Determination of doxorubicin amount conjugated to mPEG-b-PCL copolymer via pH sensitive hydrazone bond pH duyarlı hidrazon bağıyla mPEG-b-PCL kopolimerine konjuge edilen doksorubisin miktarının belirlenmesi

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Işik G., TEZCANER A., Hasirci N., KIZILTAY A.

Turk Hijyen ve Deneysel Biyoloji Dergisi, vol.79, no.2, pp.279-292, 2022 (Scopus) identifier

  • Publication Type: Article / Article
  • Volume: 79 Issue: 2
  • Publication Date: 2022
  • Doi Number: 10.5505/turkhijyen.2022.04317
  • Journal Name: Turk Hijyen ve Deneysel Biyoloji Dergisi
  • Journal Indexes: Scopus, Academic Search Premier, CAB Abstracts, Veterinary Science Database, TR DİZİN (ULAKBİM)
  • Page Numbers: pp.279-292
  • Keywords: Doxorubicin, Drug conjugation, Hydrazine bond, Mpegb-pcl, Trinitrobenzene sulfonic acid
  • Middle East Technical University Affiliated: Yes


© 2022. Turk Hijyen ve Deneysel Biyoloji Dergisi. All Rights Reserved.Objective: The aim of this study was to find the efficient medium to bind an anticancer drug, Doxorubicin (DOX), to a synthesized polymer, methoxy poly(ethylene glycol)-block-polycaprolactone (mPEG-b-PCL) via pH sensitive hydrazone bonds and to determine the amount of conjugated drug. Methods: DOX conjugation was carried out in two different media [dimethyl sulfoxide (DMSO) and methanol-trifluoroacetic acid (MeOH-TFA)]. The amount of conjugated drug was determined with two different methods. One method was applied the dissolution of the conjugate in chloroform: methanol (Ch: MeOH, 1: 1 v/v) solution without considering pH responsiveness, and the other method was after breaking pH sensitive hydrazone bonds in acidic medium [using three different media as 0.1 M hydrochloric acid (HCl), concentrated HCl (12 M HCl) and concentrated sulfuric acid (18.3 M H2SO4)]. Results: The highest conjugation efficiency was obtained when the conjugation was achieved in MeOHTFA solution, and for the polymer-drug conjugates after the treatment with concentrated sulfuric acid. Conclusion: It was concluded that, MeOH-TFA method was a good method for conjugation of DOX to mPEG-b-PCL copolymer, and H2SO4 (18.3 M) method was better than any other present in literature for determination of the amount of DOX linked to the polymer via hydrazone conjugation.