Analyzing the results of finger systolic blood pressure tests in 28 healthy young adults / 中国职业医学

Objective To investigate the level of finger systolic blood pressure (FSBP) in healthy young adults. Methods A total of 28 healthy young adults were selected as the study subjects by convenient sampling method. The FSBP of the study subjects was detected at 30 and 10 ℃, and the FSBP index (Fi) was calculated. Results The FSBP of the study subjects at 30 and 10 ℃ were (102.0±16.5) and (104.4±15.2) mmHg, respectively. The FSBP in male group at 30 and 10 ℃ was (99.6±18.6) and (107.2±17.0) mmHg, respectively. The FSBP in female group at 30 and 10 ℃ was (104.4±13.9) and (101.5±2.8) mmHg, respectively. The results of factorial analysis showed that the interaction between gender and temperature on FSBP was statistically significant (P<0.05). FSBP in male group was higher at 10 than 30 ℃ (P<0.05) and higher than female group at 10 ℃ (P<0.05). There was no statistical significance for the main effect of gender, temperature, finger, or the interaction effect of gender and finger, temperature and finger for FSBP (all P>0.05). The average Fi of the study subjects was (98.0±16.6)%, with males and females having the average Fi of (100.7±20.7) % and (95.2±10.6) % respectively. The results of factorial analysis of variance showed that there was no significant difference on Fi in the main effect gender and fingers or the interaction effect between them(all P>0.05). Conclusion The FSBP test could be used as a detection method for assessing peripheral microcirculation function in Chinese population. However, further research is needed to establish reference ranges and influencing factors.

Otimização de método extrativo para raízes de Arctium lappa L / Extractive method optimization for Arctium lappa l. Roots / Optimización de un método de extracción de raíces de Arctium lappa L

Arctium lappa L. é indicada no Formulário de Fitoterápicos da Farmacopeia Brasileira para o tratamento de distúrbios urinários leves. Estudos já demonstraram o potencial antioxidante, anti-inflamatório e antidiabético deste extrato, onde foram identificados fenóis, lignanas, taninos e flavonoides. O objetivo deste trabalho foi otimizar o método extrativo de raízes de A. lappa. Realizou-se o preparo de extratos por diferentes métodos: Ultrassom, Soxhlet, maceração e turbo extração. A otimização foi realizada por turbo extração seguindo um planejamento fatorial 23, empregando como fatores: teor alcoólico, concentração da matéria prima e tempo de extração. Os extratos foram avaliados quanto ao resíduo seco, teores de fenóis e flavonoides, e atividade antioxidante. Com relação ao resíduo seco, e aos teores de fenóis e flavonoides, os métodos de ultrassom e turbo extração demonstraram melhor poder extrativo. Devido ao menor tempo e custo operacional, a otimização foi realizada por turbo extração, e o extrato otimizado foi obtido utilizando álcool 60%, em proporção matéria prima solvente 1:10 e tempo de extração de 15 minutos. Estas análises poderão nortear futuros testes de transposição de método para escala industrial, diminuindo mão de obra, tempo e custos, visando obter produtos fitoterápicos mais eficientes, com valor acessível à população.

Arctium lappa L. is indicated in the Brazilian Pharmacopeia Herbal Medicines Form for the treatment of mild urinary disorders. Studies have already demonstrated the antioxidant, anti-inflammatory and antidiabetic potential of this extract, where phenols, lignans, tannins and flavonoids were identified. The objective of this work was to optimize the extractive method of A. lappa roots. Extracts were prepared by different methods: Ultrasound, Soxhlet, maceration and vortical extraction. The optimization was performed by vortical extraction following a 23 full factorial design, using as factors: alcohol content, drug concentration and extraction time. The extracts were evaluated for dry residue, phenols and flavonoids contents, and antioxidant activity. Regarding the dry residue, and the phenols and flavonoids contents, the ultrasound and vortical extraction methods showed better extractive power. Due to the lower operating time and cost, the optimization was performed by vortical extraction, and the optimized extract was obtained using 60% alcohol, in a 1:10 drug solvent ratio and extraction time of 15 minutes. These assessments guide the future tests of transposition of the method to an industrial scale, reducing manpower, time and costs, aiming to obtain more efficient phytotherapic products, with affordable value for the population.

