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Articles 1 - 16 of 16
Full-Text Articles in Chemicals and Drugs
Electromechanical Effects On Micro And Nano Particles Generated From Drug Delivery Devices And Their Implications In Flow And Deposition Efficiency, Mohammed Ali, Mark Miller
Electromechanical Effects On Micro And Nano Particles Generated From Drug Delivery Devices And Their Implications In Flow And Deposition Efficiency, Mohammed Ali, Mark Miller
Technology Faculty Publications and Presentations
This experimental investigation was undertaken to quantify the electrostatic charge and aerodynamic size distribution of the medicinal drug particles inhaled through an in-vitro mouth-throat (MT) in order to compare the amount of drugs can be delivered to the human lung while mimicking a patient is either sitting or lying. The MT model is a cadaver-based replica cast of human oral-pharyngeal-laryngeal region. Tested drug aerosols were generated by a commercially available metered dose inhaler (MDI). The MT model was placed inside a humidity (95%) and temperature (37oC) controlled chamber. Its mouth-inlet was positioned horizontally and vertically to simulate sitting …
Milk Exosomes: Nature's Abundant Nanoplatform For Theranostic Applications, Benilde Adriano, Nycol Cotto, Neeraj Chauhan, Meena Jaggi, Subhash C. Chauhan, Murali M. Yallapu
Milk Exosomes: Nature's Abundant Nanoplatform For Theranostic Applications, Benilde Adriano, Nycol Cotto, Neeraj Chauhan, Meena Jaggi, Subhash C. Chauhan, Murali M. Yallapu
School of Medicine Publications and Presentations
Exosomes are a unique subpopulation of naturally occurring extracellular vesicles which are smaller intracellular membrane nanoparticle vesicles. Exosomes have proven to be excellent nanocarriers for carrying lipids, proteins, mRNAs, non-coding RNAs, and DNAs, and disseminating long-distance intercellular communications in various biological processes. Among various cell-line or biological fluid derived exosomes, milk exosomes are abundant in nature and exhibit many nanocarrier characteristics favorable for theranostic applications. To be an effective delivery carrier for their clinical translation, exosomes must inbuilt loading, release, targeting, and imaging/tracking characteristics. Considering the unmet gaps of milk exosomes in theranostic technology it is essential to focus the …
New Dithiocarbamates As A Possible Human Serum Albumin Metal Carrier In Drug Delivery Systems And Their Antioxidant And Antiproliferative Activities, Saadi M.D. Al-Nuzal, Azhar M. Haleem, Ken Czerwinski, Salah M. Haleem
New Dithiocarbamates As A Possible Human Serum Albumin Metal Carrier In Drug Delivery Systems And Their Antioxidant And Antiproliferative Activities, Saadi M.D. Al-Nuzal, Azhar M. Haleem, Ken Czerwinski, Salah M. Haleem
Chemistry and Biochemistry Faculty Research
New mono- and bis-dithiocarbamates were prepared from the reaction of organic dihydrazides -NHNH-(C=O)(CH2)x-(C=O)NHNH- (where x = 0, 2, 4) and basic carbon disulfide with varying chain length 10-14 atom as a human serum metal carrier. The products were characterized by various spectrophotometric such as 1H and 13C NMR and elemental analysis. Their antiproliferative activities were examined on two species of the standard strains of the Gram-positive Staphylococcus aureus ATCC 25923 and Gram-negative Escherichia coli ATCC 25922 by following the procedure of broth micro-dilution method (BMM), which was applied at the concentrations: 0.0, 100, 200, and 300 ppm for each compound. …
Click-Free Synthesis Of A Multivalent Tricyclic Peptide As A Molecular Transporter, Sumit Kumar, Dindyal Mandal, Shaima Ahmed El-Mowafi, Saghar Mozaffari, Rakesh Kumar Tiwari, Keykavous Parang
Click-Free Synthesis Of A Multivalent Tricyclic Peptide As A Molecular Transporter, Sumit Kumar, Dindyal Mandal, Shaima Ahmed El-Mowafi, Saghar Mozaffari, Rakesh Kumar Tiwari, Keykavous Parang
Pharmacy Faculty Articles and Research
The cellular delivery of cell-impermeable and water-insoluble molecules remains an ongoing challenge to overcome. Previously, we reported amphipathic cyclic peptides c[WR]4 and c[WR]5 consisting of alternate arginine and tryptophan residues as nuclear-targeting molecular transporters. These peptides contain an optimal balance of positive charge and hydrophobicity, which is required for interactions with the phospholipid bilayer to facilitate their application as a drug delivery system. To further optimize them, we synthesized and evaluated a multivalent tricyclic peptide as an efficient molecular transporter. The monomeric cyclic peptide building blocks were synthesized using Fmoc/tBu solid-phase chemistry and cyclization in the …
