Preliminary study on fabrication, characterization and synergistic anti-lung cancer effects of self-assembled micelles of covalently conjugated celastrol-polyethylene glycol-ginsenoside Rh2.

Drug Delivery
Peng LiYang Ling

Abstract

The aim of this study was to develop an amphipathic polyethylene glycol (PEG) derivative that was bi-terminally modified with celastrol and ginsenoside Rh2 (Celastrol-PEG-G Rh2). Such derivative was capable of forming novel, celastrol-loaded polymeric micelles (CG-M) for endo/lysosomal delivery and thereby synergistic treatment of lung cancer. Celastrol-PEG-G Rh2 with a yield of 55.6% was first synthesized and characterized. Its critical micellar concentration was 1 × 10-5 M, determined by pyrene entrapment method. CG-M had a small particle size of 121.53 ± 2.35 nm, a narrow polydispersity index of 0.214 ± 0.001 and a moderately negative zeta potential of -23.14 ± 3.15 mV. Celastrol and G Rh2 were rapidly released from CG-M under acidic and enzymatic conditions, but slowly released in normal physiological environments. In cellular studies, the internalization of celastrol and G Rh2 by human non-small cell lung cancer (A549) cells treated with CG-M was 5.8-fold and 1.8-fold higher than that of non-micelle control. Combinational therapy of celastrol and G Rh2 using CG-M exhibited synergistic anticancer activities in cell apoptosis and proliferation assays via rapid drug release within endo/lysosomes. Most importantly, the celastr...Continue Reading

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Citations

Aug 1, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Shuyu ZhanJeffrey Wang
Dec 29, 2020·Frontiers in Pharmacology·Jinfeng ShiChaomei Fu
Feb 25, 2021·Evidence-based Complementary and Alternative Medicine : ECAM·Heeok HongSeong Gu Hwang
May 17, 2021·International Journal of Pharmaceutics·Yuyao LiaoXinyuan Shi
Jun 29, 2021·Frontiers in Pharmacology·Pushkaraj Rajendra WaghJeffrey Wang

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