Arctium lappa L. está indicado en la Formulacao de Fitoterápicos da Farmacopeia Brasileira para el tratamiento de trastornos urinarios leves. Los estudios han demostrado el potencial antioxidante, antiinflamatorio y antidiabético de este extracto, donde se identificaron fenoles, lignanos, taninos y flavonoides. El objetivo de este trabajo fue optimizar el método extractivo de las raíces de A. lappa. Los extractos se prepararon por diferentes métodos: Ultrasonido, Soxhlet, maceración y turboextracción. La optimización se realizó mediante turboextracción siguiendo una planificación factorial de 23, empleando como factores: tenor alcohólico, concentración de materia prima y tiempo de extracción. Se evaluaron los extractos para determinar el residuo seco, el contenido de fenoles y flavonoides y la actividad antioxidante. En cuanto al contenido de residuo seco, fenoles y flavonoides, los métodos de extracción por ultrasonidos y turbo demostraron un mejor poder de extracción. Debido al menor tiempo y coste operativo, la optimización se realizó mediante turboextracción, y el extracto optimizado se obtuvo utilizando alcohol 60%, en proporción disolvente-materia 1:10 y tiempo de extracción de 15 minutos. Estos análisis podrán orientar futuros ensayos de transposición del método para escala industrial, reduciendo mano de obra, tiempo y costes, con el objetivo de obtener productos fitoterapéuticos más eficientes, con valor accesible para la población.

Protocol-optimizing study of combining Tuina and horse-riding squat exercise for knee osteoarthritis / 针灸推拿医学（英文版）

Objective: To evaluate the efficacy of Tuina (Chinese therapeutic massage) manipulation plus horse-riding squat exercise in treating knee osteoarthritis (KOA) and optimize the combining protocol. Methods: Based on a 2×2 factorial design, 120 eligible KOA patients were randomized into a manipulation group (group A1B2), a manipulation plus horse-riding squat group (group A1B1), a sitting knee-adjustment group (group A2B2 group), and a sitting knee-adjustment plus horse-riding squat group (group A2B1), with 30 cases in each group. The intervention was conducted three times a week, lasting for four weeks. The Western Ontario and McMaster Universities osteoarthritis index (WOMAC) was taken as the major measure for efficacy evaluation (including three component scores, pain, stiffness, and daily function, and total score). Results: The three component scores (pain, stiffness, and daily function) and the total score of WOMAC showed significant differences after the intervention in the four groups (P<0.05). There were significant inter-group differences in the WOMAC stiffness score amongst the four groups after the intervention (P<0.05). In group A1B1, the step length, stride, walking speed, and knee joint flexion angle changed significantly after treatment (P<0.05). After the intervention, the step length changed significantly in group A1B2 (P<0.05), and the walking speed changed significantly in group A2B1 (P<0.05). There were no significant differences in the step length, stride, walking speed, or knee joint flexion angle among the four groups (P>0.05). The extensor peak torque at 180 °/s changed significantly in group A1B2 after treatment (P<0.05). Neither the intra-group nor the inter-group comparisons of the four groups revealed significant differences in the other isokinetic muscle strength parameters (P>0.05). The main effect of manipulation showed significant in affecting the WOMAC pain and total scores (P<0.05). The main effect of horse-riding squat exercise showed significant in affecting the WOMAC pain and stiffness scores (P<0.05). Conclusion: The four treatment protocols all can improve the symptoms of KOA, for instance, relieving pain and stiffness, and enhancing daily function. Group A2B1 produces the most eminent effect in relieving joint stiffness. The main effects of both manipulation and horse-riding squat exercise are significant in reducing pain. Besides, the main effect of horse-riding squat exercise is significant in relieving joint stiffness.

Combined effects of fluoride exposure and low nutrition on osteogenesis and osteoclastic differentiation in rats / 中华地方病学杂志

