Wu, Xiang Lan Kim, Jong Ho Koo, Heebeom Bae, Sang Mun Shin, Hyeri Kim, Min Sang Lee, Byung-Heon Park, Rang-Woon Kim, In-San Choi, Kuiwon Kwon, Ick Chan Kim, Kwangmeyung Lee, Doo Sung 2024-01-20T20:01:44Z 2024-01-20T20:01:44Z 2021-09-02 2010-02 1043-1802 https://pubs.kist.re.kr/handle/201004/131765 Herein, we prepared tumor-targeting peptide (AP peptide; CRKRLDRN) conjugated pH-responsive polymeric micelles (pH-PMs) in cancer therapy by active and pH-responsive tumor targeting delivery systems, simultaneously. The active tumor targeting and tumoral pH-responsive polymeric micelles were prepared by mixing AP peptide conjugated PEG-poly(D,L-lactic acid) block copolymer (AP-PEG-PLA) into the pH-responsive micelles of methyl ether poly(ethylene glycol) (MPEG)-poly(beta-amino ester) (PAE) block copolymer (MPEG-PAE). These mixed amphiphilic block copolymers were self-assembled to form stable AP peptide-conjugated and pH-responsive APPEG-PLA/MPEG-PAE micelles (AP-pH-PMs) with an average size of 150 nm. The AP-pH-PMs containing 10 wt % of AP-PEG-PLA showed a sharp pH-dependent micellization/demicellization transition at the tumoral acid pH. Also, they presented the pH-dependent drug release profile at the acidic pH of 6.4. The fluorescence dye, TRITC, encapsulated AP-pH-PMs (TRITC-AP-pH-PMs) presented the higher tumor-specific targeting ability in vitro cancer cell culture system and in vivo tumor-bearing mice, compared to control pH-responsive micelles of MPEG-PAE. For the cancer therapy, the anticancer drug, doxorubicin (DOX), was efficiently encapsulated into the AP-pH-PMs (DOX-AP-pH-PMs) with it higher loading efficiency. DOX-AP-pH-PMs efficiently deliver anticancer drugs in MDA-MB231 human breast tumor-bearing mice, resulted in excellent anticancer therapeutic efficacy, compared to free DOX and DOX encapsulated MEG-PAE micelles, indicating the excellent tumor targeting ability of AP-pH-PMs. Therefore, these tumor-targeting peptide-conjugated and pH-responsive polymeric micelles have great potential application in cancer therapy. English AMER CHEMICAL SOC GLYCOL CHITOSAN NANOPARTICLES BLOCK-COPOLYMER MICELLES IN-VIVO EXPLOITATION EFFICACY RELEASE Tumor-Targeting Peptide Conjugated pH-Responsive Micelles as a Potential Drug Carrier for Cancer Therapy Article 10.1021/bc9005283 1 BIOCONJUGATE CHEMISTRY, v.21, no.2, pp.208 - 213 BIOCONJUGATE CHEMISTRY 21 2 208 213 scie scopus 000274514300003 2-s2.0-77049115727 Biochemical Research Methods Biochemistry & Molecular Biology Chemistry, Multidisciplinary Chemistry, Organic Biochemistry & Molecular Biology Chemistry Article GLYCOL CHITOSAN NANOPARTICLES BLOCK-COPOLYMER MICELLES IN-VIVO EXPLOITATION EFFICACY RELEASE