1228151-23-2Relevant academic research and scientific papers
Novel naproxen-peptide-conjugated amphiphilic dendrimer self-assembly micelles for targeting drug delivery to osteosarcoma cells
Zhao, Yinbo,Zeng, Qi,Wu, Fengbo,Li, Jing,Pan, Zhaoping,Shen, Pengfei,Yang, Lu,Xu, Ting,Cai, Lulu,Guo, Li
, p. 60327 - 60335 (2016/07/11)
The aim of the current study was to synthesize and prepare novel self-assembly micelles loaded with curcumin (Cur) based on naproxen (Nap)-conjugated amphiphilic dendrimers. The apoptosis-inducing capacity of Nap-conjugated dendrimers and curcumin, the efficiency of uptake and the potential molecular mechanism on human osteosarcoma cells were investigated. The Nap-conjugated amphiphilic dendrimers were successfully synthesized, and the corresponding Cur-loaded micelles were conventionally prepared via self-assembly. These micelles showed good drug-encapsulating capacity, physiochemical properties, and drug-release profiles. The cellular proliferation and uptake assay suggested that the Cur-M-Nap induced more apoptosis of MG-63 human osteosarcoma cells. The western blot results suggested that these Nap-modified micelles could enhance the Cur-inducing apoptosis, mainly via intrinsic pathways and inhibition of the inflammation pathway. In summary, the Cur-loaded amphiphilic dendrimer-based micelles were successfully developed and they enhanced drug delivery to MG-63 cells. Mechanistic experiments suggested that Cur loaded into amphiphilic dendrimer-based micelles had a higher proliferation-inhibiting ability than free Cur, and could induce more apoptosis.
Design, synthesis and biological evaluation of enzymatically cleavable NSAIDs prodrugs derived from self-immolative dendritic scaffolds for the treatment of inflammatory diseases
Wei, Jinbao,Shi, Jianyou,Zhang, Jing,He, Gu,Pan, Junzhu,He, Jun,Zhou, Rui,Guo, Li,Ouyang, Liang
supporting information, p. 4192 - 4200 (2013/07/27)
It has been reported that delivery systems based on dendritic prodrugs of Nonsteroidal Anti-Inflammatory Drugs (NSAIDs) improved the properties of drug molecules and reduced the side effects and irritation on the gastric mucosa. To find a more effective way in NSAIDs dendritic prodrugs, in this paper, three different dendritic scaffolds of enzymatically cleavable naproxen conjugates have been synthesized in a convergent approach and well characterized by NMR and MS techniques. These self-immolative dendritic NISADs prodrugs programmed to release multiple molecules of the potent naproxen after a single enzymatic activation step, and in 50% human plasma, the drug released from the compound T3 reaching 47.3% after 24 h in vitro assay. Moreover, all prodrugs were also found to maintain more significant anti-inflammatory activity, no significant cytotoxicity against HEK293 cells and less degree of ulcerogenic potential in vivo than their monomeric counterpart naproxen. These results provided an effective entry to the development of new dendritic NSAIDs prodrugs.
Synthesis of water-soluble first generation janus-type dendrimers bearing Asp oligopeptides and naproxen
Ouyang, Liang,Ma, Lifang,Li, Yanhua,Pan, Junzhu,Guoa, Li
experimental part, p. 256 - 266 (2010/08/07)
To construct a water-soluble and bone-targeting non-steroidal anti-inflammatory dendritic drug carrier, a series of Asp oligopeptides and naproxen based poly amido-ester Janus dendrimers were synthesized using a conventional method and their water solubility was preliminary evaluated. The corresponding small dendritic linkers contain two or three drug moieties on the surface and two or three oligopeptides groups at the focal terminus. This design provided an effective entry for the synthesis of multiple drug carriers with water-soluble and bone-targeting.
