The use of natural extracts with photoprotective activity: a 2015-2023 patent prospection.

Synthetic sunscreen offers protection against excessive exposure to ultraviolet (UV) radiation from the sun, and protects the skin from possible damage. However, they have low efficacy against the formation of reactive oxygen species (ROS), which are highly reactive molecules that can be generated in the skin when it is exposed to UV radiation, and are known to play a role in oxidative stress, which can contribute to skin aging and damage. Thus, there is an ongoing search for sunscreens that do not have these negative effects. One promising source for these is natural products. Therefore, the current patent review summarizes topical formulations made from natural compounds that have antioxidant properties and can be used as photoprotective or anti-aging agents, either using a single natural extract or a combination of extracts. The review reports basic patent information (applicant country, type of applicant, and year of filing) and gives details about the invention, including its chemical composition, and the in vitro and in vivo tests performed. These patents describe natural products that can be used to protect the skin and validate their efficacy, and safety, in addition to standardizing their formulations. The compositions described illustrate the consistent innovation in the use of natural products to protect against UV damage and photoaging disorders, a promising field which is receiving growing global recognition.

Atividade fotoprotetora e antioxidante de compostos fenólicos: uma revisão sistemática de testes in vitro / Photoprotective and antioxidant activity of phenolic compounds: a systematic review of in vitro tests / Actividad fotoprotectora y antioxidante de compuestos fenólicos: una revisión sistemática de ensayos in vitro

RESUMO Introdução: Os compostos fenólicos, devido a sua estrutura química, possuem a capacidade de absorver a energia ultravioleta e reduzir a formação de radicais livres. Objetivo: Avaliar a atividade fotoprotetora e antioxidante de compostos fenólicos a partir da observação de resultados in vitro e verificar a importância do uso de modelos biológicos nessa perspectiva. Metodologia: Foi realizada uma pesquisa de artigos publicados, na base de dados Pubmed, entre 2010 e 2020, que atendessem aos objetivos deste trabalho, 44 artigos foram selecionados. Resultados: Os métodos instrumentais utilizados para avaliação da atividade fotoprotetora apresentaram boa correlação in vivo e mostram-se rápidos e eficazes na determinação do fator de proteção solar. Além desses, têm-se aplicado métodos biológicos para a avaliação de aspectos que não são mensurados por métodos físico-químicos, relacionado aos danos ao DNA, decorrentes da exposição solar. Para a avaliação da atividade antioxidante, o método do radical DPPH foi empregado em 92,6 % dos estudos analisados e foi observado que os antioxidantes podem incrementar a proteção solar e, ainda, auxiliar na estabilidade de filtros solares sintéticos. Conclusão: Os compostos fenólicos, especialmente aqueles com propriedades antioxidantes, podem ser utilizados como agentes fotoprotetores em formulações tópicas para reduzir os danos à pele induzidos pela radiação UV.

SUMMARY Introduction: Phenolic compounds, due to their chemical structure, can absorb ultraviolet energy and reduce the formation of free radicals. Aim: To evaluate the photoprotective and antioxidant activity of phenolic compounds from the observation of in vitro results and to verify the importance of the use of biological models in this perspective. Methodology: A search for articles published in the Pubmed database was carried out between 2010 and 2020, which met the objectives of this work, 44 articles were selected. Results: According to the literature, the instrumental methods used to assess independent photoprotective activity, good correlation in vivo, and demonstrating rapid and effective determination of the sun protection factor. In addition to these, biological methods have been provided for the evaluation of aspects not measured by physical-chemical methods, related to DNA damage, resulting from sun exposure. For the evaluation of antioxidant activity, the DPPH radical method was registered in 92.6 % of published studies and it was observed that antioxidants can increase sun protection and also help in the stability of synthetic sunscreens. Conclusion: Phenolic compounds, especially with antioxidant properties, can be used as photoprotective agents in topical formulations to reduce skin damage induced by UV radiation.

