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Miconazole is a synthetic derivative of imidazole, a medication with a broad-spectrum antifungal agent that is used to treat localized vaginal, skin, and nail infections. The aim of the study was to develop an innovative technique to improve the permeability and efficacy of topical miconazole nitrate. A nanoemulgel of miconazole nitrate was formulated by the incorporation of a nanoemulsion and a hydrogel. The nanoemulsion was first optimized using a self-emulsifying technique, and the drug was then loaded into the optimum formulation and evaluated prior to mixing with the hydrogel. Miconazole nitrate nanoemulgel formulations were evaluated for their physical characteristics and antifungal activity. Based on the results, the formulation with 0.4 % Carbopol showed the highest release profile (41.8 mg/ml after 2 h); thus, it was chosen as the optimum formulation. A cell diffusion test was performed to examine the ability of the Miconazole nitrate nanoemulgel to penetrate the skin and reach the bloodstream. Percentage cumulative drug releases of 29.67 % and 23.79 % after 6 h were achieved for the MNZ nanoemulgel and the commercial cream, Daktazol, respectively. The antifungal activity of the novel MNZ nanoemulgel formulation was tested against Candida albicans and compared to Daktazol cream and almond oil; the results were: 40.9 ± 2.3 mm, 25.4 ± 2.7 mm and 18 ± 1.9 mm, respectively. In conclusion, a novel MNZ nanoemulgel showing superior antifungal activity compared to that of the commercial product has been developed. This nanotechnology technique is a step toward making pharmaceutical dosage forms that has a lot of promise.
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The purpose of this questionnaire-based cross-sectional study was to investigate the knowledge, perceptions, and attitudes regarding halal pharmaceuticals among sharia practitioners in Palestine. A total of 420 sharia practitioners with different educational levels were included. This was a cross-sectional study conducted between March and July 2021 with the use of a standardized, self-administered questionnaire. Volunteers were selected throughout Palestine using a systematic random selection approach. The data were summarized using descriptive statistics (mean, standard deviation, frequency, percentage, median, and interquartile range). The Chi-square and Fisher's exact tests were used to examine the relationship between demographic factors and the knowledge, attitude, and perception scores, respectively. The results revealed that sharia practitioners have relatively good and positive knowledge toward halal pharmaceuticals. The main knowledge of most halal pharmaceuticals was about 50.2%, yet there is still significant latitude in their knowledge of a few issues. The main attitude and perception score was about 96.4%. The results showed a positive and fair correlation between knowledge and attitude (r = 0.153, P < 0.001) and also between knowledge and perception (r = 0.341, P < 0.001). In addition, there is a good correlation between attitude and perception (r = 0.681, P < 0.001). The study concluded that better knowledge of halal pharmaceuticals is associated with positive perceptions and behaviors. The government, pharmaceutical manufacturers, religious scholars, and health care professionals should collaborate to achieve the goal of using halal medications.
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This study aimed to develop a topical emulgel formulation from olive oil and lemongrass (LG) extracts and to evaluate its in vitro and in vivo (sensorial) properties in addition to its sun protection factor (SPF) value. The primary emulsion and the gel were prepared separately, and then they were levigated together to formulate the emulgel. The produced emulgel was evaluated for its physical appearance, pH, spreadability, and stability. The SPF value of emulgel was evaluated by applying the Mansur equation. Moreover, an in vivo sensorial assessment was conducted on the emulgel through a crossover study by including 20 volunteers. The results confirm good stability for emulgel formulations because there was no significant change in the pH value, no micelle inversion, or phase separation detected. The emulgel recorded a moderate SPF value (5.5) which can be useful for daily use, especially in tanned skin subjects. Moreover, the sensorial assessment of LG and blank emulgels showed a significant change in the cooling effect, odor, and smoothness and add some kind of moisture. In fact, there was a significant difference in overall properties between the two formulations where the p-value was less than 0.05. It is concluded the emulgel formulation containing LG and olive oil could be beneficial in terms of applicability and stability and can be easily formulated in pharmaceutical facilities. Besides, it would be useful for daily use because of the overall suitable properties, especially odor, feel, and SPF value.
