Search

MS‐275, a histone deacetylase inhibitor, has proven anticancer activities against various malignancies. However, its clinical application has been constrained by dose‐limiting toxicity, off‐target effects, and variable clinical outcomes. Clinical data suggest that sustained low MS‐275 doses could achieve a more selective and consistent effect. This study aimed at enhancing the anticancer activity of MS‐275 by encapsulating it in D‐α‐tocopheryl polyethylene glycol 1000 succinate (TPGS) micelles. The produced nanoformulations were characterized by their low polydispersity (0.201), negative zeta potential (−0.397 mV), and high entrapment efficiency (98.8%). Experimental evaluation of the formulation showed a significant reduction in HepG2, HCT116, and MCF7 cells' viability, associated with enhanced apoptosis at a lower IC50 compared to MS‐275 alone. The formulation was further examined on cancer cells xenografted on the chorioallantoic membrane (CAM) of chick embryos. The results showed a substantial reduction in tumor size. TPGS micelles alone induced an accumulation in G1 and slightly reduced the cellular viability of the examined cell lines. Our results suggest that encapsulating MS‐275 in TPGS micelles represents a promising strategy to enhance MS‐275 therapeutic impact while minimizing its pharmacological dosage. [ABSTRACT FROM AUTHOR]

The current study focuses on the preparation and optimization of lipid PLGA hybrid nanoparticles of 5-fluorouracil (5-FU-LPHNs) using a three-factor, three-level Box-Behnken design for sustained release and enhanced in-vitro anticancer efficacy. The morphology of the developed 5-FU-LPHNs was spherical and found in the range of 155.7–316.4 nm, entrapment efficiency (80%–92%), polydispersity index (0.11–0.19) and zeta potential (−19.7 mV to −29.4 mV) depicting nano-sized and stable nanoparticles. The XRD and DSC investigations showed the absence of characteristic peaks of 5-fluorouracil in the developed formulations indicating amorphization and successful encapsulation of 5-fluorouracil in the developed LPHNs. The in-vitro release showed a biphasic release pattern with an initial burst release pursued by sustained release up to 72 h. The in-vitro cytotoxicity studies of the developed 5-FU-LPHNs were found more cytotoxic than the free drug solution in HT-29 and HCT116 cancer cell lines. In both cell lines, the half maximal inhibitory concentration (IC50) values of 5-FU-LPHNs were approximately 2.06-fold and 1.83-fold, less than that of the 5-FU solution (p <.05). These results suggest that the developed LPHNs can be used as a potential drug delivery approach for the effective delivery of 5-fluorouracil with enhanced anticancer efficacy to colorectal tumors. [ABSTRACT FROM AUTHOR]

Objective of the research was to potentiate solubility of Rosuvastatin by nanogels synthesized by free radical polymerization. Surface morphology and structural compatibility were studied through scanning electron microscopy (SEM) and Fourier Transform Infrared (FTIR) spectroscopy. Zeta sizer was used for particle size analysis. Swelling, in-vitro release and solubility studies were accomplished in different media. Similarly, results of in-vitro release of nanogels and commercially available tablets of Rosuvastatin were compared in different dissolution media. Biocompatibility study was performed in healthy rabbits for safety profile. FTIR spectroscopy confirmed the presence of corresponding peaks of respective functional groups of individual constituents and that of the drug in unloaded and loaded nanogels. SEM images depicted the fluffy appearance of nanogels with small pores inside the structure. Particle size of the optimized formulation was in the range of 217.70 ± 2.23 for unloaded and 257.33 ± 2.11 for loaded nanogels. Percent drug loading, in-vitro drug release and solubility profiles were also satisfactory. In comparison with commercially available tablet Rovista®, in-vitro release profiles of synthesized nanogels showed better response. Moreover, synthesized nanogels were also biocompatible. It was concluded that the solubility of Rosuvastatin was potentially enhanced by nanogels and such formulation can also be used for other poorly soluble drugs. [ABSTRACT FROM AUTHOR]

Poly(lactic‐co‐glycolic acid) (PLGA) nanoparticles (NPs) are commonly used for drug delivery because of their favored biocompatibility and suitability for sustained and controlled drug release. To prolong NP circulation time, enable target‐specific drug delivery and overcome physiological barriers, NPs camouflaged in cell membranes have been developed and evaluated to improve drug delivery. Here, we discuss recent advances in cell membrane‐coated PLGA NPs, their preparation methods, and their application to cancer therapy, management of inflammation, treatment of cardiovascular disease and control of infection. We address the current challenges and highlight future research directions needed for effective use of cell membrane‐camouflaged NPs. [ABSTRACT FROM AUTHOR]