RESUMEN Introducción: Los compuestos fenólicos, por su estructura química, tienen la capacidad de absorber la energía ultravioleta y reducir la formación de radicales libres. Objetivo: Evaluar la actividad fotoprotectora y antioxidante de compuestos fenólicos a partir de la observación de resultados in vitro y comprobar la importancia del uso de modelos biológicos en esta perspectiva. Metodología: Se realizó una búsqueda de artículos publicados en la base de datos Pubmed entre 2010 y 2020, que cumplieron con los objetivos de este trabajo, se seleccionaron 44 artículos. Resultados: Los métodos instrumentales utilizados para evaluar la actividad fotoprotectora mostraron una buena correlación in vivo y demostraron ser rápidos y eficientes en la determinación del factor de protección solar. Además de estos, se aplicaron métodos biológicos para evaluar aspectos no medidos por métodos físico-químicos, relacionados con el daño en el ADN por exposición solar. Para la evaluación de la actividad antioxidante se utilizó el método radical DPPH en el 92,6% de los estudios analizados y se observó que los antioxidantes pueden aumentar la protección solar y también ayudar en la estabilidad de los protectores solares sintéticos. Conclusión: Los compuestos fenólicos, especialmente aquellos con propiedades antioxidantes, pueden utilizarse como agentes fotoprotectores en formulaciones tópicas para reducir el daño cutáneo inducido por la radiación UV.

Structure, Solubility and Stability of Orbifloxacin Crystal Forms: Hemihydrate versus Anhydrate.

Orbifloxacin (ORBI) is a widely used antimicrobial drug of the fluoroquinolone class. In the official pharmaceutical compendia the existence of polymorphism in this active pharmaceutical ingredient (API) is reported. No crystal structure has been reported for this API and as described in the literature, its solubility is very controversial. Considering that different solid forms of the same API may have different physicochemical properties, these different solubilities may have resulted from analyses inadvertently carried out on different polymorphs. The solubility is the most critical property because it can affect the bioavailability and may compromise the quality of a drug product. The crystalline structure of ORBI determined by SCXRD is reported here for the first time. The structural analysis reveals that the ORBI molecule is zwitterionic and hemihydrated. ORBI hemihydrated form was characterized by the following techniques: TG/DTA, FTIR-ATR, and PXRD. A second crystalline ORBI form is also reported: the ORBI anhydrous form was obtained by heating the hemihydrate. These ORBI solid forms were isomorphous, since no significant change in unit cell and space group symmetry were observed. The solid-state phase transformation between these forms is discussed and the equilibrium solubility data were examined in order to check the impact of the differences observed in their crystalline structures.

Antioxidant Activity and Validation of Quantification Method for Lycopene Extracted from Tomato.

Lycopene is a carotenoid found in tomatoes with potent antioxidant activity. The aim of the study was to obtain an extract containing lycopene from four types of tomatoes, validate a quantification method for the extracts by HPLC, and assess its antioxidant activity. Results revealed that the tomatoes analyzed contained lycopene and antioxidant activity. Salad tomato presented the highest concentration of this carotenoid and antioxidant activity. The quantification method exhibited linearity with a correlation coefficient of 0.9992. Tests for the assessment of precision, accuracy, and robustness achieved coefficients with variation of less than 5%. The LOD and LOQ were 0.0012 and 0.0039 µg/mL, respectively. Salad tomato can be used as a source of lycopene for the development of topical formulations, and based on performed tests, the chosen method for the identification and quantification of lycopene was considered to be linear, precise, exact, selective, and robust.

Quality evaluation of the Finasteride polymorphic forms I and II in capsules.

Finasteride (FNS) is a specific competitive inhibitor of steroid type-II 5α-reductase and is widely used for the treatment of benign prostatic hyperplasia, prostate cancer, and androgenetic alopecia. FNS has two polymorphic forms identified as Form I and Form II. It is known that polymorphism can cause significant differences in the physicochemical properties of a compound such as melting point, density, morphology, solubility, and color. Thus, proper qualitative and quantitative monitoring of the solid-state forms is crucial to ensure high-quality products. There are no published papers studying the influence of the FNS polymorphs on the physicochemical quality of capsules. Furthermore, the available analytical methods are time-consuming, expensive, use buffer or do not demonstrate stability-indicating capacity. The aim of this work was to validate a rapid high-performance liquid chromatography (HPLC) method to evaluate FNS in capsules and to study the physicochemical properties of polymorphic forms, evaluating their possible influence in the dissolution profile and stability of FNS in capsules. Capsules containing Forms I and II of FNS were prepared and subjected to quality control studies, dissolution profiles and a stability study at 50°C. A significant effect of polymorphism on the FNS solubility and dissolution properties was observed. These results suggest that changes in the effects of FNS can occur if a suitable control study is not performed on the raw material used to produce the capsules.

