Formulation of boron encapsulated smart nanocapsules for targeted drug delivery to the brain

Drug delivery through the Blood–Brain Barrier (BBB) represents a significant challenge. Despite the current strategies to circumvent the BBB, nanotechnology offers unprecedented opportunities for combining selective delivery, improved bioavailability, drug protection, and enhanced pharmacokinetics profiles. Chitosan nanocarriers allow for a more efficacious strategy at the cellular and sub-cellular levels. Boron Neutron Capture Therapy (BNCT) is a targeted chemo-radiotherapeutic technique that allows the selective depletion of cancer cells by means of selective tagging of cancer cells with10B, followed by irradiation with low-energy neutrons. Consequently, the combination of a polymer-based nanodelivery system enclosing an effective BNCT pharmacophore can potentially lead to the selective delivery of the load to cancer cells beyond the BBB. In this work, synthesized novel boronated agents based on carborane-functionalized Delocalized Lipophilic Cations (DLCs) are assessed for safety and selective targeting of tumour cells. The compounds are then encapsulated in nanocarriers constituted by chitosan to promote permeability through the BBB. Additionally, chitosan was used in combination with polypyrrole to form a smart composite nanocapsule, which is expected to release its drug load with variations in pH. Results indicate the achievement of more selective boron delivery to cells via carboranyl DLCs. Finally, preliminary cell studies indicate no toxicity was detected in chitosan nanocapsules, further enhancing its viability as a potential delivery vehicle in the BNCT of brain tumours

PALLADIUM (II)-CATALYZED SELECTIVE REDUCTION OF 4’-(PHENYLETHYNL)ACETOPHENONE IN THE PRESENCE OF A FORMIC ACID-TRIETHYLAMINE MIXTURE

An efficient and straightforward palladium acetylacetonate-catalyzed hydrogen transfer of 4\u27- (phenylethynyl)acetophenone was developed in this study. Formic Acid was found to be the best hydrogen source in this catalytic system in the presence of triethylamine. Excellent conversions and selectivity were obtained in reducing the starting internal aromatic alkyne to either (E)-1-(4- styrylphenyl)ethanone or an interesting cyclic product, 1-(phenanthrene-3-yl)ethenone, over the ketone functional group present. Over-reduction was rarely seen. The reaction conditions were optimized in terms of the choice of the palladium catalyst, temperature, solvent, and the H-donor/base combination. Using this catalytic system, a one-step synthetic pathway of the hindered cyclic ketone was afforded in excellent yields

The Therapeutic Wound Healing Bioactivities of Various Medicinal Plants

The skin serves as the body’s first line of defense, guarding against mechanical, chemical, and thermal damage to the interior organs. It includes a highly developed immune response that serves as a barrier against pathogenic infections. Wound healing is a dynamic process underpinned by numerous cellular activities, including homeostasis, inflammation, proliferation, and remodeling, that require proper harmonious integration to effectively repair the damaged tissue. Following cutaneous damage, microorganisms can quickly enter the tissues beneath the skin, which can result in chronic wounds and fatal infections. Natural phytomedicines that possess considerable pharmacological properties have been widely and effectively employed forwound treatment and infection prevention. Since ancient times, phytotherapy has been able to efficiently treat cutaneous wounds, reduce the onset of infections, and minimize the usage of antibiotics that cause critical antibiotic resistance. There are a remarkable number of wound-healing botanicals that have been widely used in the Northern Hemisphere, including Achiella millefolium, Aloe vera, Althaea officinalis, Calendula officinalis, Matricaria chamomilla, Curcuma longa, Eucalyptus, Jojoba, plantain, pine, green tea, pomegranate, and Inula. This review addresses the most often used medicinal plants from the Northern Hemisphere that facilitate the treatment of wounds, and also suggests viable natural alternatives that can be used in the field of wound care