Drug Delivery In Catheterized Arterial Blood Flow With Atherosclerosis, Saulo Orizaga, Daniel N. Riahi, Jose R. Soto
Drug Delivery In Catheterized Arterial Blood Flow With Atherosclerosis, Saulo Orizaga, Daniel N. Riahi, Jose R. Soto
School of Mathematical and Statistical Sciences Faculty Publications and Presentations
We study the problem of drug delivery in a catheterized artery in the presence of atherosclerosis. The problem is modeled in the context of a two-phase flow system which consists of red blood cells and blood plasma. The coupled differential equations for fluid (plasma) and particles (red cells) are solved for the relevant quantities in the reasonable limits. The drug delivery problem is modeled with a partial differential equation that is developed in terms of the drug concentration, blood plasma velocity, hematocrit value and the diffusion coefficient of the drug/fluid. A conservative-implicit finite difference scheme is develop in order to …
Prospects For Rnai Therapy Of Covid-19, Hasan Uludağ, Kylie Parent, Hamidreza Montazeri Aliabadi, Azita Haddadi
Prospects For Rnai Therapy Of Covid-19, Hasan Uludağ, Kylie Parent, Hamidreza Montazeri Aliabadi, Azita Haddadi
Pharmacy Faculty Articles and Research
COVID-19 caused by the SARS-CoV-2 virus is a fast emerging disease with deadly consequences. The pulmonary system and lungs in particular are most prone to damage caused by the SARS-CoV-2 infection, which leaves a destructive footprint in the lung tissue, making it incapable of conducting its respiratory functions and resulting in severe acute respiratory disease and loss of life. There were no drug treatments or vaccines approved for SARS-CoV-2 at the onset of pandemic, necessitating an urgent need to develop effective therapeutics. To this end, the innate RNA interference (RNAi) mechanism can be employed to develop front line therapies against …
Comparative Molecular Transporter Properties Of Cyclic Peptides Containing Tryptophan And Arginine Residues Formed Through Disulfide Cyclization, Eman H. M. Mohammed, Dindyal Mandal, Saghar Mozaffari, Magdy Abdel-Hamied Zahran, Amany Mostafa Osman, Rakesh Kumar Tiwari, Keykavous Parang
Comparative Molecular Transporter Properties Of Cyclic Peptides Containing Tryptophan And Arginine Residues Formed Through Disulfide Cyclization, Eman H. M. Mohammed, Dindyal Mandal, Saghar Mozaffari, Magdy Abdel-Hamied Zahran, Amany Mostafa Osman, Rakesh Kumar Tiwari, Keykavous Parang
Pharmacy Faculty Articles and Research
We have previously reported cyclic cell-penetrating peptides [WR]5 and [WR]4 as molecular transporters. To optimize further the utility of our developed peptides for targeted therapy in cancer cells using the redox condition, we designed a new generation of peptides and evaluated their cytotoxicity as well as uptake behavior against different cancer cell lines. Thus, cyclic [C(WR)xC] and linear counterparts (C(WR)xC), where x = 4–5, were synthesized using Fmoc/tBu solid-phase peptide synthesis, purified, and characterized. The compounds did not show any significant cytotoxicity (at 25 µM) against ovarian (SK-OV-3), leukemia (CCRF-CEM), gastric adenocarcinoma (CRL-1739), breast …
Novel Elvitegravir Nanoformulation For Drug Delivery Across The Blood-Brain Barrier To Achieve Hiv-1 Suppression In The Cns Macrophages, Yuqing Gong, Pallabita Chowdhury, Prashanth K.B. Nagesh, Mohammad A. Rahman, Kaining Zhi, Murali M. Yallapu, Santosh Kumar
Novel Elvitegravir Nanoformulation For Drug Delivery Across The Blood-Brain Barrier To Achieve Hiv-1 Suppression In The Cns Macrophages, Yuqing Gong, Pallabita Chowdhury, Prashanth K.B. Nagesh, Mohammad A. Rahman, Kaining Zhi, Murali M. Yallapu, Santosh Kumar
School of Medicine Publications and Presentations
The use of antiretroviral therapy (ART) has remarkably decreased the morbidity associated with HIV-1 infection, however, the prevalence of HIV-1-associated neurocognitive disorders (HAND) is still increasing. The blood-brain barrier (BBB) is the major impediment for penetration of antiretroviral drugs, causing therapeutics to reach only suboptimal level to the brain. Conventional antiretroviral drug regimens are not sufficient to improve the treatment outcomes of HAND. In our recent report, we have developed a poloxamer-PLGA nanoformulation loaded with elvitegravir (EVG), a commonly used antiretroviral drug. The nanoformulated EVG is capable of elevating intracellular drug uptake and simultaneously enhance viral suppression in HIV-1-infected macrophages. …
