Search

Innovative approaches such as photodynamic therapy (PDT) and photothermal therapy (PTT) have made nanomedicines a promising frontier in cancer theranostics. The combination of nanocarriers with photothermal agents and photosensitizers (PSs) has shown excellent promise for the diagnosis and the treatment of cancer, primarily at the cellular, vascular, and tumor microenvironment level. Using nanocarriers in PDT has revolutionized precision and efficacy, allowing the drug to reach cancer cells faster and offering high enhancing PS accumulation. These agents are activated by light of specific wavelengths, leading to localized cytotoxicity, offering highly selective cancer therapy. Nanomaterials such as gold and silver nanoparticles have enabled remarkable progress in cancer hyperthermia using PTT. The unique optical properties of these nanoparticle-based nanomedicines make them ideal candidates for converting light energy into heat, selectively ablating the cancer cells. In this review, nanomedicine-integrated phototherapeutic agents are discussed and the most important recent developments in PDT and PTT are examined, as well as how nanoparticle-based formulations improve diagnosis and treatment. In addition, nanocarriers used in cancer phototherapy and their mode of action are discussed. Nanocarriers are useful for drug delivery as well as for imaging and diagnostic purposes during cancer treatment. In this review, we explore the role of nanoparticles in improving phototherapy precision and selectivity while minimizing collateral tissue damage. It specifies a comprehensive impression of the current research on cancer therapy, underscoring its potential to revolutionize the treatment paradigm by highlighting the current state of research.

The lipid-based colloidal carriers, such as nanostructured lipid carriers (NLCs), solid lipid nanoparticles (SLNs), nanocapsules, liposomes, and microemulsion, are the latest and significant entrants in the development of drug delivery systems owing to their myriad advantages. The NLCs are second-generation SLNs having unstructured matrix, have high drug loading, and provide long-term drug stability in comparison to SLNs and other colloidal systems, which show lower drug loading and experience burst release/drug expulsion during storage. This review is aimed to summarize the formulation development and optimization strategies for NLCs as reported in the literature collected from authentic databases. Various types of NLCs, formulation components, methods of preparation, characterization parameters, optimization (statistical designs) strategies, toxicity, regulatory aspects, and their applications in oral, parenteral, ocular, pulmonary, nose-to-brain, tumor targeting, and transdermal drug delivery have been dealt in detail. Patents granted on the NLCs have also been enlisted.

Graphene, owing to its unique chemical structure and extraordinary chemical, electrical, thermal, optical, and mechanical properties, has opened up a new vista of applications, specifically as novel sensing platforms. The last decade has seen an extensive exploration of graphene and graphene-based materials either alone or modified with nanoparticles and polymers for the fabrication of nanoscale biosensors. These biosensors displayed excellent conductivity, high sensitivity, and selectivity, good accuracy, and precision, rapid detection with low detection limits as well as long-term stability. The unmatched properties of graphene and graphene-based materials have been applied for the detection of a number of chemical and biological molecules successfully for the diagnosis of a variety of diseases, pathogens, and biomarkers of the diseases. This review is aimed to cover the fabrication methods, functionalization techniques, and biomedical applications along with the recent advancements in the field of development of graphene-based biosensors. Recent clinical trials and patents as well as market trends and opportunities associated with graphene-based biosensors are also summarized. The application of graphene-based biosensors in the detection of SARS-CoV-2 causing COVID-19 is also reviewed.

Depending upon the metal coordination capacity and the binding sites of proteins, interaction between metal and proteins leads to a number of changes in the protein molecule which may include the change in conformation, unfolding, overall charge, and aggregation in some cases. In this study, Cu(ii) and Ag(i) metal ions were selected to investigate aggregation of bovine serum albumin (BSA) molecule upon interaction by measuring the size and charge of the aggregates using nano-Zetasizer instrument. Two concentrations of metal ions were made to interact with a specific concentration of BSA and the size and zeta potential of BSA aggregates were measured from 0 min upto 18 h. The Cu(ii) and Ag(i) metal ions showed almost similar behavior in inducing the BSA aggregation and the intensity of peak corresponding to the normal-sized protein decreased with time, whereas the peak corresponding to the protein aggregate increased. However, the effect on zeta potential of the aggregates was observed to be different with both metal ions. The aggregation of protein due to interaction of different metal ions is important to study as it gives insight to the pathogenesis of many neurological disorders and would result in developing effective ways to limit their exposure.

Clopidogrel (CLOP) is widely used worldwide for cardiovascular complications. CLOP is highly metabolized in the liver to its active metabolite by cytochrome P450 enzymes. Studies have shown that khat, an addictive substance, is a powerful inhibitor of cytochrome P450 enzymes and can influence the metabolism of drugs that are concomitantly used. Therefore, this study was designed to evaluate the effects of khat on the pharmacokinetics of CLOP in rats. In this study, rats were administered either CLOP alone or CLOP combined with khat and their plasma were obtained at different time intervals and analyzed using the newly developed and validated liquid chromatography with tandem mass spectrometry (LC-MS/MS) method using foretinib (FTB) as the internal standard. The corresponding peak area of the analyte versus FTB was used for calculating the peak ratio. The validated LC-MS/MS method resulted in the separation of the well-defined quantifiable peaks of CLOP, FTB, and CLOP metabolite within 7 min. Results showed a significant influence of khat on the peak ratio of CLOP metabolite, which was found to be significantly decreased (P < 0.05) in comparison to CLOP alone, suggesting significant decrease in the conversion of CLOP to its active metabolite due to the inhibition of CYP450 enzymes by khat. Therefore, there might be a need for dose adjustment for regular khat chewers using CLOP.

