La(Ⅲ) , Y(Ⅲ) complexes with diglycol aldehyde bis-arginine (H2DAAR) and tetraglycol aldehyde bis-lysine (H2TALY) Schiff bases were synthesized. They were characterized and formulated as La( H2DAAR) (NO3)3 ?6H2Oand Y...La(Ⅲ) , Y(Ⅲ) complexes with diglycol aldehyde bis-arginine (H2DAAR) and tetraglycol aldehyde bis-lysine (H2TALY) Schiff bases were synthesized. They were characterized and formulated as La( H2DAAR) (NO3)3 ?6H2Oand Y (H2TALY)(NO3)3 ·5H2Oseparately by elemental analyses. The obtained complexes were investigated in detail by high resolution solid state (HRSS) 13C NMR using cross polarization, magic angle spinning (CPMAS) , and total suppression of sidebands (TOSS)techniques. The results are supported by the liquid state 2D-1 H-13 C COSY NMR spectra. Some new information about the splitting peaks of 13C for -CH=N- group and alkene carbon bands, etc. in HRSS 13C NMR spectra are given.展开更多
Stimuli-responsive drug delivery systems based on polymeric micelles can achieve controlled drug release to improve the therapeutic outcome and reduce unwanted systematic toxicity and side effects of the cytotoxic dru...Stimuli-responsive drug delivery systems based on polymeric micelles can achieve controlled drug release to improve the therapeutic outcome and reduce unwanted systematic toxicity and side effects of the cytotoxic drug in chemotherapy but often face challenging synthesis and purification of functionalized biocompatible polymer materials and low drug loading efficiency. In the present study, we reported a novel redox-responsive self-assembly polymeric micelle system, mPEG-β-CD/Ad-SS-CPT, to achieve high loading efficiency and selective delivery of camptothecin(CPT) in a reductive environment inside cancer cells. The host-guest supramolecular micelles utilized a simple β-CD modified PEG, mPEG-β-cyclodextrin(mPEG-β-CD), as the polymeric host with the ease of synthesis and purification. The guest prodrug Ad-SS-CPT contained the disulfide bond as the redox sensitivity group. The selective cleavage of disulfide bond and subsequent drug release in a reductive environment could potentially reduce system toxicity and improve the therapeutic outcome of CPT. In vitro studies showed that the micelles exhibited excellent cytotoxicity against He La cells comparable to the free drug. The host-guest polymeric micelles also showed great potentials for multi-drug co-delivery. Collectively, our current findings provided a general and convenient approach to design drug delivery systems based on stimuli-responsive polymeric micelles for disease treatment.展开更多
基金Project supported by the National Natural Science Foundation of China (Grant No. 29671026)the Natural Science Foundation of Zhejiang Province (Grant No. 296062)the Laboratory of MRAMP (Grant No. 971502)
文摘La(Ⅲ) , Y(Ⅲ) complexes with diglycol aldehyde bis-arginine (H2DAAR) and tetraglycol aldehyde bis-lysine (H2TALY) Schiff bases were synthesized. They were characterized and formulated as La( H2DAAR) (NO3)3 ?6H2Oand Y (H2TALY)(NO3)3 ·5H2Oseparately by elemental analyses. The obtained complexes were investigated in detail by high resolution solid state (HRSS) 13C NMR using cross polarization, magic angle spinning (CPMAS) , and total suppression of sidebands (TOSS)techniques. The results are supported by the liquid state 2D-1 H-13 C COSY NMR spectra. Some new information about the splitting peaks of 13C for -CH=N- group and alkene carbon bands, etc. in HRSS 13C NMR spectra are given.
基金National Key Research and Development Program of China (Grant No. 2019YFA0904800)Science and Technology Commission of Shanghai Municipality (Grant No. 11DZ2260600 and 10DZ2220500)Shanghai Natural Science Fund (Grant No. 20ZR1414700)。
文摘Stimuli-responsive drug delivery systems based on polymeric micelles can achieve controlled drug release to improve the therapeutic outcome and reduce unwanted systematic toxicity and side effects of the cytotoxic drug in chemotherapy but often face challenging synthesis and purification of functionalized biocompatible polymer materials and low drug loading efficiency. In the present study, we reported a novel redox-responsive self-assembly polymeric micelle system, mPEG-β-CD/Ad-SS-CPT, to achieve high loading efficiency and selective delivery of camptothecin(CPT) in a reductive environment inside cancer cells. The host-guest supramolecular micelles utilized a simple β-CD modified PEG, mPEG-β-cyclodextrin(mPEG-β-CD), as the polymeric host with the ease of synthesis and purification. The guest prodrug Ad-SS-CPT contained the disulfide bond as the redox sensitivity group. The selective cleavage of disulfide bond and subsequent drug release in a reductive environment could potentially reduce system toxicity and improve the therapeutic outcome of CPT. In vitro studies showed that the micelles exhibited excellent cytotoxicity against He La cells comparable to the free drug. The host-guest polymeric micelles also showed great potentials for multi-drug co-delivery. Collectively, our current findings provided a general and convenient approach to design drug delivery systems based on stimuli-responsive polymeric micelles for disease treatment.
