The objective of the present study is to develop and evaluate microsphere and tablet in capsule s... more The objective of the present study is to develop and evaluate microsphere and tablet in capsule system for the treatment of rheumatoid arthritis as a dual pulse release system. The capsule system contains enteric coated cap filled with microspheres (sustained release) that lock the impermeable capsule body (coated with ethyl cellulose). The capsule body consists of diclofenac sodium loaded core tablet in the bottom (immediate release), which is sealed with swellable hydrogel plug tablet. Formulations selected for capsule system were MP1 due to least particle size (90.44±0.20 μm) and maximum cumulative release (91.49±0.20 %), T3 for least disintegration time (4±0.040 min) and maximum cumulative release (85.50±0.09 %) and HP2 for maintenance of lag phase that was 6 h and in vitro study was Performed. This formulation included two pulses in one system for reduction of dose frequency and better treatment of night pain and morning stiffness in rheumatoid arthritis patients.
Cardiovascular & Hematological Agents in Medicinal Chemistry
: Surgery, radiation, chemotherapy, and targeted therapy were the four basic kinds of cancer trea... more : Surgery, radiation, chemotherapy, and targeted therapy were the four basic kinds of cancer treatment until recently. Immuno-oncology (IO), or the concept that cancer cells were damaged by activating the body's immune system, has emerged and is explained as a unique and crucial method for treating different cancers over the last decade. The US Food and Drug Administration and the European Medicines Agency both approved this newly recognized way of treating cancer in 2020. Within IO, different therapeutic classes have arisen, which are the subject of this article. Immune checkpoint inhibitors are currently the most well-known therapeutic class of immuno-oncology medications due to their amazing ability to show efficacy in a variety of tumor types. Biomarkers were tested for different tumors like gastrointestinal cancer, whole Head, lower and upper part Neck cancer, and also cervical cancer by programmed death-ligand 1 (PD-L1) check point and their targets and are currently being utilized prior to treatment by using Pembrolizumab. However, the significance of PD-L1 expression for immune check point reticence therapy in other/different onco-cancer types remains unclear. Homogenized immuneoncology drugs with regular therapy have been recently studied and clinical efficacy outcomes have shown to be significantly improved. While IO agents are fast transforming the marketed treatment for cancer patients, there are still a number of obstacles to overcome in terms of associating their adverse effects and confirming those different healthcare systems, such as financing these expensive therapies. In addition to cancer vaccines and chimeric antigen receptor T-cell treatments, other IO drugs are in pipeline containing chimeric antigen receptor T-cell therapies; earlier ones have their own set of toxicities and high cost related challenges.
Lung cancer is a heterogeneous group of malignancies with high incidence worldwide. It is the mos... more Lung cancer is a heterogeneous group of malignancies with high incidence worldwide. It is the most frequently occurring cancer in men and the second most common in women. Due to its frequent diagnosis and variable response to treatment, lung cancer was reported as the top cause of cancer-related deaths worldwide in 2020. Many aberrant signaling cascades are implicated in the pathogenesis of lung cancer, including those involved in apoptosis (B cell lymphoma protein, Bcl-2-associated X protein, first apoptosis signal ligand), growth inhibition (tumor suppressor protein or gene and serine/threonine kinase 11), and growth promotion (epidermal growth factor receptor/proto-oncogenes/phosphatidylinositol-3 kinase). Accordingly, these pathways and their signaling molecules have become promising targets for chemopreventive and chemotherapeutic agents. Recent research provides compelling evidence for the use of plant-based compounds, known collectively as phytochemicals, as anticancer agents...
Analgesic drugs like morphine and non-steroidal anti-inflammatory drugs exhibit several harmful e... more Analgesic drugs like morphine and non-steroidal anti-inflammatory drugs exhibit several harmful effects. Here, we show for the first time the analgesic activity of Ficus palmata L. fruit extract (FPFE) on different analgesic rat models along with the in silico studies of some of the main phytochemicals of this plant. We performed in vivo pain models, along with in silico docking studies against the active site of COX-2 protein and mu-opioid receptors. A significant (p < 0.05) analgesic effect of FPFE was observed, and it was found that rutin has good pose and score as compared to diclofenac and morphinan antagonist (X-ligand), and psoralen has binding affinity almost equal to diclofenac, but a lower binding affinity as compared to rutin. The results proved that F. palmata fruits have the potential to ameliorate painful conditions.
Nonvitamin and Nonmineral Nutritional Supplements, 2019
Summary Borage ( Borago officinalis L.) is considered as a native of both Europe and Asia. Severa... more Summary Borage ( Borago officinalis L.) is considered as a native of both Europe and Asia. Several species around the globe fall under the denomination of “borage”. The presence of the highest γ-linolenic acid content in the seeds of borage makes borage distinctively important mainly for the nutraceutical and pharmaceutical research. γ-Linolenic acid is an omega -6 polyunsaturated fatty acid which cannot be synthesized in the body and hence falls into the category of essential fatty acids. Borage seeds’ oil is utilized in various disease conditions such as atherosclerosis, inflammatory disorders, Alzheimer’s disease, asthma, and gastrointestinal disorders. Borage is also being extensively used as one of the potential ingredients for the development of various formulations ranging from emulsions to the green synthesis of nanoparticles. This chapter encompasses the availability, therapeutic benefits, drug interactions, and adverse drug reaction of borage. The chapter also entails, in ...