Development and validation of UV spectrophotometric method for orbifloxacin assay and dissolution studies

New, simple and cost effective UV-spectrophotometric method was developed for the estimation of orbifloxacin in pharmaceutical formulation. Orbifloxacin was estimated at 290 nm in 0.5 M hydrochloric acid. Linearity range was found to be 1.0-6.0 μg mL-1. The method was tested and validated for various parameters according to main guidelines. The proposed method was successfully applied for the determination of orbifloxacin in tablets. The results demonstrated that the procedure is accurate, precise and reproducible, while being simple, economical and less time consuming. It can be suitably applied for the estimation of orbifloxacin in routine quality control and dissolution studies.

Um método espectrofotométrico novo, simples e de baixo custo foi desenvolvido para a determinação de orbifloxacino em formulação farmacêutica. O orbifloxacino foi determinado em 290 nm utilizando ácido clorídrico 0,5 M como solvente. O intervalo de linearidade usado foi de 1,0 a 6,0 μg mL-1. O método foi testado e validado em vários parâmetros de acordo com os principais guias. O método proposto foi aplicado com sucesso para a determinação de orbifloxacino em comprimidos. Os resultados demonstraram que este procedimento é exato, preciso e reprodutível, ao mesmo tempo em que é simples, barato e de mais rápida execução e pode ser adequadamente aplicado para a determinação de orbifloxacino na rotina do controle de qualidade e em estudos de dissolução de comprimidos contendo este fármaco.

A novel and rapid microbiological assay for ciprofloxacin hydrochloride.

The present work reports a simple, fast and sensitive microbiological assay applying the turbidimetric method for the determination of ciprofloxacin hydrochloride (CIPRO HCl) in ophthalmic solutions. The validation method yielded good results and included excellent linearity, precision, accuracy and specificity. The bioassay is based on the inhibitory effect of CIPRO HCl upon the strain of Staphylococcus epidermidis ATCC 12228 used as the test microorganism. The results were treated statistically by analysis of variance (ANOVA) and were found to be linear (r=0.9994, in the range of 14.0-56.0 µg/mL), precise (intraday RSD%=2.06; interday RSD%=2.30) and accurate (recovery=99.71%). The turbidimetric assay was compared to the UV spectrophotometric and HPLC methods for the same drug. The turbidimetric bioassay described on this paper for determination of ciprofloxacin hydrochloride in ophthalmic solution is an alternative to the physicochemical methods disclosed in the literature and can be used in quality control routine.

Corrositex®, BCOP and HET-CAM as alternative methods to animal experimentation / Corrositex®, BCOP e HET-CAM como métodos alternativos à experimentação animal

Tests in animals are used as models in toxicological and investigative studies. However, such tests have been considered inhumane because they can cause pain and suffering to experimental animals, while these methods can often be subjective. Protests calling for animal protection have questioned the effectiveness of in vivo tests and suggest the introduction of alternative, in vitro methods. International organizations, such as the Interagency Coordinating Committee on the Validation of Alternative Methods (ICCVAM), the National Institute of Health (NIH), the Organization for Economic Co-operation and Development (OECD), that regulate and develop new alternative animal models, have indicated the running of preliminary assays and execution of sequential tests, which consider physical-chemical properties and data of in vitro assays, before performing in vivo studies. Towards this background, the objective of the present article was to select promising alternative methods such as Corrositex®, BCOP and HET-CAM, intended to refine or replace the use of animals and reduce their suffering.

Testes em animais são utilizados como modelos em estudos toxicológicos e de pesquisa. Entretanto, tais testes têm sido considerados desumanos, porque causam dor e sofrimento aos animais experimentais, porquanto estes métodos podem, freqüentemente, ser subjetivos. Protestos clamando pela proteção animal têm questionado a eficácia dos testes in vivo e sugerem a introdução de métodos alternativos in vitro. Organizações internacionais, tais como Comitê de Coordenação Interagências de Métodos de Validação Alternativos (ICCVAM), Instituto Nacional de Saúde (NIH), Organização para Cooperação Econômica e Desenvolvimento (OECD), que regulam e desenvolvem novos métodos alternativos aos modelos animais, indicaram a realização de ensaios preliminares e a execução de testes seqüenciais, que consideram as propriedades físico-químicas e os dados dos ensaios in vitro, antes de efetuarem estudos in vivo. Nessa direção, o objetivo do presente artigo foi selecionar métodos alternativos promissores, tais como Corrositex®, BCOP e HET-CAM, com o intuito de aperfeiçoar ou substituir o uso de animais e reduzir seus sofrimento.