Abstract

Oligo(ε-caprolactone) and oligolactide were synthesized via ring-opening polymerization of cyclic esters in the presence of creatinine as initiators. Thus obtained oligomers were successfully used in the synthesis of novel polyurethane conjugates of norfloxacin. The structures of the polymers and conjugates were elucidated by means of MALDI-TOF MS, NMR and IR studies.

Highlights

  • Pharmacy is one of the most important areas of applications of polymers

  • We describe the synthesis of a series of linear polyurethane conjugates of norfloxacin

  • The aim was to obtain a low-molecular weight polyesters, terminated at both sides by hydroxyl groups, which can be subsequently used as segments in polyurethane conjugates

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Summary

Introduction

Pharmacy is one of the most important areas of applications of polymers. They are used as active macromolecular pharmaceutical substances, blood substitutes, auxiliary materials and excipients, reagents for synthesis of macromolecular prodrugs, in polymeric drug delivery systems, therapeutic systems, etc. [1,2,3,4,5,6,7,8,9,10,11]. Pharmacy is one of the most important areas of applications of polymers They are used as active macromolecular pharmaceutical substances, blood substitutes, auxiliary materials and excipients, reagents for synthesis of macromolecular prodrugs, in polymeric drug delivery systems, therapeutic systems, etc. Polyesters, polyethers and polycarbonates are usually used as oligomers They were successfully synthesized by ring opening polymerization of cyclic monomers in the presence of cationic or anionic initiators, as well as coordinating and enzymatic catalysts [19,20,21,22,23,24,25,26,27,28,29,30,31]. The anticancer action of norfloxacin is supposed to be improved by anchoring the drug, using a chemical linkage, to biodegradable oligomers Such delivery systems can transport the drug molecules more efficiently and . We believe that the obtained polyurethanes can find practical applications as effective drug delivery systems transporting active substances to specific body locations at the required rate

Ring-opening polymerization of cyclic esters
H OCHCOCHC OCH2CH2O CCHOCCHO H x
Synthesis of polyurethane conjugates of norfloxacin
OCNR1NCO
Synthesis methods*
C N CH2CH2CH2CH2CH2CH2 N C O g a d
Experimental
Instrumentation
Oligoesters synthesis
Macromolecular conjugates synthesis
Biodegradation of polyurethane conjugates
IR and NMR data
Conclusions
Full Text
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