Search

Vernonia amygdalina Del. is a perennial tropical shrub from Asteraceae. The fresh leaf of V. amygdalina is consumed as a vegetable due to its medicinal and nutritional properties. The present study focused on the quantification of bioactive compounds, luteolin-7-O-glucoside, luteolin-7-O-glucuronide, and 1,5-O-dicaffeoylquinic acid from aqueous leaf extract of V. amygdalina. The study also aims to investigate the effects of the aqueous leaf extract of V. amygdalina on cytochrome P450 2C9 (CYP2C9), and cytochrome P450 3A4 (CYP3A4) in hepatic cells of control and diabetic rats. The quantification of the bioactive compounds was conducted using ultra-high-performance liquid chromatography multiple reactions monitoring tandem mass spectrometry (UHPLC-MS/MS-MRM) technique. The effect of the extract on CYP2C9 and CYP3A4 activities was determined using a fluorometric screening kit according to the manufacturer's instructions. The three bioactive compounds were detected and quantified in the aqueous leaf extract. Results showed that the content of luteolin-7-O-glucuronide (47 μg/mg) was the highest followed by luteolin-7-O-glucoside (3.5 μg/mg) and 1,5-O-dicaffeoylquinic acid (1.07 μg/mg). The extract showed an inhibitory effect on CYP3A4 and CYP2C9 enzyme activities in control and diabetic rats. The UHPLC-MS/MS-MRM method is sensitive and reliable for the quality control of V. amygdalina leaf extract. The inhibitory effect of the extract suggests that concomitant use of V. amygdalina leaf preparations with conventional drugs metabolized and eliminated from the body by CYP3A4 and CYP2C9 enzymes may lead to possible interaction. [ABSTRACT FROM AUTHOR]

With approximately 18 million people affected by cancer in 2020 globally, scientists are exploring innovative approaches to develop effective treatments for various types of cancer. Traditional chemotherapy drugs, although effective against cancer cells, often lead to significant side effects on healthy tissues, such as hair loss, anemia, and nausea. To discover safer alternatives, researchers are investigating natural bioactive compounds found abundantly in plants. Luteolin, a flavonoid found in celery and artichokes, stands out due to its diverse anti-carcinogenic properties, including inhibiting proliferation, inducing apoptosis, activating autophagy, and inhibiting angiogenesis and metastasis. However, the therapeutic potential of luteolin is hindered by challenges related to its bioavailability and solubility. This critical review explores the specific anti-carcinogenic properties of luteolin while analyzing the impact of its limited bioavailability and solubility on effectiveness. Additionally, it investigates the outcomes of encapsulating luteolin in nanoformulations, providing insights into potential strategies for enhancing its anti-carcinogenic effects. Finally, the review compares the efficacy of luteolin with and without nanoformulations. This review provides valuable insights into the potential of utilizing luteolin-loaded nanoformulations as a safer and more effective method for treating cancer, contributing to the ongoing efforts in improving cancer care and outcomes worldwide. [ABSTRACT FROM AUTHOR]

Background: Quetiapine fumarate (QTP) is commonly prescribed for schizophrenic patient, typically available in tablet or oral suspension form, presenting challenges such as administration difficulties, fear of choking and distaste for its bitter taste. Fast melt films (FMF) offer an alternative dosage form with a simple development process, ease of administration and rapid drug absorption and action onset. Objective: This study aims to prepare FMF with different formulations using solvent casting methods and to compare the effects of different drying methods, including oven drying and freeze drying, on the properties of the films. Methods: Various formulations were created by manipulating polymer types (starch, hydroxypropyl methylcellulose (HPMC) and guar gum) at different concentrations, along with fixed concentrations of QTP and other excipients. Characterization tests including surface morphology, weight, thickness, pH, tensile strength, elongation length, Young's modulus, folding endurance and disintegration time were conducted. The optimal FMF formulation was identified and further evaluated for moisture and drug content, dissolution behavior, accelerated stability, X-ray diffraction (XRD), and palatability. Results: FMF containing 10 mg guar gum/film developed using oven drying emerged as the optimum choice, exhibiting desirable film appearance, ultra-thin thickness (0.453 ± 0.002 mm), appropriate pH for oral intake (pH 5.0), optimal moisture content of 11.810%, rapid disintegration (52.67 ± 1.53 s), high flexibility (folding endurance > 300 times) and lower Young's modulus (1.308 ± 0.214). Conclusion: Oven drying method has been proven to be favorable for developing FMF containing QTP, meeting all testing criteria and providing an alternative option for QTP prescription. [ABSTRACT FROM AUTHOR]

