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Nanoliposomes (NLs) are ideal carriers for delivering complex molecules and phytochemical products, but ginger by-products, despite their therapeutic benefits, have poor bioavailability due to their low water solubility and stability. Crude ginger extracts (CGEs) and 6-gingerol were individually encapsulated within NLs for in vitro activity assessment. In vitro evaluation of anti-proliferative and anti-inflammatory properties of encapsulated 6-gingerol and CGE was performed on healthy human periodontal ligament (PDL) fibroblasts and MDA-MB-231 breast cancer cells. Encapsulation efficiency and loading capacity of 6-gingerol reached 25.23% and 2.5%, respectively. NLs were found stable for up to 30 days at 4°C with a gradual load loss of up to 20%. In vitro cytotoxic effect of encapsulated 6-gingerol exceeded 70% in the MDA-MB-231 cell line, in a comparable manner with non-encapsulated 6-gingerol and CGE. The effect of CGE with an IC50 of 3.11 ± 0.39, 7.14 ± 0.80, and 0.82 ± 0.55 µM and encapsulated 6-gingerol on inhibiting IL-8 was evident, indicating its potential anti-inflammatory activity. Encapsulating 6-gingerol within NLs enhanced its stability and facilitated its biological activity. All compounds, including vitamin C, were equivalent at concentrations below 2 mg/mL, with a slight difference in antioxidant activity. The concentrations capable of inhibiting 50% of 2,2-diphenyl-1-picrylhydrazyl (DPPH) substrate were comparable.
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Anti-Inflamatórios , Catecóis , Álcoois Graxos , Lipossomos , Zingiber officinale , Álcoois Graxos/química , Álcoois Graxos/farmacologia , Humanos , Catecóis/química , Catecóis/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/farmacocinética , Lipossomos/química , Linhagem Celular Tumoral , Zingiber officinale/química , Antineoplásicos/química , Antineoplásicos/farmacologia , Antineoplásicos/farmacocinética , Sobrevivência Celular/efeitos dos fármacos , Nanopartículas/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Interleucina-8/metabolismo , Proliferação de Células/efeitos dos fármacosRESUMO
Colorectal cancer (CRC) is the fourth most common cause of malignant tumor death. The development of novel, more effective drugs is desperately needed to treat CRC. Zingiber officinale is believed to possess anticancer properties due to its flavonoids and phenols. Using Soxhlet (SOXT) and maceration (MACR) techniques, the present study aimed to evaluate the amounts of quercetin, gallic acid, rutin, naringin, and caffeic acid in ginger capsules of Z. officinale. High-performance liquid chromatography (HPLC)/ultraviolet was used for separation and quantitation. In vitro toxicity evaluation of ginger capsules on the CRC cell line HT-29 was also conducted to assess the anticancer activity of the supplement. The cell line HT-29 (HTB-38) colorectal adenocarcinoma was utilized for the antiproliferative effect of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide. Ginger herbal supplement extract at dosages of 200 and 100 µg had strong cytotoxic effects (IC50 < 50 µg/mL) on HT-29 CRC cells via MACR. This extract is comparable to the SOXT extract, which has an IC50 of less than 50 µg/mL. The anticancer effect of ginger herbal supplement formulations against CRC lines was investigated, and the results obtained from both the MACR and SOXT extraction procedures were noteworthy. The quercetin content was the highest of all the extracts according to the HPLC data.
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Chronic wounds have become a major concern for healthcare systems, as they have been related to diabetic foot ulcers, venous leg ulcers and pressure ulcers. Oleuropein is an active compound that is extracted from olive leaves and it has the ability to reduce injury to tissues owing to its antioxidant effect, hence improving wound healing. The poor pharmacokinetics of oleuropein have limited its use clinically. This work is aimed toward studying the impact of PEGylated and non-PEGylated nanoliposomes loaded with oleuropein, as a carrier model, on wound-healing activity. The thin film hydration method was used to compose PEGylated and non-PEGylated liposomes, both loaded with oleuropein. The results indicated that each free, PEGylated and non-PEGylated composition was within the limit of optimum nanoliposome characterization. The results showed that non-PEGylated compositions produced higher efficiency in encapsulation (47.09 ± 10.06%) than the PEGylated ones (20.97 ± 10.52%). The PEG-nanoliposomes loaded with oleuropein (PEG-oleu) had mean size, charge and polydispersity index of 129.35 nm, -9.55 mV and 0.1010, respectively. The scratch assay results proved that PEGylated liposomal compositions have a more rapid wound-healing activity than non-PEGylated ones at different time intervals at 0, 2, 24 and 28 h.
