PEGylated non-ionic surfactant vesicles as drug delivery systems for Gambogenic acid

Abstract

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.

Lung cancer combination therapy: co-delivery of paclitaxel and doxorubicin by nanostructured lipid carriers for synergistic effect

“…The release behavior of DOX and PTX from NLC were assessed in phosphate-buffered saline (PBS) by the dialysis method (Lin et al, 2013;Lv et al, 2014). Briefly, the NLC were suspended in 5 mL of the PBS release medium and transferred into a dialysis bag (MWCO 3500 Da).…”

Nanosuspensions as delivery system for gambogenic acid: characterization and in vitro/in vivo evaluation

“…However, the poor solubility, short biological half-life and excessive vascular irritation of GNA hindered its clinical application (Hua et al, 2015). In order to enhance delivery efficiency and bioavailability of GNA, we have used nanotechnology and successfully prepared PEGylated non-ionic surfactant vesicles and solid lipid nanoparticles of GNA in previous researches (Huang et al, 2013;Lin et al, 2013). Nevertheless, low drug encapsulation efficiency and drug loading, residual organic solvent, especially a large amount of excipients and surfactants used in these nano-carriers will cause many side effects, such as toxicity and hemolysis.…”

A novel glyceryl monoolein-bearing cubosomes for gambogenic acid: Preparation, cytotoxicity and intracellular uptake

“…The samples were assayed for GNA by using HPLC method reported earlier (Lin et al, 2013). HPLC was equipped with Shimadzu LC-15C, SPD-15CUV-spectrophotometric detector system.…”

“…The last but not the least, nanotechnology is a rapidly progressing field and now being applied in the treatment of various cancer therapy (Xia et al, 2013;Zhang et al, 2013). From this point of view, in our previous researches we have successfully prepared GNA PEGylated Niosomes (PEG-NISVs), solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) (Lin et al, 2013;Huang et al, 2013) which effectively reduced toxicity and improved the physical stability of GNA. Nevertheless, these nanocarriers still bear the problems such as low drug encapsulation efficiency, drug loading and residual organic solvent, which were not as economically as possible in industrial production (Sun et al, 2013).…”