Cyclodextrin inclusion complexes improving antibacterial drug profiles: an update systematic review.

Aim: The study aimed to review experimental models using cyclodextrins to improve antibacterial drugs' physicochemical characteristics and biological activities. Methods: The following terms and their combinations were used: cyclodextrins and antibacterial agents in title or abstract, and the total study search was conducted over a period up to October 2022. The review was carried out using PubMed, Scopus and Embase databases. A total of 1580 studies were identified, of which 27 articles were selected for discussion in this review. Results: The biological results revealed that the antibacterial effect of the inclusion complexes was extensively improved. Cyclodextrins can enhance the therapeutic effects of antibiotics already existing on the market, natural products and synthetic molecules. Conclusion: Overall, CDs as drug-delivery vehicles have been shown to improve antibiotics solubility, stability, and bioavailability, leading to enhanced antibacterial activity.

The overuse of drugs can cause bacteria to become less susceptible to them. This is known as resistance. One idea on how to tackle this resistance is by using cyclodextrins (CDs). CDs can change how drugs work, making them better at fighting bacteria. As CDs are already used in making drugs, they are a good choice for the basis of creating new drugs.

New drugs against multidrug-resistant Gram-negative bacteria: a systematic review of patents.

Background: Antimicrobial resistance has been a threat to human health ever since the accelerated consumption of antibiotics began. Materials & methods: The present systematic review was carried out using a free and specialized online database - Espacenet - and a survey for patents of antimicrobial agents from 2010 to 2021, selecting 33 recent patents that claimed compounds with antimicrobial activity against resistant strains of Gram-negative bacteria. Results: Some different and new approaches to the development of the patented antibacterial agents were identified, such as antimicrobial peptides, nanomaterials and natural extracts. Conclusion: Some alternatives to modern antibiotics with diminished effectiveness due to antimicrobial resistance were spotted. Nevertheless, many challenges remain to establish a robust and sustainable antibacterial R&D pipeline.

Development and in vitro characterization of an oral self-emulsifying delivery system (SEDDS) for rutin fatty ester with high mucus permeating properties.

The aim of this study was to develop and evaluate a self-emulsifying delivery system (SEDDS) for oral rutin fatty ester administration and to improve its mucus permeating properties by the incorporation of the silicon polymer poly [dimethylsiloxane-co-(3-(2-(2-hydroxyethoxy)ethoxy)propyl]methylsiloxane] (PDMSHEPMS) in the formulation. In order to increase the lipophilicity of the flavonoid and to dissolve it in SEDDS, enzymatic acylation of rutin with lauric acid was catalyzed by lipase from Candida antarctica in acetone. Different formulations were evaluated regarding their emulsifying properties and ability to dissolve the rutin ester. Suitable SEDDS was chosen and characterized regarding droplet size, polydispersity index, and zeta potential. The rutin fatty ester was loaded into SEDDS to 7% (w/w). Different concentrations of PDMSHEPMS were incorporated in SEDDS for following mucus permeation studies. Formulation with 10% of PDMSHEPMS showed 1.9-fold increase in mucus permeation compared to the formulation without PDMSHEPMS. Furthermore, the formulation with 10% of PDMSHEPMS showed a significant increase in mucus permeation compared with rutin fatty ester without formulation. According to these results, SEDDS containing PDMSHEPMS might be a promising strategy to increase the oral bioavailability of rutin.

Optimization of flavonoid extraction from Passiflora quadrangularis leaves with sedative activity and evaluation of its stability under stress conditions

Abstract Passiflora species have been widely used in folk medicine as tranquilizers, and previous pharmacological studies have reported sedative activity for P. quadrangularis L., Passifloraceae, leaf extracts. The aim of this work was to contribute to the standardization of P. quadrangularis leaf extract with sedative activity. For this purpose, the extraction of total flavonoids was optimized, evaluating variables such as drug-solvent ratio, extraction solvents and extraction time, using Response Surface Methodology. The stability of total and individual flavonoids on the optimized extract of P. quadrangularis leaves under stress conditions was also evaluated. Sedative activity was verified by the ethyl ether-induced hypnosis test in Swiss ICR mice. Based on the results, the highest concentration of total flavonoids was obtained at a drug-solvent ratio of 1:15 (w:v), extraction solvent EtOH:H2O (1:1, v/v) and percolation time of 48 h. Regarding stability under stress conditions, it was found that the flavonoids from the optimized extract are photostable, and practically stable under neutral hydrolysis and oxidation, but labile by acid and basic hydrolysis, with the main degradation products being identified. Finally, it was demonstrated that the optimized extract improves the sedative effect when compared to previously evaluated extract in the ethyl ether-induced hypnosis test.

