Liposome-based drug delivery of various anticancer agents of synthetic and natural product origin: a patent overview

2020 ◽  
Vol 9 (3) ◽  
pp. 87-116
Author(s):  
Naseem Akhtar ◽  
Salman AA Mohammed ◽  
Varsha Singh ◽  
Ahmed AH Abdellatif ◽  
Hamdoon A Mohammad ◽  
...  

Phospholipid-based liposomal vesicles are among the most effective delivery options currently available for various classes of anticancer drugs. The patents granted to inventions disclosing details on liposomal delivery module by the US Patent and Trademark Office, European Patent Office, and world patent holdings through WIPO (World Intellectual Property Organization) patenting have been sorted based upon liposome, and anticancer keywords within the abstract and claims sections of the patents for the period between 2000 and 2019, thereby disclosing novel liposome formulations encapsulating single, or combination of chemotherapeutic agents that have been far more chemically and physiologically stable, therapeutically efficacious, and comparatively less toxic than their nonliposomal free-drug counterparts. The added stability, site-specific transport, and payload delivery, enhanced bioavailability, fast body clearance, and biocompatibility together with the controlled and sustained delivery-related benefits claimed in the patent literature have been exclusively discussed with a focus on the last 5-year period.

Author(s):  
Janaina Martins Oliveira Soares ◽  
Leisson Domingues Pinheiro ◽  
Maurícia Macedo Ramalho ◽  
Ítalo Flexa Di Paolo

Resumo: Este trabalho desperta uma análise das evoluções nas pesquisas e desenvolvimento de patentes no tratamento do clareamento da Melanose. O objetivo da pesquisa é realizar um levantamento de documentos de patentes existentes sobre gel facial a base de bicarbonato e clara de ovo para tratamento de melasma, nas modalidades de invenção ou modelo de utilidade, quanto à titularidade, nacionalidade e sua inserção no mercado. A metodologia empregada foi à busca na base de dados States Patente and Trademark Office (USPTO), Instituto Nacional de Propriedade Intelectual (INPI), Escritório Europeu de Patentes (EPO) e World Intellectual Property Organization (WIPO). Foi realizada a seleção dos documentos de interesse através de análise de seus resumos. Observa-se que a maioria das pesquisas realizadas no Brasil gera um número insuficiente de registro de propriedade ou são pouco voltadas para o mercado. O referido estudo foi de significativa relevância para o desenvolvimento do conhecimento sobre o produto almejado, e quais os meios dentro da Legislação vigente para proteger a criação e inovação tecnológica.Descritores: Patentes, Melanose, Documentos, Tecnologia de Produtos. Patent registration of facial gel based on sodium bicarbonate and egg white for melasma treatmentAbstract: This article arouses an analysis of the evolutions in the research and development of patents in the treatment of the bleaching of Melanose. The objective of the research is to data survey of existing patent documents on facial gel based on sodium bicarbonate and egg white for the treatment of melasma, in the invention modalities or utility model, regarding ownership, nationality and the insertion in the market. The methodology used was to search the US Patent and Trademark Office (USPTO), the National Intellectual Property Institute (INPI), The European Patent Office (EPO) and the World Intellectual Property Organization (WIPO). The selection of the documents of interest was done through analysis of their abstracts. It is observed that most of the research carried out in Brazil generates an insufficient number of property registration or it is not very market oriented. This study was of significant relevance for the development of knowledge about the product targeted, and which means within the current legislation to protect the creation and technological innovation.Descriptors: Patents, Melanose, Documents, Product Technology. Registros de patentes de gel facial a base de bicarbonato de sodio y clara de huevo para tratamiento de melasmaResumen: Este trabajo despierta un análisis de las evoluciones en las investigaciones y desarrollo de patentes en el tratamiento del blanqueamiento de la melanosis. El objetivo de la investigación es realizar un levantamiento de documentos de patentes existentes sobre gel facial a base de bicarbonato y clara de huevo para tratamiento de melasma, en las modalidades de invención o modelo de utilidad, en cuanto a la titularidad, nacionalidad y su inserción en el mercado. La metodología empleada fue la búsqueda en la base de datos de los Estados Unidos de la Patente y Trademark Office (USPTO), el Instituto Nacional de Propiedad Intelectual (INPI), la Escritório Europeu de Patentes (EPO) y World Intellectual Property Organization (WIPO). Fue realizada la selección de los documentos de interés a través del análisis de sus resúmenes. Se observa que la mayoría de las investigaciones realizadas en Brasil generan un número insuficiente de registro de propiedad o son poco orientadas hacia el mercado. Este estudio fue de significativa relevancia para el desarrollo del conocimiento sobre el producto deseado, y cuáles los medios dentro de la Legislación vigente para proteger la creación e innovación tecnológica.Descriptores: Patentes, Melanosis, Documentos, Tecnología de Productos.