Cassia alata, a traditional herb with a global presence, is renowned for its anti-inflammatory, antibacterial, and antifungal properties, making it a go-to remedy for skin ailments. While it has demonstrated wound healing capabilities in both in vitro and in vivo studies, the precise mechanisms remain elusive. This review aims to highlight its key phytochemicals, their effects, and the mechanism of action. The compounds that have been reviewed and discussed include kaempferol, apigenin, quercetin, rhein, and rutin. These polyphenols play important roles in normal and impaired wound healing processes, encompassing hemostasis, inflammation, proliferation, and tissue remodeling. [ABSTRACT FROM AUTHOR]

Objective: To investigate the interrelationship between cardiovascular health awareness, risk perception, behavioural intention, and INTERHEART risk stratification in a middle-aged adult population in Malaysia. Methods: A cross-sectional survey with convenience sampling was conducted during November 2022 and January 2023. Participants completed validated questionnaires assessing cardiovascular health awareness, risk perception of cardiovascular diseases, behavioural intention towards adopting healthy habits, and INTERHEART risk stratification score (IHRS) based on established risk factors. A total of 602 respondents were included in the final analysis. Data were analysed with independent t-test/one-way ANOVA or Mann- Whitney/Kruskai-Wailis to test the differences, Pearson correlation or linear regression test to analyze the association of independent and dependent variables. Results: There was a significant positive correlation between medical knowledge related to cardiovascular disease (CVD) and knowledge related to CVD risk prevention, risk perception, behavioural intention and IHRS (P<0.05, Pearson correlation). Notably, individuals with higher IHRS tended to have lower knowledge related to CVD and CVD risk prevention, risk perception, and behavioural intention. Males, laborers, active/former smokers, individuals with lower household income and educational levels, those involved in occupations not related to the healthcare sector, and those who did not receive the CVD health brochure or are unaware of health self-assessment tools are likely to have lower levels of knowledge, risk perception, and poorer behavioural intention regarding cardiovascular health (P<0.05, one-way ANOVA). While educational level, smoking status, awareness about CVD poster, self-assessment tools were repeatedly significantly associated with knowledge related to CVD and CVD risk prevention, risk perception, behavioral intention and/or IHRS (P<0.05, linear regression). Conclusions: These findings underscore the importance of promoting cardiovascular health awareness and risk perception among middle-aged adults to foster positive BI and reduce CVD risk. Tailored interventions targeting specific risk factors identified by INTERHEART may enhance risk stratification accuracy and facilitate targeted preventive strategies. [ABSTRACT FROM AUTHOR]