PLGA-Gold Nanocomposite: Preparation and Biomedical Applications

A composite system consisting of both organic and inorganic nanoparticles is an approach to prepare a new material exhibiting “the best of both worlds”. In this review, we highlight the recent advances in the preparation and applications of poly(lactic-co-glycolic acid)-gold nanoparticles (PLGA-GNP). With its current clinically use, PLGA-based nanocarriers have promising pharmaceutical applications and can “extract and utilize” the fascinating optical and photothermal properties of encapsulated GNP. The resulting “golden polymeric nanocarrier” can be tracked, analyzed, and visualized using the encapsulated gold nanoprobes which facilitate a better understanding of the hosting nanocarrier’s pharmacokinetics and biological fate. In addition, the “golden polymeric nanocarrier” can reveal superior nanotherapeutics that combine both the photothermal effect of the encapsulated gold nanoparticles and co-loaded chemotherapeutics. To help stimulate more research on the development of nanomaterials with hybrid and exceptional properties, functionalities, and applications, this review provides recent examples with a focus on the available chemistries and the rationale behind encapsulating GNP into PLGA nanocarriers that has the potential to be translated into innovative, clinically applicable nanomedicine.A.M.A. acknowledge funding support from the University of Jordan. The APC was funded by the University of Illinois at Urbana-Champaign

COVID-19 Vaccination: From Interesting Agent to the Patient

The vaccination for the novel Coronavirus (COVID-19) is undergoing its final stages of analysis and testing. It is an impressive feat under the circumstances that we are on the verge of a potential breakthrough vaccination. This will help reduce the stress for millions of people around the globe, helping to restore worldwide normalcy. In this review, the analysis looks into how the new branch of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) came into the forefront of the world like a pandemic. This review will break down the details of what COVID-19 is, the viral family it belongs to and its background of how this family of viruses alters bodily functions by attacking vital human respiratory organs, the circulatory system, the central nervous system and the gastrointestinal tract. This review also looks at the process a new drug analogue undergoes, from (i) being a promising lead compound to (ii) being released into the market, from the drug development and discovery stage right through to FDA approval and aftermarket research. This review also addresses viable reasoning as to why the SARS-CoV-2 vaccine may have taken much less time than normal in order for it to be released for use

Formulation of Boron Encapsulated Smart Nanocapsules for Targeted Drug Delivery to the Brain

Drug delivery through the Blood–Brain Barrier (BBB) represents a significant challenge. Despite the current strategies to circumvent the BBB, nanotechnology offers unprecedented opportunities for combining selective delivery, improved bioavailability, drug protection, and enhanced pharmacokinetics profiles. Chitosan nanocarriers allow for a more efficacious strategy at the cellular and sub-cellular levels. Boron Neutron Capture Therapy (BNCT) is a targeted chemo-radiotherapeutic technique that allows the selective depletion of cancer cells by means of selective tagging of cancer cells with 10B, followed by irradiation with low-energy neutrons. Consequently, the combination of a polymer-based nanodelivery system enclosing an effective BNCT pharmacophore can potentially lead to the selective delivery of the load to cancer cells beyond the BBB. In this work, synthesized novel boronated agents based on carborane-functionalized Delocalized Lipophilic Cations (DLCs) are assessed for safety and selective targeting of tumour cells. The compounds are then encapsulated in nanocarriers constituted by chitosan to promote permeability through the BBB. Additionally, chitosan was used in combination with polypyrrole to form a smart composite nanocapsule, which is expected to release its drug load with variations in pH. Results indicate the achievement of more selective boron delivery to cells via carboranyl DLCs. Finally, preliminary cell studies indicate no toxicity was detected in chitosan nanocapsules, further enhancing its viability as a potential delivery vehicle in the BNCT of brain tumours