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Glucosídeos Iridoides , Lipossomos , Cicatrização , PolietilenoglicóisRESUMO
The abstract discusses the development of rutin-loaded nanoliposomes and their anti-colorectal cancer activity against human carcinoma cells (HT-29). The study characterizes the nanoliposomes using the thin-film hydration method and analyzes their size, charge, and polydispersity index. The encapsulation efficiency and drug loading ability of rutin at different concentrations were investigated. The nanoliposomes were found to be stable for up to one month at 4 °C and showed sustained drug release for up to 24â h. The anti-cancer activity of the rutin-loaded nanoliposomes was found to be concentration-dependent and significantly improved compared to free rutin. PEGylated nanoliposomes with rutin (1.8â mg/ml) showed the highest encapsulation efficiency and drug loading ability, along with improved selectivity against cancer cells. Overall, the study provides important insights into the potential use of rutin-loaded nanoliposomes for the treatment of colorectal cancer.
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Carcinoma , Rutina , Humanos , Rutina/farmacologia , Lipossomos , Células HT29 , PolietilenoglicóisRESUMO
Olive leaf extract is a valuable source of phenolic compounds; primarily, oleuropein (major component) and rutin. This natural olive leaf extract has potential use as a therapeutic agent for cancer treatment. However, its clinical application is hindered by poor pharmacokinetics and low stability. To overcome these limitations, this study aimed to enhance the anticancer activity and stability of oleuropein and rutin by loading them into PEGylated Nano-phytosomes. The developed PEGylated Nano-phytosomes exhibited favorable characteristics in terms of size, charge, and stability. Notably, the anticolonic cancer activity of the Pegylated Nano-phytosomes loaded with oleuropein (IC50=0.14â µM) and rutin (IC50=0.44â µM) surpassed that of pure oleuropein and rutin alone. This outcome highlights the advantageous impact of Nano-phytosomes to augment the anticancer potential of oleuropein and rutin. These results present a promising pathway for the future development of oleuropein and rutin Nano-phytosomes as effective options for passive tumor-targeted therapy, given their improved stability and efficacy.
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Neoplasias , Olea , Rutina/farmacologia , Antioxidantes , Iridoides/farmacologia , Glucosídeos Iridoides , Polietilenoglicóis , Folhas de Planta , Extratos Vegetais/farmacologiaRESUMO
The synthesis of reliable biological nanomaterials is a crucial area of study in nanotechnology. In this study, Emericella dentata was employed for the biosynthesis of AgNPs, which were then combined with synthesized biochar, a porous structure created through biomass pyrolysis. The synergistic effects of AgNPs and biochar were evaluated through the assessment of pro-inflammatory cytokines, anti-apoptotic gene expression, and antibacterial activity. Solid biosynthesized AgNPs were evaluated by XRD and SEM, with SEM images revealing that most of the AgNPs ranged from 10 to 80 nm, with over 70% being less than 40 nm. FTIR analysis indicated the presence of stabilizing and reducing functional groups in the AgNPs. The nanoemulsion's zeta potential, hydrodynamic diameter, and particle distribution index were found to be -19.6 mV, 37.62 nm, and 0.231, respectively. Biochar, on the other hand, did not have any antibacterial effects on the tested bacterial species. However, when combined with AgNPs, its antibacterial efficacy against all bacterial species was significantly enhanced. Furthermore, the combined material significantly reduced the expression of anti-apoptotic genes and pro-inflammatory cytokines compared to individual treatments. This study suggests that low-dose AgNPs coupled with biochar could be a more effective method to combat lung cancer epithelial cells and pathogenic bacteria compared to either substance alone.
