Tumor-targeting peptide conjugated pH-responsive micelles as a potential drug carrier for cancer therapy
- Tumor-targeting peptide conjugated pH-responsive micelles as a potential drug carrier for cancer therapy
- Xiang Lan Wu; 김종호; 구희범; 배상문; 신혜리; 김민상; 이병헌; 박랑운; 김인산; 최귀원; 권익찬; 김광명; 이두성
- Issue Date
- Bioconjugate chemistry
- VOL 21, NO 2, 208-213
- 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( -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 a 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.
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