Prunus cerasoides D. Don is a plant of great venerative value in the Himalayan region. The fruits... more Prunus cerasoides D. Don is a plant of great venerative value in the Himalayan region. The fruits and seed kernels of this plant are traditionally used for the treatment of urinary stones. Present study was aimed to demonstrate the in vitro and preclinical antilithic potential of the hydroethanolic extract of Prunus cerasoides fruits against calcium oxalate urolithiasis. In vitro antiurolithiatic screening was done by nucleation, and aggregation assay, while preclinical evaluation was carried out on ethylene glycol (0.75% v/v) and ammonium chloride (1% w/v) rendered urolithiasic male Wistar rats. P. cerasoides fruit extract induced nucleation of multiple small sized calcium oxalate crystals and inhibited their aggregation in the metastable solutions. P. cerasoides fruit extract to a large extent prevented lithogenic treatment induced anorexia, weight loss, polydipsia, polyuria, crystalluria, hypercalciuria, hyperoxaluria, hyperuricosuria, hyperphosphaturia, hypocitraturia and hypoma...
: Reactive nitrogen species (RNS) and reactive oxygen species (ROS), collectively known as reacti... more : Reactive nitrogen species (RNS) and reactive oxygen species (ROS), collectively known as reactive oxygen and nitrogen species (RONS), are the products of normal cellular metabolism and interact with several vital biomolecules including nucleic acid, proteins, and membrane lipids and alter their function in an irreversible manner which can lead to cell death. There is an imperative role for oxidative stress in the pathogenesis of cognitive impairments and the development and progression of neural injury. Elevated production of higher amounts of nitric oxide (NO) takes place in numerous pathological conditions, such as neurodegenerative diseases, inflammation, and ischemia, which occur concurrently with elevated nitrosative/oxidative stress. The enzyme nitric oxide synthase (NOS) is responsible for the generation of NO in different cells by conversion of Larginine (Arg) to L-citrulline. Therefore, the NO signaling pathway represents a viable therapeutic target. Naturally occurring polyphenols targeting the NO signaling pathway can be of major importance in the field of neurodegeneration and related complications. Here, we comprehensively review the importance of NO and its production in the human body and afterwards highlight the importance of various natural products along with their mechanisms against various neurodegenerative diseases involving their effect on NO production.
The objective of the present study is to develop and evaluate microsphere and tablet in capsule s... more The objective of the present study is to develop and evaluate microsphere and tablet in capsule system for the treatment of rheumatoid arthritis as a dual pulse release system. The capsule system contains enteric coated cap filled with microspheres (sustained release) that lock the impermeable capsule body (coated with ethyl cellulose). The capsule body consists of diclofenac sodium loaded core tablet in the bottom (immediate release), which is sealed with swellable hydrogel plug tablet. Formulations selected for capsule system were MP1 due to least particle size (90.44±0.20 μm) and maximum cumulative release (91.49±0.20 %), T3 for least disintegration time (4±0.040 min) and maximum cumulative release (85.50±0.09 %) and HP2 for maintenance of lag phase that was 6 h and in vitro study was Performed. This formulation included two pulses in one system for reduction of dose frequency and better treatment of night pain and morning stiffness in rheumatoid arthritis patients.
Cardiovascular & Hematological Agents in Medicinal Chemistry
: Surgery, radiation, chemotherapy, and targeted therapy were the four basic kinds of cancer trea... more : Surgery, radiation, chemotherapy, and targeted therapy were the four basic kinds of cancer treatment until recently. Immuno-oncology (IO), or the concept that cancer cells were damaged by activating the body's immune system, has emerged and is explained as a unique and crucial method for treating different cancers over the last decade. The US Food and Drug Administration and the European Medicines Agency both approved this newly recognized way of treating cancer in 2020. Within IO, different therapeutic classes have arisen, which are the subject of this article. Immune checkpoint inhibitors are currently the most well-known therapeutic class of immuno-oncology medications due to their amazing ability to show efficacy in a variety of tumor types. Biomarkers were tested for different tumors like gastrointestinal cancer, whole Head, lower and upper part Neck cancer, and also cervical cancer by programmed death-ligand 1 (PD-L1) check point and their targets and are currently being utilized prior to treatment by using Pembrolizumab. However, the significance of PD-L1 expression for immune check point reticence therapy in other/different onco-cancer types remains unclear. Homogenized immuneoncology drugs with regular therapy have been recently studied and clinical efficacy outcomes have shown to be significantly improved. While IO agents are fast transforming the marketed treatment for cancer patients, there are still a number of obstacles to overcome in terms of associating their adverse effects and confirming those different healthcare systems, such as financing these expensive therapies. In addition to cancer vaccines and chimeric antigen receptor T-cell treatments, other IO drugs are in pipeline containing chimeric antigen receptor T-cell therapies; earlier ones have their own set of toxicities and high cost related challenges.
