Abstract

Osteoarthritis (OA) is a chronic disease caused by the damage of articular cartilage. Kartogenin (KGN) is a well-recognized small molecule which could induce MSCs chondrogenesis and promote cartilage repair treatments. Nano-level micells could be a suitable drug carrier technology for the treatments. In this study, the acid-responsive methoxy poly(ethylene oxide)-hydrazone-poly(ε-caprolactone) copolymers, mPEG-Hz-b-PCL, were synthesized. The structure was characterized by 1H NMR. The evaluation of a designed kartogenin drug delivery system (DDS) of hydrazone-linkage-based pH responsive mPEG-Hz-b-PCL nanomicelles for treatment of osteoarthritis could be carried out.

Highlights

  • Osteoarthritis (OA) is a common disease, which is characterized by articular cartilage destruction and local inflammation, resulting in pain and disability (Hunziker et al, 2002)

  • Methoxy polyethylene glycol-hydrazone-blockpolycaprolactone(mPEG-Hz-b-PCL) block copolymer could be prepared as shown in Scheme 1

  • The characteristic peaks at 1.37, 1.64, 2.30, and 4.05 ppm were assigned to the methylene protons of -O(O) CCH2CH2CH2CH2CH2O(H4,H6,H9), -CH2CH2CH2CH2CH2 (H5,H10), -OCCH2(H3,H8), and -CH2O(O)C(H7,H7′) in the PCL segment of methoxy polyethylene glycol (mPEG)-Hz-b-PCL block polymer

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Summary

Introduction

Osteoarthritis (OA) is a common disease, which is characterized by articular cartilage destruction and local inflammation, resulting in pain and disability (Hunziker et al, 2002). Preparation of KGN-loaded mPEG-Hz-b-PCL nanomicelles solution could be carried out by dissolution of 10 mg of KGN molecule and 50 mg of amphiphilic mPEG-Hz-b-PCL block copolymer in 5 ml acetone to prepare a mixed solution. The in vitro release of KGN molecule from different hydrazonelinkage based mPEG-Hz-b-PCL block copolymer solutions was determined using HPLC.

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