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Neoplasias Pulmonares , Nanopartículas Metálicas , Humanos , Testes de Sensibilidade Microbiana , Nanopartículas Metálicas/química , Bactérias , Citocinas/farmacologia , Antibacterianos/farmacologia , Antibacterianos/química , Neoplasias Pulmonares/tratamento farmacológico , Extratos Vegetais/químicaRESUMO
This study was conducted to compare dissolution profiles of four Jordanian registered sildenafil (SDF) products to the originator. Dissolution samples were analyzed utilizing a validated and stability-indicating HPLC method in human plasma. Validation was performed for specificity, linearity, limit of detection, lower limit of quantification, precision, trueness and stability. SDF was extracted from plasma samples using liquid-liquid extraction. The analysis was performed utilizing isocratic elution on C18 column with 1.0 ml/min flow rate. The regression value was â¼0.999 over 3 days with drug recovery between 86.6 to 89.8%with 10 ng/ml lower limit of quantitation. This method displayed a good selectivity of SDF with improved stability under various conditions. The method was used for SDF quantification in dissolution medium. Similarity factors for local products varied according to the used mediums, but all SDF local products passed the dissolution in vitro test since all of them showed a released of >85% after 60 min at the dissolution mediums.
[Box: see text].
Assuntos
Citrato de Sildenafila , Citrato de Sildenafila/sangue , Citrato de Sildenafila/química , Citrato de Sildenafila/análise , Cromatografia Líquida de Alta Pressão/métodos , Humanos , Medicamentos Genéricos/química , Medicamentos Genéricos/análise , Solubilidade , Jordânia , Estabilidade de Medicamentos , Limite de DetecçãoRESUMO
Nano-phytosomes are considered as an efficient drug delivery system for phytochemicals. Phytosomes enhance stability and significantly improves phytochemicals bioavailability and therapeutic efficacy. Thorough meta-analysis of 93 articles, phytochemical versus phytosomes size, charge, polydispersity index (PDI) and IC50 values were investigated. Multivariate Analysis of Covariance revealed significant phytochemicals type effects, even when accounting for cancer cell type and phospholipid type as covariates. Least Significant Difference (LSD) post hoc tests described unique attributes among various phytosomes. Flavonoid-based phytosomes exhibited larger particle sizes than others. In contrast, terpenoid-based phytosomes displayed significantly lower charges. Flavonoids demonstrated higher poly dispersity index (PDI) values than alkaloids and polyphenols. Alkaloids exhibited more extensive PDI values, while polyphenols had lower PDI values than terpenoids. Furthermore, flavonoid-containing nanoparticles exhibited higher IC50 values than terpenoids. In conclusion, nano-phytosomes offer promising prospects for revolutionising drug delivery methodologies and advancing the development of innovative therapeutic solutions in the domain of cancer therapy.
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Introduction: This study aimed to assess the antimicrobial activity of carvacrol in combination with approved antibiotics against methicillin-resistant Staphylococcus aureus (MRSA). Carvacrol, a phenolic monoterpenoid component of essential oils, has demonstrated antimicrobial properties against gram positive and gram negative bacteria. The study evaluated the antimicrobial effects of carvacrol combined with sulfamethoxazole, linezolid, minocycline, and trimethoprim. Methods: The MRSA strain (ATCC-33591) was used, and various assays, including MIC determination, checkerboard assay, and microdilution assay were conducted. Results: The results showed that the combination of carvacrol with antibiotics yielded better outcomes compared to monotherapy, leading to reduced bacterial colonization. Carvacrol, sulfamethoxazole, and trimethoprim exhibited weak anti-staphylococcal effects, while linezolid and minocycline demonstrated stronger effects. This suggests that conventional antibiotic therapy may not be sufficient to effectively treat MRSA infections, potentially causing delays in healing or an exacerbation of the condition. Carvacrol combinations with two antibiotics displayed superior results compared to other pairs, indicating synergistic or additive effects of carvacrol with linezolid, minocycline, and sulfamethoxazole. Conclusion: These findings propose a new approach for developing drug molecules for MRSA treatment which combine volatile oils with available regimens. Further studies are recommended to evaluate the efficacy and biosafety of these combinations using in vivo or ex vivo models, aiming to minimize side effects and facilitate human trials. This study provides valuable insights into the potential use of carvacrol-antibiotic combinations as a novel therapeutic approach against MRSA.