Formation of smart nanocapsules for targeted drug delivery

Drug delivery through the Blood Brain Barrier (BBB) represent a significant challenge in transporting active pharmaceutical ingredients into the brain. Nanotechnology offers unprecedented opportunities to not only circumvent the BBB, but also have the ability to selective deliver drugs to target site. Polymeric nano-carriers allow for a more efficacious drug targeting strategy at cellular and sub-cellular level, they can also be used for sustained release of drug, henceforth prolonging effect of drug leading to fewer side effects. Boron Neutron Capture therapy (BNCT) is a targeted chemo-radiotherapeutic technique that allows the selective depletion of cancer cells by means of selective tagging of cancer cells with boron, followed by irradiation with low-energy neutrons. This results is the selective destruction of cancer cells. Consequently, the combination of a polymer based nano-delivery system enclosing an effective BNCT pharmacophore can potentially lead to the selective delivery of the load to cancer cells beyond the BBB. In this work, novel boronated agents, based on carboranyl-functionalised Delocalized Lipophilic Cations (DLCs), which selectively target the mitochondria of tumour cells, were synthesised. Literature suggests that the treatment of tumour and cancer stem cells using these types of agents induce selective and permanent cancer cell growth arrest through activation of the p53/p21 axis. The drugs were then encapsulated in nano-carriers constituted by chitosan, modified with moieties that are expected to promote permeability through the BBB. Also, the same functionalised chitosan was used in combination with poly-pyrrole to form a smart composite nano-shell of reduced size, which are expected to release their drug load with variations in pH. Results indicate achievement of more selective boron delivery to cells via carboranyl DLCs. Carboranyl DLCs have shown a 10 fold increase in boron uptake into CaCo2 cells as opposed to non-synthesised boron, we hypothesise this is due to the selective tagging of boron enforced via the DLCs. Furthermore, alkyl-glycerol functionalised chitosan has shown great potential in improving the nano-vehicles physical characteristics, modified chitosan, when compared to pristine chitosan, decreased size of nanoparticles by an average of 200mm, resulting in nano-vehicles in the range of between 50-300mm. Furthermore the charge profile of the nano-vehicles decreased, with values between 15-30mV, forming a less toxic, more favourable delivery vehicle towards cancer drug delivery. The addition of poly-pyrrole to chitosan to form a composite nano-vehicle enhanced the release profile in more acidic environments. This is due, in part to the pyrrole protonating in more acidic environments, in addition to protecting the chitosan from degradation occurring, henceforth preventing early degradation of the nano-vehicle. Finally, preliminary cell studies indicate that no toxicity was detected in alkyl-glycerol functionalised chitosan nanocapules, in addition, alkyl-glycerol functionalised chitosan improved permeation of delivery vehicle across a cellular monolayer, this was due to two factor, the decreased size and increased hydrophobicity of the nano-vehicle. Therefore we conclude that poly-pyrrole in combination with alkyl-glycerol functionalised chitosan as part of a nano-vehicle has the potential to not only enhance its potential of surpassing the BBB but also be a suitable delivery vehicle in the BNCT of brain tumours

SARS-CoV-2: An Analysis of the Vaccine Candidates Tested in Combatting and Eliminating the COVID-19 Virus

Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2), better known as COVID-19, is a highly contagious virus, transferable via air droplets from close human-human contact. The pandemic has led to over 6.5 million deaths worldwide, making it the largest global health crisis since the influenza pandemic in 1918. SARS-CoV-2 rapidly spread around the world, forcing the World Health Organization (WHO) to deem it a global health pandemic after three months of its initiation. The virus has wreaked havoc on many countries worldwide, overwhelming healthcare systems, hence damaging many economies. Even though research has progressed the understanding of the SARS-CoV-2 virus, the information gathered about the vaccine trials and their findings have been scarcely distributed to the public in a single study. The information available to scientists has therefore given researchers a pathway to building an efficacious vehicle to substantially decrease the spread of the virus. The vaccines formulated had many challenges due to multiple factors such as viral mutations and clinical trial delays. This paper will aim to educate readers on the processes that the vaccine candidates took, and better understand the procedures; additionally, we’ll look at all candidates’ findings that went into clinical trials, assessing, analyzing, and evaluating the 27 vaccine candidates that went into phase III trials and the 13 candidates that went into either phase I/II trials