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PURPOSE: The aim of this work is to optimize a polyethylene glycolated (PEGylated) polymer-lipid hybrid nanoparticulate system for the delivery of anastrozole (ANS) to enhance its biopharmaceutical attributes and overall efficacy. METHODS: ANS loaded PEGylated polymer-lipid hybrid nanoparticles (PLNPs) were prepared by a direct emulsification solvent evaporation method. The physical incorporation of PEG was optimized using variable ratios. The produced particles were evaluated to discern their particle size and shape, zeta-potential, entrapment efficiency, and physical stability. The drug-release profiles were studied, and the kinetic model was analyzed. The anticancer activity of the ANS PLNPs on estrogen-positive breast cancer cell lines was determined using flow cytometry. RESULTS: The prepared ANS-PLNPs showed particle sizes in the range of 193.6 ± 2.9 to 218.2 ± 1.9 nm, with good particle size uniformity (i.e., poly-dispersity index of around 0.1). Furthermore, they exhibited relatively low zeta-potential values ranging from -0.50 ± 0.52 to 6.01 ± 4.74. The transmission electron microscopy images showed spherical shape of ANS-PLNPs and the compliance with the sizes were revealed by light scattering. The differential scanning calorimetry DSC patterns of the ANS PLNPs revealed a disappearance of the characteristic sharp melting peak of pure ANS, supporting the incorporation of the drug into the polymeric matrices of the nanoparticles. Flow cytometry showed the apoptosis of MCF-7 cell lines in the presence of ANS-PLNPs. CONCLUSION: PEGylated polymeric nanoparticles presented a stable encapsulated system with which to incorporate an anticancer drug (ANS) with a high percentage of entrapment efficiency (around 80%), good size uniformity, and induction of apoptosis in MCF-7 cells.
RESUMO
OBJECTIVE: In the present study, Solenostemma argel effervescent tablets were prepared from Argel methanolic extract. METHODS: The tablets were examined for their ability to impede carbon tetrachloride (CCl4)-induced lipid peroxidation in mice liver. The antioxidant activities of the enzymes; super-oxide dismutase (SOD), glutathione peroxidase (GS-PX) along with malondialdehyde level were tested in liver tissues. RESULTS: The obtained results indicated that the antioxidant enzyme activities were remarkably reduced while the level of Malondialdehyde (MDA), which shows lipid peroxidation, and the activity of alanine aminotransferase (a liver function test) were remarkably intensified following intra-peritoneal i.p injection with the single sub-lethal hepatotoxic dose of CCl4 compared to the control. A necrotic lesion in the liver of mice injected with CCl4 was observed by the histopathological examination. The damaging influence of CCl4 was improved by the retreatment with Argel or BHT, which could also be observed in the normal appearance of the liver tissue. CONCLUSION: In this study, it was concluded that S. Argel and butylated hydroxytoluene (BHT) could be effective by decreasing lipid peroxidation and increasing the activities of antioxidant enzymes. Therefore, Argel might be applied as a hepatoprotective agent without any side effects.