Enhancing the water dispersibility of paclitaxel by complexation with hydrophobic peptides.
The complex between paclitaxel (Ptx) and a peptide mixture (Pep) was prepared to enhance of the water-dispersibility of Ptx. Pep was prepared by enzymatic hydrolysis of casein, followed by fractionation using ammonium sulfate precipitation and ultrafiltration. The Ptx and Pep complex (Ptx-Pep) was prepared by mixing an ethanol solution of Ptx and an aqueous solution of Pep followed by lyophilization. The water dispersibility test of Ptx-Pep prepared using different fractions of Pep demonstrated that a fraction (Pep-A), containing relatively hydrophobic peptides with high molecular weights, was effective in enhancing the water dispersibility of Ptx. The sequences of the major peptides in Pep-A were identified by matrix-assisted laser desorption/ionization time-of-flight/time-of-flight mass spectrometry with "LIFT" technique. The water dispersibility of the complex between Ptx and Pep-A (Ptx-Pep-A) was independent of pH, even though it is positively or negatively charged under strongly acidic and neutral conditions. As the particle size of Ptx-Pep-A in aqueous media was 147-215 nm, Ptx-Pep-A was present as a hydrocolloidal material in aqueous media.
Department of Applied Chemistry, Faculty of Engineering, University of Miyazaki, 1-1 Gakuen Kibanadai Nishi, Miyazaki 889-2192, Japan. Electronic address: na14001@student.miyazaki-u.ac.jp.
Asuka
A
Inada
Department of Applied Chemistry, Faculty of Engineering, University of Miyazaki, 1-1 Gakuen Kibanadai Nishi, Miyazaki 889-2192, Japan. Electronic address: oshimat@cc.miyazaki-u.ac.jp.
Tatsuya
T
Oshima
Department of Applied Chemistry, Faculty of Engineering, University of Miyazaki, 1-1 Gakuen Kibanadai Nishi, Miyazaki 889-2192, Japan. Electronic address: t0g202u@cc.miyazaki-u.ac.jp.
Yoshinari
Y
Baba
D000595:Amino Acid Sequence; D000645:Ammonium Sulfate / Q000737:chemistry; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry*; D002364:Caseins / Q000737:chemistry; D003102:Colloids / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D057927:Hydrophobic and Hydrophilic Interactions; D008969:Molecular Sequence Data; D008970:Molecular Weight; D017239:Paclitaxel / Q000737:chemistry*; D010316:Particle Size; D010455:Peptides / Q000737:chemistry*; D012995:Solubility; D014462:Ultrafiltration; D014867:Water
D000972:Antineoplastic Agents, Phytogenic; D002364:Caseins; D003102:Colloids; D010455:Peptides; D014867:Water; D017239:Paclitaxel; D000645:Ammonium Sulfate
Complex; Dispersibility; Paclitaxel; Peptide; Solubility