Orally disintegrating tablets (ODTs) are designed to dissolve in the oral cavity within 3 min, providing a convenient option for patients as they can be taken without water. Direct compression is the most common method used for ODTs formulations. However, the availability of single composite excipients with desirable characteristics such as good compressibility, fast disintegration, and a good mouthfeel suitable for direct compression is limited. This research was proposed to develop a co-processed excipient composed of xylitol, mannitol, and microcrystalline cellulose for the formulation of ODTs. A total of 11 formulations of co-processed excipients with different ratios of ingredients were prepared, which were then compressed into ODTs, and their characteristics were thoroughly examined. The primary focus was on evaluating the disintegration time and hardness of the tablets, as these factors are important in ensuring the ODTs meet the desired criteria. The model drug, Mirtazapine was then incorporated into the chosen optimized formulation. The results showed that the formulation comprised of 10% xylitol, 10% mannitol and 80% microcrystalline cellulose demonstrated the fastest disintegration time (1.77 ± 0.119 min) and sufficient hardness (3.521 ± 0.143 kg) compared to the other formulations. Furthermore, the drug was uniformly distributed within the tablets and fully released within 15 min. Therefore, the developed co-processed excipients show great potential in enhancing the functionalities of ODTs, offering a promising solution to improve the overall performance and usability of ODTs in various therapeutic applications. [ABSTRACT FROM AUTHOR]

Sea cucumber is a bioremediator as it can composite organic matter and excrete inorganic matter. Sea cucumber has the potential to serve as a bioindicator in marine habitat as they provide an integrated insight into the status of their environment over long periods. Sea cucumbers are sensitive to the organic concentration in the marine environment and can effectively provide an early warning system for any organic contamination that can negatively impact the ecosystem. The availability of a reference transcriptome for sea cucumber would constitute an essential tool for identifying genes involved in crucial steps of the defence pathway. De novo assembly of RNA-seq data enables researchers to study the transcriptomes without needing a genome sequence. In this study, sea cucumbers fed with Kappaphycus alvarezii powder were treated with 0.20 mg/L copper concentration comprehensive transcriptome data containing 75,149 Unigenes, with a total length of 20,460,032 bp. A total of 8820 genes were predicted from the unigenes, annotated, and functionally categorized into 25 functional groups with approximately 20% cluster in signal transduction mechanism. The reference transcriptome presented and validated in this study is meaningful for identifying a wide range of gene(s) related to the bioindication of sea cucumber in a high copper environment. [ABSTRACT FROM AUTHOR]

Simple Summary: Luteolin is a natural compound from plants with various medicinal benefits, including anti-cancer activities. However, luteolin has limited use clinically due to its low solubility and absorption into the body. Hence, the objective of this research work was to formulate and optimize a luteolin nanomicelle formulation with improved solubility. The nanomicelle was prepared using D-α-tocopheryl polyethylene glycol 100 succinate (TPGS) and poloxamer (Pol). The solubility of Lut-loaded micelles increased up to 459-fold compared to pure Lut in water. The release study showed that Lut-loaded micelles exhibited sustained release behavior. The effects of copolymers, hydration temperature and duration, and freezing temperature were studied to find out the optimum formulation of a luteolin–micelle complex. This study has demonstrated that several factors need to be considered when developing such nanoparticles in order to obtain a well-optimized micelle. The formulation has potential to be utilized in cancer therapy. Background: Luteolin is a flavonoid compound that has been widely studied for its various anti-cancer properties and sensitization to multidrug-resistant cells. However, the limited solubility and bioavailability of Lut hindered its potential clinical use. Theoretically, the combination of this compound with vitamin E TPGS and poloxamer 407 can produce a synergistic effect to enhance tumor apoptosis and P-glycoprotein inhibition. This study aimed to develop and optimize vitamin E TPGS/Poloxamer 407 micelles loaded with luteolin through investigating certain factors that can affect the encapsulation efficiency and particle size of the micelle. Methods: A micelle was prepared using the film hydration method, and the micellar solution was lyophilized. The cake formed was analyzed. The factors investigated include the concentrations of the surfactants, ratio of vitamin E TPGS/Poloxamer 407, temperature of the hydrating solution, duration of hydration, and freezing temperature before lyophilization. The effects of these factors on the encapsulation efficiency and particle size of the micelle were also studied. The encapsulation efficiency was measured using a UV-Vis spectrophotometer, while particle size was measured using dynamic light scattering. Results: The optimized micelle was found to have 90% encapsulation efficiency with a particle size of less than 40 nm, which was achieved using a 10% concentration of surfactants at a vitamin E TPGS/Poloxamer 407 ratio of 3:1. The optimized temperature for hydrating the micellar film was 40 °C, the optimized mixing time was 1 h, and the optimized freezing temperature was −80 °C. The solubility of the luteolin-loaded micelles increased 459-fold compared to pure Lut in water. The critical micelle concentration of the vitamin E TPGS/Poloxamer 407 micelle was 0.001 mg/mL, and the release study showed that luteolin-loaded micelles exhibited sustained release behavior. The release of luteolin from a micelle was found to be higher in pH 6.8 compared to pH 7.4, which signified that luteolin could be accumulated more in a tumor microenvironment compared to blood. Conclusion: This study demonstrated that several factors need to be considered when developing such nanoparticles in order to obtain a well-optimized micelle. [ABSTRACT FROM AUTHOR]

