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임철원,조은범,김덕준 한국화학공학회 2019 Korean Journal of Chemical Engineering Vol.36 No.1
Mesoporous silica nanoparticles (MSNs) conjugating doxorubicin (DOX) via a pH-sensitive cleavable linkage, hydrazine (HYD) were synthesized. MSN-HYD-DOX were encapsulated with the polyaspartamide (PASPAM) grafted with the hydrophilic o-(2-aminoethyl)-o'-methylpoly(ethylene glycol) (PEG) and the cell permeating ligand, biotin (Biotin). The chemical structure of the synthesized MSN-HYD-DOX and PASPAM-g-PEG/Biotin was confirmed using FT-IR and 1H-NMR spectroscopy. The mean diameter of the MSN-HYD-DOX@PASPAM-g-PEG/Biotin nanoparticle was 142 nm and 121 nm, respectively, examined by dynamic light scattering (DLS) and transmission electron microscope (TEM). The HYD bond was effectively cleaved in acidic condition, and thus DOX was released much faster at pH 5.0 than at pH 7.4. The cell viability in MSN-HYD-DOX@PASPAM-g-PEG/Biotin system was much lower than that of the free DOX drug because of efficient intracellular drug delivery associated with the biotin ligand.
임철원,김덕준 한국고분자학회 2021 한국고분자학회 학술대회 연구논문 초록집 Vol.46 No.1
Nanoparticles with bone targeting ability and pH-sensitivity were prepared with polyaspartamide derivatives based on polysuccinimide grafted with octadecyl amine, hydrazine and polyethylene glycol For the bone targeting, alendronate, which has bone affinity, was grafted to PEG and doxorubicin was conjugated with linkers of acid sensitive hydrazone bonds, which can be cleaved most effectively in an intracellular acidic environment. At pH 5.0, ∼ 75% of the drug was released from ALN-PEG/C18/HYD-DOX-g-PASPAM due to the effective cleavage of HYD under the acidic condition. Also, ALN-bound particles were more effectively adsorbed on the surface of bone than ALN-unbound particles. According to an in vivo antitumor activity test, the volume of tumor treated with ALN-PEG/C18/HYD-DOX-g-PASPAM decreased (1550 mm<sup>3</sup>) when compared with the PBS control sample (3850 mm<sup>3</sup>), proving that ALN-PEG/C18/HYD-DOX-g-PASPAM is an effective drug delivery system for the treatment of bone metastasis of breast cancer.
임철원,김덕준 한국고분자학회 2021 한국고분자학회 학술대회 연구논문 초록집 Vol.46 No.2
In this study, this biocompatible and biodegradable PSI-based nano-aggregates were developed as a wound closing/healing adhesives. In addition to its adhesive effect without toxicity, antifungal drug was loaded for faster wound healing. The hydrophobic C18 and DOPA were grafted onto the PSI to form adhesive nano-aggregates. Neomycin (NEO), an antifungal drug, is conjugated with glycine to enable pH-dependent drug release. While the chemical and physical structure of the synthesized polymers and nano aggreages were analyzed, the drug release patterns as well as wound adhesional properties of nano aggregates were in vitro and in vivo investigated. As a nano-adhesive that simultaneously release antifungal drugs, this material is expected to have a significant impact on wound healing efficiency.