Lung cancer is a heterogeneous group of malignancies with high incidence worldwide. It is the mos... more Lung cancer is a heterogeneous group of malignancies with high incidence worldwide. It is the most frequently occurring cancer in men and the second most common in women. Due to its frequent diagnosis and variable response to treatment, lung cancer was reported as the top cause of cancer-related deaths worldwide in 2020. Many aberrant signaling cascades are implicated in the pathogenesis of lung cancer, including those involved in apoptosis (B cell lymphoma protein, Bcl-2-associated X protein, first apoptosis signal ligand), growth inhibition (tumor suppressor protein or gene and serine/threonine kinase 11), and growth promotion (epidermal growth factor receptor/proto-oncogenes/phosphatidylinositol-3 kinase). Accordingly, these pathways and their signaling molecules have become promising targets for chemopreventive and chemotherapeutic agents. Recent research provides compelling evidence for the use of plant-based compounds, known collectively as phytochemicals, as anticancer agents...
Analgesic drugs like morphine and non-steroidal anti-inflammatory drugs exhibit several harmful e... more Analgesic drugs like morphine and non-steroidal anti-inflammatory drugs exhibit several harmful effects. Here, we show for the first time the analgesic activity of Ficus palmata L. fruit extract (FPFE) on different analgesic rat models along with the in silico studies of some of the main phytochemicals of this plant. We performed in vivo pain models, along with in silico docking studies against the active site of COX-2 protein and mu-opioid receptors. A significant (p < 0.05) analgesic effect of FPFE was observed, and it was found that rutin has good pose and score as compared to diclofenac and morphinan antagonist (X-ligand), and psoralen has binding affinity almost equal to diclofenac, but a lower binding affinity as compared to rutin. The results proved that F. palmata fruits have the potential to ameliorate painful conditions.
Nonvitamin and Nonmineral Nutritional Supplements, 2019
Summary Borage ( Borago officinalis L.) is considered as a native of both Europe and Asia. Severa... more Summary Borage ( Borago officinalis L.) is considered as a native of both Europe and Asia. Several species around the globe fall under the denomination of “borage”. The presence of the highest γ-linolenic acid content in the seeds of borage makes borage distinctively important mainly for the nutraceutical and pharmaceutical research. γ-Linolenic acid is an omega -6 polyunsaturated fatty acid which cannot be synthesized in the body and hence falls into the category of essential fatty acids. Borage seeds’ oil is utilized in various disease conditions such as atherosclerosis, inflammatory disorders, Alzheimer’s disease, asthma, and gastrointestinal disorders. Borage is also being extensively used as one of the potential ingredients for the development of various formulations ranging from emulsions to the green synthesis of nanoparticles. This chapter encompasses the availability, therapeutic benefits, drug interactions, and adverse drug reaction of borage. The chapter also entails, in ...
Prunus cerasoides D. Don is a plant of great venerative value in the Himalayan region. The fruits... more Prunus cerasoides D. Don is a plant of great venerative value in the Himalayan region. The fruits and seed kernels of this plant are traditionally used for the treatment of urinary stones. Present study was aimed to demonstrate the in vitro and preclinical antilithic potential of the hydroethanolic extract of Prunus cerasoides fruits against calcium oxalate urolithiasis. In vitro antiurolithiatic screening was done by nucleation, and aggregation assay, while preclinical evaluation was carried out on ethylene glycol (0.75% v/v) and ammonium chloride (1% w/v) rendered urolithiasic male Wistar rats. P. cerasoides fruit extract induced nucleation of multiple small sized calcium oxalate crystals and inhibited their aggregation in the metastable solutions. P. cerasoides fruit extract to a large extent prevented lithogenic treatment induced anorexia, weight loss, polydipsia, polyuria, crystalluria, hypercalciuria, hyperoxaluria, hyperuricosuria, hyperphosphaturia, hypocitraturia and hypoma...
: Reactive nitrogen species (RNS) and reactive oxygen species (ROS), collectively known as reacti... more : Reactive nitrogen species (RNS) and reactive oxygen species (ROS), collectively known as reactive oxygen and nitrogen species (RONS), are the products of normal cellular metabolism and interact with several vital biomolecules including nucleic acid, proteins, and membrane lipids and alter their function in an irreversible manner which can lead to cell death. There is an imperative role for oxidative stress in the pathogenesis of cognitive impairments and the development and progression of neural injury. Elevated production of higher amounts of nitric oxide (NO) takes place in numerous pathological conditions, such as neurodegenerative diseases, inflammation, and ischemia, which occur concurrently with elevated nitrosative/oxidative stress. The enzyme nitric oxide synthase (NOS) is responsible for the generation of NO in different cells by conversion of Larginine (Arg) to L-citrulline. Therefore, the NO signaling pathway represents a viable therapeutic target. Naturally occurring polyphenols targeting the NO signaling pathway can be of major importance in the field of neurodegeneration and related complications. Here, we comprehensively review the importance of NO and its production in the human body and afterwards highlight the importance of various natural products along with their mechanisms against various neurodegenerative diseases involving their effect on NO production.
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