Peruvioses A to F, sucrose esters from the exudate of Physalis peruviana fruit as α-amylase inhibitors.

The fruit of Physalis peruviana is widely used in traditional Colombian medicine as an antidiabetic treatment. The aim of the study reported here was to identify the compounds responsible for the hypoglycemic activity using the α-amylase inhibition test. Bioguided fractionation of a dichloromethane extract of the sticky exudate that covers the fruit allowed the isolation and identification of three new sucrose esters, named as peruvioses C-E (1-3), along with the known peruvioses A (6), B (5) and F (4), the structures of which were elucidated by extensive NMR and MS experiments. These compounds proved to be responsible for the hypoglycemic activity observed in the extract. Peruviose D (2) showed the highest activity, with an inhibitory activity value of 84.8%. This is the first study to establish the potential of sucrose esters as α-amylase inhibitors and to explain the hypoglycemic effect that has traditionally been attributed to gooseberry fruit.

Phytochemical analysis, antioxidant and anti-inflammatory activity of calyces from Physalis peruviana.

Physalis peruviana calyces are used extensively in folk medicine. The crude ethanolic extract and some fractions of calyces were evaluated in order to explore antioxidant and anti-inflammatory activities. The anti-inflammatory activity was evaluated by the TPA-induced ear edema model. The antioxidant in vitro activity was measured by means of the superoxide and nitric oxide scavenging activity of the extracts and fractions. The butanolic fraction was found to be promising due to its anti-inflammatory and antioxidant activities. Therefore, a bio-assay guided approach was employed to isolate and identify rutin (1) and nicotoflorin (2) from their NMR spectroscopic and MS data. The identification of rutin in calyces of P. peruviana supports the possible use of this waste material for phytotherapeutic, nutraceutical and cosmetic preparations.

Gibbs energy of transfer processes for the antimicrobial agent Triclosan from water to some organic solvents at 25.0 °C

The thermodynamic function Gibbs energy for the dissolution processes of triclosan (TS) was calculated from solubility values obtained at 25.0 °C in organic solvents with different hydrogen-bonding capability. TS solubility was determined in ethanol, octanol, water-saturated octanol, isopropyl myristate, chloroform, and heptane. The excess Gibbs energy and the activity coefficients of the solute were also calculated. In addition, the corresponding Gibbs energies of the drug transfer process from water to the organic solvents under investigation were also calculated by means of previous reports. In all cases, this thermodynamic property comprised a negative value, indicating the preference of TS for all the organic media evaluated.

En este trabajo se presentan las energías de Gibbs para los procesos de disolución del triclosan (TS) en solventes orgánicos de diferente capacidad de formación de enlace de hidrógeno, las cuales fueron calculadas a partir de los valores de solubilidad a 25,0 °C. La solubilidad del TS se determinó en etanol, octanol, octanol saturado de agua, miristato de isopropilo, cloroformo, y heptano. Así mismo se calcularon las energías de Gibbs de exceso y los coeficientes de actividad del soluto en los mismos solventes. Adicionalmente, mediante el uso de valores previamente reportados en la literatura, se calcularon las energías de Gibbs de transferencia del TS desde el agua hasta los solventes orgánicos comprendidos en el estudio. En todos los casos, esta propiedad termodinámica fue negativa demostrando la preferencia del TS por los medios orgánicos evaluados.

Sistemas osmóticos de administración oral / Osmotically controlled oral drug delivery systems

Considerando que a nivel mundial el diseño de nuevos fármacos involucra un costo muy alto, tanto en tiempo como en dinero, la preocupación en los últimos años se ha centrado en diseñar y desarrollar medicamentos que controlen la liberación del activo, de manera que se les pueda dar un valor agregado a moléculas ya existentes, lo que significa una menor inversión en términos de costos. En este sentido, para la presente revisión se seleccionó el sistema de liberación osmótica, uno de los medicamentos de liberación controlada con más participación en el mercado en el mundo. En este escrito se muestran los aspectos fisicoquímicos relacionados con su formulación, las clases de sistemas osmóticos de administración oral existentes y sus aplicaciones, así como el estado del arte en este contexto. Hacia el futuro, estos sistemas osmóticos parecen ser muy promisorios, debido a sus ventajas y gran mercado potencial