Objective:To investigate the combined effect of fluoride exposure and low nutrition on osteogenesis and osteoclastic differentiation in rats.Methods:SD rats were divided into four groups by the method of random number table, namely normal nutrition group, low nutrition treatment group, fluoride exposure group and co-treatment of fluoride and low nutrition group according to 2 × 2 factorial experimental design, 8 rats in each group, half male and half female. Five months after the experiment, immunohistochemistry was used to test the expression levels of femoral alkaline phosphatase (ALP), runt-related transcription factor 2 (Runx2), osteoprotegerin (OPG) and receptor activator of nuclear factor kappa B ligand (RANKL). Analysis of variance of factorial design was used to determine the interaction between fluoride exposure and low nutrition on osteogenesis and osteoclastic differentiation.Results:The immunohistochemical results of bone tissue showed that there were significant differences in the expression levels of osteogenesis differentiation markers ALP and Runx2 between different groups ( F = 25.98, 17.77, P < 0.001). Compared with normal nutrition group (0.005 2 ± 0.002 7, 0.003 1 ± 0.001 4), the expression levels of ALP and Runx2 in fluoride exposure group were higher (0.019 5 ± 0.005 0, 0.014 4 ± 0.004 4, P < 0.05). There was no significant difference between low nutrition treatment group (0.002 6 ± 0.001 8, 0.004 4 ± 0.003 2) and co-treatment of fluoride and low nutrition group (0.003 6 ± 0.000 7, 0.002 9 ± 0.000 8, P > 0.05). The expression levels of ALP and Runx2 in co-treatment of fluoride and low nutrition group were lower than those of fluoride exposure group ( P < 0.05). There were significant differences in the expression level osteoclastic differentiation marker of RANKL and the ratio of RANKL/OPG ( F = 10.50, 31.05, P < 0.001). Among them, the RANKL/OPG ratio (0.115 3 ± 0.039 5) in fluoride exposure group was lower than that in normal nutrition group (1.426 3 ± 0.777 2), and the RANKL expression level and RANKL/OPG ratio (0.019 5 ± 0.007 7, 7.258 7 ± 3.674 3) in co-treatment of fluoride and low nutrition group were higher than those in normal nutrition group (0.004 4 ± 0.002 5, 1.426 3 ± 0.777 2, P < 0.05). However, there was no significant difference in the RANKL expression level and RANKL/OPG ratio (0.004 0 ± 0.001 9, 2.022 3 ± 0.753 7) in low nutrition treatment group ( P > 0.05). The expression level of RANKL and the ratio of RANKL/OPG in the co-treatment of fluoride and low nutrition group were higher than those in low nutrition treatment group and fluoride exposure group ( P < 0.05). The 2 × 2 analysis of variance of factorial design showed that fluoride exposure and low nutrition had interaction on ALP, Runx2, RANKL expression levels and RANKL/OPG ratio ( F = 4.38, 19.39, 22.12, 108.00, P < 0.05), antagonistic effect on ALP and Runx2 expression, synergistic effect on RANKL expression and RANKL/OPG ratio. Conclusions:In rat bone tissue, fluoride exposure promotes osteogenesis differentiation, inhibits osteoclastic differentiation dominated by active osteogenic function. The interaction between fluoride and low nutrition on osteogenesis and osteoclastic differentiation is antagonistic osteogenesis differentiation and synergistic promotion of osteoclastic differentiation. Normal nutrition conditions are material basis of osteogenesis differentiation, and low nutrition is the inducement of enhanced osteoclastic differentiation.

How to use analysis of variance correctly——an analysis of variance for the univariate quantitative data collected from the fractional factorial design / 四川精神卫生

The purpose of this paper was to introduce the fractional factorial design and its quantitative data analysis of variance and the SAS implementation. The fractional factorial designs were very similar to the factorial designs and the orthogonal designs， but they had some differences. The fractional factorial design required significantly fewer combinations of levels than the factorial design of the same size， and even saved sample size than the orthogonal design of the same size. In general， the precision of the results obtained by a fractional factorial design was lower than an orthogonal design and much lower than a factorial design. The fractional factorial design was suitable for the trial tests with many experimental factors， and its main purpose was to explore experimental factors that had a greater impact on the quantitative experimental results. When performing ANOVA and regression analysis on quantitative data with a fractional factorial design， it should be clear which factors or interactions had confounded effects.

How to use analysis of variance correctly——an analysis of variance for the univariate quantitative data collected from the factorial design / 四川精神卫生

The purpose of this paper was to introduce the factorial design and its quantitative data analysis of variance and the SAS implementation. Factorial design could not only present the main effect magnitude of all experimental factors， but also comprehensively reflected the size of each-order interaction effect among multiple factors. However， this design required a large sample size. This paper introduced the calculation formulas of the analysis of variance for quantitative data with two-factor factorial design， and realized the analysis of variance for quantitative data with two-factor and three-factor factorial design through two examples with the help of SAS software， and multiple comparisons of interaction effects were also performed.

