No abstract

With the aim to develop a lipid nanoparticle for biochanin A (BCA) by emulsion-evaporation and low temperature-solidification technique. The results revealed that BCA-PEG-NLC not only have small mean particle (148.5 ± 2.88 nm) with narrow polydispersity index (PI) (0.153 ± 0.01), encapsulation capacity (99.62 ± 0.06%), payload (9.06 ± 0.01%), zeta potential (-19.83 ± 1.19 mV), but also slower release rate compared with BCA suspension over 48 h by the dialysis method (n=3). The crystallinity of lipid matrix within BCA-PEG-NLC was evaluated by differential scanning calorimetry (DSC) which verified the BCA successfully into the nanoparticles. Particularly, in pharmacokinetic, the BCA-PEG-NLC of Cmax values and AUC (area under curve) was higher than BCA suspension (approximately 15.8 and 2.9 times, respectively), meanwhile, the mean residence time (MRT) was significantly longer. Furthermore, in vitro cytotoxicity BCA-PEG-NLC showed higher cytotoxicity against MCF-7 cell line compared with BCA suspension. This study suggested that PEG-NLC is a novel anti-cancer nanoparticle, which could provide attractive treatment for a wide variety of tumors and improved the oral bioavailability of poorly water-soluble drug.

Gambogenic acid (GNA), a popular Chinese traditional medicine, has its limitations of coming into use due to its low aqueous solubility and poor bioavailability. In this study, therefore, the PEGylated non-ionic surfactant vesicles drug delivery systems were prepared from biocompatible non-ionic surfactant of Span60, cholesterol and dicetyl phosphate (DCP) by the improved ethanol injection method, and were modified with a polyethylene glycol monostearate15 (PEG15-SA). PEG15-SA, as a biocompatible, non-toxic and non-immunogenic hydrophilic segment, was grafted onto the surface of colloidal niosomes carries to reduce the uptake by the reticuloendothelial system (RES), prolonging the circulation time and attaining higher entrapment efficiency. To our knowledge, this work is the first to report that PEG15-SA was applied to coating of niosomes for encapsulation of GNA. The optimized PEG-GNA-NISVs (P-GNA-NISVs) were characterized in terms of mean vesicles size, polydispersity index (PDI), Zeta potential and entrapment efficiency of the P-GNA-NISVs. The results showed that the mean diameter, PDI, Zeta potential, and the entrapment efficiency of the P-GNA-NISVs were 70.1 nm, 0.166, À44.3 mV and 87.74%, respectively. Furthermore, the release studies of GNA from PEGylated niosomes in vitro and the pharmacokinetics in vivo exhibited a prolonged release profile as studied over 24 h. In conclusion, the result suggests that P-GNA-NISVs prepared in this way not only have higher encapsulation capacity, more colloidal stability but also offer an approach that the PEGylated niosomes is a promising carrier for anticancer GNA.

No abstract

The aim of present study was to develop folic acid (FA)‐modified nonionic surfactant vesicles (NISVs, niosomes) as carrier systems for targeted delivery of gambogenic acid (GNA). The FA‐GNA‐NISVs exhibited a mean particle size of 180.77 ± 2.41 nm with a narrow poly dispersion index of 0.147 ± 0.08 determined by dynamic light scattering. Transmission electron microscopy also revealed that the FA‐GNA‐NISVs were spherical with double‐layer structure. Entrapment efficiency (EE%) and zeta potential of the optimal FA‐GNA‐NISVs were 87.84 ± 1.06% and −37.33 ± 0.33 mV, respectively. Differential scanning calorimetry demonstrated that the GNA was in a molecular or amorphous state inside the FA‐NISVs in vitro release profiles suggested that FA‐GNA‐NISVs could release GNA at a sustained manner, and less than 60% of GNA was released from the FA‐NISVs within 12 hours of dialysis. in vivo pharmacokinetic results illustrated that FA‐GNA‐NISVs had considerably higher Cmax, area under curve (AUC0 − t) and accumulation in lung. The cell proliferation study shown that the FA‐GNA‐NISVs significantly enhanced the in vitro cytotoxicity against A549 cells. Flow cytometry and fluorescence microscopy further demonstrated that the FA‐GNA‐NISVs increased apoptosis compared with nonmodified GNA‐NISVs and free GNA. Moreover, FA‐GNA‐NISVs induced A549 cell apoptosis in a dose‐dependent manner. In addition, cellular uptake assays showed a higher uptake of FA‐GNA‐NISVs than GNA‐NISVs as well as free GNA. Taken together, it could be concluded that FA‐GNA‐NISVs were proposed as a novel targeting carriers for efficient delivering of GNA to cancers cells.