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Cancer is considered one of the top global causes of death. Natural products have been used in oncology medicine either in crude form or by utilizing isolated secondary metabolites. Biologically active phytomolecules such as gallic acid and quercetin have confirmed antioxidant, anti-bacterial, and neoplastic properties. There is an agreement that microorganisms could mediate oncogenesis or alter the immune system. This research project aims to develop a novel formulation of co-loaded gallic acid and quercetin into nanoliposomes and investigate the efficacy of the free and combined agents against multiple cancerous cell lines and bacterial strains. Thin-film hydration technique was adopted to synthesize the nanocarriers. Particle characteristics were measured using a Zetasizer. The morphology of nanoliposomes was examined by scanning electron microscopy, Encapsulation efficiency and drug loading were evaluated using High-Performance Liquid Chromatography. Cytotoxicity was determined against Breast Cancer Cells MCF-7, Human Carcinoma Cells HT-29, and A549 Lung Cancer Cells. The antibacterial activities were evaluated against Acinetobacter baumannii, Escherichia coli, Proteus mirabilis, Pseudomonas aeruginosa, and Staphylococcus aureus. Therapeutic formulas were categorized into groups: free gallic acid, free quercetin, free-mix, and their nano-counterparts. Findings revealed that drug loading capacity was 0.204 for the mix formula compared to 0.092 and 0.68 for free gallic acid and quercetin, respectively. Regarding the Zeta potential, the mix formula showed more amphiphilic charge than the free quercetin and free gallic acid formulas (P-values 0.003 and 0.002 receptively). On the contrary, no significant difference in polydispersity indices was reported. Lung cancerous cells were the most affected by the treatments. The best estimated IC50 values were observed in breast and lung cancer lines for the nano-gallic acid and co-loaded particles. The nano-quercetin formula exhibited the least cytotoxicity with an IC50 value of ≥200 µg/mL in both breast (MCF-7) and colorectal adenocarcinoma cell lines (HT-29) with no activity against the lung. A remarkable improvement in the efficacy of quercetin was measured after mixing it with gallic acid against the breast and lungs. The tested therapeutic agents exhibited antimicrobial activity against gram-positive bacteria. Nano-liposomes can either enhance or reduce the cytotoxicity activity of active compounds depending on the physical and chemical properties of drug-loaded and type of cancer cells.
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Cancer is a major public health problem, and chemotherapy plays a significant role in the management of neoplastic diseases. However, chemotherapy-induced cardiotoxicity is a serious side effect secondary to cardiac damage caused by antineoplastic's direct and indirect toxicity. Currently, there are no reliable and approved methods for preventing or treating chemotherapy-induced cardiotoxicity. Understanding the mechanisms of chemotherapy-induced cardiotoxicity may be vital to improving survival. The independent risk factors for developing cardiotoxicity must be considered to prevent myocardial damage without decreasing the therapeutic efficacy of cancer treatment. This systematic review aimed to identify and analyze the evidence on chemotherapy-induced cardiotoxicity, associated risk factors, and methods to decrease or prevent it. We conducted a comprehensive search on PubMed, Google Scholar, and Directory of Open Access Journals (DOAJ) using the following keywords: "doxorubicin cardiotoxicity", "anthracycline cardiotoxicity", "chemotherapy", "digoxin decrease cardiotoxicity", "ATG7 activators", retrieving 59 articles fulfilling the inclusion criteria. Therapeutic schemes can be changed by choosing prolonged infusion application over boluses. In addition, some agents like Dexrazoxane can reduce chemotherapy-induced cardiotoxicity in high-risk groups. Recent research found that Digoxin, ATG7 activators, Resveratrol, and other medical substances or herbal compounds have a comparable effect on Dexrazoxane in anthracycline-induced cardiotoxicity.