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Cymbopogon , Óleos Voláteis , Química Farmacêutica/métodos , Estudos Cross-Over , Géis , HumanosRESUMO
Plumbago europaea L. is a plant utilized in Palestinian ethnomedicine for the treatment of various dermatological diseases. The current investigation was designed to isolate plumbagin from P. europaea leaves, roots and for the first time from the stems. Moreover, it aimed to evaluate the antimycotic activity against three human fungal pathogens causing dermatophytosis, also against an animal fungal pathogen. The qualitative analysis of plumbagin from the leaves, stems, and roots was conducted using HPLC and spectrophotometer techniques, while the structure of plumbagin was established utilizing Proton and Carbon-13 Nuclear Magnetic Resonance (NMR) and Infrared (IR) techniques. The entire plant constituents were determined by GC-MS. Moreover, the antimycotic activity against Ascosphaera apis, Microsporum canis, Trichophyton rubrum, and Trichophyton mentagrophytes was assessed utilizing the poison food technique method. The percentage of plumbagin recorded in the leaves, stems, and roots was found to be 0.51±0.001%, 0.16±0.001%, and 1.65±0.015%, respectively. The GC-MS examination declared the presence of 59 molecules in the plant extract. The plant extract and pure plumbagin exhibited complete inhibition against all tested dermatophytes at 6.0mg/mL for the extracts and 0.2mg/mL for plumbagin. P. europaea root is the best source of plumbagin and the plant extract could represent a potential drug candidate for the treatment of dermatophytosis infections. Further studies required to design suitable dosage forms from the natural P. europaea root extracts or plumbagin alone, to be utilized for the treatment of dermatological and veterinary ailments.
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Antifúngicos/isolamento & purificação , Naftoquinonas/isolamento & purificação , Folhas de Planta/química , Raízes de Plantas/química , Caules de Planta/química , Plumbaginaceae/química , Antifúngicos/farmacologia , Arthrodermataceae/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Microsporum/efeitos dos fármacos , Estrutura Molecular , Naftoquinonas/farmacologia , Onygenales/efeitos dos fármacos , Espectrofotometria InfravermelhoRESUMO
BACKGROUND: The use of naturally occurring bioactive materials is getting great attention owing to their safety and environmental properties. Oily compounds, known as oleoresins, are expected to provide an important source for the natural products industry aiming to develop novel treatments for skin conditions. In this work, Capsicum annuum oleoresin nanoemulgel formulations have been prepared and investigated for their antibacterial and anticancer properties. METHODOLOGY: Several C. annuum oleoresin nanoemulgel formulations were prepared by incorporating a Carbopol 940 gel in a self-nanoemulsifying nanoemulsion consisting of C. annuum, tween 80, and span 80. The systems were characterized for particle size, polydispersity index (PDI), zeta potential, and rheology. The in vitro antimicrobial and cytotoxic activities of the optimum formulation were evaluated. RESULTS: The selected formulation is composed of 40% tween, 10% span 80, and 40% C. annuum oleoresin. This formulation produced a stable nanoemulsion with a narrow PDI value of 0.179 ± 0.08 and a droplet size of 104.0 ± 2.6 nm. Results of the in vitro antimicrobial studies indicated high potency of the systems against methicillin-resistant Staphylococcus aureus (MRSA) (zone of inhibition of 29 ± 1.9 mm), E. coli (33 ± 0.9 mm), K. pneumonia (30 ± 1.4 mm), and C. albicans (21 ± 1.5 mm), as compared to the reference antibiotic, ampicillin (18 ± 1.4 mm against K. pneumonia), and antifungal agent, fluconazole (12 ± 0.1 mm against C. albicans). Furthermore, cytotoxicity results, expressed as IC50 values, revealed that the oleoresin and its nanoemulgel had the best effects against the HepG2 cell line (IC50 value of 79.43 µg/mL for the nanoemulgel) and MCF7 (IC50 value of 57.54 µg/mL), and the most potent effect was found against 3T3 (IC50 value of 45.7 µg/m- L). On the other side, the system did not substantially exhibit activity against By-61 and Hela. CONCLUSION: C. annuum oleoresin and its nanoemulgel can be considered valuable sources for the discovery of new antibacterial, antifungal, and anticancer compounds in the pharmaceutical industry, especially due to their potent activity against various cancer cell lines as well as bacterial and fungal strains.