Atopic dermatitis (AD) is an inflamed skin condition with relapsing pruritus and cutaneous physiological dysfunction. This skin disorder is widespread around the world and frequently affects infants, children and adults. Natural products with bioactive lead compounds are the source of natural medicines for complementary and alternative therapy in managing AD. Cassia alata has been used traditionally as a remedy for a variety of health issues. In Asian countries, it is used as an ethnomedicine to treat skin conditions such pityriasis versicolor, ringworm, scabies, shingles, urticaria and itching. According to previously published studies, the phytochemicals in C. alata may have a wide range of significant pharmacological effects. AD management is highlighted here, as this review explores the literature on the pharmacological effects of C. alata and its phytochemical content. Specifically, antibacterial, wound healing, anti-inflammatory and antioxidant effects are reviewed and discussed in relation to AD management. [ABSTRACT FROM AUTHOR]

Flibanserin has been recently approved by the USFDA for treating female sexual interest disorder. It is currently not included in any of the Pharmacopoeias. No stability indicating method information about flibanserin has been reported in the literature. Flibanserin stock solution (1 mg/mL) was prepared and serially diluted (concentration ranged 1-20 µg/mL). Flibanserin solutions (1-20 µg/mL) were analysed using RP-HPLC under isocratic elution of mobile phase acetonitrile and ammonium acetate (60:40; V/V) at 1 mL/minute. This HPLC method was validated for linearity, accuracy, precision, robustness, limit of detection (LOD) and limit of quantification (LOQ), according to ICH guidelines. Results showed that the method developed has promising linearity (r2 = 0.9993), accuracy, precision (0.92-1.61%), robustness, LOD and LOQ. The developed HPLC method for evaluation of flibanserin was found reliable, precise, sensitive, accurate and repeatable for routine analysis and quality control of flibanserin. It is suitable to be used as stability indicating method in pharmaceutical analysis. [ABSTRACT FROM AUTHOR]

Background: Bauhinia kockiana originates from Peninsular Malaysia and it is grown as a garden ornamental plant. Our previous study reported that this plant exhibited fairly strong antioxidant and antimicrobial activities. This paper focused on the assessment of the antibacterial activity of B. kockiana towards methicillin-resistance Staphylococcus aureus (MRSA), to purify and to identify the antibacterial compounds, and to determine the mechanism of antibacterial activity. Methods: Antibacterial activity of B. kockiana flower was evaluated qualitatively and quantitatively using disc diffusion assay and microbroth dilution method. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of extracts were examined. Phytochemical analysis was performed to determine the classes of phytochemicals in the extracts. Bioactivity guided isolation was employed to purify the antibacterial agents and identified via various spectroscopy methods. Scanning electron microscopy (SEM) technique was used to evaluate the antibacterial mechanism of extract and compounds isolated. Results: B. kockiana flower was found to exhibit fairly strong antibacterial activity towards both strains of MRSA bacteria used, MIC varies from 62.5–250 μg/mL. Tannins and flavonoids have been detected in the phytochemical analysis. Gallic acid and its ester derivatives purified from ethyl acetate extract could inhibit MRSA at 250–500 μg/mL. SEM revealed that the cells have undergone plasmolysis upon treatment with the extract and compounds. Conclusion: Tannins and polyphenols are the antibacterial components towards MRSA in B. kockiana. Massive leakage of the cell content observed in treated cells showed that the phytochemicals have changed the properties of the cell membranes. Amphiphilic nature of the compounds exhibited the antibacterial activity towards MRSA via three stages: (1) cell membrane attachment; (2) cell membrane fluidity modification; and (3) cell membrane structure disruption. [ABSTRACT FROM AUTHOR]

