Penetration of the blood–brain barrier (BBB) and the blood–brain tumor barrier (BBTB) remains a significant challenge for the delivery of drugs in the treatment of glioma. Therefore, the development of targeted preparations with the ability to penetrate the BBB and BBTB, and target gliomas, is an important approach if we are to improve the efficacy of glioma treatment. In the current study, an active targeting preparation based on PLGA nanoparticles coated with erythrocyte membranes (RBCNPs) and dual-modified with ^DWSW and NGR peptide ligands (^DWSW/NGR-RBCNPs). Euphorbia factor L1 (EFL1) extracted from euphorbiae semen was used as the model drug. The final nanoparticles were characterized by in vivo and in vitro tests. In vitro results showed that EFL1-loaded ^DWSW/NGR-RBCNPs were taken up by cells and had the ability to penetrate the BBB and BBTB and produce cytotoxic effects. Furthermore, in vivo studies in mice showed that when injected intravenously, these specialized NPs could enter the brain, target tumor tissue, and significantly extend life span. The results showed that dual-targeting EFL1-loaded ^DWSW/NGR-RBCNPs have significant potential as a nanotherapeutic tool for the treatment of brain glioma.

We developed a novel preparative method for nanoparticle albumin-bound (nab) paclitaxel with high drug loading, which was based on improved paclitaxel solubility in polyethylene glycol (PEG) and self-assembly of paclitaxel in PEG with albumin powders into nanoparticles. That is, paclitaxel and PEG were firstly dissolved in ethanol, which was subsequently evaporated under vacuum. The obtained liquid was then mixed with human serum albumin powders. Thereafter, the mixtures were added into phosphate-buffered saline and nab paclitaxel suspensions emerged after ultrasound. Nab paclitaxel was finally acquired after dialysis and freeze drying. The drug loading of about 15% (W/V) were realized in self-made nab paclitaxel, which was increased by approximately 50% compared to 10% (W/V) in Abraxane. Now this new preparative method has been authorized to obtain patent from China and Japan. The similar characteristics of self-made nab paclitaxel compared to Abraxane were observed in morphology, encapsulation efficiency, in vitro release, X-ray diffraction analysis, differential scanning calorimetry analysis, and circular dichroism spectra analysis. Consistent concentration-time curves in rats, biodistributions in mice, anti-tumor activities in mice, and histological transmutation in mice were also found between Abraxane and self-made nanoparticles. In a word, our novel preparative method for nab paclitaxel can significantly improve drug loading, obviously decrease product cost, and is considered to have potent practical value.

Even the potential of T cell-mimicking nanotrap for long term viral control due to its overcoming of human immunodeficiency virus (HIV) genetic diversity and viral resistance, the robust HIV inhibition was not expected because these nanotraps displayed no obvious advantages compared with the infinite host cells. Herein, a glycoprotein 120 (gp120)-targeting polypeptide UM15 reinforced lymphocyte-mimicking nanotrap was constructed, and its improved HIV-1 inhibiting efficacy was validated. According to the results, the constructed nanotraps exhibited evident escaping ability from uptake of the mononuclear phagocyte system and highly improved binding ability with gp120 proteins. The constructed nanotraps neutralized all tested HIV-1 pseudo typed viruses with IC80 of 21.0 µg/mL, and inhibited both X4-tropic and R5-tropic HIV-1 with IC80 of 34.4 and 20.6 µg/mL, respectively. Approximately 40% of gp120 was observed to be shed from pseudo virus, and above 40% bystander T cells were prevented from gp120-induced death by the constructed nanotraps. The safety of the constructed nanotraps was confirmed both in vitro and in mice. Therefore, the constructed nanotraps could specifically neutralize free HIV-1, selectively bind with gp120 expressing HIV-1 infected cells, cause gp120 shedding, inhibit gp120-induced bystander T cell killing on the premise of safety, and were considered as promising therapeutic agents for precise inhibition of HIV.