Author(s):  
Janaina Martins Oliveira Soares ◽  
Leisson Domingues Pinheiro ◽  
Maurícia Macedo Ramalho ◽  
Ítalo Flexa Di Paolo

Resumo: Este trabalho desperta uma análise das evoluções nas pesquisas e desenvolvimento de patentes no tratamento do clareamento da Melanose. O objetivo da pesquisa é realizar um levantamento de documentos de patentes existentes sobre gel facial a base de bicarbonato e clara de ovo para tratamento de melasma, nas modalidades de invenção ou modelo de utilidade, quanto à titularidade, nacionalidade e sua inserção no mercado. A metodologia empregada foi à busca na base de dados States Patente and Trademark Office (USPTO), Instituto Nacional de Propriedade Intelectual (INPI), Escritório Europeu de Patentes (EPO) e World Intellectual Property Organization (WIPO). Foi realizada a seleção dos documentos de interesse através de análise de seus resumos. Observa-se que a maioria das pesquisas realizadas no Brasil gera um número insuficiente de registro de propriedade ou são pouco voltadas para o mercado. O referido estudo foi de significativa relevância para o desenvolvimento do conhecimento sobre o produto almejado, e quais os meios dentro da Legislação vigente para proteger a criação e inovação tecnológica.Descritores: Patentes, Melanose, Documentos, Tecnologia de Produtos. Patent registration of facial gel based on sodium bicarbonate and egg white for melasma treatmentAbstract: This article arouses an analysis of the evolutions in the research and development of patents in the treatment of the bleaching of Melanose. The objective of the research is to data survey of existing patent documents on facial gel based on sodium bicarbonate and egg white for the treatment of melasma, in the invention modalities or utility model, regarding ownership, nationality and the insertion in the market. The methodology used was to search the US Patent and Trademark Office (USPTO), the National Intellectual Property Institute (INPI), The European Patent Office (EPO) and the World Intellectual Property Organization (WIPO). The selection of the documents of interest was done through analysis of their abstracts. It is observed that most of the research carried out in Brazil generates an insufficient number of property registration or it is not very market oriented. This study was of significant relevance for the development of knowledge about the product targeted, and which means within the current legislation to protect the creation and technological innovation.Descriptors: Patents, Melanose, Documents, Product Technology. Registros de patentes de gel facial a base de bicarbonato de sodio y clara de huevo para tratamiento de melasmaResumen: Este trabajo despierta un análisis de las evoluciones en las investigaciones y desarrollo de patentes en el tratamiento del blanqueamiento de la melanosis. El objetivo de la investigación es realizar un levantamiento de documentos de patentes existentes sobre gel facial a base de bicarbonato y clara de huevo para tratamiento de melasma, en las modalidades de invención o modelo de utilidad, en cuanto a la titularidad, nacionalidad y su inserción en el mercado. La metodología empleada fue la búsqueda en la base de datos de los Estados Unidos de la Patente y Trademark Office (USPTO), el Instituto Nacional de Propiedad Intelectual (INPI), la Escritório Europeu de Patentes (EPO) y World Intellectual Property Organization (WIPO). Fue realizada la selección de los documentos de interés a través del análisis de sus resúmenes. Se observa que la mayoría de las investigaciones realizadas en Brasil generan un número insuficiente de registro de propiedad o son poco orientadas hacia el mercado. Este estudio fue de significativa relevancia para el desarrollo del conocimiento sobre el producto deseado, y cuáles los medios dentro de la Legislación vigente para proteger la creación e innovación tecnológica.Descriptores: Patentes, Melanosis, Documentos, Tecnología de Productos.


2020 ◽  
Vol 26 (41) ◽  
pp. 7452-7475 ◽  
Author(s):  
Marta A. Andrade ◽  
Luísa M.D.R.S. Martins

: The development of safe and effective chemotherapeutic agents is one of the uppermost priorities and challenges of medicinal chemistry and new transition metal complexes are being continuously designed and tested as anticancer agents. Scorpionate ligands have played a great role in coordination chemistry, since their discovery by Trofimenko in the late 1960s, with significant contributions in the fields of catalysis and bioinorganic chemistry. Scorpionate metal complexes have also shown interesting anticancer properties, and herein, the most recent (last decade) and relevant scorpionate complexes reported for application in medicinal chemistry as chemotherapeutic agents are reviewed. The current progress on the anticancer properties of transition metal complexes bearing homo- or hetero- scorpionate ligands, derived from bis- or tris-(pyrazol-1-yl)-borate or -methane moieties is highlighted.


