Utilization of dynamic light scattering to evaluate Pterodon emarginatus oleoresin-based nanoemulsion formation by non-heating and solvent-free method

Abstract Pterodon emarginatus Vogel, Fabaceae, is a great source of bioactive compounds. The most known and studied herbal derivative from this species is an ambar-colored oleoresin that contains vouacapane diterpenes and volatile terpenoids, such as β-caryophyllene. Some recent papers aimed to generate nanoemulsions using this oleoresin for biological applications. However, they used high-energy methods that elevate costs of the process or heating procedures, which offer the disadvantage of possible volatile substances loss. Thus, as part of our ongoing studies with nanobiotechnology of natural products, especially regarding preparation of nanoemulsions with promising plant-based oils by low cost and low energy methods, we decided to evaluate the ability of non-heating and solvent-free method to generate P. emarginatus oleoresin-based nanoemulsions. Two non-ionic surfactants were used to generate the nanoemulsions by a simple homogenization method with vortex stirrer. Low mean droplet size (<180 nm) and low polydispersity index (<0.200) were observed even after one day of preparation. The low coefficient of variation for the analyzed parameters of different batches and similar profile for droplet size distribution suggested reproducibility of the method. After 30 days, some degree of droplet growth was observed on nanoemulsion prepared with polyethyleneglycol 400 monooleate, while almost no alteration was observed for nanoemulsion prepared with polysorbate 85. Programmed temperature ramp analysis revealed that no major effects on droplet size and polydispersity index were observed, suggesting the robustness of formed nanoemulsions. Thus, the present study shows for the first time the formation of sucupira-based nanoemulsions by a simple, low cost and ecofriendly method. This study opens new perspectives for bioactive evaluation of this novel nano-product.

Bioactive compounds in Bidens pilosa L. populations: a key step in the standardization of phytopharmaceutical preparations

The total flavonoid content (TFC), total polyphenols content (TPC), and in vitro antioxidant activity (AA) of six Bidens pilosa L., Asteraceae, populations harvested from different localities were evaluated in this work. The plants were separated in roots, stems, and leaves/flowers, and the influence of extraction methods was investigated.Areversed-phase high-performance liquid chromatography method (HPLC) was developed and employed to obtain characteristic HPLC fingerprints of the bioactive compounds present in the extractive solutions, which were correlated with the TFC, TPC, and AA. Extractive solutions of leaves/flowers presented a higher AA when compared with those obtained from other parts of the plant (IC50 of 35.35±0.10 µg/mL). The stem extracts presented the lowest AA (IC50 117.2±1.96 µg/mL). A direct correlation of AA with TFC and TPC was evidenced. The highest AA was obtained by dynamic maceration and was statistically different from the AA presented by the extractive solutions obtained by other extraction methods. The results of this work evidenced differences that can be found at different stages of development of phytopharmaceutical preparations from B. pilosa and highlighted the importance of using the concentration of marker compounds as well as HPLC fingerprints as quality control parameters.

Evaluación de la estructura para la producción e indicación de fitofármacos en adultos mayores con afecciones respiratorias. Colón, 1 ene- 30 jun de 2008 / Evaluation of the structure for the production and indication of phytopharmaceutical products in elder people with respiratory diseases. Colon, January 1st-June 30th 2008

El aumento de la esperanza de vida es uno de los mayores logros obtenidos en los avances en medicina y de la mejor calidad de vida de las personas. La población adulta mayor crece rápidamente en casi todos los países, por lo que urge tomar medidas encaminadas a proteger la salud y bienestar futuro de este grupo poblacional, prestando particular interés en la búsqueda de terapias menos agresivas y sin efectos secundarios. Esta investigación evaluó la disponibilidad de recursos humanos y materiales para la atención al tratamiento con fitofármacos de los adultos mayores con afecciones respiratorias, en el área de salud del Policlínico Dr Francisco Figueroa Véliz, del municipio Colón, provincia de Matanzas. El diseño metodológico utilizado responde a los principios, leyes y categorías del materialismo dialéctico y su método científico. Para la recolección de información se utilizó un instrumento confeccionado por el equipo de trabajo para estos fines y validado en su funcionamiento. Se encontró que todas las unidades organizativas del área de salud presentan problemas con los recursos disponibles que conforman su estructura.

The increase of the life-expectancy is one of the highest achievements obtained as a result of the medicine advances and the better people’s life quality. Elder people population grows fast almost in all the countries, so it is necessary to introduce measures to protect the future wellbeing and health of this group of population, giving particular attention to less aggressive therapies, without secondary effects. This research evaluated the availability of the human resources and materials to treat elder people with respiratory diseases with phytopharmaceutical products in the health area of the Policlinic Dr Francisco Figueroa Veliz, of the municipality of Colon, province of Matanzas. The methodological design used is in correspondence with the principles, laws and categories of the dialectic materialism and its scientific method. To collect data we used an instrument elaborated by the working team with this aim and validated in its functioning. We found that all the organizational units of the health area have problems with the available resources forming their structures.

Medical Herbalism and Herbal Clinical Research: A Global Perspective.