Antibody-Drug Conjugates For Cancer Therapy: Chemistry To Clinical Implications, Nirnoy Dan, Saini Setua, Vivek K. Kashyap, Sheema Khan, Meena Jaggi, Murali M. Yallapu, Subhash C. Chauhan
Antibody-Drug Conjugates For Cancer Therapy: Chemistry To Clinical Implications, Nirnoy Dan, Saini Setua, Vivek K. Kashyap, Sheema Khan, Meena Jaggi, Murali M. Yallapu, Subhash C. Chauhan
School of Medicine Publications and Presentations
Chemotherapy is one of themajor therapeutic options for cancer treatment. Chemotherapy is often associated with a low therapeutic window due to its poor specificity towards tumor cells/tissues. Antibody-drug conjugate (ADC) technology may provide a potentially new therapeutic solution for cancer treatment. ADC technology uses an antibody-mediated delivery of cytotoxic drugs to the tumors in a targeted manner, while sparing normal cells. Such a targeted approach can improve the tumor-to-normal tissue selectivity and specificity in chemotherapy. Considering its importance in cancer treatment, we aim to review recent efforts for the design and development of ADCs. ADCs are mainly composed of an …
Ph-Dependent Silica Nanoparticle Dissolution And 1 Cargo Release, Giorgia Giovaninni, Colin J. Moore, Andrew John Hall, Hugh Byrne, Vladimir Gubala
Ph-Dependent Silica Nanoparticle Dissolution And 1 Cargo Release, Giorgia Giovaninni, Colin J. Moore, Andrew John Hall, Hugh Byrne, Vladimir Gubala
Articles
The dissolution of microporous silica nanoparticles (NP) in aqueous environments of different biologically relevant pH was studied in order to assess their potential as drug delivery vehicles. Silica NPs, loaded with fluorescein, were prepared using different organosilane precursors (tetraethoxysilane, ethyl triethoxysilane or a 1:1 molar ratio of both) and NP dissolution was evaluated in aqueous conditions at pH 4, pH 6 and pH 7.4. These conditions correspond to the acidity of the intracellular environment (late endosome, early endosome, cytosol respectively) and gastrointestinal tract (‘fed’ stomach, duodenum and jejunum respectively). All NPs degraded at pH 6 and pH 7.4, while no …
Development Of Polyvinylpyrrolidone/Paclitaxel Self-Assemblies For Breast Cancer, Pallabita Chowdhury, Prashanth K.B. Nagesh, Sheema Khan, Bilal B. Hafeez, Subhash C. Chauhan, Meena Jaggi, Murali M. Yallapu
Development Of Polyvinylpyrrolidone/Paclitaxel Self-Assemblies For Breast Cancer, Pallabita Chowdhury, Prashanth K.B. Nagesh, Sheema Khan, Bilal B. Hafeez, Subhash C. Chauhan, Meena Jaggi, Murali M. Yallapu
School of Medicine Publications and Presentations
The goal of this investigation was to develop and demonstrate a polymer/paclitaxel self-assembly (PTX-SA) formulation. Polymer/PTX-SAs were screened based on smaller size of formulation using dynamic light scattering analysis. Additionally, fluorescence microscopy and flow cytometry studies exhibited that polyvinylpyrrolidone (PVP)-based PTX-SAs (PVP/PTX-SAs) had superior cellular internalization capability in MCF7 and MDA-MB-231 breast cancer cells. The optimized PVP/PTX-SAs exhibited less toxicity to human red blood cells indicating a suitable formulation for reducing systemic toxicity. The formation of PVP and PTX self-assemblies was confirmed using fluorescence quenching and transmission electron microscopy which indicated that the PVP/PTX-SAs were spherical in shape with an …
Borneol, A Novel Agent That Improves Central Nervous System Drug Delivery By Enhancing Blood–Brain Barrier Permeability, Qun-Lin Zhang, Bingmei M. Fu, Zhang-Jin Zhang
Borneol, A Novel Agent That Improves Central Nervous System Drug Delivery By Enhancing Blood–Brain Barrier Permeability, Qun-Lin Zhang, Bingmei M. Fu, Zhang-Jin Zhang
Publications and Research
The clinical application of central nervous system (CNS) drugs is limited by their poor bioavailability due to the blood–brain barrier (BBB). Borneol is a naturally occurring compound in a class of ‘orificeopening’ agents often used for resuscitative purposes in traditional Chinese medicine. A growing body of evidence confirms that the ‘orifice-opening’ effect of borneol is principally derived from opening the BBB. Borneol is therefore believed to be an effective adjuvant that can improve drug delivery to the brain. The purpose of this paper is to provide a comprehensive review of information accumulated over the past two decades on borneol’s chemical …