Desirability Function in analytical method development for determination of glitazones and metabolites employing HF-LPME

Abstract Thiazolidinedione, often shortened to TZD or glitazone, helps lower insulin resistance, which is the underlying problem for many people with type 2 diabetes. The two most known glitazones are pioglitazone (PGZ), with the brand name medicine Actos®, and rosiglitazone (RSG), which is Avandia®. This study presented a multivariate optimization in the microextraction procedure employing Fractional Factorial Design (FFD) combined with Desirability Function (DF) to determine TZD and metabolites in biological samples. Microextraction requires several parameters to be optimized; however, most of them still use univariate optimization. Finding optimum conditions by simple response is relatively simple, but the problems, in case of microextractions, are often more complex when it has more responses. For example, changing one factor that promotes one response may suppress the effect of the others. Thus, this multivariate optimization was applied for two bioanalytical methods for determination of TZD and metabolites, one by HPLC and other by CE, both using Hollow Fiber Liquid-Phase Microextraction (HF-LPME). The results establish the optimal values and elucidate how the factors that affect HF-LPME procedure perform in extraction efficiency for TZDs. Additionally, this study demonstrates that DF can be an important tool to optimize microextraction procedures.

Optimization and Quest of HPMC loaded Stavudine Controlled Release Dosage Development by Central Composite Design utilizing Reduced Factorial Screening Technique

Abstract The current research focused on screening and finding the significant independent variables in stavudine loaded tablet, followed by optimizing the best formulation using central composite design. The objective of the study to develop stavudine loaded controlled release tablet utilizing reduced factorial design, followed by optimization technique as well as characterization of prepared tablets. Preliminary trial batches were prepared using different grades of hydroxypropyl methylcellulose. The resolution-IV reduced factorial design was selected to screen the significant independent variables in the dosage form design. A total number of eight runs were prepared and responses were recorded. The signified factors identified by half-normal and Pareto chart. The prepared tablets are evaluated for various physiochemical characterizations. Three dependent responses such as hardness, dissolution at 6 hour and 12 hours are considered in optimization process. Later on, drug-polymer interaction study was carried out. The principal of the study design based on finding the best formulation with prefixed set parameter values utilizing the concept of screening technique. It observed that HPMC K15M (57.18 %), HPMC K100 (66.32 %) and PVP K30 (7.97 %) as best composition in a formulation batch would fulfill the predetermined parameter with specific values.

Optimization of Diltiazem hydrochloride osmotic formulation using QBD approach

Abstract Diltiazem hydrochloride (DLH) is a calcium channel blocker useful for the treatment of angina pectoris, arrhythmia, and hypertension. DLH having a short half-life needs frequent administration for successful treatment but this poses a problem of poor patient compliance. These requirements are served by elementary osmotic pump tablets (EOP) based controlled-release (CR) systems. Quality by design (QbD) approach assists in screening various factors with subsequent assessment of critical parameters that can have a major impact on the scalability of EOP. Tablets were formulated using wet granulation method followed by osmotic coating. Factorial design based QbD strategy aided in defining the risk assessment of influential variables such as hydrophilic polymers and osmotic coat component on the in-vitro release kinetics of the designed EOP tablets. These formulated EOP systems followed zero-order kinetics, a characteristic feature of EOPs. EOP tablets were formulated applying a systematic QbD statistical approach. The formulated DLH EOP systems with improved concentration-independent behavior helped to address the challenges of IR formulation. Application of QbD strategy in ascertaining the scalability of DLH EOP formulation would help pharmaceutical industries in the translation of EOP based drug delivery systems from R&D to market.

The implementation of variance analysis and analysis of interactive effect in multi-factor research design / 中国职业医学

Multi-factor research design is widely applied in scientific research. It can simultaneously explore the effects of multiple factors on outcome indicators. The consideration of the interactive effects of different factors is a critical issue when analyzing this type of data. The analytic strategy for main effects or simple effects depends on the significance of the interactive effect. However, many researchers tend to skip the analysis on interactive effects, or wrongly select statistical analysis method because of ignoring the test result. In this study, SPSS 20.0 and R 3.6.1 statistical software were used to simulate and illustrate how to analyze data from two most popular multi-factor design data——factorial design and repeated measurement design. The significance of evaluating interactive effect and corresponding key point analysis was explained. The possible consequences of ignoring the statistical significance of interactive effects were indicated, that include leading to low inspection efficiency, prone to draw wrong conclusions, loss of valuable information in the original data, or loss of practical significance of the analytic results. It is suggested that in the analysis of research data, we should first judge whether there are interactive effects, and then correctly choose main effect analysis or single effect analysis to avoid one-sided and wrong conclusions.

