Embelin is the only known non-peptide small-molecule X-linked inhibitor of the apoptosis protein (XIAP) - an anti-apoptotic protein considered a promising cancer therapeutic target. Embelin acts as an NF-κB blocker and potential suppressor of tumorigenesis. It also exhibits potent cytotoxic, antioxidant and cancer chemopreventive effects. Given the potential uses of embelin, it is recommended that further investigations take place to properly explore its pharmacological and clinical effects.
Composite alginate microsphere systems are the ideal carriers for controlled delivery applications because of their ability to encapsulate a myriad of therapeutic drugs, proteins, enzymes, DNA, antisense oligonucleotides, vaccines, growth factors and chemokines as well as the ease of processing, mechanical properties, biocompatibility, high bioavailability, controlled release rates, stability, suitability for different administration modes, targeted/localized delivery of different agents and large-scale production with cost-effectiveness. This article presents updated information of applying microalginate-based technologies and tools in the biomedical field which will benefit research scientists and clinical physicians or biopharmaceutical industries keen in the development of application-based new therapeutic and diagnostic strategies for various diseases. Furthermore, this technology will play more important roles in biosensors, vaccination, tissue engineering, cancer chemotherapeutics and stem cell research.
Plasmonic nanostructures of silver and gold synthesized by conventional toxic and cumbersome methodologies raise huge concern for their clinical application, which necessitates the use of a greener approach. Herein, embelin, a benzoquinone derivative extracted from the fruits of Embelia tsjeriam-cottam, with immense medicinal value, is used as a reducing and stabilizing agent for the synthesis of quasispherical gold and silver nanoparticles as well as gold nanostars. A sunlight-assisted synthesis resulted in embelinstabilized silver nanoparticles of bimodal size distribution (∼3 and 15 nm) with potent antibacterial activity against Staphylococcus aureus and Escherichia coli. Similarly, embelin was also used for the synthesis of polyhedral gold nanoparticles of 12−15 nm in size and absorbance at 540 nm. These highly faceted and multitwinned gold nanoparticles facilitated the formation of 120 nm sized embelin-stabilized gold nanostars absorbing at NIR wavelength (800 nm). The embelinstabilized nanoparticles demonstrated excellent compatibility toward cells and human blood. Additionally, the gold nanostars exhibited superior computed tomographic (CT) contrast characteristics and marked photothermal cytotoxicity toward oral epithelial carcinoma cells. This study thus proposes, for the first time, the synthesis of biocompatible plasmonic nanostructures using embelin and their potential use as antibacterial, CT imaging, and photothermal agents.
Herein we report synthesis, characterization and preclinical applications of a novel hybrid nanomaterial Toco-Photoxil developed using vitamin E modified gold coated poly (lactic-co-glycolic acid) nanoshells incorporating Pgp inhibitor d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) as a highly inert and disintegrable photothermal therapy (PTT) agent. Toco-Photoxil is highly biocompatible, physiologically stable PTT material with an average diameter of 130 nm that shows good passive accumulation (2.3% ID) in solid tumors when delivered systemically. In comparison to its surface modified counterparts such as IR780-Toco-Photoxil, FA-Toco-Photoxil or FA-IR780-Toco-Photoxil accumulation are merely ~0.3% ID, ~0.025% ID and ~0.005% ID in folate receptor (FR) negative and positive tumor model. Further, Toco-Photoxil variants are prepared by tuning the material absorbance either at 750 nm (narrow) or 915 nm (broad) to study optimal therapeutic efficacy in terms of peak broadness and nanomaterial’s concentration. Our findings suggest that Toco-Photoxil tuned at 750 nm absorbance is more efficient (P = 0.0097) in preclinical setting. Toco-Photoxil shows complete passiveness in critical biocompatibility test and reasonable body clearance. High tumor specific accumulation from systemic circulation, strong photothermal conversion and a very safe material property in body physiology makes Toco-Photoxil a superior and powerful PTT agent, which may pave its way for fast track clinical trial in future.
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