenges facing block copolymer micelles for cancer therapy: In vivo barriers and clinical translation.
August 2015, Advanced drug delivery reviews,
E V Batrakova, and T Y Dorodnych, and E Y Klinskii, and E N Kliushnenkova, and O B Shemchukova, and O N Goncharova, and S A Arjakov, and V Y Alakhov, and A V Kabanov
Drug Delivery: Hydrophobic Drug Encapsulation into Amphiphilic Block Copolymer Micelles.
January 2021, Methods in molecular biology (Clifton, N.J.),
E V Batrakova, and T Y Dorodnych, and E Y Klinskii, and E N Kliushnenkova, and O B Shemchukova, and O N Goncharova, and S A Arjakov, and V Y Alakhov, and A V Kabanov
Block Copolymer Micelles in Nanomedicine Applications.
July 2018, Chemical reviews,
E V Batrakova, and T Y Dorodnych, and E Y Klinskii, and E N Kliushnenkova, and O B Shemchukova, and O N Goncharova, and S A Arjakov, and V Y Alakhov, and A V Kabanov
Polydispersity-Driven Block Copolymer Amphiphile Self-Assembly into Prolate-Spheroid Micelles.
February 2012, ACS macro letters,
E V Batrakova, and T Y Dorodnych, and E Y Klinskii, and E N Kliushnenkova, and O B Shemchukova, and O N Goncharova, and S A Arjakov, and V Y Alakhov, and A V Kabanov
Minocycline block copolymer micelles and their anti-inflammatory effects on microglia.
March 2010, Macromolecular bioscience,
E V Batrakova, and T Y Dorodnych, and E Y Klinskii, and E N Kliushnenkova, and O B Shemchukova, and O N Goncharova, and S A Arjakov, and V Y Alakhov, and A V Kabanov
Bacterial anti-adhesive properties of a monolayer of zwitterionic block copolymer micelles.
August 2014, Materials science & engineering. C, Materials for biological applications,
Copied contents to your clipboard!