This review aims to sensitize researchers, regulators and other stakeholders to the centrality of clinical research to drug development from herbs used in Traditional Medicine (TM). The review uncovered and dwelt on the fact that: While clinical trials of chemical medicines (pharmaceuticals) tend to come late in the drug development chain, the reverse is often the case with herbal medicines (phytomedicines). Once the decision is made to develop a single phytochemical entity (phytopharmaceutical, example: artemisinin) from a plant, the need for such sensitization is particularly desirable, given their huge socioeconomic implications. The review emphasized that drug development from a traditional herb can: i) take the route of standardization of the herb or its extract for immediate use without further chemical manipulations; or ii) proceed along the line of isolation and other manipulations aimed at optimising bioactivity. By the first route, development proceeds directly from confirming that the pharmacological property of the herb tallies with its traditional indication, leading instantly to value addition to traditional knowledge accumulated over years. This is because herbal medicines based on time tested traditions need not undergo phased trials as would a novel pharmaceutical (or an old herb for a new indication), since their long histories often offer evidence of their safety and efficacy. In the second route, clinical studies usually come later in the chain. This is because, unlike the traditional therapeutic, the new phytopharmaceutical, taken out of its natural microenvironment and subjected to various chemical manipulations, including purification, is no longer the equivalent of the ancient remedy with predicable effects. Moreover, in this later case, interest in the new entity (an artificially concentrate isolate) may shift completely from the traditional indication of the herb, hence the need for phased trials of phytopharmaceuticals (or an old herb for a new indication), despite their natural origin.

Desarrollo tecnológico de un medicamento sedante de origen natural a partir de Justicia pectoralis Jacq / Technological development of a sedative medicine of natural origin from Justicia pectoralis Jacq

Introducción: el empleo de las materias primas de origen natural, como ingrediente farmacéutico activo, se difunde cada vez más en la industria farmacéutica para la elaboración de medicamentos. Justicia pectoralis Jacq (Acantaceae) es una planta herbácea que se emplea como sedante tradicionalmente por la población cubana, conocida como tilo. Objetivo: desarrollar un medicamento, en forma de jarabe, que contenga como sustancia activa el extracto seco de J pectoralis 0,6 por ciento m/v. Métodos: se efectuó el estudio de formulación, microbiológico y de estabilidad químico-física, almacenado a temperatura ambiente en frascos de vidrio ámbar por 125 mL. Resultados: se obtuvo un jarabe con adecuadas características organolépticas, estable desde el punto de vista microbiológico, físico y químico, durante 36 meses en las condiciones estudiadas. Conclusiones: el medicamento desarrollado fue correctamente formulado desde el punto de vista galénico y cumple con los requisitos de calidad establecidos para este tipo de forma farmacéutica

Introduction: the use of natural raw materials as active ingredient is increasingly spreading in the drug industry for the manufacture of pharmaceuticals. Justicia pectoralis Jacq(Acantaceae) is a herbaceous plant traditionally used as sedative by the Cuban population which knows it as lime tea. Objective: to develop syrup containing the dry extract from J. pectoralis 0,6 percent m/v as active principle. Methods: the formulation, microbiological and chemical/physical stability studies were performed on the product stored at room temperature in 125 mL amber-coloured glass containers. Results: the syrup had adequate organoleptic characteristics and was stable from the microbiological, physical and chemical viewpoints for 36 months under the studied conditions. Conclusions: this pharmaceutical was properly formulated from the galenic viewpoint and met all the set quality requirements for this type of pharmaceutical form

Acute and chronic toxicological studies of the Brazilian phytopharmaceutical product Ierobina / Estudos de toxicidade aguda e crônica do produto fitoterápico brasileiro Ierobina

Ierobina® is a Brazilian phytopharmaceutical product employed for the treatment of dyspepsia (280 mg/kg/day). Despite its widespread use in the country for over 75 years, only recently its therapeutic efficacy has been attested in animals; however, no toxicological investigations have been carried out for the product to date. In this paper we evaluated the acute toxicity of Ierobina® administrated by gavage in mice (single doses of 2100 mg/kg, 6300 mg/kg and 12600 mg/kg), along with its chronic effects in rats, after product administration per os daily, at the doses of 2800 mg/kg and 5600 mg/kg, for 180 days. The product had low acute toxicity; all observed alterations were reversible and no animal died during the experiments. In chronic toxicological studies, Ierobina® administration for 180 days did not cause any changes in hematological and biochemical parameters, with the exception of decreasing the levels of alanine transaminase, aspartate transaminase and creatinine. However, histological evaluation of kidney, liver and other selected organs showed normal architecture, suggesting no morphological disturbances. Hence, considering the obtained results and the fact that Ierobina® has been commercialized for decades in Brazil, without any notified case of toxicity, it seems that the product is safe for human use.

A Ierobina® é um produto utilizado popularmente, no Brasil, para tratamento de dispepsia, na dose de 280 mg/kg/dia. Apesar de seu largo uso nos últimos 75 anos, recentemente foi comprovada sua eficácia em animais; porém, nenhuma avaliação de seu perfil toxicológico foi realizada. O objetivo do presente estudo foi avaliar a toxicidade aguda (doses únicas de 2100 mg/kg, 6300 mg/kg ou 12600 mg/kg), em camundongos, e crônica (doses de 2800 mg/kg ou 5600 mg/kg, por 180 dias), em ratos, após administração per os de Ierobina®. No teste de toxicidade aguda, as doses administradas não produziram nenhuma mortalidade e os sinais observados foram todos reversíveis. No teste de toxicidade crônica, não foram verificadas diferenças significativas nas análises hematológicas, macroscópicas e microscópicas. Nos exames de bioquímica sérica, diferença significativa foi observada somente na avaliação da alanina transaminase, aspartato transaminase e creatinina, porém, sem importância clínica. Assim, considerando os resultados obtidos e o fato de ser a Ierobina® um produto comercializado há décadas, sem qualquer notificação de casos de toxicidade, podemos concluir que o produto parece ser de segurança adequada para uso humano.