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Anti-Infecciosos , Capsicum , Staphylococcus aureus Resistente à Meticilina , Extratos Vegetais , Pneumonia , Humanos , Escherichia coli , Antibacterianos/farmacologia , Anti-Infecciosos/farmacologia , Candida albicansRESUMO
Pomegranate (Punica granatum) is a tree of the Punicaceae family that is widespread all over the world and has several types and therapeutic uses. The current study aimed to investigate the phytochemical compounds by GC analysis and carried out physical characterization of the pomegranate seed oil and its self-nanoemulsifying system. Then antioxidant, anti-diabetic, and anti-lipase activities were investigated for both.The pomegranate seed oil was extracted, and its self-nanoemulsifying system was then prepared. Phytochemical compounds were analyzed by GC, and physical characterization was established of the pomegranate seed oil and its self-nanoemulsifying system. Then antioxidant, anti-diabetic, and anti-lipase activities were investigated for both.The GC-MS analysis revealed that punicic acid, ß-eleosteric acid, catalpic acid, α-eleosteric acid, and oleic acid were the most predominant compounds in pomegranate seed oil. Other active compounds like linoleic acid, palmitic acid, stearic acid, and α-linolenic acid were detected in trace percentages. The self-nanoemulsifying system was prepared using various concentrations of surfactant (Tween 80), co-surfactant (Span 80), and pomegranate seed oil. The selected formulation had a PDI of 0.229 ± 0.09 and a droplet size of 189.44 ± 2.1 nm. The free radical scavenging activity of pomegranate seed oil, the self-emulsifying system, and Trolox was conducted using DPPH. The oil-self-nanoemulsifying system showed potent antioxidant activity compared to Trolox. Also, pomegranate oil inhibited α-amylase with a weak IC50 value of 354.81 ± 2.3 µg/ml. The oil self-nanoemulsifying system showed potent activity compared to acarbose and had a weaker IC50 value (616.59 ± 2.1 µg/ml) and a potent IC50 value (43.65 ± 1.9 µg/ml) compared to orlistat.Pomegranate seed oil self-nanoemulsifying system could be applied in the future for the preparation of possible oral medications for the prevention and treatment of oxidative stress, diabetes, and obesity due to its high activity against free radical, amylase, and lipase enzymes compared to pomegranate seed oil itself and the references used. This study reveals that self-nanoemulsion systems can enhance oil drug formulations by improving pharmacokinetics and pharmacodynamics, acting as drug reservoirs, and facilitating efficient oil release.
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Antioxidantes , Emulsões , Hipoglicemiantes , Óleos de Plantas , Punica granatum , Sementes , Punica granatum/química , Antioxidantes/química , Antioxidantes/farmacologia , Sementes/química , Emulsões/química , Óleos de Plantas/química , Óleos de Plantas/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análise , Fármacos Antiobesidade/química , Fármacos Antiobesidade/farmacologia , Lipase/antagonistas & inibidores , Lipase/metabolismo , Nanopartículas/químicaRESUMO
This study explores the realm of personalized medicine by investigating the utilization of 3D-printed dosage forms, specifically focusing on patient-specific enteric capsules designed for the modified release of ketoprofen, serving as a model drug. The research investigates two distinct scenarios: the modification of drug release from 3D-printed capsules crafted from hydroxypropyl methylcellulose phthalate:polyethylene glycol (HPMCP:PEG) and poly(vinyl alcohol) (PVA), tailored for pH sensitivity and delayed release modes, respectively. Additionally, a novel ketoprofen-loaded self-nanoemulsifying drug delivery system (SNEDDS) based on pomegranate seed oil (PSO) was developed, characterized, and employed as a fill material for the capsules. Through the preparation and characterization of the HPMCP:PEG based filament via the hot-melt extrusion method, the study thoroughly investigated its thermal and mechanical properties. Notably, the in vitro drug release analysis unveiled the intricate interplay between ketoprofen release, polymer type, and capsule thickness. Furthermore, the incorporation of ketoprofen into the SNEDDS exhibited an enhancement in its in vitro cylooxygenase-2 (COX-2) inhibitory activity. These findings collectively underscore the potential of 3D printing in shaping tailored drug delivery systems, thereby contributing significantly to the advancement of personalized medicine.
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Cápsulas , Liberação Controlada de Fármacos , Emulsões , Cetoprofeno , Medicina de Precisão , Impressão Tridimensional , Cetoprofeno/química , Medicina de Precisão/métodos , Humanos , Emulsões/química , Polietilenoglicóis/química , Sistemas de Liberação de Medicamentos/métodos , Preparações de Ação Retardada , Metilcelulose/química , Metilcelulose/análogos & derivados , Álcool de Polivinil/químicaRESUMO
BACKGROUND: The use of conventional medical therapies has proven to have many setbacks and safety concerns that need further improvement. However, herbal medicine has been used for over 2000 years, and many studies have proven the use of herbs to be effective and safe. This article discussed the efficacy of different herbal products used in the management of obesity. To evaluate the efficacy of seven herbal-based weight loss products currently available on the Palestinian market, using in vitro assays to screen for antioxidants, anti-amylase, and anti-lipase effects for each product. METHOD: Pancreatic lipase and salivary amylase inhibitory activities, as well as antioxidant analysis, were tested in vitro on a variety of herbal products. Then the IC50 was measured for each test. RESULTS: The anti-lipase assay results, IC50 values in (µg/mL) of each of the seven products (Product A, product B, product C, product D, product E, product F, and product G) were 114.78, 532.1, 60.18, 53.33, 244.9, 38.9, and 48.97, respectively. The IC50 value for orlistat (Reference) was 12.3 µg/ml. On the other hand, the IC50 value for alpha amylase inhibition of the seven products (Product A, product B, product C, product D, product E, product F, and product F) were 345.93, 13,803.84 (Inactive), 73.79, 130.91, 165.95, 28.18, and 33.11 µg/ml respectively, while acarbose (Reference) was 23.38 µg/ml. The antioxidant activity (IC50 values) for the seven products (Product A, product B, product C, product D, product E, product F, and product F) were 1258.92, 707.94, 79.43, 186.20, 164.81, 17.53, and 10.47 µg/ml respectively. While the IC50 value for Trolox was 2.70 µg/ml. CONCLUSION: It can be concluded that the seven products showed varied anti-lipase, anti-amylase, and antioxidant effects. However, products F and G showed superiority in all categories.