Extracción e identificación de lípidos polares de las microalgas Nannochloropsis oceanica y Desmodesmus asymmetricus / Extraction and identification of polar lipids from microalgae Nannochloropsis oceanica and Desmodesmus asymmetricus / Extração e identificação os lipídios polares das microalgas Nannochloropsis ocean ca e Desmodesmus asymmetricus

Resumen Los lípidos polares de las microalgas sor de gran interés debido a su aplicación como ingredientes naturales novedosos para las industrias cosmética, nutricional y farmacéutica. Por ello, el presente trabajo buscó determinar el efecto de los principales factores en la extracción e identificación de los lípidos polares de las microalgas Nannochloropsis oceanica y Desmodesmus asymmetricus, mediante el diseño de superficie de respuesta de Box-Behnken y el diseño factorial completo, respectivamente. Estas cepas del Banco de Germoplasma de Organismos Acuáticos (BGOA - IMARPE) fueron cultivadas en un invernadero, en biorreactores de 30 litros, centrifugadas y liofilizadas. Los lípidos fueron extraídos con cloroformo-metanol, fraccionados y analizados con un espectrómetro de masas Waters Xevo G2-XS QTOF. La maximización de la extracción de los lípidos totales determinó un valor óptimo de la relación masa-solvente de 25mg/3 mL, una proporción 1:1 de cloroformo-metanol, aproximadamente, y un tiempo del baño de ultrasonido entre 10 y 30 min. Los principales lípidos polares identificados para N. oceanica fueron lisofosfatidilcolina (LPC), diacilgliceril-N,N,N-trimetilhomoserina (DGTS), digalactosil diacilglicerol (DGDG) y monogalactosil diacilglicerol (MGDG) y para D. asymmetricus fueron sulfoquinovosil diacilglicerol (SQDG), LDGTS, DGTS, DGDG y MGDG.

Abstract The microalgae polar lipids are of great interest due to their application as novel natural ingredients for the cosmetic, nutritional, and pharmaceutical industry. For this reason, the present work sought to determine the effect of the main factors in the extraction and identification of polar lipids from the microalgae Nannochloropsis oceanica and Desmodesmus asymmetricus, using Box-Behnken response surface methodology design and full factorial design, respectively. These strains from the Germplasm Bank of Aquatic Organisms (BGOA - IMARPE) were grown in a greenhouse, in 30 L bioreactors, centrifuged and lyophilized. The lipids were extracted with chloroform-methanol, fractionated and analyzed with the Waters Xevo G2-XS QTOF mass spectrometer. The maximization of total lipid extraction determined an optimal value of the mass-solvent ratio of 25 mg / 3 mL, an approximate ratio of chloroform-methanol 1:1 and an ultrasound bath time between 10 and 30 min. The main polar lipids identified for the N. oceanica microalgae were lysophophatidylcholine (LPC), diacylglyceryl-N,N,N-trimethylhomoserine (DGTS), digalactosyldiacylglycerol (DGDG), and monogalactosyldiacylglycerol (MGDG) and for D. asymmetricus were sulfoquinovosyl diacylglycerol (SQDG), LDGTS, DGTS, DGDG, and MGDG.

Resumo Os lipídios polares das microalgas possuem grande interesse em sua aplicação como novos ingredientes naturais na indústria cosmética, nutricional e farmacêutica. A presente pesquisa procura determinar o efeito dos principais fatores na extração e identificação dos lipídios polares das microalgas Nannochloropsis oceanica e Desmodesmus asymmetricus, por meio do um experimento de Box-Behnken e um experimento fatorial completo, respectivamente. As cepas do Banco do Germoplasma do Organismos Aquáticos (BGOA - IMARPE), foram cultivadas em casa de vegetação, em biorreatores do 30 L, centrifugadas e liofilizadas. Os lipídios foram extraídos com clorofórmio-metanol, fracionados e analisados com o espectrómetro do massa Waters Xevo G2-XS QTOF. A maximização da extração lipídica determinou um valor ótimo da razão massa-solvente de 25 mg / 3 mL, uma proporção aproximadamente clorofórmio-metanol de 1:1 e no tempo do banho de ultrassom entre 10 e 30 minutos. Os principais lipídios polares identificados para das microalgas N. oceanica foram lisofosfatidilcolina (LPC), diacilgliceril-N,N,N-trimetil-homoserina (DGTS), digalactosil diacilglicerol (DGDG) e monogalactosil diacilglicerol (MGDG), e para D. asymmetricus foram sulfoquinovosil diacilglicerol (SQDG), LDGTS, DGTS, DGDG e MGDG.