Aim: The aim of this study was to optimize, develop, characterize and evaluate a topical nanobigel (BG) formulation containing Berberine (BRB) that exhibits anti-melanogenic properties. Materials & methods: The Berberine-loaded bigel (BRB@BG) formulation was prepared by homogenously mixing the optimized hydrogel and oleogel. BRB@BG was characterized in vitro and cytotoxicity study was conducted to evaluate its effects on murine skin melanoma B16F10 cell lines. Results: The optimized BRB@BG exhibited uniform texture with nanometric size, desirable spreadability and extrudability, suitable for topical applications. Cytotoxicity studies revealed that BRB@BG had a lower IC50 value (4.84 μg/ml) on B16F10 cell lines compared with drug alone. Conclusion: In conclusion, the developed BRB@BG formulation showed good potential as safe and effective topical treatment for hyperpigmentation. Plain Language Summary Hyperpigmentation is a common skin disease in which the melanin content becomes abnormally high. The existing treatment options are associated with side effects and therefore research is being aimed to develop a topical nanoformulation based on natural compounds. Berberine (BRB) is one such natural compound that is known to inhibit the production of melanin in skin. This study was aimed to develop a bigel formulation of BRB that can be applied on skin, which can treat the hyperpigmentation and is safe. The developed nanomedicine was found to have all good properties of a topical formulation and was more effective than the drug alone. Various studies on animals were conducted to assess its safety and it was found that the formulation did not show any toxicity to the skin. Article highlights Berberine, an isoquinoline alkaloid is reported to have antimelanogenic effect but is associated with poor oral bioavailability. Berberine-loaded bigel (BRB@BG) was prepared by homogenously mixing the optimized hydrogel and oleogel. The prepared BRB@BG was characterized using in vitro methods, TEM and trinocular microscopy. Cytotoxicity study was conducted to evaluate the effects of BRB@BG on the murine skin melanoma B16F10 cell lines. Safety of the developed formulation was performed using Draize test followed by histopathology and in ovo irritation studies. The developed formulation showed all desirable properties of an ideal topical formulation. The IC50 values obtained after cytotoxicity studies was found to be lower than the plain drug showing better efficacy. The developed formulation showed no toxicity in any of the safety evaluation test. [ABSTRACT FROM AUTHOR]

Currently, acetylcholinesterase (AChE) inhibiting drugs in clinical use, such as tacrine, donepezil, rivastigmine, and galanthamine, are associated with serious side effects and short half-lives. In recent years, numerous phytochemicals have been identified as inhibitors of cholinesterases with potential applications in the management of Alzheimer's disease (AD). In this study three natural coumarins, 2'-O-ethylmurrangatin (1), murranganone (2), and paniculatin (3) isolated previously by our group from the leaves of Murraya paniculata, were tested against the two cholinesterases (ChE) enzymes, AChE and butyrylcholinesterase (BChE) using in vitro assay. Molecular docking was performed to highlight the structural properties that contribute to the molecular recognition pattern in the inhibition of ChE and the structural differences resulting in the selectivity of these compounds toward AChE. Classical enzyme inhibition kinetics data suggested that compounds 2 and 3 were potent inhibitors of AChE and BChE, while 1 was found inactive against both enzymes. The findings from molecular docking studies revealed the competitive and non-competitive inhibition mechanisms of compounds 2 and 3 against both enzymes. Molecular docking and simulations have revealed that hydrogen bonding, mediated by ketone and hydroxyl functionalities in various positions, significantly contributes to the binding of the inhibitor to the receptor. According to MD simulation studies, the stability of the ligand-AChE complex for the most active compound (3) is found to be comparable to that of the widely used drug Tacrine. In addition, to evaluate the drug-likeness of compounds, in silico ADME evaluation was performed, and the compounds presented good ADME profiles. Data suggested that the coumarin nucleus having diverse side chains at the C-8 position can serve as a potential inhibitor of cholinesterases and can act as a lead to develop a new semisynthetic drug for the treatment of AD. [ABSTRACT FROM AUTHOR]

Background: One of the imperative progressions within the pharmaceutical industry, especially drugs, is the expanded utilization of materials in order to enhance its dissolution, solubility and bioavailability. Planetary ball monomill approach can be the latest entrant to Green nanotechnology - being solvent-free, eco-friendly, costeffective, and sustainable particle size reduction approach. Objectives: Salicylic acid nanopowder (SA-NP) was aimed to be prepared using planetary ball monomill by dry milling technique to enhance its solubility and bioavailability. Methods: Various milling parameters such as milling speed, milling time and number of balls was varied and their effect on dependent responses including size (nm) and polydispersity indices (PDI) were evaluated using a 3-Factorial-3-Level Box-Behnken statistical design. Particle size and PDI analysis was performed using light scattering technique. Results: The particle size of salicylic acid obtained by optimizing the dry milling parameters was Z-Average (d.nm): 776.3 nm and PDI: 0.600 up to Z-Average (d. nm): 205.0 nm and PDI: 0.383. Conclusions: Dry milling can be used for the preparation of nanopowders of drug candidates with poor water-solubility issues. Present day medications have nano-scaled active ingredients which are rapidly absorbed by the human body as compared to the conventional ones. Enlarged surface area increases the solubility of the drug, thereby improves its bioavailability. [ABSTRACT FROM AUTHOR]