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Fármacos Antiobesidade , Extratos Vegetais , Plantas Medicinais , alfa-Amilases/química , Antioxidantes/química , Antioxidantes/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Oriente Médio , Fármacos Antiobesidade/química , Fármacos Antiobesidade/farmacologiaRESUMO
PURPOSE: The goal of this study was to make Benzoyl Peroxide (BPO) nanoemulgel to improve its ability to kill bacteria. BPO has trouble getting into the skin, being absorbed by the skin, staying stable, and being spread out. METHODS: A BPO nanoemulgel formulation was prepared by combining BPO nanoemulsion with Carbopol hydrogel. The drug was tested for solubility in various oils and surfactants in order to select the best oil and surfactant for the drug, and then the drug nanoemulsion formulation was prepared using a self-nano-emulsifying technique with Tween 80, Span 80, and lemongrass oil. The drug nanoemulgel was looked at in terms of its particle size, polydispersity index (PDI), rheological behavior, drug release, and antimicrobial activity. RESULTS: Based on the solubility test results, lemongrass oil was the best solubilizing oil for drugs, while Tween 80 and Span 80 demonstrated the highest solubilizing ability for drugs among the surfactants. The optimum self-nano-emulsifying formulation had particle sizes of less than 200 nm and a PDI of close to zero. The results showed that incorporating the SNEDDS formulation of the drug with Carbopol at various concentrations did not cause a significant change in the particle size and PDI of the drug. The zeta potential results for drug nanoemulgel were negative, with more than 30 mV. All nanoemulgel formulations exhibited pseudo-plastic behavior, with 0.4% Carbopol exhibiting the highest release pattern. The drug nanoemulgel formulation worked better against bacteria and acne than the product on the market. CONCLUSION: Nanoemulgel is a promising way to deliver BPO because it makes the drug more stable and increases its ability to kill bacteria.
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BACKGROUND: Many modern pharmaceutical researchers continue to focus on the discovery and evaluation of natural compounds for possible therapies for obesity, diabetes, infections, cancer, and oxidative stress. Extraction of Ocimum basilicum seed essential oil and evaluation of its antioxidant, anti-obesity, antidiabetic, antibacterial, and cytotoxic activities were the goals of the current study. METHOD: O. basilicum seed essential oil was extracted and evaluated for its anticancer, antimicrobial, antioxidant, anti-obesity, and anti-diabetic properties utilizing standard biomedical assays. RESULTS: O. basilicum seed essential oil showed good anticancer activity against Hep3B (IC50 56.23 ± 1.32 µg/ml) and MCF-7 (80.35 ± 1.17 µg/ml) when compared with the positive control, Doxorubicin. In addition, the essential oil showed potent antibacterial (against Klebsiella pneumoniae, Escherichia coli, Staphylococcus aureus, Proteus mirabilis, and Pseudomonas aeruginosa) and antifungal (against Candida albicans) activities. Moreover, as for the anti-amylase test, IC50 was 74.13 ± 1.1 µg/ml, a potent effect compared with the IC50 of acarbose, which was 28.10 ± 0.7 µg/ml. On the other hand, for the anti-lipase test, the IC50 was 112.20 ± 0.7 µg/ml a moderate effect compared with the IC50 of orlistat, which was 12.30 ± 0.8 µg/ml. Finally, the oil had a potent antioxidant effect with an IC50 of 23.44 ± 0.9 µg/ml compared with trolox (IC50 was 2.7 ± 0.5 µg/ml). CONCLUSION: This study has provided initial data that supports the importance of O. basilcum essential oil in traditional medicine. The extracted oil not only exhibited significant anticancer, antimicrobial, and antioxidant properties but also antidiabetic and anti-obesity effects, which provided a foundation for future research.
