Pomegranate extract-loaded solid lipid nanoparticles: design, optimization, and in vitro cytotoxicity study

Abstract

Background Pomegranate extract (PE) is a natural product with potent antioxidant and anticancer activity because of its polyphenols content. The main purpose of this study was to maximize the PE chemotherapeutic efficacy by loading it in an optimized solid lipid nanoparticles (SLNs) formula. Materials and methods The influence of independent variables, which were lipid concentration (X 1 ), surfactant concentration (X 2 ) and cosurfactant concentration (X 3 ), on dependent ones, which were particle size (Y 1 ), polydispersity index (Y 2 ), zeta potential (Y 3 ), entrapment efficiency (Y 4 ) and cumulative % drug release (Y 5 ), were studied and optimized using the Box–Behnken design. Fifteen formulations of PE-SLNs were prepared using hot homogenization followed by ultra-sonication technique. Response surface plots, Pareto charts and mathematical equations were produced to study the impact of independent variables on the dependent quality parameters. The anti-proliferative activity of the optimized formula was then evaluated in three different cancer cell lines, namely, MCF-7, PC-3 and HepG-2, in addition to one normal cell line, HFB-4. Results The results demonstrated that the particle sizes ranged from 407.5 to 651.9 nm and the entrapment efficiencies ranged from 56.02 to 65.23%. Interestingly, the 50% inhibitory concentration of the optimized formula had more than a 40-fold improved effect on the cell growth inhibition in comparison with its free counterpart. Furthermore, it was more selective against cancer cells than normal cells particularly in MCF-7 breast cancer cells. Conclusion These data proved that nanoencapsulation of PE enhanced its anticancer efficacy. Therefore, our results suggested that a PE-loaded SLNs optimized-formula could be a promising chemo therapeutic agent.

Effects of Quercetin-Loaded Nanoparticles on MCF-7 Human Breast Cancer Cells

“…In recent years, SLNs have extensively used as a carrier for various anticancer drugs and phyto-bioactive compounds [21,27]. For example, Tamoxifen-loaded SLNs suppress breast tumors in rats [25], and pomegranate extract-loaded SLNs effectively prevent the proliferation of various cancer cells such as PC-3, MCF-7 and HepG2 [28]. The SLNs have a high drug-loading capacity, increase the blood circulation time, modulate release kinetic, increase the therapeutic efficacy of anticancer drugs, and protects the encapsulated compound from chemical degradation [29,30,31].…”

Ucuùba (Virola surinamensis) Fat-Based Nanostructured Lipid Carriers for Nail Drug Delivery of Ketoconazole: Development and Optimization Using Box-Behnken Design

“…In several studies related to the optimization of NLC production it was observed that the relative concentration of surfactant and lipids strongly affects the stability of the formulation [23]. The physical-chemical and biopharmaceutical characteristics of NLC, such as size, entrapment efficiency (EE), physical stability, drug release and morphology, are also strongly influenced by the choice and amount of lipids and surfactant [23,24,25]. Thus, an optimization of NLC production with the aid of design of experiment could be carried out with the objective of modulating the amount of liquid and solid lipids and surfactant to obtain the most desirable properties in terms particle size, entrapment efficiency and stability.…”

Os efeitos da Punica granatum L. em diferentes concentrações sobre duas linhagens celulares: estudo in vitro

“…Note-se que esses efeitos podem explicar alguns achados do nosso estudo 16 . Neste, foi possível observar que o extrato da PG possui efeitos citotóxicos com efeitos inibitórios para proliferação celular nas células KB em relação às FLM durante os testes realizados 17,18 .…”