State Key Laboratory of Long acting

Yantai, China

State Key Laboratory of Long acting

Yantai, China
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Zhang X.,Yantai University | Zhang X.,State Key Laboratory of Long acting | Zhang X.,Luye Pharmaceutical Co. | Li X.,Yantai University | And 14 more authors.
International Journal of Nanomedicine | Year: 2017

Glioma has one of the highest mortality rates among primary brain tumors. The clinical treatment for glioma is very difficult due to its infiltration and specific growth locations. To achieve improved drug delivery to a brain tumor, we report the preparation and in vitro and in vivo evaluation of curcumin nanoparticles (Cur-NPs). The cyclic hexapeptide c(RGDf(N-me)VK)-C (cHP) has increased affinity for cells that overexpress integrins and was designed to target Cur-NPs to tumors. Functional polyethyleneglycol-modified poly(d,l-lactide-co-glycolide) (PEG-PLGA) conjugated to cHP was synthesized, and targeted Cur-NPs were prepared using a self-assembly nanoprecipitation process. The physicochemical properties and the in vitro cytotoxicity, accuracy, and penetration capabilities of Cur-NPs targeting cells with high levels of integrin expression were investigated. The in vivo targeting and penetration capabilities of the NPs were also evaluated against glioma in rats using in vivo imaging equipment. The results showed that the in vitro cytotoxicity of the targeted cHP-modified curcumin nanoparticles (cHP/Cur-NPs) was higher than that of either free curcumin or non-targeted Cur-NPs due to the superior ability of the cHP/Cur-NPs to target tumor cells. The targeted cHP/Cur-NPs, c(RGDf(N-me)VK)-C-modified Cur-NPs, exhibited improved binding, uptake, and penetration abilities than non-targeting NPs for glioma cells, cell spheres, and glioma tissue. In conclusion, c(RGDf(N-me)VK)-C can serve as an effective targeting ligand, and cHP/Cur-NPs can be exploited as a potential drug delivery system for targeting gliomas. © 2017 Zhang et al.

Wang A.,Jilin University | Wang A.,Yantai University | Wang L.,Jilin University | Sun K.,Yantai University | And 6 more authors.
Pharmaceutical Research | Year: 2012

Purpose To prepare rotigotine loaded microspheres (RoMS) to achieve continuous dopaminergic stimulation (CDS) for the treatment of Parkinson's disease (PD) and investigate both the therapeutic benefit and inducibility of AIMs of administration of RoMS combination with L-DOPA in 6-OHDA-leisioned rats. Methods Rotigotine was encapsulated into poly(lactic-co-glycolic acid) (PLGA) microspheres by an oil-in-water emulsion solvent evaporation technique. In vitro characteristics and in vivo pharmacokinetics of RoMS either in rat blood or brain (by microdialysis) were investigated. Contraversive rotations and AIMs were observed to investigate the therapeutic benefit and the propensity to induce dyskinesia of RoMS or RoMS combination with L-DOPA in 6-OHDA-lesioned rats. Results RoMS displayed continuous-release characteristics of rotigotine in animals and exhibited a steady efficacy lasted for 2 weeks in 6-OHDA-lesioned rats. No significant difference of the therapeutic benefit between the treatment of RoMS and pulsatile LDOPA combination and mono L-DOPA was found. While the dyskinesia was significantly decreased with the treatment of RoMS and pulsatile L-DOPA combination compared to mono L-DOPA. Conclusions RoMS could supply an alternative of CDS for the treatment of PD and the study indicates a potential advantage of RoMS for the treatment of mild and advanced PD patient in combination with L-DOPA. © Springer Science+Business Media, LLC 2012.

Chen D.,Yantai University | Yu H.,Yantai University | Mu H.,Yantai University | Mu H.,State Key Laboratory of Long acting | And 3 more authors.
Artificial Cells, Nanomedicine and Biotechnology | Year: 2014

In this study, we report the novel double pH-sensitive mixed micelles to fabricate multicore niosomes for drug delivery. The double pH-sensitive mixed micelles (PMM) were prepared with different pH-sensitive polymers, mPEG2000-Hz-CHEMS and mPEG2000-IS (2:1 w/w). Ginsenoside Rh2-loaded DPMM was mixed with Pluronic F-68, in the aqueous medium, and multicore niosomes were fabricated. The size of multicore niosomes were around 100-300 nm with a high encapsulation efficiency of G-Rh2. The G-Rh2-MCN could release encapsulated G-Rh2 with an accelerated rate under lower pH conditions with lower cytotoxicity and good antitumor efficacy. © 2014 Informa Healthcare USA, Inc.

Yao C.,Yantai University | Wang W.,Yantai University | Zhou X.,Yantai University | Qu T.,Yantai University | And 5 more authors.
Journal of Ocular Pharmacology and Therapeutics | Year: 2011

Purpose: The purpose of this study was to investigate the effects of poly(amidoamine) (PAMAM) dendrimers on ocular absorption of puerarin. Methods: The samples of rabbits' aqueous humor were collected by in vivo microdialysis. The ocular pharmacokinetic properties of puerarin were measured to evaluate the effects of PAMAM dendrimers on ocular absorption of puerarin. Results: In the pharmacokinetic studies, the AUC 0∼∞ values of puerarin solution with 0.2% (w/v) PAMAM dendrimers (G3.0, G4.0, G5.0) were greater than those in the control group by 2.3-, 3.5-, and 2.1-folds, respectively. The C max values of puerarin solution with 0.2% (w/v) PAMAM dendrimers were 1.5, 2.5, and 1.3 times the values of the control group and the t 1/2 values were significantly longer than that of control group. Conclusions: Using PAMAM dendrimers might be a promising strategy to enhance the absorption of puerarin. The generation of PAMAM dendrimers may play a key role in increasing the ocular absorption of puerarin. © Mary Ann Liebert, Inc.

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