Stabilization and sustained release of zeylenone, a soft cytotoxic drug, within polymeric micelles for local antitumor drug delivery

Hu, Xiaoyun; Han, Rong; Quan, Li-Hui; Liu, Chunyu

doi:10.1016/j.ijpharm.2013.04.007

Cited by 23 publications

(23 citation statements)

References 16 publications

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“…When the CA loading was 1.89% (w/w), the EE was higher than 98% ( Table 1). The ability of PEG-PLGA micelles to encapsulate hydrophobic drugs was documented previously [32,36,37]. In the present study, the encapsulation of CA inside the micelle cores was confirmed by 1 H NMR results and the morphological examination of the micelles before and after nebulization was performed using TEM (Supplemental Figs.…”

Section: Characterization Of Micellessupporting

confidence: 82%

“…Micelles loaded either with CA or a mixture of CA and Nile red or coumarin-6 (5:1) were prepared according to the previously published solvent evaporation method [32]. Briefly, CA, Nile red/coumarin-6 and mPEG 2000 -PLGA 5000 (1:40, w/w) were codissolved in dichloromethane.…”

Section: Preparationmentioning

confidence: 99%

“…The CA or Nile red/coumarin-6 loading content (DL) and encapsulation efficiency (EE) were determined as reported previously [32].…”

Section: Encapsulation Efficiencymentioning

confidence: 99%

See 2 more Smart Citations

Pulmonary delivered polymeric micelles – Pharmacokinetic evaluation and biodistribution studies

Yang

Quan

et al. 2014

European Journal of Pharmaceutics and Biopharmaceutics

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Section: Characterization Of Micellessupporting

confidence: 82%

Section: Preparationmentioning

confidence: 99%

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Pulmonary delivered polymeric micelles – Pharmacokinetic evaluation and biodistribution studies

Yang

Quan

et al. 2014

European Journal of Pharmaceutics and Biopharmaceutics

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“…Amphiphilic derivatization of PLGA can be achieved by conjugation of hydrophilic polymer chains, such as, PEG [87,40,37] and poly(ethyleneimine) (PEI) [57]. The drug is loaded into the polymeric micelle via incorporation into the core [37], chemical conjugation to the block copolymer [87,40], or simple surface adsorption [57]. PLGA-based polymeric micelles have shown promise in cancer therapy [87,40,37] and gene delivery [57].…”

Section: Micellesmentioning

confidence: 99%

“…The drug is loaded into the polymeric micelle via incorporation into the core [37], chemical conjugation to the block copolymer [87,40], or simple surface adsorption [57]. PLGA-based polymeric micelles have shown promise in cancer therapy [87,40,37] and gene delivery [57].…”

Section: Micellesmentioning

confidence: 99%

Advanced Engineering Approaches in the Development of PLGA-Based Nanomedicines

El-Hammadi¹,

Arias²

2015

Handbook of Nanoparticles

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Drug molecules often display little affinity for nonhealthy tissues and/or cells, leading to inefficiency, and high incidence of severe side effects. To face the problem, numerous strategies have been postulated, i.e., chemical modifications to the drug molecule, and proper engineering of drug nanocarriers. In this line, the introduction of poly(D,L-lactide-co-glycolide) nanoparticles in the drug delivery arena has been hypothesized to optimize drug biodistribution and concentration into the targeted site, thus improving the therapeutic effect while reducing the associated drug toxicity. Recent advances in the field have been devoted to the optimization of the in vivo fate and effectiveness of poly(D,L-lactide-co-glycolide)-based drug nanocarriers, i.e., by passive targeting strategies based on the functionalization of the particle surface with special biomolecules, and/or active targeting stratagems thanks to modifications leading to stimuliresponsive nanoparticles. In this chapter, we analyze the current state of the art and future perspectives in the formulation of poly(D,L-lactide-co-glycolide)-based nanomedicines against severe diseases.

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Zeylenone synergizes with cisplatin in osteosarcoma by enhancing DNA damage, apoptosis, and necrosis via the Hsp90/AKT/GSK3β and Fanconi anaemia pathway

Yang

Xiao

Sun

et al. 2021

Phytotherapy Research

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A safer and more effective combination strategy designed to enhance the efficacy and minimize the toxicity of cisplatin in osteosarcoma (OS) is urgently needed. Zeylenone (zey), a cyclohexene oxide compound, exerted an obvious inhibitory effect on several cancer cell lines and exhibited little cytotoxicity towards normal cells, enabling zey to play a unique role in combination therapy. Thus, the study aimed to determine whether the combination of zey and cisplatin produces synergistic antitumour effects on OS and to further explore molecular mechanisms. Initially, we found that zey potentiated the anti-osteosarcoma efficacy of cisplatin and exhibited synergistic interactions with cisplatin in vitro, which also were confirmed in vivo by using xenograft model. Mechanistically, zey and cisplatin synergistically induced DNA damage, cell cycle arrest, necrosis, and apoptosis in OS cells. Importantly, zey had a high binding affinity for Hsp90 and reduced the expression of Hsp90, which further induced the suppression of AKT/GSK3β signalling axis and the degradation of Fanconi anaemia (FA) pathway proteins. Thus, the Hsp90/AKT/GSK3β and FA pathway are the key to the synergism between zey and cisplatin. Overall, zey shows promise for development as a cisplatin chemosensitizer with clinical utility in restoring cisplatin sensitivity of cancer cells.

show abstract

Stabilization and sustained release of zeylenone, a soft cytotoxic drug, within polymeric micelles for local antitumor drug delivery

Cited by 23 publications

References 16 publications

Pulmonary delivered polymeric micelles – Pharmacokinetic evaluation and biodistribution studies

Pulmonary delivered polymeric micelles – Pharmacokinetic evaluation and biodistribution studies

Advanced Engineering Approaches in the Development of PLGA-Based Nanomedicines

Zeylenone synergizes with cisplatin in osteosarcoma by enhancing DNA damage, apoptosis, and necrosis via the Hsp90/AKT/GSK3β and Fanconi anaemia pathway

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