Prodrug-based nano-delivery strategy to improve the antitumor ability of carboplatin in vivo and in vitro

Abstract

Chemotherapy plays a major role in the treatment of cancer, but it still has great limitations in anti-tumor effect. Carboplatin (CAR) is the first-line drug in the treatment of non-small cell lung cancer, but the therapeutic effect is demonstrated weak. Therefore, we modified CAR with hexadecyl chain and polyethylene glycol, so as to realize its liposolubility and PEGylation. The synthesized amphiphilic CAR prodrugs could self-assemble into polymer micelles in water with an average particle size about 11.8 nm and low critical micelles concentration (0.0538 mg·mL –1 ). In vivo pharmacodynamics and cytotoxicity experiment evidenced that the polymer micelles were equipped with preferable anti-tumor effect, finally attained the aim of elevating anti-tumor effect and prolonging retention time in vivo . The self-assembled micelles skillfully solve the shortcomings of weak efficacy of CAR, which provides a powerful platform for the application of chemical drug in oncology.

Chinese medicinal herbs as potential prodrugs for obesity

“…Currently, prodrugs are further developed through the combination of “Nanotechnology.” Prodrugs with nanotechnology have many advantages, e.g., greater bioavailability, higher drug encapsulation, and loading efficiency, as well as the control of drug release ( Luo et al, 2014 ; Lang et al, 2021 ; Zhang et al, 2021 ; Zhang et al, 2022b ). Growing evidence has shown that the combination of nanotechnology and prodrug is more effective to treat obesity than the usage of prodrugs alone.…”

Novel Pt(IV) prodrug self-assembled nanoparticles with enhanced blood circulation stability and improved antitumor capacity of oxaliplatin for cancer therapy

“…The critical micelle concentration of PEG-OXA NPs was measured according to our previous report (Lang et al., 2021 ) using Nile red as fluorescence probe. Briefly, Phosphate Buffered Saline (PBS) solution of PEG-OXA prodrug in different concentrations was added to the vials containing dried Nile red and sonicated for 40 min and deposited for 4 h. The fluorescence spectrum of Nile red excited at 543 nm and emissive at 660 nm was collected at room temperature using multifunctional enzyme marker (SpectraMax M2e, Sunnyvale, CA).…”

Carboplatin Niosomal Nanoplatform for Potentiated Chemotherapy

“…23 Ten days after tumor cells injection and tumor development, animals were randomly divided into four groups (n= 20) and received CB, NS-CB, PEG-NS-CB, and PBS as the control group (groups 1-4, respectively) intravenously at the CB concentration of 1.5 mg/kg at 72 h intervals and for six times. 23,24 The mean weight of animals in each group was measured every 3 days and for 42 days. The volume of the tumor was measured on days 10, 16, 22, 28, 34, and 42 after tumor cell inoculation and calculated according to the long diameter (a) and the short diameter (b).…”

“…The inhibition rate of the tumor was expressed as tumor volume = a£b 2 /2. 24 Also, the number of animals in each group was measured until the end of the study. At the end of day 42, all the animals were euthanized with CO 2 , and their livers and kidneys were harvested.…”