Bioresponsive gingerol-loaded alginate-coated niosomal nanoparticles for targeting intracellular bacteria and cancer cells.

Targeting and treating intracellular pathogen infections has been long-standing challenge, particularly in light of the escalating prevalence of antimicrobial resistance. Herein, an optimum formulation of alginate (AL)-coated niosome-based carriers for delivery of herbal extract Gingerol (Gin) was developed to treat intracellular pathogen infections and cancer cells. We used Gin-Nio@AL as a model drug to assess its efficacy against Gram-negative/positive bacteria and breast cancer cell lines. Our investigation affirmed its heightened antibacterial and anticancer properties. The antibacterial activity of Gin-Nio@AL against intracellular Staphylococcus aureus (S. aureus) and pseudomonas aeruginosa (P. aeruginosa) was also tested. In the current study, the niosome nanoparticles containing herbal extract Gingerol were optimized regarding lipid content and Surfactant per Cholesterol molar ratio. The developed formulation provided potential advantages, such as smooth globular surface morphology, small diameter (240.68 nm), pH-sensitive sustained release, and high entrapment efficiency (94.85 %). The release rate of Gin from AL-coated niosomes (Gin-Nio@AL) in physiological and acidic pH is lower than uncoated nanoparticles (Gin-Nio). Besides, the release rate of Gin from niosomal formulations increased in acidic pH. The Gin-Nio@AL demonstrated good antimicrobial activity against S. aureus and P. aeruginosa, and compared to Gin-Nio, the MIC values decreased to 7.82 ± 0.00 and 1.95 ± 0.00 µg/mL, respectively. In addition, the time-kill assay results showed that the developed formulation significantly reduced the number of bacteria in both strains compared to other tested groups. The microtiter data and scanning electron microscope micrography showed that Gin-Nio@AL has a more significant inhibitory effect on biofilm formation than Gin-Nio and Gin. The cell cytotoxicity evaluation showed that Gin-Nio@AL reduced the survival rate of MDA-MB-231 cancer cells to 52.4 % and 45.2 % after 48 h and 72 h, respectively. The elimination of intracellular pathogens was investigated through a breast cancer cell infection in an in vitro model. Gin-Nio@AL exhibited an enhanced and sustained intracellular antibacterial activity against pathogens-infected breast cancer cells compared to other tested formulations. Overall, Gin-Nio@AL enables the triggered release and targeting of intra-extra cellular bacteria and cancer cells and provides a novel and promising candidate for treating intracellular pathogen infections and cancer cells.

Current advances in niosomes applications for drug delivery and cancer treatment.

The advent of nanotechnology has led to an increased interest in nanocarriers as a drug delivery system that is efficient and safe. There have been many studies addressing nano-scale vesicular systems such as liposomes and niosome is a newer generation of vesicular nanocarriers. The niosomes provide a multilamellar carrier for lipophilic and hydrophilic bioactive substances in the self-assembled vesicle, which are composed of non-ionic surfactants in conjunction with cholesterol or other amphiphilic molecules. These non-ionic surfactant vesicles, simply known as niosomes, can be utilized in a wide variety of technological applications. As an alternative to liposomes, niosomes are considered more chemically and physically stable. The methods for preparing niosomes are more economic. Many reports have discussed niosomes in terms of their physicochemical properties and applications as drug delivery systems. As drug carriers, nano-sized niosomes expand the horizons of pharmacokinetics, decreasing toxicity, enhancing drug solvability and bioavailability. In this review, we review the components and fabrication methods of niosomes, as well as their functionalization, characterization, administration routes, and applications in cancer gene delivery, and natural product delivery. We also discuss the limitations and challenges in the development of niosomes, and provide the future perspective of niosomes.

In silico and in vitro studies of GENT-EDTA encapsulated niosomes: A novel approach to enhance the antibacterial activity and biofilm inhibition in drug-resistant Klebsiella pneumoniae.

Klebsiella pneumoniae (Kp) is a common pathogen inducing catheter-related biofilm infections. Developing effective therapy to overcome antimicrobial resistance (AMR) in Kp is a severe therapeutic challenge that must be solved. This study aimed to prepare niosome-encapsulated GENT (Gentamicin) and EDTA (Ethylenediaminetetraacetic acid) (GENT-EDTA/Nio) to evaluate its efficacy toward Kp strains. The thin-film hydration method was used to prepare various formulations of GENT-EDTA/Nio. Formulations were characterized for their physicochemical characteristics. GENT-EDTA/Nio properties were used for optimization with Design-Expert Software. Molecular docking was utilized to determine the antibacterial activity of GENT. The niosomes displayed a controlled drug release and storage stability of at least 60 days at 4 and 25 °C. GENT-EDTA/Nio performance as antimicrobial agents has been evaluated by employing agar well diffusion method, minimum bactericidal concentration (MBC), and minimum inhibitory concentration (MIC) against the Kp bacteria strains. Biofilm formation was investigated after GENT-EDTA/Nio administration through different detection methods, which showed that this formulation reduces biofilm formation. The effect of GENT-EDTA/Nio on the expression of biofilm-related genes (mrkA, ompA, and vzm) was estimated using QRT-PCR. MTT assay was used to evaluate the toxicity effect of niosomal formulations on HFF cells. The present study results indicate that GENT-EDTA/Nio decreases Kp's resistance to antibiotics and increases its antibiotic and anti-biofilm activity and could be helpful as a new approach for drug delivery.

Synthesis and Characterization of Tetracycline Loaded Methionine-Coated NiFe2O4 Nanoparticles for Anticancer and Antibacterial Applications.

In the present study, nickel ferrite (NiFe2O4)-based smart magnetic nanoparticles were fabricated and coated with methionine. Physiochemical characterization of the obtained Met-NiFe2O4 nanoparticles revealed the presence of methionine coating over the nanoparticle surface. Drug release study indicated that Tet-Met-NiFe2O4 nanoparticles possess pH-responsive controlled drug release behavior for tetracycline (Tet). The drug loading content for Tet was found to be 0.27 mg/L of nanoparticles. In vitro cytotoxicity test showed that the Met-NiFe2O4 nanoparticles is biocompatible. Moreover, this magnetic nanostructured material shown strong anticancer property as these nanomaterials significantly reduced the viability of A375 cells when compared to free Tet solution. In addition, Tet-Met-NiFe2O4 nanoparticles also showed strong antibacterial activity against different bacterial pathogens.