As a potential anticancer agent, curcumin (Cum) has been reported for its chemopreventive and chemotherapeutic activity in a series of cancers through influencing cell cycle arrest, differentiation, apoptosis, etc. Therefore, the potential activity against various cancers of Cum raises the possibility of its application as a novel model drug in nanoparticle-based delivery systems. The current study reported a spherical core–shell structure curcumin-loaded nanoparticle (Cum-np) formed by amphilic methoxy polyethylene glycol–poly(caprolactone) (mPEG–PCL) block copolymers. Characterization tests indicated that Cum was incorporated into mPEG–PCL-based nanoparticles with high encapsulation efficiency due to its lipophilicity. The incorporated Cum could be released from Cum-np in a sustained manner. Cum was effectively transported into the cells by nanoparticles through endocytosis and localized around the nuclei in the cytoplasms. In vitro studies proved that the cytotoxicity of Cum-np would be pro-apoptosis effect against rat C6 glioma cell line in a dose-dependent manner. The present results suggest that Cum-np could be a potential useful chemotherapeutic formulation for malignant glioma therapy. Moreover, the development of traditional Chinese medicine with nanoscale drug formation warrants more intensive research for its clinical applications.

Resveratrol (trans-3,4',5-trihydroxystilbene, RES) is a naturally occurring lipophilic antioxidant that has been intensively studied for its promising efficacy in treating oxidative stress-associated disorders. Despite the array of bioactivities that it possesses, RES has low bioavailability due to its poor aqueous solubility and dissolution properties. Recent nanotechnology has led to the effective development of drug delivery systems. In this study, RES-loaded nanoparticles (RES-NPs) were prepared based on amphiphilic methoxy-polyethyleneglycol-poly-caprolactone (mPEG-PCL) block copolymers, which improve the physical properties of resveratrol in aqueous solution. The antioxidative capacity of RES-NPs was then evaluated sequentially in vitro and in vivo. RES-NPs exhibited stronger radical scavenging and anti-lipid peroxidization compared to that of raw RES in aqueous solution. The pre-treatment of irradiated Caenorhabditis elegans (C. elegans) with RES-NPs extended both the maximum and mean life span. Furthermore, the RES-NPs were capable of alleviating injury from gamma-ray radiation and amyloid-beta peptide overexpression toxicity in C. elegans through radical scavenging and over-regulation of SOD-3 expression. The enhancement of in vitro antioxidation properties in aqueous solution and protection against oxidative stress in C. elegans induced by both gamma-ray radiation and amyloid-beta peptide confirmed the successful development of antioxidant nanoparticles.

Human serum albumin (HSA) is an intrinsic protein and important carrier that transports endogenous as well as exogenous substances. We demonstrated the regional accumulation of albumin in the ischemia-reperfusion (I/R) brain, which providing the footstone for the application of HSA based nanoparticles in study of cerebral I/R injury. Resveratrol is potential in treatment of cerebral I/R injury but restricted for its water insolubility and short half-life in vivo. Herein, we prepared resveratrol (RES)-encapsulated by HSA nanoparticles (RES-HSA-NPs) to facilitate the application of resveratrol in protection from cerebral I/R injury. RES-HSA-NPs demonstrated spherical shape, a diameter about 100 nm, a highest resveratrol encapsulation efficiency of 60.9 ± 5.07%, and controlled release pattern with the maximum release ratio of 50.2 ± 4.91% (in pH=5.0 PBS) and 26. 2 ± 2.73% (in pH=7.4 PBS), respectively, after 90h incubation at 37 °C. After intravenous injection into transient middle cerebral artery occlusion (tMCAO) rats, RES-HSA-NPs improved neurological score and decreased infarct volume at 24 hours after tMCAO in a dose dependent manner. A single dose of 20 mg/Kg RES-HSA-NPs via tail vein improved neurological outcomes and decreased infarct volume at 24 h and 72 h in tMCAO rats. Ischemia-reperfusion increased oxidative stress (indicated by products of lipid peroxidation, MDA) and neuronal apoptosis (indicated by yellow-brown TUNEL-positive cells), 20 mg/Kg of RES-HSA-NPs via tail vein administration significantly attenuated oxidative stress and neuronal apoptosis. These results demonstrated the potential of RES-HSA-NPs in therapy of cerebral ischemia-reperfusion injury.

Paclitaxel (Ptx), one of the most widely used anticancer agents, has demonstrated extraordinary activities against a variety of solid tumors. However, the therapeutic response of Ptx is often associated with severe side effects caused by its nonspecific cytotoxic effects and special solvents (Cremophor EL^®). The current study reports the stable controlled release of Ptx/tetrandrine (Tet)-coloaded nanoparticles by amphilic methoxy poly(ethylene glycol)–poly(caprolactone) block copolymers. There were three significant findings. Firstly, Tet could effectively stabilize Ptx-loaded nanoparticles with the coencapsulation of Tet and Ptx. The influence of different Ptx/Tet feeding ratios on the size and loading efficiency of the nanoparticles was also explored. Secondly, the encapsulation of Tet and Ptx into nanoparticles retains the synergistic anticancer efficiency of Tet and Ptx against mice hepatoma H22 cells. Thirdly, in the in vivo evaluation, intratumoral administration was adopted to increase the site-specific delivery. Ptx/Tet nanoparticles, when delivered intratumorally, exhibited significantly improved antitumor efficacy; moreover, they substantially increased the overall survival in an established H22-transplanted mice model. Further investigation into the anticancer mechanisms of this nanodelivery system is under active consideration as a part of this ongoing research. The results suggest that Ptx/Tet-coloaded nanoparticles could be a potential useful chemotherapeutic formulation for liver cancer therapy.