Nanogel-Based Delivery System for Lemongrass Essential Oil: A Promising Approach to Overcome Antibiotic Resistance in Pseudomonas aeruginosa Infections.

The emergence of antibiotic-resistant strains of Pseudomonas aeruginosa (P. aeruginosa) presents a substantial obstacle in medical environments. To effectively tackle this problem, we suggest an innovative approach: employing a delivery system based on nanogels to administer lemongrass essential oil (LGO). Developed PVA and PLGA nanoparticle formulation efficiently encapsulates LGO with 56.23% encapsulation efficiency by solvent extraction technique, preserving stability and bioactivity. Nanogel: 116 nm size, low polydispersity (0.229), -9 mV zeta potential. The nanogel's controlled release facilitated targeted LGO delivery via pH-controlled dissolution. Pure LGO had the highest release rate, while LGO-NP and LGO-NP-CG exhibited slower rates. In 15 h, LGO-NP released 50.65%, and LGO-NP-CG released 63.58%, releasing 61.31% and 63.58% within 24 h. LGO-NP-CG demonstrated superior antioxidant activity, a lower MIC against P. aeruginosa, and the most potent bactericidal effect compared to other formulations. This underscores the versatile efficacy of LGO, suggesting its potential to combat antibiotic resistance and enhance treatment effectiveness. Moreover, employing a nanogel-based delivery approach for LGO offers an efficient solution to combat drug resistance in P. aeruginosa infections. By employing strategies such as nanogel encapsulation and controlled release, we can enhance the effectiveness of LGO against antibiotic-resistant strains. This study establishes a robust foundation for exploring innovative approaches to treating P. aeruginosa infections using nanomedicine and paves the way for investigating novel methods of delivering antimicrobial drugs. These efforts contribute to the ongoing battle against antibiotic resistance.

Coumarin-Encapsulated Solid Lipid Nanoparticles as an Effective Therapy against Methicillin-Resistant Staphylococcus aureus.

Bacterial infections caused by antibiotic-resistant pathogens are a significant public health problem. This is because the transmission of infectious diseases is shifting, and new antibiotic-resistant strains of bacteria are emerging. The development of biofilms that are resistant to antibiotics poses another hurdle to drugs and treatment alternatives. Therefore, there is an urgent need to develop innovative strategies to effectively eliminate antibiotic-resistant microorganisms effectively. Natural coumarins have broad spectrum bioactivity and the potential for lower resistance. Coumarin is a secondary metabolite found in certain plants, fungi, and bacteria. It is highly effective against methicillin-resistant Staphylococcus aureus (MRSA). Therefore, coumarin can be used as an alternative to combat MRSA. However, most antibacterial agents lack selective targeting of pathological sites, limiting the efficacy of their antibacterial activity. Efficient MRSA treatments can be achieved through nanoparticle (NPs)-based targeted therapies. To address this challenge, a novel coumarin-loaded solid lipid nanocarrier for MRSA was developed to overcome this challenge. The developed systems exhibited a particle size of 138.5 ± 76.06 nm and a polydispersity index (PDI) of 0.245 ± 0.00. The zeta potential of coumarin-loaded SLNs was reported to be -22.2 ± 8.15 mV with a spherical shape. The encapsulation efficiency of coumarin was reported to be 63.09 ± 3.46% in the final formulation. The developed formulation was biocompatible with a minimum inhibitory concentration (MIC) of 1.08 µg/mL. This study suggests that coumarin-loaded SLNs can effectively treat MRSA infections.

Solubility Enhancement, Formulation Development, and Antibacterial Activity of Xanthan-Gum-Stabilized Colloidal Gold Nanogel of Hesperidin against Proteus vulgaris.

The objective of the study was to develop a transdermal nanoformulation of hesperidin (HSP) against Proteus vulgaris (P. vulgaris). Based on the low water solubility of HSP, we prepared HSP-enabled AuNPs stabilized with xanthan gum (XA), referred to as HSP@XA@AuNPs. The HSP@XA@AuNP formulation was evaluated for particle size (43.16 nm), PDI (0.565), zeta potential (-31.9 mV), and entrapment efficiency (56.7%). The HSP@XA@AuNPs gel was developed by incorporating selected formulation grades into a 1% Carbopol gel base and characterized by physical evaluation and rheological studies. The color of the HSP@XA@AuNP gel was light pink, and the texture was very smooth and non-greasy. The gel was shown to be odorless. A field emission scanning electron microscope (FESEM) was used to investigate the shape of HSP@XA@AuNPs further. The drug release was 73.08% for the HSP@XA@AuNPs and 86.26% for the HSP@XA@AuNPs gel in 500 min. The prepared gel showed antimicrobial activity against P. vulgaris with an MIC of 1.78 µg/mL. In conclusion, the HSP@XA@AuNPs gel could be an advanced modality for treating P. vulgaris.

Solubility enhancement, formulation development and antifungal activity of luliconazole niosomal gel-based system.

Luliconazole is a potential prescription candidate drug for the treatment of topical fungal infections. However, it has water solubility and skin permeability limitations. To overcome these limitations, a niosomal gel of luliconazole was formulated using Span 60, cholesterol, and chloroform to improve its bioavailability and to reduce its toxicity. Niosomes were analyzed by transmission electron microscopy (TEM) and Fourier transform infrared spectroscopy (FTIR) for morphological and spectral studies respectively. The formulations had ideal nanometric vesicle sizes, encapsulation efficiency (88.891% ± 0.0364%), Zeta potential (-40.1 mV), and storage instability was not observed. The sustained-release profile of niosomal gel was observed for up to 24 h. The highest R2 value was 0.913; the Higuchi model was considered the best fit model for the niosomal formulations. Cytotoxicity studies confirmed the biocompatibility of the niosomal gel of luliconazole. Based on the results, it can be concluded that niosomal luliconazole may enhance the activity of luliconazole against Candida albicans (C. albicans).

