The Benefits and Challenges of Antibiotics-Non-Steroidal Anti-Inflammatory Drugs Non-Covalent Reaction.

Recently, non-covalent reactions have emerged as approaches to improve the physicochemical properties of active pharmaceutical ingredients (API), including antibiotics and non-steroidal anti-inflammatory drugs (NSAIDs). This review aimed to present and discuss the non-covalent reaction products of antibiotics, including salt and neutral multi-component solid forms, by framing their substituents and molar ratios, manufacturing techniques, characterization methods, benefits, potency changes, and toxicity, and is completed with an analysis of the development of computational models used in this field. Based on the data, NSAIDs are the most-developed drugs in multi-component system preparations, followed by antibiotics, i.e., antituberculosis and fluoroquinolones. They have reacted with inorganic elements, excipients, nutraceuticals, natural products, and other drugs. However, in terms of treatments for common infections, fluoroquinolones are more frequently used. Generally, NSAIDs are acquired on an over-the-counter basis, causing inappropriate medication. In addition, the pKa differences between the two groups of medicine offer the potential for them to react non-covalently. Hence, this review highlights fluoroquinolone-NSAID multi-component solid systems, which offer some benefits. These systems can increase patient compliance and promote the appropriate monitoring of drug usage; the dual drug multi-component solids have been proven to improve the physicochemical properties of one or both components, especially in terms of solubility and stability. In addition, some reports show an enhancement of the antibiotic activity of the products. However, it is important to consider the possibility of activity changes, interaction, and toxicity when using drug combinations. Hence, these aspects also are discussed in this review. Finally, we present computational modeling, which has been utilized broadly to support multi-component system designs, including coformer screening, preparation methods, and structural modeling, as well as to predict physicochemical properties, potency, and toxicity. This integrated review is expected to be useful for further antibiotic-NSAID multi-component system development.

Secondary Metabolites from Marine-Derived Fungi and Actinobacteria as Potential Sources of Novel Colorectal Cancer Drugs.

Colorectal cancer is one of the most common cancers diagnosed in the world. Chemotheraphy is one of the most common methods used for the pharmacological treatment of this cancer patients. Nevertheless, the adverse effect of chemotherapy is not optimized for improving the quality of life of people who are older, who are the most vulnerable subpopulation. This review presents recent updates regarding secondary metabolites derived from marine fungi and actinobacteria as novel alternatives for cytotoxic agents against colorectal cancer cell lines HCT116, HT29, HCT15, RKO, Caco-2, and SW480. The observed marine-derived fungi were from the species Aspergillus sp., Penicillium sp., Neosartorya sp., Dichotomomyces sp., Paradendryphiella sp., and Westerdykella sp. Additionally, Streptomyces sp. and Nocardiopsis sp. are actinobacteria discussed in this study. Seventy one compounds reviewed in this study were grouped on the basis of their chemical structures. Indole alkaloids and diketopiperazines made up most compounds with higher potencies when compared with other groups. The potency of indole alkaloids and diketopiperazines was most probably due to halogen-based functional groups and sulfide groups, respectively.

ArtinM Grafted Phospholipid Nanoparticles for Enhancing Antibiotic Cellular Uptake Against Intracellular Infection.

BACKGROUND AND AIM: An antimicrobial delivery in the form of surface-modified lectin of lipid nanoparticles was proposed to improve cellular accumulation. ArtinM, an active toll-like receptor 2 (TLR2) agonist lectin isolated from cempedak (Arthocarpus integrifolia) seeds, was selected to induce cellular engulfment of nanoparticles within infected host cells. MATERIALS AND METHODS: Lipid nanoparticles were prepared using the emulsification technique before electrostatic adsorption of artinM. The formula comprising of rifampicin, soy phospholipid, and polysorbate 80 was optimized by Box-Behnken design to produce the desired particle size, entrapment efficiency, and drug loading. The optimum formula was characterized for morphology, in vitro release, and cellular transport. RESULTS AND DISCUSSION: Soy phospholipid showed a profound effect on controlling drug loading and entrapment efficiency. Owing to its surface activity, polysorbate 80 contributed significantly to reduce particle size; however, a higher ratio to lipid concentration resulted in a decrease of rifampicin encapsulation. The adsorption of artinM on the surface of nanoparticles was accomplished by electrostatic binding at pH 4, where this process maintained the stability of encapsulated rifampicin. A high proportion of artinM adsorbed on the surface of the nanoparticles shown by haemagglutination assay, zeta potential measurement, and transmission electron microscopy imaging. Cellular uptake revealed by confocal microscopy showed the success in transporting Nile-red labelled nanoparticles across fibroblast cells. CONCLUSION: The delivery system of nanoparticles bearing artinM becomes a potential platform technology for antibiotic targeting in the treatment of life-threatening chronic diseases caused by intracellular infections.