2019 ◽  
Vol 19 (10) ◽  
pp. 765-781
Author(s):  
Seema Rohilla ◽  
Harish Dureja ◽  
Vinay Chawla

Anticancer agents play a vital role in the cure of patients suffering from malignancy. Though, the chemotherapeutic agents are associated with various adverse effects which produce significant toxic symptoms in the patients. But this therapy affects both the malignant and normal cells and leads to constricted therapeutic index of antimalignant drugs which adversely impacts the quality of patients’ life. Due to these adversities, sufficient dose of drug is not delivered to patients leading to delay in treatment or improper treatment. Chemoprotective agents have been developed either to minimize or to mitigate the toxicity allied with chemotherapeutic agents. Without any concession in the therapeutic efficacy of anticancer drugs, they provide organ specific guard to normal tissues.


2018 ◽  
Vol 15 (2) ◽  
pp. 179-207
Author(s):  
Ashaparna Mondal ◽  
Priyankar Paira

Background: Currently ruthenium complexes are immerging as effective anticancer agents due to their less toxicity, better antiproliferative and antimetastatic activity, better stability in cellular environment and most importantly variable oxidation and co-ordination states of ruthenium allows binding this molecule with a variety of ligands. So in past few years researchers have shifted their interest towards organoruthenium complexes having good fluorescent profile that may be applicable for cancer theranostics. Nowadays, photodynamic therapy has become more acceptable because of its easy and effective approach towards killing cancer cells. Objective: Objective of this review article is to shed light on synthesis, characterization, stability and fluorescence studies of various ruthenium [Ru(II) and Ru(III)] complexes and different bioactivity studies conducted with the synthesized compounds to test their candidacy as potent chemotherapeutic agents. Methods: Various heterocyclic ligands containing N,O and S as heteroatom mainly were prepared and subjected to complexation with ruthenium-p-cymene moiety. In most cases [Ru(η6-p-cymene)(µ-Cl)Cl]2 was used as ruthenium precursor and the reactions were conducted in various alcohol medium such as methanol, ethanol or propanol. The synthesized complexes were characterized by 1H NMR and 13C NMR spectroscopy, GC-MS, ESI-MS, elemental analysis and single crystal X-ray crystallography methods. Fluorescence study and stability study were conducted accordingly using water, PBS buffer or DMSO. Stable compounds were considered for cell viability studies. To study the efficacy of the compounds in ROS generation as photosensitizers, in few cases, singlet oxygen quantum yields in presence of light were calculated. Suitable compounds were selected for in vitro & in vivo antiproliferative, anti-invasive activity studies. Result: Many newly synthesized compounds were found to have less IC50 compared to a standard drug cysplatin. Those compounds were also stable preferably in physiological conditions. Good fluorescence profile and ROS generation ability were observed for few compounds. Conclusion: Numerous ruthenium complexes were developed which can be used as cancer theranostic agents. Few molecules were synthesized as photosensitizers which were supposed to generate reactive singlet oxygen species in targeted cellular environment in presence of a particular type of light and thereby ceasing cancer cell growth.


2020 ◽  
Vol 26 (1) ◽  
pp. 6-13 ◽  
Author(s):  
Ulviye Acar Çevik ◽  
Derya Osmaniye ◽  
Serkan Levent ◽  
Begüm Nurpelin Sağlik ◽  
Betül Kaya Çavuşoğlu ◽  
...  

AbstractCancer is one of the most common causes of death in the world. Despite the importance of combating cancer in healthcare systems and research centers, toxicity in normal tissues and the low efficiency of anticancer drugs are major problems in chemotherapy. Nowadays the aim of many medical research projects is to discover new safer and more effective anticancer agents. 1,3,4-Thiadiazole compounds are important fragments in medicinal chemistry because of their wide range of biological activities, including anticancer activities. The aim of this study was to determine the capacity of newly synthesized 1,3,4-thiadiazole compounds as chemotherapeutic agents. The structures of the obtained compounds were elucidated using 1H-NMR, 13C-NMR and mass spectrometry. Although the thiadiazole derivatives did not prove to be significantly cytotoxic to the tumour tissue cultures, compound 4i showed activity against the C6 rat brain cancer cell line (IC50 0.097 mM) at the tested concentrations.


2016 ◽  
Vol 9 (2) ◽  
pp. 219 ◽  
Author(s):  
Lilia Calheiros de Oliveira Barretto ◽  
Joicy Manuela Vilanova Gois ◽  
Dian Souza De Oliveira ◽  
Gennaro Junho Gama ◽  
Gabriel Francisco Da Silva ◽  
...  