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Antineoplásicos , Dexrazoxano , Policetídeos , Humanos , Resveratrol/farmacologia , Resveratrol/uso terapêutico , Cardiotoxicidade/etiologia , Cardiotoxicidade/prevenção & controle , Antraciclinas , DigoxinaRESUMO
The prevalence of juvenile obesity is increasing, reaching epidemic proportions, presenting a link not only to NAFLD (non-alcoholic fatty liver disease) but to abnormal lipid profiles and liver enzyme abnormalities. Liver ultrasonography is a sensitive and specific tool for the recognition of NAFLD. This study aims to assess the association between NAFLD and juvenile obesity and to determine the other related changes in a set of indicators, including lipid profile abnormalities and serum transaminases. The sample included 470 obese and 210 non-obese individuals aged 6-16. Anthropometric measures were assessed, with the serum lipid profile and liver transaminases, and abdominal ultrasonography was used to detect NAFLD. Fatty liver was found in 38% of the obese subjects and none of the non-obese subjects. Within obese subjects, mean body mass index (BMI) and waist circumference increased significantly in patients with NAFLD compared to those without fatty liver. Moreover, LDL (low-density lipoprotein), CHOL (cholesterol), and serum liver enzymes were significantly higher in the presence of NAFLD. In conclusion, NAFLD commonly associates with juvenile obesity, relating to obesity and the abnormal lipid profile (including elevated CHOL and LDL) among obese people, reflecting elevated liver transaminases, which increase the risk of cirrhosis.
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Hepatopatia Gordurosa não Alcoólica , Humanos , Obesidade , Transaminases , LipídeosRESUMO
Traditional healers are often practiced in rural areas owing to cultural beliefs and are known to provide various forms of healthcare and home remedies. Patients in the Mediterranean region rely on traditional medicine to cure a variety of health concerns, like skin burns. This study was conducted to identify the various practices used by traditional healers for treating skin burns. The survey was conducted in 18 Arab countries, including Syria, Iraq, Jordan, Saudi Arabia, Egypt, United Arab Emirates, Algeria, Bahrain, Palestine, Kuwait, Oman, Qatar, Lebanon, Yemen, Tunisia, Oman, Morocco, and Sudan. Between September 2020 and July 2021, an online questionnaire was administered to 7530 participants from 12 Asian and 5 African countries. The survey was designed to gather information from common medicinal plant users and herbalists on their practices as specialists in using various herbal and medicinal plant products for diagnosis and treatment. Among the participants, 2260 had a scientific background in plant application, and the study included one phytotherapeutic professional. The crude-extraction technique was favored, by Arabic folk, for plant preparation over the maceration and decoction method. Olive oil was the most commonly used product among participants as an anti-inflammation and for scar reduction. Aloe vera, olive oil, sesame, Ceretonia siliqua, lavender, potato, cucumber, shea butter, and wheat flour are used as crude drugs to reduce pain because of their analgesic and cooling effects. The present study is the first database of medicinal plants with burn-healing properties conducted in Arab countries. These plants can be employed in the search for new bioactive substances through pharmacochemical investigations, as well as in the development of new formulations containing a combination of these plants.
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Queimaduras , Plantas Medicinais , Humanos , Mundo Árabe , Farinha , Queimaduras/tratamento farmacológico , Triticum , LíbanoRESUMO
Cosmetics, cosmeceuticals, and variable healthcare products used parabens, among other excipients, for their preservative and antimicrobial activities. Paraben derivatives exhibit distinguished physiochemical properties that enable them to be compatible with the formulation of cosmetic agents in different dosage forms. In addition to their potency and efficacy, parabens are economically efficient as they have low-manufacturing costs. Despite the desirable characteristics, the safety of parabens use is controversial after detecting these chemicals in various biological tissues after repetitive and long-term use of formulations containing them. The use of parabens drew public health attention after scientific reports linked skin exposure to parabens with health issues, in particular, breast cancer. In response, worldwide authorities set regulations for the allowance concentrations of paraben to be used in variable cosmetic products.
