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Pharmaceutical composition comprising at least one anticancer drug and at least one polymer

A composition and polymer technology, applied in the field of improved anticancer drug composition, and improved composition for cancer treatment, which can solve the problems of low clinical side effects, no side effects of hair loss or hair loss, etc.

Inactive Publication Date: 2009-07-29
PANACEA BIOTEC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although various attempts have been made previously to provide anticancer compositions with improved efficacy, none of these compositions exhibited low clinical side effects, and in particular, none of these compositions provided a reduction in particularly distressing alopecia or hair loss. Ways to lose side effects

Method used

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  • Pharmaceutical composition comprising at least one anticancer drug and at least one polymer
  • Pharmaceutical composition comprising at least one anticancer drug and at least one polymer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0104] Example 1: Synthesis of PLGA nanoparticles encapsulating paclitaxel:

[0105] Nanoparticles were synthesized from d,l-lactic-co-glycolic acid (PLGA) by w / o / w double emulsification using a double emulsification process. In a typical experiment, 100 mg of PLGA was dissolved in 2 mL of dichloromethane and 10 mg of paclitaxel was dissolved in 1.0 mL of absolute ethanol. The two solutions were slowly mixed together with stirring. A first water-in-oil (w / o) emulsion was prepared by emulsifying 500 μL of phosphate buffered saline in the above solution. The first water-in-oil emulsion was then further emulsified in a poly-N-acetylacrylamide solution to form a water-in-oil-in-water (w / o / w emulsion). The w / o / w emulsion thus prepared was homogenized to form paclitaxel-loaded nanoparticles after evaporation of the solvent. The solution is then centrifuged and selectively isolates nanoparticles in the desired size range. The nanoparticles were then dispersed in sterile water and...

Embodiment 2

[0106] Example 2: Covalent binding of PLGA to pullulan micellar nanoaggregates and loading of paclitaxel:

[0107] PLGA was covalently bound to pullulan by activating PLGA with N-hydroxysuccinimide. The pullulan-PLGA complex was purified by gel filtration and characterized by FTIR, H-NMR and mass spectrometry. The hydrophobically treated pullulan solution was lyophilized and kept deep frozen for future use.

[0108] 100 mg of hydrophobized pullulan was dissolved in 10 mL of water and the solution was vortexed to form micelles. A paclitaxel solution prepared in ethanol was slowly added to the micellar solution and dissolved until the solution was clear, indicating that the drug was encapsulated in the micellar formulation. Drug-loaded particles in the desired range are preferentially isolated and the solution is lyophilized.

[0109] Encapsulation efficiency or loading capacity and paclitaxel release behavior from nanoparticles were determined by standard techniques using HP...

Embodiment 3

[0114] Embodiment 3: Preparation of paclitaxel-human serum albumin nanoparticles:

[0115] Dissolve 1800mg of human serum albumin in sterile water for injection. Separately 200 mg of paclitaxel was dissolved in ethanol. Slowly add the alcohol solution into the aqueous solution of human serum albumin under high-speed stirring. The resulting emulsion is passed through a high pressure homogenizer for a time sufficient to obtain the desired nanoparticle size. Ethanol was removed from the nanoparticles under reduced pressure, after which they were particle sieved, first through a 0.2 micron filter and then through a 0.1 micron filter. Fractionated nanoparticles were sterile filtered through a 0.2 micron filter, ultrafiltered, and lyophilized in vials. Measure various parameters of particles.

[0116] Table 1:

[0117] Test No.

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Abstract

The present invention relates to novel and improved compositions of anticancer drugs, preferably taxanes, such as paclitaxel and docetaxel, their derivatives or their analogues, methods of manufacturing these compositions and methods of fractionating the particles in particular size range and methods of treating cancer patients with these compositions, which provide reduced chemotherapy-induced side-effects especially reduced chemotherapy-induced- alopecia. The composition is such that there is substantially no free drug in the said composition.

Description

[0001] This invention relates to new and improved anticancer drug compositions. The present invention relates to novel and improved compositions for the treatment of cancer having substantially reduced chemotherapy-induced side effects. [0002] The present invention relates to novel and improved anticancer drug compositions, including but not limited to alkylating agents, antimetabolite drugs, antibiotic anticancer drugs, plant alkaloid drugs, anthracenediones, natural products, Hormones, hormone antagonists, miscellaneous agents, radiosensitizers, platinum coordination complexes, adrenocortical inhibitors, immunosuppressants, functional therapeutic agents, gene therapy agents, antisense therapeutic agents, tyrosine Kinase inhibitors, monoclonal antibodies, immunotoxins, radioimmunoconjugates, cancer vaccines, interferons, interleukins, substituted ureas, taxanes, and COX-2 inhibitors. [0003] The present invention relates to novel and improved anticancer drug compositions, p...

Claims

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Application Information

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IPC IPC(8): A61K45/08A61P35/00
Inventor 阿马尔吉特·辛格塞尔伯吉特·辛格阿贾·K·古普塔曼格史·M·库尔卡尼
Owner PANACEA BIOTEC
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