The Design And Development Of Carvedilol Gastroretentive Floating Drug Delivery Systems Using Hydrophilic Polymers And In Vitro Characterization

Objective: The primary aim of the present examination was to create carvedilol phosphate floating tablets using factorial designs and for retention in the upper portion of the gastrointestinal (GI) tract to sustain the dissolution where the solubility of carvedilol phosphate is more in an acidic medium. Methods: The floating tablets of carvedilol phosphate were ready to employ different concentrations and a combination of these polymers of Na-alginate, Carbopol 934P, and sodium carboxymethyl cellulose (NaCMC) with lubricants magnesium stearate by direct compression technique. In the present experiment, involved sodium bicarbonate and citric acid as a gas-producing agent. Fifteen formulations structured and judged for pre-compression components like the angle of repose, bulk and tapped density, Hausner’s ratio, compressibility index, and post-compression factors are weight uniformity, hardness, drug content, friability, in vitro buoyancy, dissolution studies, and Fourier transforms infrared spectroscopy (FTIR). Results: The drug released 90.02% in 12 h by combining NaCMC (7.5 mg) and Na-alginate (7.5 mg) in the formulation F14 towards the achievement of sustained release. Batch F14 selected as optimized, as provided desired zero-order release profile as well as floating lag time 20 s and total floating time>12 h, and the mechanism of drug release observed (n = 1.098, super case-II transport). Conclusion: From the results fulfilled that all the preparation found to be within the pharmacopeia limits and was the best dosage form to treat moderate heart failure and hypertension. The in vitro dissolution profiles of all formulations placed into various kinetic models, the statistical parameters like slope, regression coefficient and intercept determined. The gastro-retentive dosage form to maintain the sustain drug delivery, which would improve the maximum therapeutic efficacy and patient compliance.

Estimulación de las funciones ejecutivas y su influencia en el rendimiento académico en escolares de primero básico / Stimulation of the executive functions and their influence on academic performance of students of first grade of elementary school

Resumen El estudio de la estimulación de las funciones ejecutivas (FE) en la infancia ha generado un creciente interés investigativo en la última década, especialmente por su relación con el desempeño académico y éxito escolar. De acuerdo a esto, el presente estudio tiene por objetivo estudiar el efecto de un programa de estimulación de las FE sobre el desempeño ejecutivo y el rendimiento académico de una muestra de 43 estudiantes de primero básico de la comuna de Valparaíso (Chile), de edades entre 6 y 7 años. Para ello, se implementó un diseño factorial mixto. La intervención duró 12 semanas y se llevó a cabo en el aula, dirigida por un educador diferencial y con el apoyo de la profesora del curso. Los resultados evidencian la existencia de un efecto significativo del programa implementado en la mejora del desempeño ejecutivo de los participantes, particularmente del grupo experimental. Tales efectos no fueron replicados en el rendimiento académico, lo que podría encontrar una posible explicación en los factores contextuales relacionados con las condiciones de precariedad de la institución educativa. Se observó además un efecto diferenciado del programa sobre el componente de control inhibitorio. Los hallazgos generales ponen de manifiesto la relevancia de la estimulación de las FE en la infancia temprana y los beneficios que esto puede reportar en contextos educativos. Además, sugiere el potencial aporte de la incorporación de este tipo de intervenciones en las prácticas docentes cotidianas.

Prednisolone encapsulated PLGA nanoparticles: Characterization, cytotoxicity, and anti-inflammatory activity on C6 glial cells

Prednisolone, a popular glucocorticoid (GC) known for its ability to inhibit cytokine release, is also employedextensively in cancer therapy. GCs have been used to treat brain tumors to reduce tumor-associated edema. They areknown to exhibit different effects on different cell lines and in some cases are known to be neurotoxic. In this study,we have investigated and compared the cytotoxic and anti-inflammatory effects of prednisolone and prednisoloneencapsulated Poly Lactic-co-Glycolic acid (PLGA) nanoparticles (NPs) on C6 cells that are cancerous but are knownfor their similarity to astrocyte cells. Design expert software was used to analyze the effect of different variablesfor NP formulation. By varying different parameters, NPs were synthesized and characterized using particle sizeanalyzer and zeta potential. The surface morphology of the NPs was analyzed using scanning electron microscopy.Lipopolysaccharide activated C6 glial cells witnessed significantly lower cell proliferation in the presence of the drugduring the 48 hours of incubation and the prednisolone encapsulated NPs were able to attenuate pro-inflammatorycytokines like Tumor necrosis factor alpha (TNF-α) and nitric oxide substantially even after the 72 hours of incubationwhen compared with the free drug. The results suggested that prednisolone was more effective as an anti-inflammatorydrug in the PLGA nanoformulation

Venlafaxine Hydrochloride Controlled Release Bilayer Tablets: Optimization Of Formulation Variable By Using Dyspnea On Exertion