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Anti-Infecciosos , Ocimum basilicum , Óleos Voláteis , Antioxidantes/farmacologia , Hipoglicemiantes/farmacologia , Anti-Infecciosos/farmacologia , Óleos Voláteis/farmacologia , Antibacterianos/farmacologiaRESUMO
BACKGROUND: Cancer is one of the most dangerous and widespread diseases in the world today and it has risen to the position of the leading cause of death around the globe in the last few decades. Due to the inherent resistance of many types of cancer to conventional radiotherapy and chemotherapy, it is vital to develop innovative anticancer medications. Recently, a strategy based on nanotechnology has been used to improve the effectiveness of both old and new cancer drugs. OBJECTIVES: The present study aimed to design and synthesize a series of phenyl-isoxazole-Carboxamide derivatives, evaluate their anticancer properties, and improve the permeability of potent compounds into cancer cells by using a nano-emulgel strategy. METHODS: The coupling reaction of aniline derivatives and isoxazole-Carboxylic acid was used to synthesize a series of isoxazole-Carboxamide derivatives. IR, HRMS, 1H-NMR, and 13C-NMR spectroscopy techniques, characterized all the synthesized compounds. The in-vitro cytotoxic evaluation was performed by using the MTS assay against seven cancer cell lines, including hepatocellular carcinoma (Hep3B and HepG2), cervical adenocarcinoma (HeLa), breast carcinoma (MCF-7), melanoma (B16F1), colorectal adenocarcinoma (Caco-2), and colon adenocarcinoma (Colo205), as well as human hepatic stellate (LX-2) in addition to the normal cell line (Hek293T). A nano-emulgel was developed for the most potent compound, using a self-emulsifying technique. RESULTS: All synthesized compounds were found to have potent to moderate activities against B16F1, Colo205, and HepG2 cancer cell lines. The results revealed that the 2a compound has broad spectrum activity against B16F1, Colo205, HepG2, and HeLa cancer cell lines with an IC50 range of 7.55-40.85 µM. Moreover, compound 2e was the most active compound against B16F1 with an IC50 of 0.079 µM compared with Dox (IC50 = 0.056 µM). Nanoemulgel was used to increase the potency of the 2e molecule against this cancer cell line, and the IC50 was reduced to 0.039 µM. The antifibrotic activities were investigated against the LX-2 cell line, and it was found that our synthesized molecules showed better antifibrotic activities at 1 µM than 5-FU, and the cell viability values were 67 and 95%, respectively. CONCLUSION: This study suggests that a 2e nano-formalized compound is a potential and promising anti-melanoma agent.
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In addition to their wide therapeutic application, benzoates and benzoic acid derivatives are the most commonly utilized food preservatives. The purpose of this study was to estimate the antioxidant, anti-diabetic, and anti-obesity activities of four 2-(phenylthio)-ethyl benzoate derivatives utilizing standard biomedical assays. The results revealed that the 2a compound has potent antidiabetic activity through the inhibition of α-amylase and α-glycosidase with IC50 doses of 3.57 ± 1.08 and 10.09 ± 0.70 µg/ml, respectively, compared with the positive control acarbose (IC50 = 6.47 and 44.79 µg/ml), respectively. In addition, by utilizing the ß-carotene linoleic acid and DPPH methods, the 2a compound showed the highest antioxidant activity compared with positive controls. Moreover, the 2a compound showed potential anti-lipase activity with an IC50 dose of 107.95 ± 1.88 µg/ml compared to orlistat (IC50 = 25.01 ± 0.78 µg/ml). A molecular docking study was used to understand the interactions between four derivatives of (2-(phenylthio)-ethyl benzoate with α-amylase binding pocket. The present study concludes that the 2a compound could be exploited for further antidiabetic, antioxidant, and anti-obesity preclinical and clinical tests and design suitable pharmaceutical forms to treat these global health problems.
