DDS catalog request

PUREBRIGHT® MB Series

Advantage of PUREBRIGHT® MB Series
  ・ High Performance of Solubility to any Hydrophobic Drugs
    ・ Phosphorylcholine-Base Biocompatible Polymer
    ・ No Irritation
    ・ No Toxicity
    ・ Nano Particle Drug Delivery

NOF provides unigue hydrophilic polymers (PUREBRIGHT® MB) that allow ready solubilization of hydrophobic drugs in aqueous solutions. These polymers consist of copolymers of 2-methacryloyloxyethyl phosphorylcholine (MPC™) and n-butyl methacrylate (BMA). Introduction of hydrophobic BMA units leads to solubilization of drugs via hydrophobic interactions.

Patent No. : JP3571878, JP4233251, US6214957


High Performance of Solubility to any Hydrophobic Drugs

1. High Performance of Solubility

Lyophilized paclitaxel with PUREBRIGHT® MB-37

Paclitaxel : 2mg
PUREBRIGHT® MB-37 : 30mg
Distilled water : 1ml

T. Konno, J. Watanabe, K. Ishihara, J.Biomed. Mater. Res., 65A, 210-215 (2003)
Ishihara et al. Patent JP2004-175752A

2. Solubilization of Paclitaxel

Solubilization of Paclitaxel

3. Typical solubilization Method

Typical solubilization Method

4. Relative solubilization activity of PUREBRIGHT® MB series to DMSO solution

Relative solubilization activity of PUREBRIGHT® MB series to DMSO solution

References:
  1. K. Ishihara, et al., J. Biomed. Mater. Res., in press (2002)
  2. T. Konno, et., Proceed. Int'l. Symp. Control. Rel. Bioact. Mater., 29, 464 (2002)
  3. Efficacy of an MPC-BMA Co-polymer as a Nanotransporter for Paclitaxel (ANTICANCER RESEARCH 27: 1431-1436(2007))

5. Toxicological Data

Safety data of PUREBRIGHT® MB-37 series shows similar activity in comparison with other solubilizers, such as poloxamer and polyoxyethylene castor oil. LDs of more than 25,000mg/kg (mice, orally) and more than 1,000mg/kg (rats, iv) have been obtained.

Toxicological Data



6. Unique Feature : Water soluble film of drug and PUREBRIGHT® MB-37 series

Water soluble film of drug and PUREBRIGHT® MB-37 series Water soluble film can be also obtained with evaporating solution in which drugs and PUREBRIGHT® MB-37 series are dissolved.

References:
K.Ishihara, et al., J.Biomed.Mater.Res. ,65A, 2. 210-215 (2003)
T.Konno, et al., Proceed.Int'l.Symp.Control.Rel.Bioact.Mater., 29, 464 (2002)


7. Pharmaceutical Application (Published) :

  1. Oncology Drug Formulation
    • 1) H. Takeuchi et al., "Molecular Diagnosis and Translymphatic Chemotherapy Targeting Sentinel Lymph Nodes of Patients with Early Gastrointestinal Cancers"; Digestion 82, 187-191(2010).
    • 2) T. Kamei et al., "Spatial distribution of intraperitoneally administrated palitaxel nanoparticles soluybilized with poly (2-methacryloxyethyl phosphorylcholine-co n-butyl methacrylate) in peritoneal metastatic nodules"; Cancer Sci.102(1),200-205 (2010).
    • 3) D. Soma et al., "Intraperitoneal administration of paclitaxel solubilized with poly(2-methacryloxyethyl phosphorylcholine-co n-butyl methacrylate) for peritoneal dissemination of gastric cancer"; Cancer Sci. 100(10), 1979-1985 (2009).
  2. DNA Delivery
    M. Ukawa et al., "2-Methacryloyloxyethyl phosphorylcholine polymer (MPC)-coating improves the transfection activity of GALA-modified lipid nanoparticles by assisting the cellular uptake and intracelluar dissociation of plasmid DNA in primary hepatocytes"; Biomaterials 31(24),6355 - 6362 (2010).
    // <!--[CDATA[ swfobject.registerObject("movie"); // ]]-->