The current research work was to develop bilayer tablet of venlafaxine hydrochloride to increase drug efficacy for efficient treatment of depression. The satisfactory result of treatment can be achieved upon the maintenance of drug concentration within an effective level in the body, so a uniform and constant drug supply are desirable. An immediate layer of venlafaxine HCl was formulated using super disintegrants, i.e., croscarmellose sodium (CCS) and sodium starch glycolate (SSG); tablet compact by direct compression. HPMC K100M and ethylcellulose (EC) were utilized as release retarding polymers in sustained release layer by wet granulation technique with the help of PVP K30 in IPA solution (10%) as a granulating agent. Full 32 factorial designs were used to find out the optimum quantity of release retardant polymers. Bilayer tablet was evaluated for various parameters, i.e. hardness, friability, weight variation, % drug content, disintegration time (IR layer), and % drug release study. Statically, an analysis was carried out using factor X1 (HPMC K100M) and X2 (EC) for dependent variable % drug release at 8, 12, and 20 hours. A formulation was optimized and a formulation containing 305.36 mg of HPMC K100M and 54.03 mg of ethyl cellulose. Optimized formulation show 47.12 ± 2.1, 59.89 ± 2.2, and 89.06 ± 2.3 drug release at 8, 12, and 20 hours, respectively, which is almost similar to theoretical dose calculation with similarity factor f2 97, 99, and 98%, respectively. Bilayer tablet formulation was observed to be stable and fulfilled all compendia specifications.

Electrohydrodynamic atomization, a promising avenue for fast-dissolving drug delivery system: Lessons from tadalafil-loaded composite nanofibers

The utilization of electrospinning in drug delivery has thrived in recent years, with the ability to incorporate drugsand enhance dissolution; this technique is employed to improve the dissolution of poorly water-soluble selectivephosphodiesterase-5 inhibitor, tadalafil. The strategy involved direct electrospinning of tadalafil/polyvinylpyrrolidoneand polyethylene oxide (PEO) solution. The optimization process included a 32 full factorial design based on theinfluence of polymers concentration as independent variables on the electrospun yield, loading efficiency, nanofibersdiameter, number of beads, and in vitro release. Optimization studies revealed the negative influence of bothpolymers on the electrospun yield, while the loading efficiency and in vitro dissolution rate were reduced by the PEOconcentration solely. The higher polymer concentrations were favorable for the declination of beads number, and adriving factor for fiber diameter reduction. Further physicochemical characterization of the optimized formulationrevealed the presence of the drug in an amorphous state or molecular dispersion within the polymer matrix. In vitrodissolution studies revealed about 81.5% ± 8.34% release in less than 2 minutes compared to a negligible dissolutionof free drug. From the derived outcomes, the electrohydrodynamic spun tadalafil-loaded nanofibers pave the way fordissolution enhancement for insoluble low bioavailability class II drugs.

Anti-Parkinson mechanism of Foshou Powder based on factorial design / 中草药

Objective: To explore the effects and potential mechanism of Foshou Powder on Parkinson’s disease. Methods: Reserpine was injected in KM mice to establish Parkinson’s disease model, and hypothermia and akinesia were measured to evaluate the effects of volatile oil of Angelica sinensis, Ligusticum chuanxiong and combination. The human monoamine oxidase (hMAO) activity and inhibition mode were measured by fluorescence spectrophotometry in vitro with kynuramine as the common substrate of human monoamine oxidase A (hMAO-A) and human monoamine oxidase B (hMAO-B). On this basis, the 2 × 4 factorial design was applied to research the interaction between Angelica sinensis volatile oil and Ligusticum chuanxiong volatile oil. Results: The antagonistic experiments of reserpine showed that the application of Angelica sinensis volatile oil and Ligusticum chuanxiong volatile oil significantly improved hypothermia and akinesia. Enzyme activity test revealed that volatile oil of Angelica sinensis and Ligusticum chuanxiong had competitive inhibitory effects on hMAO-A and hMAO-B, and the combination of the two substances had significant synergistic effect on the activity of both hMAO. Conclusion: Angelica sinensis and Ligusticum chuanxiong in Foshou Powder have significant synergistic effects in the prevention and treatment of Parkinson’s disease, which may be related to the inhibition of MAO activity.

