METHODS: This nanocomposite consists of zinc layered hydroxide intercalated with protocatechuate (an anionic form of protocatechuic acid), that has been synthesized using a direct method with zinc oxide and protocatechuic acid as precursors.
RESULTS: The resulting protocatechuic acid nanocomposite (PAN) showed a basal spacing of 12.7 Å, indicating that protocatechuate was intercalated in a monolayer arrangement, with an angle of 54° from the Z-axis between the interlayers of the zinc layered hydroxide, and an estimated drug loading of about 35.7%. PAN exhibited the properties of a mesoporous type material, with greatly enhanced thermal stability of protocatechuate as compared to its free counterpart. The presence of protocatechuate in the interlayers of the zinc layered hydroxide was further supported by Fourier transform infrared spectroscopy. Protocatechuate was released from PAN in a slow and sustained manner. This mechanism of release was well represented by a pseudo-second order kinetics model. PAN has shown increased cytotoxicity compared to the free form of protocatechuic acid in all cancer cell lines tested. Tumor growth suppression was extensive, particularly in HepG2 and HT29 cell lines.
CONCLUSION: PAN is suitable for use as a controlled release formulation, and our in vitro evidence indicates that PAN is an effective anticancer agent. PAN may have potential as a chemotherapeutic drug for human cancer.
OBJECTIVE: In the current study, aqueous extract of Thymus vulgaris (T. vulgaris) was used to synthesize the AgNPs using green synthesis techniques followed by checking the effectiveness and various biological activities of these AgNPs.
METHODS: At first, the plant samples were proceeded for extraction of aqueous extracts followed by chromatography studies to measure the phenolics and flavonoids. The synthesis and characterization of AgNPs were done using green synthesis techniques and were confirmed using Fourier transform infra-red (FT-IR) spectroscopy, UV-visible spectroscopy, scanning electron microscope (SEM), zeta potential, zeta sizer and X-Ray diffraction (XRD) analysis. After confirmation of synthesized AgNPs, various biological activities were checked.
RESULTS: The chromatography analysis detected nine compounds accounting for 100% of the total amount of plant constituents. The FT-IR, UV-vis spectra, SEM, zeta potential, zeta sizer and XRD analysis confirmed the synthesis of AgNPs and the variety of chemical components present on the surface of synthesized AgNPs in the plant extract. The antioxidant activity of AgNPs showed 92% inhibition at the concentration of at 1000 µg/mL. A greater inhibitory effect in anti-diabetic analysis was observed with synthesized AgNPs as compared to the standard AgNPs. The hemolytic activity was low, but despite low concentrations of hemolysis activity, AgNPs proved not to be toxic or biocompatible. The anti-inflammatory activity of AgNPs was observed by in-vitro and in-vivo approaches in range at various concentrations, while maximum inhibition occurs at 1000 µg (77.31%).
CONCLUSION: Our data showed that the potential biological activities of the bioactive constituents of T. vulgaris can be enhanced through green synthesis of AgNPs from T. vulgaris aqueous extracts. In addition, the current study depicted that AgNPs have good potential to cure different ailments as biogenic nano-medicine.
Methods: The 5-FU-loaded NPs were prepared utilizing a simple double emulsion method using polycaprolactone (PCL) and polylactic-co-glycolic acid (PLGA) with or without PEG 6000. The surface charge, particle size, and shape of NPs were evaluated by standard procedures. Both Fourier Transform Infrared Spectroscopy and X-ray diffraction spectra of the 5-FU loaded NPs were compared against the pure 5-FU. The in vitro release profile of 5-FU from the NPs was monitored by the dialysis tubing method. Cell death and apoptosis induction in response to 5-FU NP exposure were measured by MTT and Annexin-V/7-amino-actinomycin D (7-AAD) assays, respectively, in Daoy, HepG2, and HT-29 cancer cell lines.
Results: The 5-FU loaded NPs were found to be spherical in shape with size ranging between 176±6.7 and 253.9±8.6 nm. The zeta potential varied between -7.13± 0.13 and -27.06±3.18 mV, and the entrapment efficiency was between 31.96% and 74.09%. The in vitro release of the drug followed a two-phase mode characterized by rapid release in the first 8 hrs followed by a period of slow release up to 72 hrs with composition-based variable extents. Cells exposed to NPs demonstrated a significant cell death which correlated with the ratio of PEG in the formulations in Daoy and HepG2 cells but not in HT-29 cells. Formulations (F1-F3) significantly induced early apoptosis in HT-29 cell lines.
Conclusion: The physical PEGylation significantly enhanced the entrapment and loading efficiencies of 5-FU into NPs formulated with PLGA and PCL. It also fostered the in vitro cytotoxicity of 5-FU-loaded NPs in both Daoy and HepG2 cells. Induction of early apoptosis was confirmed for some of the formulations.