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Cosmecêuticos , Cosméticos , Cosmecêuticos/efeitos adversos , Cosméticos/química , Excipientes , Humanos , Parabenos/efeitos adversos , Conservantes Farmacêuticos/efeitos adversosRESUMO
Introduction: Helicobacter pylori is Gram-negative helical bacteria that inhibit stomach mucosal lining and establish infection. Urease enzyme was confirmed to be pivotal target in which its suppression will prompt bacteria treatment and eradication. Methods: Series of naturally bioactive compounds were selected based on ethnobotanical and molecular modeling techniques with potential urease inhibitory effect. The selected phytochemical compounds were in-silico and in-vitro assayed against urease enzyme, minimal inhibitory concentrations (MIC) and a synergistic effect was studied and cultured specifically for H. pylori. Results: Terpineol was considered as the most active compound with an IC50 of 1.443 µg/ml (R 2 = 0.9374). The synergistic effect of terpineol and metronidazole indicated a possible additive effect (fractional inhibitory concentration result is 0.78) with improvement of MIC results for both terpineol and metronidazole. Conclusion: This study suggests that terpineol is best to be considered as a lead compound for H. pylori infection treatment and could be a potent inhibitor when combined with metronidazole targeting urease enzyme.
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BACKGROUND: Nutrients are widely used for treating illnesses in traditional medicine. Ginger has long been used in folk medicine to treat motion sickness and other minor health disorders. Chronic non-healing wounds might elicit an inflammation response and cancerous mutation. Few clinical studies have investigated 6-gingerol's wound-healing activity due to its poor pharmacokinetic properties. However, nanotechnology can deliver 6-gingerol while possibly enhancing these properties. Our study aimed to develop a nanophytosome system loaded with 6-gingerol molecules to investigate the delivery system's influence on wound healing and anti-cancer activities. METHODS: We adopted the thin-film hydration method to synthesize nanophytosomes. We used lipids in a ratio of 70:25:5 for DOPC(dioleoyl-sn-glycero-3-phosphocholine): cholesterol: DSPE/PEG2000, respectively. We loaded the 6-gingerol molecules in a concentration of 1.67 mg/mL and achieved size reduction via the extrusion technique. We determined cytotoxicity using lung, breast, and pancreatic cancer cell lines. We performed gene expression of inflammation markers and cytokines according to international protocols. RESULTS: The synthesized nanophytosome particle sizes were 150.16 ± 1.65, the total charge was -13.36 ± 1.266, and the polydispersity index was 0.060 ± 0.050. Transmission electron microscopy determined the synthesized particles' spherical shape and uniform size. The encapsulation efficiency was 34.54% ± 0.035. Our biological tests showed that 6-gingerol nanophytosomes displayed selective antiproliferative activity, considerable downregulation of inflammatory markers and cytokines, and an enhanced wound-healing process. CONCLUSIONS: Our results confirm the anti-cancer activity of PEGylated nanophytosome 6-gingerol, with superior activity exhibited in accelerating wound healing.
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Catecóis , Álcoois Graxos , Álcoois Graxos/farmacologia , Catecóis/farmacocinética , Tamanho da Partícula , CicatrizaçãoRESUMO
BACKGROUND: Medicinal plants have proven their value as a source of molecules with therapeutic potential, and recent studies have shown that capsaicin has profound anticancer effects in several types of human cancers. However, its clinical use is handicapped due to its poor pharmacokinetics. This study aims to enhance capsaicin's pharmacokinetic properties by loading the molecule into nanoliposomes model and testing its anticancer activity. METHODS: Nanoliposomes were prepared using the thin-film method, and characteristics were examined followed by qualitative and quantitative analyses of encapsulation efficiency and drug loading using HPLC at different lipid/capsaicin ratios. Cell viability assay (MTT) was used to determine IC50. RESULTS: Capsaicin-loaded nanoliposomes showed optimum characteristics of morphology, particle size, zeta potential, and stability. In vitro anticancer activity of capsaicin and capsaicin-loaded nanoliposomes were compared against MCF7, MDA-MB-231, K562, PANC1, and A375 cell lines. Capsaicin-loaded nanoliposomes showed significant improvement in anticancer activity against cancers cell lines studied (p < 0.001), with increased selectivity against cancer cells compared to capsaicin. CONCLUSION: The encapsulated capsaicin nanoliposomes produced an improvement in pharmacokinetics properties, enhancing the anticancer activity and selectivity compared with capsaicin. This model seems to offer a potential for developing capsaicin formulations for the prevention and treatment of cancer.
