Biotransformation of rifampicin by Aspergillus niger and antimicrobial activity of proposed metabolites.

Drug biotransformation studies emerges as an alternative to pharmacological investigations of metabolites, development of new drug candidates with reduced investment and most efficient production. The present study aims to evaluate the capacity of biotransformation of rifampicin by the filamentous fungus Aspergillus niger ATCC 9029. After incubation for 312 h, the drug was metabolized to two molecules: an isomer (m/z 455) and the rifampicin quinone (m/z 821). The monitoring of metabolite formation was performed by high-performance liquid chromatography, followed by their identification through ultra-high-performance liquid chromatography coupled to tandem mass spectrometer. In vitro antimicrobial activity of the proposed metabolites was evaluated against Staphylococus aureus microorganism, resulting in the loss of inhibitory activity when compared with the standards, with minimum inhibitory concentration of 7.5 µg/ml. The significant biotransformation power of the ATCC 9029 strain of A. niger was confirmed in this study, making this strain a candidate for pilot studies in fermentation tanks for the enzymatic metabolization of the antimicrobial rifampicin. The unprecedented result allows us to conclude that the prospect of new biotransforming strains in species of anemophilic fungi is a promising choice.

Amazonia Products in Novel Lipid Nanoparticles for Fucoxanthin Encapsulation.

Lipid nanoparticles (LNs) are traditional systems able to effectively increase skin hydration. However, due to its reduced viscosity, LNs suspensions are less attractive for skin administration. To overcome this disadvantage, the LN were incorporated in the semi-solid formulation is easy manipulation. This study demonstrated that it is possible to obtain novel LN-loaded fucoxanthin (LN-FUCO) for topical administration containing a combination of bacuri butter and tucumã oil prepared by high shear homogenization for improved stability. The particle size was found to be 243.0 nm and the entrapment efficiency up to 98% of FUCO was incorporated and achieved the suitability of formula. The LN-FUCO hydrogel characteristics of slight acidity, drug content near 100%, and nanometric mean size assure to this formulation high compatibility to dermal application. Photostability assay by UVA, LN-FUCO, and LN-FUCO hydrogel improved photostability and conferred greater protection against FUCO degradation. The results obtained from in vitro skin permeation studies presented a significant difference between LN-FUCO hydrogel and FUCO (p < 0.05), with no detection of the drug in the receptor medium. Therefore, high shear homogenization is demonstrated to be a simple, available, and effective method to prepare high-quality LN-FUCO hydrogel for topical application.

In vitro evaluation of cutaneous penetration of acyclovir from semisolid commercial formulations and relation with its effective antiviral concentration

ABSTRACT The evaluation of drug permeation/penetration of semisolid formulations into animal skin can be useful to supplement the pharmaceutical equivalence. This paper describes the in vitro assessment of acyclovir (ACV) into porcine skin from commercial formulations with etermination of drug concentration in different layers of cutaneous tissue to correlate with effective antiviral concentration in order to improve the equivalence decision. Studies were conducted using Franz cells and porcine skin. Selected pharmaceutical creams containing ACV had identical (reference and generic) and different (similar) excipients. A software program was employed for the simulation of antiviral effectiveness in the skin. Regarding ACV skin penetration, the first batch of the generic product showed a significant difference from reference and similar products, while in the second batch all products demonstrated equivalent drug penetration in the skin. Simulation studies suggest that formulations analysed exhibit a pharmacological effect even when in contact with Herpes simplex strains of high IC50 (inhibitory concentration required to reduce viral replication by 50%). According to results, it can be assumed that the in vitro cutaneous permeation/penetration study does not supply sensitivity information regarding small alterations of ACV semisolid formulations due to the variability inherent to the method, although it can be relevant to pharmaceutical equivalence studies in the development of semisolid products.

Influência da adição de extrato de chá-verde sobre a estabilidade e efeito fotoprotetor de emulsões fps 15 / Influence of green tea extract on the stability and photoprotective effect of spf 15 emulsions

A inserção de produtos de origem vegetal em cosméticos podem melhorar as suas características. Nesse estudo, objetivou-se o desenvolvimento de formulações fotoprotetoras contendo extrato glicólico de Camelia sinensis, a avaliação da atividade fotoprotetora in vitro após a adição do extrato vegetal, bem como a avaliação das características organolépticas, a determinação do valor de pH e comportamento reológico durante 30 dias de avaliação, quando as formulações foram armazenadas nas temperaturas de 25±2°C; 5±2 °C e 40±2 °C. Após 15 dias, alterações nas características organolépticas e reológicas foram observadas nas formulações armazenadas em altas temperaturas. Em 30 dias, as formulações mantidas a temperatura ambiente e em geladeira mantiveram as características organolépticas, apesar das alterações reológicas. Observou-se uma tendência a aumento do efeito fotoprotetor com a formulação contendo FPS15 e extrato glicólico de chá verde, entretanto, não se pode atribuir melhora na estabilidade física da emulsão pela adição do extrato.

The addition of plant material to a cosmetic may improve its characteristics. The stability profile allows the performance, safety, efficacy and consumer acceptance of an emulsion to be assessed. A stability study provides information about the behavior of the product over a given time interval, under various environmental conditions. The aims of this study were to prepare sunscreen formulations containing a glycolic extract of green tea (Camellia sinensis) and to assess the photoprotective activity in vitro, the organoleptic characteristics, pH and rheological behavior over a period of 30 days, during which the formulations were stored at temperatures of 25±2°C, 5±2°C and 40±2°C. After 15 days, changes in rheological characteristics were observed in the formulation stored at the higher temperatures. After 30 days, changes were observed at other temperatures. The addition of the extract significantly changed the rheological profile of the sunscreen formulations tested. An increase in the photoprotective effect was observed when the emulsion base was compared with the emulsion containing green tea extract. However, there was no evidence of an improvement of stability when the plant extract was added to the emulsions.