RESUMEN
Cancer has a significant social consequence all around the globe. In 2020, approximately 19.3 million new cases of cancer were diagnosed worldwide, with about 10 million cancer deaths. In the next two decades, suspected cases are anticipated to increase by roughly 47%. The rising number of cancer patients, as well as the inadequacy of traditional chemotherapeutic agents, radiation, and invasive surgical procedures, all rely on massive cell death with hardly any selectivity, causing severe toxicities. In comparison to synthetic medications, there has subsequently been a surge in international interest in non-synthetic and alternative remedies, owing to improved adaptability and reduced side effects of drug responses. Several people with cancer prefer alternative and complementary therapy treatments, and natural remedies play a crucial role in cancer chemoprevention as they are thought to be harmless, offer fewer negative effects, and become less sufficient to evoke addiction by the wider population. Chemopreventive, antimetastatic, cytotoxic, and anti-angiogenic actions are among the promising clinical advantages, which have been established in vitro research and certain clinical trials; nevertheless, additional clinical trials are needed. This review examines several phytochemicals that may have anti-cancer and chemopreventive properties.
Asunto(s)
Antineoplásicos , Neoplasias , Humanos , Fitoquímicos/farmacología , Fitoquímicos/uso terapéutico , Fitoquímicos/química , Neoplasias/tratamiento farmacológico , Neoplasias/prevención & control , Quimioprevención/métodos , Antineoplásicos/farmacología , Antineoplásicos/uso terapéuticoRESUMEN
Tyrosine kinases are known to play a role in tumour growth and proliferation, and they have become common drug targets. Tyrosine kinase inhibitors (TKIs) prohibit associated kinases from phosphorylating tyrosine residues in their substrates, preventing downstream signaling pathways from being activated. Multiple robust and well-tolerated TKIs targeting single or multiple targets, including EGFR, ALK, ROS1, HER2, NTRK, VEGFR, RET, MET, MEK, FGFR, PDGFR, and KIT, have been developed over the last two decades, contributing to our understanding of precision cancer medicine based on a patient's genetic alteration profile. The epidermal growth factor receptor (EGFR) family consists of four transmembrane tyrosine kinases (EGFR1/ErbB1, Her2/ErbB2, Her3/ErbB3, and Her4/ErbB4) and thirteen polypeptide ligands produced by them. Multiple solid tumours, including breast, pancreatic, head and neck, kidney, vaginal, renal, colon, and non-small cell lung cancer, overexpress EGFRs. Overexpression of these genes stimulates downstream signaling channels, causing cell proliferation, differentiation, cell cycle progression, angiogenesis, cell motility, and apoptosis inhibition. EGFRs' high expression and/or adaptive activation coincide with the pathogenesis and development of many tumours, making them appealing candidates for both diagnosis and therapy. Several strategies for targeting these receptors and/or the EGFR-mediated effects in cancer cells have been established. The majority of methods include the development of anti-EGFR antibodies and/or small-molecule EGFR inhibitors. This review presents the recent advances in EGFR TKIs and their role in the treatment of cancer.
Asunto(s)
Carcinoma de Pulmón de Células no Pequeñas , Neoplasias Pulmonares , Humanos , Femenino , Carcinoma de Pulmón de Células no Pequeñas/tratamiento farmacológico , Neoplasias Pulmonares/tratamiento farmacológico , Proteínas Proto-Oncogénicas , Inhibidores de Proteínas Quinasas/farmacología , Inhibidores de Proteínas Quinasas/uso terapéutico , Quinasas de Proteína Quinasa Activadas por Mitógenos , Tirosina/uso terapéuticoRESUMEN
Herbal medicines are being used by humans since the oldest civilizations and have been an integral part of traditional and alternative medicines. In recent times, pharmaceutical and biomedical scientists are taking interest in developing nutraceutical-based medicines to overcome the side effects and adverse drug reactions caused by allopathic medicines. Nutraceuticals have started occupying the global market. Nutraceuticals have gained widespread acceptance due to their efficacy in treating difficult to treat diseases, low toxicity, low cost, easy accessibility, etc. Safety and efficacy are other important factors in the commercialization process of nutraceuticals. Different novel advanced drug delivery systems have been constantly studied to improve the efficacy and bioavailability of medicines obtained from herbal sources. The transdermal drug delivery system provides a potent alternative to the conventional method of using nutraceuticals. The development of transdermal system-based nutraceuticals could provide the advantage of enhanced bioavailability, improved solubility, bypass of the first-pass metabolism, and targeted delivery of drugs in brain-related disorders. It additionally provides the advantage of being non-invasive. This article reviews the potential effects of various nutraceuticals in brain-related disorders as well as trends in transdermal nano-systems to deliver such nutraceuticals. We have also focused on advantages, applications as well as recent United States-based patents which emphasize emerging interest towards transdermal nutraceuticals in brain disorders.
Asunto(s)
Enfermedades del Sistema Nervioso Central , Suplementos Dietéticos , Disponibilidad Biológica , Sistemas de Liberación de Medicamentos , HumanosRESUMEN
BACKGROUND: Carvedilol, the anti-hypertensive drug, has poor bioavailability when administered orally. Ethosomes-mediated transdermal delivery is considered a potential route of administration to increase the bioavailability of carvedilol. The central composite design could be used as a tool to optimize ethosomal formulation. Thus, this study aims to optimize carvedilol-loaded ethosomes using central composite design, followed by incorporation of synthesized ethosomes into hydrogels for transdermal delivery of carvedilol. RESULTS: The optimized carvedilol-loaded ethosomes were spherical in shape. The optimized ethosomes had mean particle size of 130 ± 1.72 nm, entrapment efficiency of 99.12 ± 2.96%, cumulative drug release of 97.89 ± 3.7%, zeta potential of - 31 ± 1.8 mV, and polydispersity index of 0.230 ± 0.03. The in-vitro drug release showed sustained release of carvedilol from ethosomes and ethosomal hydrogel. Compared to free carvedilol-loaded hydrogel, the ethosomal gel showed increased penetration of carvedilol through the skin. Moreover, ethosomal hydrogels showed a gradual reduction in blood pressure for 24 h in rats. CONCLUSIONS: Taken together, central composite design can be used for successful optimization of carvedilol-loaded ethosomes formulation, which can serve as the promising transdermal delivery system for carvedilol. Moreover the carvedilol-loaded ethosomal gel can extend the anti-hypertensive effect of carvedilol for a longer time, as compared to free carvedilol, suggesting its therapeutic potential in future clinics.