Enhancing the solubility of nitazoxanide with solid dispersions technique: formulation, evaluation, and cytotoxicity study.

Nitazoxanide (NTZ) is a synthetic form of nitrothiazole with a broad range of applications as an antiparasitic, antibacterial and antiviral agent. NTZ is a highly low aqueous soluble drug which possesses solubility of 0.00755 mg/mL and typically low bioavailability of 1%. Low aqueous solubility is usually regarded as prime prerequisites for enhanced absorption and bioavailability. The purpose of this study is to improve in vitro dissolution of the poorly soluble drug NTZ through amorphous solid dispersion technology. Three solid dispersions of NTZ were successfully prepared by hot-melt technique. It was further evaluated for drug content, DSC, XRD, SEM, TEM, FT-IR, in-vitro drug release study, in vitro MTT safety on HEK-293 and A-549 and stability study. The results of XRD showed after the formation of solid dispersions. The number of crystalline peaks has disappeared and confirmed the amorphous form of the drug. An in vitro release study showed that NTZ effectively released from solid dispersion into a simulated gastric releasing medium (pH 1.2). Further, the cytotoxicity study gave an indication of safe for human. Also, stability studies depicted no evident difference in the physical state of solid dispersion after six months. Hence, it can be concluded that the newly developed formulation was found to be safe and stable with enhanced solubility profile.

Formulation and evaluation of gastro-retentive floating bilayer tablet for the treatment of hypertension.

The paper aimed to progress an ideal gastro retentive drug delivery system intended for directing Losartan and Hydrochlorothiazide as a fixed-dose combination for anti-hypertensive therapy. The bilayer tablets were primed through direct compression method. Losartan was formulated by means of a floating layer expending hydrophilic swellable polymer Hydroxy Propyl Methyl Cellulose K4M, ethyl cellulose (4cps) as a buoyancy enhancer, sodium bicarbonate as a gas spawning agent. The amount of polymer blends remains optimized using 23 full factorial designs. The clout of experimental factors such as swelling agent concentration, buoyancy enhancer and gas generating agent on floating lag time, total floating time, T50% and % drug release remain investigated to get optimized formulation. The responses remain analyzed using Analysis of variance, and polynomial equation stood created for every retort using Multiple linear regression analysis. Entirely preparations floated for more than 12 h. The release pattern of losartan stood fitted to diverse models based on the coefficient of correlation (r). All the formulations, except F2, showed the Korsemeyer-Peppas model as the best fit model. Formulation F2 showed the zero-order model. Diffusion exponents (n) remained indomitable designed for entirely formulations (0.45-0.89), accordingly the chief drug discharge mechanism was non-fickian (anamolous) transport. Formulation F4 containing 20% w/w Hydroxy Propyl Methyl Cellulose K4M, 15% Sodium bicarbonate and 5% ethyl cellulose (4cps) was the best formulation as per the range of drug release remain institute to be more than 95 % in 12h and floating lag time was 20.15 s. The immediate-release layer stood optimized using crospovidone and Indion 414 as a super disintegrant. Formulation A8 containing 2% Indion 414 was considered as optimized formulation as it released 99% drug within 35 min and possessed less disintegration time. Optimized formulation F4 from the controlled-release layer and A8 from immediate-release layer was used to formulate bilayer tablet. The optimized formulation was imperilled to stability reading for three months at 40○C/75% relative humidity. The stability revision exhibited no substantial alteration in the appearance of tablets, floating characteristics, drug content and in-vitro drug dissolution. Consequently, a biphasic drug release design was effectively accomplished over the formulation of floating bilayer tablets.

Design and synthesis of chroman derivatives with dual anti-breast cancer and antiepileptic activities.

A series of chroman derivatives was designed, prepared, and examined for their anti-breast cancer and antiepileptic activities. All synthesized compounds yielded results that were in good agreement with spectral data. The bioassay showed that some of the resultant compounds exerted remarkable inhibitory effects on growth of human breast cancer cell line MCF-7. In particular, compound 6i (the concentration required for 50% inhibition of cell growth [GI50] =34.7 µM) exerted promising anticancer activity toward MCF-7 cell line. Additionally, compounds 6b, 6c, 6d, 6e, 6g, 6i, and 6l showed advanced antiepileptic activity than reference drugs. None of the compounds showed neurotoxicity, as determined by the rotarod test. The obtained results proved that these distinctive compounds could be relevant as models for future discovery and research, as well as for the production of more number of active derivatives.

Rapid detection and quantification of dietary mutagens in food using mass spectrometry and ultra performance liquid chromatography.

Meat is universally consumed as human diet across the globe. More than 24 different types of food mutagens have been identified till date from cooked meat products. Their study therefore assumes a greater significance from the point of view of the worldwide problem of cancer. Using rapid ultra performance liquid chromatography (UPLC) and MALDI-TOF MS the detection and quantification of two main heterocyclic aromatic amines (HAAs) - MeIQx (2-amino-3,8 dimethylimidazo 4,5-f quinoxaline) and PhIP (2-amino-1-methyl-6 phenylimidazo (4,5-b pyridine) has been achieved in beef, mutton, chicken and fish samples subjected to a range of time duration and temperature. Temperature and duration of heating directly affect the generation and amount of MeIQx and PhIP. MeIQx was generated at 180°C. PhIP was not formed before 240°C except in chicken. MeIQx was found in higher amounts in chicken 128.32 ± 0.452 ng/g and in fish 44.06 ± 1.499 ng/g while PhIP was found in higher amount in mutton 40.21 ± 0.650 ng/g.