PEG-peptide conjugate containing cathepsin B degradation unit as a doxorubicin carrier system

A drug delivery system (DDS) containing a cathepsin B degradable sequence and pH-responsive histidines was prepared by methoxypolyethylene glycol and peptide conjugation. Doxorubicin was attached to the carrier system using amide linkage to give the final form of the DDS, denoted as mPEG-AT3-DOX. mPEG-AT3-DOX exhibited a bimodal size distribution at about 15 and 30 nm independent of pH, whereas the size of the control DDS containing no peptide sequence, mPEG-DOX, was measured as $\sim$ 15-20 nm. At the end of 72 h, % doxorubicin release from both of the DDSs was observed to be below 8.5 $\pm$ 3% in the absence of cathepsin B, and it increased to 17 $\pm$ 2% in the presence of cathepsin B for mPEG-AT3-DOX. Complete degradation of AT3 peptide within 3 h upon incubation with cathepsin B suggests that lower than expected doxorubicin release is likely due to the aggregation tendency of mPEG-AT3-DOX. Absolute IC$_{50}$ values indicated that the cytotoxicity trend of the samples is in the order of free DOX $\ge $ mPEG-AT3-DOX \textgreater mPEG-DOX. Considering these results, PEG-peptide-doxorubicin conjugates can be promising candidates in cancer therapy if they are designed to have more pronounced pH-responsive behavior to increase the drug release rate.
Turkish Journal of Chemistry-Cover
  • ISSN: 1300-0527
  • Yayın Aralığı: Yılda 6 Sayı
  • Yayıncı: TÜBİTAK
Sayıdaki Diğer Makaleler

Electrochemical polymerization of a new alkoxy-bridged dithieno (3,2-B:2’,3’-D) pyrrole derivative

Arif KIVRAK, Hüseyin Bekir YILDIZ, Selahattin GÖKYER, Buket BEZGİN ÇARBAŞ

Zahra KHAGHANPOUR, Sanaz NAGHIBI

Adsorptive properties of mesoporous silica modified with Lewis base molecule and its application in the preconcentration of Cu(II), Co(II), and Cd(II) from aqueous media

Janaine do Rocio IVASSECHEN, Luiz Fabricio ZARA, Alexandre de Oliveira JORGETTO, Marcos Henrique Pereira WONDRACEK, Bruno Prior ROCHA, Gustavo Rocha CASTRO, Adrielli Cristina Peres da SILVA, Valber de Albuquerque PEDROSA, Margarida Juri SAEKI

Janaíne Do Rócio IVASSECHEN, Alexandre De Oliveira JORGETTO, Marcos Henrique Pereira WONDRACEK, Adrielli Cristina Peres Da SILVA, Luiz Fabrício ZARA, Valber De Albuquerque PEDROSA, Bruno Prior ROCHA, Margarida Juri SAEKI, Gustavo Rocha CASTRO

Synthesis and characterization of new thiophene–benzimidazole-based electrochromes

Emine Gül CANSU ERGÜN

Effect of pH and $\beta$-cyclodextrin on the photophysical properties of lamotrigine

Raed GHANEM, Fakhri YOUSEF, Omar Abu AWWAD

Arif KIVRAK, Can YILMAZ, Metin KONUŞ, Halil KOCA, Selahattin AYDEMİR, Jeger Ali OAGAZ

Development of a molecularly imprinted polymer-based electrochemical sensor for tyrosinase

Aysu YARMAN

PEG-peptide conjugate containing cathepsin B degradation unit as a doxorubicin carrier system

Nesligül ŞENTÜRK, Ayben TOP

Application of a pencil graphite electrode for voltammetric simultaneous determination of ascorbic acid, norepinephrine, and uric acid in real samples

Abdulkadir LEVENT, Günay ÖNAL