Naringenin is a flavonoid found in abundance in natural plants, including citrus fruits, tomatoes, and grapefruit. Naringenin has a molecular weight of 272.26 and aqueous solubility of 43.83 ± 0.039 mcg/mL. It has a limited bioavailability due to its poor solubility thus limiting its application in pharmaceutical. This study was designed to determine the efficiency of Solid Lipid Nanoparticles (SLN) method in improving the solubility of Naringenin. Variables such as the concentration of lipid with surfactant and ultrasonification power were also studied to observe their effect on the formation of NRG-SLNs. This study was done using method of solid lipid nanoparticles. Initially, the Naringenin-Solid Lipid Nanoparticles (NRG-SLNs) were prepared in separate beaker for lipid phase containing stearic acid and aqueous phase containing distilled water with Tween 80. Both were brought to a temperature of 80ͦC. Then, aqueous phase was poured and mixed continuously at constant temperature of 80ͦC until a semi-transparent solution appears. The solution was then subjected to sonication for 10 minutes while maintaining the same temperature. The procedure was repeated with increasing concentration of lipid and surfactant and different sonication power. The samples were subjected to solubility study and encapsulation efficiency using Uv-Visible spectrophotometer. Zeta potential, particle size and polydispersion index were determined using Zetasizer. The sample was also studied for its short-term stability at room temperature for a period of 3 months. Based on the characterization, the maximum solubility of naringenin achieved was 0.8621 mg/ml, which improves from the pure naringenin. The particle size of NRG-SLNs ranged from 218 nm to 1030 nm with polydispersion index value of 0.611. The Zeta potential of the nanoparticles was -0.112 mV, which is nearly neutral. This method produces nanoparticles with encapsulation efficiency of 77.50 % to 86.21 %. The short-term stability of the NRG-SLNs was found to be good since there was only slight reduce in encapsulation efficiency with no change in colour of solution. The solid lipid nanoparticle method was successfully proven to improve the solubility and enhance the stability of naringenin, which is a lipophilic active ingredient. [ABSTRACT FROM AUTHOR]

A pharmaceutical excipient is a substance acts as a carrier incorporates active pharmaceutical ingredients. Excipient selection focuses on desirable characteristics of excipients. Limitations of using excipients which affect the characteristics of the granules and tablets. Co-processed excipients are produced by integrating one excipient into the other excipient at particle level. Such combination of two or more pharmacopeial or non-pharmacopeial excipients does not involve chemical reaction and only involve physical properties changes which is not possible by simple physical mixing. The introduced multicomponent-based excipients for formulation to obtain better features and tableting properties. The objectives of this revisit to discuss the development of co-processed excipients in the past two decades. This review summarizes the advantages of co-processed excipient, the manufacturing process, compilation of co-processed excipients in the literature, limitations, evaluation methods and future development of co-processed excipient. Co-processed excipients will undoubtedly attract attention from academia and pharmaceutical industry as more newer combinations of excipients and newer ways of co-processing become available Besides, rather using numerous excipients in formulation, it allows for the development and usage of single multifunctional excipients. [ABSTRACT FROM AUTHOR]