Novel Ph-Sensitive Cyclic Peptides, Dhammika Weerakkody, Anna Moshnikova, Naglaa Salem El-Sayed, Ramona-Cosima Adochite, Gregory Slaybaugh, Jovana Golijanin, Rakesh Tiwari, Oleg A. Andreev, Keykavous Parang, Yana K. Reshetnyak
Novel Ph-Sensitive Cyclic Peptides, Dhammika Weerakkody, Anna Moshnikova, Naglaa Salem El-Sayed, Ramona-Cosima Adochite, Gregory Slaybaugh, Jovana Golijanin, Rakesh Tiwari, Oleg A. Andreev, Keykavous Parang, Yana K. Reshetnyak
Pharmacy Faculty Articles and Research
A series of cyclic peptides containing a number of tryptophan (W) and glutamic acid (E) residues were synthesized and evaluated as pH-sensitive agents for targeting of acidic tissue and pH-dependent cytoplasmic delivery of molecules. Biophysical studies revealed the molecular mechanism of peptides action and localization within the lipid bilayer of the membrane at high and low pHs. The symmetric, c[(WE)4WC], and asymmetric, c[E4W5C], cyclic peptides translocated amanitin, a polar cargo molecule of similar size, across the lipid bilayer and induced cell death in a pH- and concentration-dependent manner. Fluorescently-labelled peptides were evaluated for targeting of acidic 4T1 mammary tumors in …
Calcium Phosphate As A Key Material For Socially Responsible Tissue Engineering, Vuk Uskoković, Victoria M. Wu
Calcium Phosphate As A Key Material For Socially Responsible Tissue Engineering, Vuk Uskoković, Victoria M. Wu
Pharmacy Faculty Articles and Research
Socially responsible technologies are designed while taking into consideration the socioeconomic, geopolitical and environmental limitations of regions in which they will be implemented. In the medical context, this involves making therapeutic platforms more accessible and affordable to patients in poor regions of the world wherein a given disease is endemic. This often necessitates going against the reigning trend of making therapeutic nanoparticles ever more structurally complex and expensive. However, studies aimed at simplifying materials and formulations while maintaining the functionality and therapeutic response of their more complex counterparts seldom provoke a significant interest in the scientific community. In this review …
Cationic Cell-Penetrating Peptides Are Potent Furin Inhibitors, Bruno Ramos-Molina, Adam N. Lick, Amir Nasrolahi Shirazi, Donghoon Oh, Rakesh Tiwari, Naglaa Salem El-Sayed, Keykavous Parang, Iris Lindberg
Cationic Cell-Penetrating Peptides Are Potent Furin Inhibitors, Bruno Ramos-Molina, Adam N. Lick, Amir Nasrolahi Shirazi, Donghoon Oh, Rakesh Tiwari, Naglaa Salem El-Sayed, Keykavous Parang, Iris Lindberg
Pharmacy Faculty Articles and Research
Cationic cell-penetrating peptides have been widely used to enhance the intracellular delivery of various types of cargoes, such as drugs and proteins. These reagents are chemically similar to the multi-basic peptides that are known to be potent proprotein convertase inhibitors. Here, we report that both HIV-1 TAT47-57 peptide and the Chariot reagent are micromolar inhibitors of furin activity in vitro. In agreement, HIV-1 TAT47-57 reduced HT1080 cell migration, thought to be mediated by proprotein convertases, by 25%. In addition, cyclic polyarginine peptides containing hydrophobic moieties which have been previously used as transfection reagents also exhibited potent furin inhibition in vitro …
In Vitro Evaluation Of The Cytotoxicity Of A Folate-Modified Β-Cyclodextrin As A New Anti-Cancer Drug Delivery System, Zlata Tofzikovskaya, Alan Casey, Orla L. Howe, Christine O'Connor, Mary Mcnamara
In Vitro Evaluation Of The Cytotoxicity Of A Folate-Modified Β-Cyclodextrin As A New Anti-Cancer Drug Delivery System, Zlata Tofzikovskaya, Alan Casey, Orla L. Howe, Christine O'Connor, Mary Mcnamara
Articles
Many chemotherapeutic drugs are therapeutically non-selective and do not distinguish between healthy cells and tumour cells which can result in severe side effects and toxicity. Drug delivery systems can be used to target specific cells and therefore may eliminate many of the side effects, increasing drug efficiency and efficacy, and controlling drug release. One possible strategy for targeted drug delivery is to use unique molecular markers such as folate receptors in cancer cells. In this work the cytotoxicity of a novel cyclodextrin-folate conjugate, 6-deoxy-6-[(1-(-2amino)ethylamino)folate-β-cyclodextrin (CDEnFA) was studied using the MTT assay and the MCF-7 (Breast), HeLa (Cervical), A549 (Lung cancer) …