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Solubilizer & Novel Excipients

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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 biocompatible, hydrophilic polymer-excipients, PUREBRIGHT® MB series that helps you soluble any hydrophobic drugs in aqueous solutions. PUREBRIGHT® MB consists of well-known biocompatible aqueous monomer, 2-methacryloyloxyethyl phosphorylcholine (MPC™) with n-butyl methacrylate (BMA) as hydrophobic part. This hydrophilic and hydrophobic balance has a flexibility to absorbe any drugs in the BMA core to make nano micelle in the solution.

table Patent No. : JP3571878, JP4233251, US6214957


High Performance of Solubility to any Hydrophobic Drugs
1. High Performance of Solubility

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 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

graph

3. Typical solubilization Method

illast

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

table

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))
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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.

table

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

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

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

Pharmaceutical Application (paper) :
  1. Oncology Drug Formulation
    • 1) Molecular Diagnosis and Translymphatic Chemotherapy Targeting Sentinel Lymph Nodes of Patients with Early Gastrointestinal Cancers (Digestion 2010;82:187-191)
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    • 2) Spatial distribution of intraperitoneally administrated palitaxel nanoparticles soluybilized with poly (2-methacryloxyethyl phosphorylcholine-co n-butyl methacrylate) in peritoneal metastatic nodules (Cancer Sci | 2010)
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    • 3) Intraperitoneal administration of paclitaxel solubilized with poly(2-methacryloxyethyl phosphorylcholine-co n-butyl methacrylate) for peritoneal dissemination of gastric cancer (Cancer Sci | October 2009 | vol. 100 | no.10)
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  2. DNA Delivery
    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 (2010) 6355 - 6362
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