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Benzoatos/farmacologia , Ácido Benzoico/farmacologia , Amilases , Fármacos Antiobesidade/farmacologia , Antioxidantes/farmacologia , Diabetes Mellitus/tratamento farmacológico , Inibidores de Glicosídeo Hidrolases/farmacologia , Humanos , Hipoglicemiantes/farmacologia , Simulação de Acoplamento Molecular , Estrutura Molecular , Obesidade/tratamento farmacológico , Extratos Vegetais/farmacologia , alfa-Amilases/antagonistas & inibidoresRESUMO
BACKGROUND: Safrole is a natural compound extracted from various plants, and has shown various biological activities. The current study aimed to investigate the antioxidant, antidiabetic, antimicrobial, and anticancer activity of safrole oil and to study the influence of safrole nanoemulgel on these activities. METHODS: The antioxidant and antidiabetic in-vitro assays were conducted using standard biomedical methods. The safrole oil nanoemulgel was developed using a self-emulsifying technique. Then the antimicrobial activity of the safrole oil and safrole nanoemulgel were performed on different microbial species, and cytotoxicity was determined against Hep3B cancer cell lines using the MTS assay. RESULTS: Safrole oil showed moderate antioxidant activity compared with standard Trolox, with IC50 value 50.28 ± 0.44 and 1.55 ± 0.32 µg/ml, respectively. Moreover, it had potent α-amylase inhibitory activity (IC50 11.36 ± 0.67 µg/ml) compared with Acarbose (IC50 value 5.88 ± 0.63). The safrole nanoemulgel had pseudo-plastic behaviour, droplet sizes below 200 nm, a polydispersity index (PDI) below 0.3, and a zeta potential of less than - 30 mV. Safrole oil has potential antimicrobial and anticancer activities, and these activities were improved with safrole nanoemulgel. CONCLUSION: The safrole oil may be applied for the prevention and treatment of oxidative stress, diabetes, different microbial species and cancer, and these activities could be improved by nano-carriers.
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Antineoplásicos , Antioxidantes , Nanoestruturas , Óleos Voláteis , Safrol , Anti-Infecciosos/análise , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antineoplásicos/análise , Antineoplásicos/química , Antineoplásicos/farmacologia , Antioxidantes/análise , Antioxidantes/química , Antioxidantes/farmacologia , Compostos de Bifenilo/química , Compostos de Bifenilo/metabolismo , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Humanos , Hipoglicemiantes/análise , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Nanoestruturas/análise , Nanoestruturas/química , Óleos Voláteis/análise , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Tamanho da Partícula , Picratos/química , Picratos/metabolismo , Safrol/análise , Safrol/química , Safrol/farmacologiaRESUMO
Currently, available therapies for diabetes could not achieve normal sugar values in a high percentage of treated patients. In this research project, a series of 17 benzodioxole derivatives were evaluated as antidiabetic agents; that belong to three different groups were evaluated against lipase and alpha-amylase (α-amylase) enzymes. The results showed that 14 compounds have potent inhibitory activities against α-amylase with IC50 values below 10 µg/ml. Among these compounds, 4f was the most potent compound with an IC50 value of 1.11 µg/ml compared to the anti-glycemic agent acarbose (IC50 6.47 µg/ml). On the contrary, these compounds showed weak or negligible activities against lipase enzyme. However, compound 6a showed the best inhibitory anti-lipase activity with IC50 44.1 µg/ml. Moreover, all the synthesized compounds were undergone Molinspiration calculation, and the result showed that all compounds obeyed Lipinski's rule of five. Molecular docking studies were performed to illustrate the binding interactions between the benzodioxole derivatives and α-amylase enzyme pocket. Related to the obtained results it was clear that the carboxylic acid, benzodioxole ring, halogen or methoxy substituted aryl are important for the anti-amylase activities. The potent inhibitory results of some of the synthesized compounds suggest that these molecules should go further in vivo evaluation. It also suggests the benzodioxole derivatives as lead compounds for developing new drug candidates.
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This study is aimed at developing coriander oil into a nanoemulgel and evaluating its antimicrobial and anticancer effects. Coriander (Coriandrum sativum) oil was developed into a nanoemulgel by using a self-nanoemulsifying technique with Tween 80 and Span 80. Hydrogel material (Carbopol 940) was then incorporated into the nanoemulsion and mixed well. After this, we evaluated the particle size, polydispersity index (PDI), rheology, antimicrobial effect, and cytotoxic activity. The nanoemulsion had a PDI of 0.188 and a particle size of 165.72 nm. Interesting results were obtained with the nanoemulgel against different types of bacteria, such as Pseudomonas aeruginosa, Klebsiella pneumoniae, and methicillin-resistant Staphylococcus aureus (MRSA), with a minimum inhibitory concentration (MIC) of 2.3 µg/ml, 3.75 µg/ml, and 6.5 µg/ml, respectively. In addition, the half-maximal inhibitory concentration (IC50) of the nanoemulgel when applying it to human breast cancer cells (MCF-7), hepatocellular carcinoma cells (Hep3B), and human cervical epithelioid carcinoma cells (HeLa) was 28.84 µg/ml, 28.18 µg/ml, and 24.54 µg/ml, respectively, which proves that the nanoemulgel has anticancer effects. The development of C. sativum oil into a nanoemulgel by using a self-nanoemulsifying technique showed a bioactive property better than that in crude oil. Therefore, simple nanotechnology techniques are a promising step in the preparation of pharmaceutical dosage forms.