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Antineoplásicos/farmacologia , Capsaicina/farmacologia , Lipossomos/farmacologia , Nanopartículas/química , Antineoplásicos/química , Capsaicina/química , Capsicum/química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Liberação Controlada de Fármacos , Humanos , Lipossomos/química , Células MCF-7 , Tamanho da PartículaRESUMO
Capsaicin (CAP) is an active component in Capsicum annuum L. known to have anti inflammatory and anticancer activity. CAP is highly lipophilic and suffers low bioavailability. Therefore, developing delivery systems that enhance solubility and bioavailability can provide more promising therapeutic applications for CAP. In the current work, CAP was complexed with ß-cyclodextrin (ßCD) to form capsaicin-in-ß-cyclodextrin (CAP-in-ßCD) inclusion complexes. Then, the CAP-in-ßCD inclusion complexes were characterized and loaded into PEGylated liposomes using the thin-film hydration extrusion method. The size, charge, and polydispersity index (PDI) of the PEGylated liposomes were characterized. The levels of IL-8 production were quantified after treatment using array beads. The results of this work showed that the successful formation of inclusion complexes at 1:5 M ratio of CAP to ßCD respectively. PEGylated liposomes loaded with ßCD/CAP inclusion complexes (CAP-in-ßCD-in-liposomes) have a hydrodynamic diameter of (181 ± 36) nm, zeta potential of (-2.63 ± 4.00) mV, encapsulation efficiency (EE) of (38.65 ± 3.70)%, drug loading (DL) of (1.65 ± 0.16)%, and a stable release profile. Both free CAP and liposomal CAP showed a significant reduction in the IL-8 production by the MDA-MB-231 and A549 cancer cell lines after treatment. In conclusion, a liposomal-based drug delivery system for CAP was achieved.
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Ciclodextrinas , Neoplasias , Capsaicina/farmacologia , Linhagem Celular , Interleucina-8 , Lipossomos , Polietilenoglicóis , SolubilidadeRESUMO
BACKGROUND: The qualified and paradigm jump in the formulation and production of cosmeceuticals refer in some way to the great revolution in nanotechnology. Nowadays, the industry of nano-formulated cosmeceuticals plays a significant and essential role in the evolution and growth of the pharmaceutical industries. This review manuscript focuses on the use of nanocarriers in delivering the cosmetic agents into the target area such as skin, hair, and nails. METHODS: Many steps were performed in the preparation of this review including identification of different classes of nanocarriers for delivery of nanocosmeceuticals, literature survey of relevantstudies regarding the applications of nanotechnology in cosmeceuticals and their toxicological effects. RESULTS: When nanoparticles introduced in the cosmetic industry, the quality and the elegance of the final products were raised significantly. Sadly, this revolution is accompanied by many health hazards as these tiny molecules can penetrate intact skin barriers and cause undesired effects. Cosmeceuticals with nanotechnology include sunscreens, hair cleansing products, nail products, and agents fighting fine lines. CONCLUSIONS: The expansion and growth of the cosmetic industry and the introduction of nanotechnology in cosmeceuticals industry necessitates the urgent need for scientific research investigating their efficacy, safety profile and use.
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Cosmecêuticos , Cosméticos , Nanopartículas , Humanos , Nanotecnologia , PeleRESUMO
BACKGROUND: Poly lactic acid and its copolymers are considered to be the preferred substrates for drug delivery devices. Poly lactic acid is a biocompatible, biodegradable and nontoxic polymer. It was approved by Food and Drug Administration and thought to be among the most attractive polymeric candidates intended for controlling drug delivery. It was utilized for the development of devices for the delivery of small molecules, proteins, genes, vaccines, anticancer drugs, and macromolecules. OBJECTIVES AND METHODS: This manuscript lists the different techniques for synthesizing poly lactic acid-based nano and microparticles such as emulsion-based methods, precipitation-based methods, direct compositing methods, in situ forming micro-particles, and microfluidic technique. CONCLUSIONS: In addition, it describes the application and use of poly lactic acid in biomedical and cosmetic delivery systems.