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Background: Melanoma is a skin cancer that requires early treatment to prevent metastasis. In particular, the superficial spreading melanoma, excisional surgery with local administration of anti-cancer drugs via microneedles is currently considered a potential combination therapy. Quercetin is a natural flavonoid having activities against melanoma cells. Unfortunately, the therapeutic effect is limited by its poor water solubility. Objectives: This study aimed to develop formulations of solid dispersion-loaded dissolving microneedles (SD-DMNs) of quercetin and to investigate their in vitro activities against melanoma cells. Methods: Quercetin solid dispersions (Q-SDs) were prepared using polyvinylpyrrolidone K30 (PVP) via a solvent technique. The optimized Q-SD was selected for preparing Q-SD-loaded dissolving microneedles (Q-SD-DMNs) using a mold casting method. Results: Q-SDs had higher water solubility than that of quercetin by 5–10 times depending on the ratio of quercetin-to-PVP. The presence of quercetin in the Q-SD and Q-SD-DMN were in an amorphous form. The obtained Q-SD-DMNs had pyramid-shaped microneedles. Their strength depended on the compositions, i.e., ratios of hyaluronic acid-to-sodium carboxymethylcellulose and the content of Q-SD. An optimized Q-SD-DMN increased the in vitro skin permeation of quercetin compared to that of microneedles containing quercetin (without being processed). From the molecular investigations, the optimized Q-SD-DMN reduced the viability of the A375 cells (melanoma cells) through the induction of cell apoptosis. It suppressed Bcl-2 gene expression and led to a lower content of Bcl-2 in the cells. Conclusions: The optimized Q-SD-DMN has a potential for use in further in vivo studies as a synergistic method of melanoma treatment. [ABSTRACT FROM AUTHOR]

Rheumatoid arthritis (RA) is a systemic, progressive, chronic autoimmune inflammatory disease that affects tissues, organs, and damages synovial joints. The RA can be treated with DMARD (disease modifying anti rheumatic drugs), such as methotrexate. However, the use of this drug long-term can cause side effects. Soft coral Lobophytum sp. has secondary metabolite compounds such as flavonoids, alkaloids, and terpenoids which has an anti-inflammatory activity, which beneficial for anti-rheumatoid arthritis agent. This study aims to determine the potential of anti RA in Lobophytum sp. using in vitro and in vivo. The anti-inflammatory assay for anti RA in vitro was performed by stabilization of human red blood cell (HRBC) membrane. In addition, anti RA was performed in arthritis model mice by induction of complete Freund's adjuvant (CFA) by administering LEA once daily orally for 15 days. It was found that the ethyl acetate of Lobophytum sp. (LEA) reduced the haemolysis and increased the stability of HRBC membrane. Furthermore, LEA also showed anti RA by decreasing the edema in mouse paw at dose of 50 mg.kg-1 BW (LEA50), 100 mg.kg-1 BW (LEA100), and 200 mg.kg-1 BW (LEA200), respectively with 2.5 mg.kg-1 BW of methotrexate as positive control (C+) with P<0.05. Moreover, LEA200 demonstrated highest efficacy and showed no significant different with C+ (P>0.05). In conclusion, our research has shown that LEA has anti-inflammatory for treatment of rheumatoid arthritis from in vitro and in vivo studies. [ABSTRACT FROM AUTHOR]

The utilization of the stems, leaves, and hulls of peanuts (Arachis hypogea) is not as popular as the seeds. This study aimed to investigate the chemical contents and pharmacological activities of A. hypogaea stems in-vitro and in-silico. This study was also completed with bibliometric analysis. The methanol extract (ME) was reextracted by ethylacetate to get ethyl acetate extract (EAE). The chemical contents of EAE were analyzed by phytochemical screening, Liquid Chromatography-Mass Spectroscopy (LC-MS/MS), TPC (Total Phenolic Content), and TFC (Total Flavonoid Content). In-vitro and in-silico studies evaluated antioxidant potency, toxicity, and cytotoxicity toward MCF-7 cell lines. The results showed that EAE contained terpenoids, flavonoids, alkaloids, and phenolics which were supported by LC-MS/MS data. The EAE was categorized as a very strong antioxidant and moderately active in both cytotoxicity and toxicity. [ABSTRACT FROM AUTHOR]

Fenofibrate (FE) has been shown to markedly reduce the progression of diabetic retinopathy and age-related macular degeneration in clinical trials and animal models. Owing to the limited aqueous solubility of FE, it may hamper ocular bioavailability and result in low efficiency to treat such diseases. To enhance the solubility of FE, water-soluble FE/cyclodextrin (CD) complex formation was determined by a phase-solubility technique. Randomly methylated-β-CD (RMβCD) exhibited the best solubility and the highest complexation efficiency (CE) for FE. Additionally, water-soluble polymers (i.e., hydroxypropyl methyl cellulose and polyvinyl alcohol [PVA]) enhanced the solubility of FE/RMβCD complexes. Solid- and solution-state characterizations were performed to elucidate and confirm the formation of inclusion FE/RMβCD complex. FE-loaded Eudragit® nanoparticle (EuNP) dispersions and suspensions were developed. The physicochemical properties (i.e., pH, osmolality, viscosity, particle size, size distribution, and zeta potential) were within acceptable ranges. Moreover, in vitro mucoadhesion, in vitro release, and in vitro permeation studies revealed that the FE-loaded EuNP eye drop suspensions had excellent mucoadhesive properties and sustained FE release. The hemolytic activity, hen's egg test on chorioallantoic membrane assay, and in vitro cytotoxicity test showed that the FE formulations had low hemolytic activity, were cytocompatible, and were moderately irritable to the eyes. In conclusion, PVA-stabilized FE/RMβCD-loaded EuNP eye drop suspensions were successfully developed, warranting further in vivo testing. [ABSTRACT FROM AUTHOR]