In the current study, diosmin (DSM)-loaded beta-cyclodextrin (β-CD)-based nanosponges (NSPs) using diphenylcarbonate (DPC) as a cross-linker were prepared. Four different DSM-loaded NSPs (D-NSP1-NSP4) were developed by varying the molar ratio of β-CD: DCP (1:15–1:6). Based on preliminary evaluations, NSPs (D-NSP3) were optimized for size (412 ± 6.1 nm), polydispersity index (PDI) (0.259), zeta potential (ZP) (−10.8 ± 4.3 mV), and drug loading (DL) (88.7 ± 8.5%), and were further evaluated by in vitro release, scanning electron microscopy (SEM), and in vitro antioxidant studies. The NSPs (D-NSP3) exhibited improved free radical scavenging activity (85.58% at 100 g/mL) compared to pure DSM. Dissolution efficiency (%DE) was enhanced to 71.50% (D-NSP3) from plain DSM (58.59%). The D-NSP3 formulation followed the Korsmeyer–Peppas kinetic model and had an n value of 0.529 indicating a non-Fickian and controlled release by diffusion and relaxation. The D-NSP3 showed cytotoxic activity against MCF-7 breast cancer, as evidenced by caspase 3, 9, and p53 activities. According to the findings, DSM-loaded NSPs might be a promising therapy option for breast cancer.
Recent interests with copper nanoparticles (Cu-NPs) has arisen because of its low cost and antibacterial properties, as it may be one of the very important alternatives to silver NPs. Pulsed laser ablation of a solid target (copper) in liquid media is used to synthesize colloidal oxide copper (Cu 2 O and CuO NPs) NPs. These oxides of copper NPs were synthesized using Nd:YAG laser energy to maintain a 40 mJ/pulse wavelength at 1064 nm. During the synthesis of colloidal NPs only two conditions were opted, employing double distilled water (without PEG) and 10% preparation of PEG. Both NPs were prepared under the similar parameters such as optimized instrument settings, laser energy and time of laser exposure (1 h ablation). Further, these copper oxide NPs were characterized by advance technologies including UV-visible, X-ray diffraction, transmission electron microscopy and attenuated total reflection Fourier transform infrared spectroscopy techniques. The significant antibacterial properties of synthesized materials were also observed. The cuprous oxide NPs, showed remarkable antibacterial effect conducted using disc diffusion techniques. The minimum inhibitory concentration and minimum bactericidal concentration of synthesized Cu 2 O NPs were recorded as 120 and 140 μg/L respectively against Staphylococcus aureus used as positive control. Therefore, based on the findings of present study Cu 2 O NPs can be exploited as stable antimicrobial agents for multipurpose uses.
Dendrimers are proven solubilizers of hydrophobic as well as hydrophilic drugs in its internal architecture. However, the toxicity of cationic dendrimers restricts its future possibilities as successful formulation. Hybrid systems such as lipid-dendrimer have shown great potential as drug delivery system due to their multifunctional adjustability, and biocompatibility. In the present study, liposomal dendrimer based nano-hybrid (called dendrosomes) of BTZ (bortezomib) were prepared and characterized through time-dependent transmission electron microscope (TEM) as well as photon correlation spectroscopy. Two types of prepared dendrosomes (DS1 and DS2) exhibited size of 145 ± 2.69 and 147 ± 3.26 nm, respectively. The overall hemolytic toxicity of the developed DS1 and DS2 dendrosomes was 4.96 ± 0.45 and 3.19 ± 0.32% (p < 0.005) respectively, which was lower than the dendrimeric formulation of BTZ encapsulated dendrimer (PD) at 50 ppm. Developed dendrosomes showed about 66.65 ± 1.5, and 69.03 ± 1.7% release of BTZ at pH 5.4 (72 h) from DS1 and DS2, respectively. Faster release of BTZ in case of acidic pH was in favour of the anti-tumor effectivity. The IC 50 (minimum inhibitory concentration) values (216.9 ± 12.35 and 299.6 ± 21.61 nM) of DS1 and DS2, respectively against A549 cells were significantly lower in comparison to BTZ alone (p < 0.0001). BTZ loaded dendrosomes (DS1) exhibited higher cellular uptake in A549 cells, as evidenced by FITC (fluorescein isothiocyanate) tagged DS1 and DS2 cell uptake images. Overall, BTZ was attempted to be delivered through developed dendrosomes and evaluated. The effectiveness of BTZ was significantly improved against A549 cells compared to other nanoformulations.
KeywordsBortezomib • PAMAM • Dendrimers • Liposomes • A549 • Dendrosomes Abbreviations BTZ Bortezomib PAMAM Polyamidoamine PD BTZ loaded PAMAM dendrimers CH Cholesterol SUV Small unilamellar vesicle LD BTZ loaded liposomes DS1 BTZ loaded dendrimers and liposomal hybrids DS2 BTZ loaded dendrimers and BTZ loaded liposomal hybrids HPLC High-performance liquid chromatography MTT 3-(4, 5-dimethyl thiazolyl-2)-2,5-diphenyltetrazolium bromide FITC Fluorescein isothiocyanate DMEM Dulbecco's modified eagle's medium FBS Fetal bovine serum * Umesh Gupta
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