Experimental design approach for development of novel microemulsion system and immediate release self microemulsifying tablet of nebivolol HCl

The objective of this study was to determine specific combination of pharmaceutical excipients that lead to formulation of efficient nebivolol hydrochloride SMEDDS and its subsequent formulation into IR-SET (Immediate release- Self emulsifying tablet) which will enhance its solubility and dissolution. Solubility and Pseudo-ternary phase studies were carried out to identify the excipients showing highest solubility and to identify the zone of microemulsion with selected ingredients. Liquid-SMEDDS (L-SMEDDS) were optimized for Concentration of oil(X1) and Smix(X2) and formulated using a combination of Kollisolv GTA as oil, Tween 80 as surfactant and propylene glycol as co-surfactant which gave smaller droplet size(Y1) 55.98nm , Emulsification time (Y2) 16±1.5 s,% transmittance (Y3) 99.94±0.47%. Neusilin US2 was used as solid carrier for solidification of L-SMEDDS in to Solid-SMEDDS (S-SMEDDS) by adsorption technique. IR-SET of nebivolol were formulated with S-SMEDDS and optimized for the concentration of binder (X1) (PVP K30) and superdisintegrant (X2) (KOLLIDON CL) which showed low Disintegration time (Y1) (92±0.5s) and low Friability(Y2)(0.424±0.03%). Also the DSC and XRD data revealed the molecular state of the drug in S-SMEDDS. The extent of in-vivo drug release and ex-vivo diffusion values from L-SMEDDS and IR-SET was much higher than pure drug and marketed tablet. In conclusion, the results showed potential of SMEDDS to improve solubility and thus the bioavailability.

Design, preparation and in vitro characterizations of fluconazole loaded nanostructured lipid carriers

Present study was aimed to prepare and characterize fluconazole loaded nanostructured lipid carriers (FLZ-NLCs) for the treatment of fungal infections. Fungal infections are tremendously widespread and are the often faced dermatological condition worldwide. FLZ-NLCs was prepared by ultrasonication emulsion technique using stearic acid (SA) as solid lipid, castor oil as liquid lipid and tween 20 as a surfactant. The mean diameter of optimized FLZ-NLCs were found to be 359.15 ± 9.83 nm. The drug content and entrapment efficiency of NLCs was found to be 102.97 ± 7.45% and 87 ± 0.59%, respectively. In vitro drug release studies of FLZ-NLCs showed 37.34 ± 2.08% drug release over a period of 72 h. The above studies confirmed the prepared FLZ-NLCs may be useful for the treatment of fungal infections.

Aplicación de un diseño factorial 23 en la extracción asistida por microondas y evaluación de la actividad antioxidante de los compuestos presentes en frutos de Vaeeinium meridionale / Application of a 23 factorial design in the assisted extraction by microwave and evaluation of the antioxidant activity of the compounds present in Vaccinium meridionale fruits

RESUMEN El arándano (Vaeeinium meridonale) forma parte de la familia Ericaceae; es un fruto rico en compuestos polifenólicos como antocianinas y flavonoides con propiedades antioxidantes, compuestos que presentan algunas características para la inhibición de radicales libres. Se empleó un diseño factorial 23 para investigar los efectos de las variables temperatura, tiempo y el porcentaje de etanol en la extracción asistida por microondas (MAE) de los antioxidantes presentes en frutos de arándanos, como técnica alternativa, con la cual se pretende una economía destacable en cuanto al empleo de disolventes, tiempo y energía, en comparación con los procesos de extracción convencionales. Las extracciones se realizaron bajo las siguientes condiciones: temperatura (343,15 -383,15 K), tiempo (5-15 minutos), %EtOH (0-80%). Se planteó un diseño factorial, con un total de 8 experimentos para determinar la influencia de la relación de las variables en el proceso de extracción de compuestos con actividad antioxidante por el método de DPPH-, obteniendo un modelo factorial de primer orden con interacciones, bajo un nivel de confianza del 100% y R2=1. El diseño experimental y la evaluación de los resultados se realizó con el software R Studio® versión libre.

SUMMARY Blueberry (Vaccinium meridionale) forms part of the family Ericaceae; it is a fruit rich in flavonoids and anthocyanins (polyphenols), which have antioxidant properties and also shows some properties suitable for inhibition of free radicals. A 23 factorial design was performed to investigate the variables effects: temperature, time and the ethanol percentage %, on the antioxidants extraction process by Microwave Assisted Extraction (MAE). The extraction conditions were: temp (343.15-383.15 K), time (5-15 min), ethanol (0- 80%). A factorial design was performed, with a total of 8 experiments, allowing to determine the influence of the relation of the variables related to the extraction process of compounds with antioxidant activity by DPPH- method, getting a first order factorial model with interactions and a 100% reliability level and a R2 =1. The experimental design and evaluation of the results were performed with the software R Studio® free version.