A Moringa oleifera Lam. é uma espécie arbórea originária do noroeste indiano, cultivada graças ao seu valor alimentar, alto teor proteico, usos na medicina tradicional, indústria e tratamento de água para o consumo humano. Por apresentar tais características, a moringa tem um grande potencial para cultivo comercial. As características de adaptação climática e de solo da planta a tornam implementável como cultivo tanto em escala industrial quanto de subsistência em grandes extensões do território brasileiro. O presente trabalho objetivou avaliar os resultados de pesquisa relativos às aplicações da moringa na tecnologia de alimentos através de pedidos de patentes. Utilizou-se as bases World Intellectual Property Organization (WIPO), Instituto Nacional de Propriedade Industrial (INPI) e European Patent Office (Espacenet). O período coberto por esta pesquisa baseia-se no período máximo permitido por cada base de dado consultada, e é corrente ao mês de outubro de 2013.


2021 ◽  
Vol 10 (14) ◽  
pp. e333101422076
Author(s):  
Nathália Andrezza Carvalho de Souza ◽  
Victória Laysna dos Anjos Santos ◽  
Tarcísio Cícero de Lima Araújo ◽  
Pedrita Alves Sampaio ◽  
Renata Rivelli Menezes de Souza ◽  
...  

The genus Mikania (Asteraceae) comprises about 450 species of these, 203 are found in Brazil and present several chemical and biological activities. Considering the variety of species and their therapeutic properties, the present study aimed to perform technological prospecting of this genus, since this approach aims to contribute to technological, scientific and innovation research. For this purpose, the patent documents were analyzed, regarding the applicant countries, year of filing and the international classification of patents of the genus Mikania. The search was conducted in the databases World Intellectual Property Organization (WIPO), European Patent Office (EPO) and the National Institute of Industrial Property (INPI) in October 2020, using the descriptor “Mikania”; present in the title and/or abstract in addition, documents that included medicinal approaches were selected. Thus, taking into consideration the filing countries, Japan, Brazil and the United States led the patent deposits, with the first document filed in 1991 and the largest number of applications in the years 2000 and 2010. The data concerning the international patent classification are concentrated in subclass A61K, which deals with preparations for medical, dental or hygienic purposes. These results demonstrated the therapeutic and technological potential of the Mikania species and thus which can be evidenced the potential of this study.


2002 ◽  
Vol 2 (3) ◽  
pp. 124-130 ◽  
Author(s):  
William L. Rust ◽  
Stephen W. Carper ◽  
George E. Plopper

This review will briefly describe integrin function, address why integrins are attractive targets for chemotherapeutic drug design, and discuss some ongoing studies aimed at inhibiting integrin activity. Integrins are cell surface heterodimeric receptors. They modulate many cellular processes including: growth, death (apoptosis), adhesion, migration, and invasion by activating several signaling pathways. Many potential chemotherapeutic agents target integrins directly (eg, polypeptides, monoclonal antibodies, adenovirus vectors). These agents may be clinically useful in controlling the metastatic spread of cancer.


Cancers ◽  
2018 ◽  
Vol 10 (10) ◽  
pp. 346 ◽  
Author(s):  
Elizabeth Varghese ◽  
Samson Samuel ◽  
Mariam Abotaleb ◽  
Sohaila Cheema ◽  
Ravinder Mamtani ◽  
...  

Among the different types of breast cancers, triple-negative breast cancers (TNBCs) are highly aggressive, do not respond to conventional hormonal/human epidermal growth factor receptor 2 (HER2)-targeted interventions due to the lack of the respective receptor targets, have chances of early recurrence, metastasize, tend to be more invasive in nature, and develop drug resistance. The global burden of TNBCs is increasing regardless of the number of cytotoxic drugs being introduced into the market each year as they have only moderate efficacy and/or unforeseen side effects. Therefore, the demand for more efficient therapeutic interventions, with reduced side effects, for the treatment of TNBCs is rising. While some plant metabolites/derivatives actually induce the risk of cancers, many plant-derived active principles have gained attention as efficient anticancer agents against TNBCs, with fewer adverse side effects. Here we discuss the possible oncogenic molecular pathways in TNBCs and how the purified plant-derived natural compounds specifically target and modulate the genes and/or proteins involved in these aberrant pathways to exhibit their anticancer potential. We have linked the anticancer potential of plant-derived natural compounds (luteolin, chalcones, piperine, deguelin, quercetin, rutin, fisetin, curcumin, resveratrol, and others) to their ability to target multiple dysregulated signaling pathways (such as the Wnt/β-catenin, Notch, NF-κB, PI3K/Akt/mammalian target of rapamycin (mTOR), mitogen-activated protein kinase (MAPK) and Hedgehog) leading to suppression of cell growth, proliferation, migration, inflammation, angiogenesis, epithelial-mesenchymal transition (EMT) and metastasis, and activation of apoptosis in TNBCs. Plant-derived compounds in combination with classical chemotherapeutic agents were more efficient in the treatment of TNBCs, possibly with lesser side effects.


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