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Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Coriandrum/química , Nanoestruturas/administração & dosagem , Neoplasias/tratamento farmacológico , Óleos Voláteis/farmacologia , Óleos de Plantas/farmacologia , Antibacterianos/química , Antineoplásicos/química , Linhagem Celular Tumoral , Emulsões , Humanos , Nanoestruturas/química , Neoplasias/metabolismo , Neoplasias/patologia , Óleos Voláteis/química , Tamanho da Partícula , Óleos de Plantas/químicaRESUMO
Cancer now is one of the leading causes of mortality in the world. There has been a lot of effort to discover new anticarcinogenic agents that allow treatment with fewer side effects. A series of isoxazole-carboxamide derivatives (2a-2g) were synthesised and evaluated for their cytotoxic activity against breast (MCF-7), cervical (HeLa), and liver (Hep3B) cancer cell lines and their antioxidant activity in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The results showed that 2d and 2e were the most active compounds against Hep3B cells, with a half-maximal inhibitory concentration (IC50) of around 23 µg/ml; 2d showed the highest activity against HeLa cells, with an IC50 15.48 µg/ml. However, 2a had the lowest IC50 (39.80 µg/ml) against MCF-7 cells. By contrast, compound 2g was inactive against all cancer cell lines, with IC50 values >400 µg/ml. Both 2d and 2e reduced Hep3B secretion of alpha-fetoprotein (to 1829.33 ± 65.91 ng/ml and 1758.66 ± 54.04 ng/ml, respectively). Furthermore, in cell cycle analysis, 2d and 2e induced a delay in the G2/M phase of 18.07%, which is similar to the doxorubicin positive control. Moreover, 2d and 2e reduced the necrosis rate of Hep3B threefold and instead shifted the cells to apoptosis. Our results indicate that 2d and 2e have potent and promising anticancer activity. However, compound 2a was the most active as antioxidant agent (IC50 = 7.8 ± 1.21 µg/ml) compared with Trolox as a positive control (IC50 2.75 µg/ml).
Assuntos
Amidas , Antineoplásicos , Antioxidantes , Proliferação de Células/efeitos dos fármacos , Isoxazóis , Neoplasias/tratamento farmacológico , Amidas/síntese química , Amidas/química , Amidas/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Antioxidantes/síntese química , Antioxidantes/química , Antioxidantes/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Células HeLa , Humanos , Isoxazóis/síntese química , Isoxazóis/química , Isoxazóis/farmacologia , Células MCF-7 , Neoplasias/metabolismo , Neoplasias/patologiaRESUMO
The use of herbal products by pregnant and lactating mothers without awareness of their harmful effects may expose both mother and fetus or infant to great dangers, such as abortion, premature delivery, uterine bleeding, and physical and mental retardation of the fetus. Thus, the aim of this study was to investigate the extent to which herbal product treatment is used and the reason for which such products are used and to ensure that these reasons are correct. An ethnopharmacological survey (cross-sectional observational design study) using a pre-piloted questionnaire was undertaken on herbal products used by pregnant and lactating women in the West Bank area of Palestine. A questionnaire was distributed to 350 pregnant and lactating women. The informed consent forms, ethics, and aims of the present study were reviewed and approved by the Institutional Review Board (IRB) at An-Najah National University. To identify the most important species used, the use value (UV) index was employed, while the SPSS program was used to analyze the data. Collected data revealed that 13 medicinal plants are utilized, while 12 plants are not used during pregnancy. Moreover, 15 plants are utilized and 9 plants are not used during lactation for treating and dealing with various problems. The most commonly used plants belonged to 14 families, including Lamiaceae, Apiaceae, Leguminosae, and Rubiaceae. The plants most used during pregnancy were sage (Salvia fruticosa), anise (Pimpinella anisum), and peppermint (Mentha × piperita). Castor (Ricinus communis) oil, ginger (Zingiber officinale), saffron (Crocus sativus), and senna (Senna alexandrina) mostly were not used by pregnant women. Moreover, cinnamon (Cinnamomum verum), anise (P. anisum), peppermint (M. piperita), and sage (S. fruticosa) were mostly used during lactation. Castor (R. communis) oil, ginger (Z. officinale), garlic (Allium sativum), and aloe (Aloe vera) mostly were not used during lactation. This study is of great importance in order to decrease the possibility of endangering the lives of fetuses and infants. A combined effort among researchers, scientists, lactating women, and pregnant women may help in changing wrong uses and thoughts about medicinal plants and help to improve the overall health of both mother and fetus.
RESUMO
OBJECTIVES: This project aims to develop a bio-natural nano-product with Cosmeceutical and pharmaceutical applications. METHODS: E. sativa oil was evaluated for its anti-oxidant, sun protection factor and elastase inhibition. Then, nanoemulgel formulations were prepared for E. sativa oil through the combination of nanoemulsion with hydrogel. E. sativa nanoemulsion formulations were prepared by the help of a selfemulsification technique. After this, the optimum formulation was mixed with Carbopol to produce the nanoemulgel. Anti-bacterial and anti-fungal activities were evaluated. RESULTS: Nanoemulsion occurred when the size of the droplets was 195.29 nm with the lowest polydispersibility index 0.207. The results of antioxidant, anti-elastase and SPF activities for E. sativa oil were 2.10 µg/ml, 25.1 µg/ml and an SPF value of 5.57, respectively. In addition, in the anti-bacterial test for Staphylococcus aureus, it was found that nanoemulgel has an inhibition zone of 2.1 cm in diameter. According to the MRSA, the inhibition zone was 1.5 cm. CONCLUSION: E. Sativa oil could be a promising candidate in cosmeceutical and pharmaceutical preparations.
Assuntos
Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Brassicaceae/química , Nanoestruturas/química , Elastase Pancreática/antagonistas & inibidores , Óleos de Plantas/isolamento & purificação , Fator de Proteção Solar , Animais , Anti-Infecciosos/isolamento & purificação , Antioxidantes/isolamento & purificação , Compostos de Bifenilo/química , Candida/efeitos dos fármacos , Composição de Medicamentos , Emulsões , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Hidrogéis/química , Picratos/química , Sementes/química , Pele/efeitos dos fármacos , Pele/enzimologia , SuínosRESUMO
PURPOSE: Fusidic acid (FA) and sodium fusidate (SF) have problems in their skin penetration and stability resulting in a reduction in their potency; therefore, the objective of this study was to develop FA and SF nanoemulgels to improve the antibacterial activity of the drugs. METHODS: FA and SF nanoemulgel formulations were prepared by the incorporation of FA and SF nanoemulsions with Carbopol hydrogel. First, the drugs were screened for their solubility in different oils and surfactants to choose the suitable oil and surfactants for the drugs, and then the drug nanoemulsion formulations were prepared by a self-nanoemulsifying technique using Tween 80, Span 20 and pine oil. The drug nanoemulgels were evaluated for their particle size, polydispersity index (PDI), rheological behaviour, drug release and anti-microbial activity. RESULTS: Based on the solubility test, pine oil was the best solubilising oil for both drugs, Tween 80 and Span 20 showed the highest solubilising ability for both the drugs among the surfactants; therefore, they were chosen as surfactant and co-surfactant, respectively. The optimum self-nanoemulsifying formulations showed a particle size for fusidic acid and Sodium fusidate of 140.58 nm and 151.86 nm respectively, and both showed a low PDI below 0.3. After incorporating both drug SNEDDS formulations with Carbopol at different concentrations, the results of the drugs particle size and PDI showed no significant difference. The zeta potential results for both drugs nanoemulgels showed a negative potential with more than 30 mV. All nanoemulgel formulations showed pseudo-plastic behaviour with the highest release pattern at 0.4% Carbopol. The antibacterial activity of both drug nanoemulgel formulations showed superiority over the market product. CONCLUSION: Nanoemulgel is a promising delivery system for FA and SF that helps in improving the stability and antibacterial activities of the drugs.
Assuntos
Antibacterianos/farmacologia , Emulsões/química , Ácido Fusídico/farmacologia , Géis/química , Nanopartículas/química , Óleos de Plantas/química , Enterococcus/efeitos dos fármacos , Tamanho da Partícula , Transição de Fase , Reologia , Solubilidade , Espectrofotometria Ultravioleta , Eletricidade EstáticaRESUMO
It is estimated by the World Health Organization (WHO) that most of the world's population depends on herbal medicine for their health care. Nigella sativa (N. sativa), also known as black-caraway and as "Kalonji," is a well-known seed all over the world. It is one of the most common medicinal plants worldwide and contains many useful chemical constituents that we can find in its fixed oil, such as thymoquinone, thymohydroquinone, dithymoquinone, thymol, nigellicine, carvacrol, nigellimine, nigellicine, nigellidine, and alpha-hederin. Due to these numerous important ingredients it was found that it affects different areas of our body and has many pharmacological effects as antibacterial, antiviral, anti-inflammatory, and wound healing effect and also for acne vulgaris, skin cancer, pigmentation, and many cosmeceutical applications. Based on the folklore usage of N. sativa seeds and oil, they are used in various systems of food and medicines. The aim of this article is to provide a detailed survey of the literature of cosmeceutical and external applications of N. sativa which is expected to stimulate further studies on this subject.