Development And Characterization Of Glimepiride Novel Solid Nanodispersion For Improving Its Oral Bioavailability,
2020
The British University in Egypt
Development And Characterization Of Glimepiride Novel Solid Nanodispersion For Improving Its Oral Bioavailability, Shady Swidan, Mona Qushawy, Ali Nasr, Yasmin Mortagi
Pharmacy
Glimepiride is an antidiabetic drug which is one of the third generation sulfonylureas. It belongs to class II, according to the BCS (Biopharmaceutical Classification System), which is characterized by low solubility and high permeability. The aim of this work was to formulate glimepiride as solid dispersion using water-soluble carriers to enhance its aqueous solubility and thus enhance its bioavailability. Nine formulations of glimepiride solid dispersion were prepared by a solvent evaporation technique using three different carriers (mannitol, polyethylene glycol 6000, and β-cyclodextrin) with three different drug carrier ratio (1:1, 1:3, and 1:6). Formulation variables were optimized using 32 full factorial …
Model-Based Dose-Exposure-Response Assessment For Lead And Backup Spectinamide In A Mouse Model Of Tuberculosis,
2020
University of Tennessee Health Science Center
Model-Based Dose-Exposure-Response Assessment For Lead And Backup Spectinamide In A Mouse Model Of Tuberculosis, Santosh Janardan Wagh
Theses and Dissertations (ETD)
Despite decades of research, tuberculosis remains the oldest pathogen-based disease that is the leading cause of death from a single infectious agent. Among many anti-tubercular therapies under investigation, the semisynthetic compounds spectinamides are a promising novel class of anti-tuberculosis agents. One such lead candidate, spectinamide 1810, and backup spectinamide 1599 have demonstrated excellent efficacy, safety, and drug-like properties in various in vitro and in vivo assessments. The dose-ranging and dose fractionation studies were designed to characterize the dose-exposure-response relationship for lead and backup spectinamide in a mouse model of Mycobacterium tuberculosis infection. In this current study, we used 26 and …
Veru-111 As An Oral Tubulin Inhibitor Suppressing Triple-Negative Breast Cancer And Evaluation Of Novel Tubulin Inhibitors For Cancer Therapy,
2020
University of Tennessee Health Science Center
Veru-111 As An Oral Tubulin Inhibitor Suppressing Triple-Negative Breast Cancer And Evaluation Of Novel Tubulin Inhibitors For Cancer Therapy, Shanshan Deng
Theses and Dissertations (ETD)
Triple negative breast cancer (TNBC) has aggressive clinical features strongly associated with poorer overall prognosis and higher mortality rates relative to other molecular subtypes. FDA-approved drugs, such as paclitaxel, are effective in treating TNBC. Yet, treatment failure is commonly observed due to the development of acquired chemoresistance, which remains a clinical challenge for TNBC therapy.
Contraceptive Methods In The United States: The Question Of Abortive Mechanisms,
2020
Liberty University
Contraceptive Methods In The United States: The Question Of Abortive Mechanisms, Tara Ferenczy
Senior Honors Theses
This thesis reviews the many methods of contraception available in the United States. Although society’s understanding of women’s health has become a major topic, there is still a significant deficit of information regarding how the accessible methods affect women’s bodies, specifically reproductive tissue. The thesis analyzes numerous contraceptive options focusing specifically on the mechanisms of action to determine whether options have abortifacient properties so that readers may develop educated opinions regarding medical and ethical uses. Information involving strengths and limitations of each technique and the effects on both the female body and the reproductive material assist in understanding the process …
Validation And Application Of A Novel Target-Based Whole-Cell Screen To Identify Antifungal Compounds,
2020
University of Tennessee Health Science Center
Validation And Application Of A Novel Target-Based Whole-Cell Screen To Identify Antifungal Compounds, Christian Alexander Dejarnette
Theses and Dissertations (ETD)
Traditional approaches to drug discovery are inefficient and have several key limitations that constrain our capacity to rapidly identify and develop novel experimental therapeutics. To address this, we have devised a second-generation target-based whole-cell screening assay based on the principles of competitive fitness, which can rapidly identify target-specific and physiologically-active compounds. Briefly, strains expressing high, intermediate, and low levels of a preselected target protein were constructed, tagged with spectrally distinct fluorescent proteins (FPs), and mixed together. The pooled strains were then grown in the presence of various small molecules, and the relative growth of each strain within the mixed culture …
Click-Free Synthesis Of A Multivalent Tricyclic Peptide As A Molecular Transporter,
2020
Chapman University
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 …
Potential Risk Factors For Mortality Due To Cardiovascular Disease Among Hemodialysed Patients In Indonesia,
2020
Pharmacy Faculty, Universitas 17 Agustus 1945 Jakarta, Indonesia
Potential Risk Factors For Mortality Due To Cardiovascular Disease Among Hemodialysed Patients In Indonesia, Diana Laila Ramatillah, Syed Azhar Syed Sulaiman, Kashif Ullah Khan
Pharmaceutical Sciences and Research
Severe vascular calcifications, alterations in cardiovascular structure and function, immune dysfunction, and anemia are adverse effects of parathyroid hormone (PTH), which may contribute to increase risk factors of cardiovascular morbidity and mortality among renal failure patients. To evaluate the potential risk factors for mortality due to cardiovascular disease among hemodialysed patients in Indonesia, this cohort study was conducted. This study included 178 patients on hemodialysis who had been followed up two times a week for nine months (prospective cohort) and 185 patients who died in the last five years (retrospective cohort). Universal sampling technique were used to select the study …
Antioxidant And Elastase Inhibitor Potential Of Petals And Receptacle Of Rose Flower (Rosa Damascena),
2020
Universitas Prima Indonesia, Medan, North Sumatra, Indonesia
Antioxidant And Elastase Inhibitor Potential Of Petals And Receptacle Of Rose Flower (Rosa Damascena), Evi Mawarni, Chrismis Novalinda Ginting, Linda Chiuman, Ermi Girsang, Rr. Anisa Siwianti Handayani, Wahyu Widowati
Pharmaceutical Sciences and Research
Free radicals can cause damage to cells or tissues, autoimmune diseases, degenerative diseases, or cancer. Therefore, the body needs important substances, namely antioxidants that can help protect the body by reducing negative effect from free radicals. Rose flower (Rosa damascena) has anthocyanin pigment which belongs to flavonoid group which has a function as antioxidant or free radical scavenger. This study aims to determine antioxidant and anti-elastase potentials of rose petals and receptacles. The method used in this study was a qualitative phytochemical test to determine the compounds contained in the Rose Petal Extract (RPE) and Rose Receptacle Extract (RRE), ABTS …
Epigenetic Diet To Modulate Immune Response Against Sars-Cov-2,
2020
Faculty of Pharmacy, Universitas Muhammadiyah Banjarmasin, South Kalimantan, Indonesia
Epigenetic Diet To Modulate Immune Response Against Sars-Cov-2, Andika Andika, Risa Ahdyani, Linda Erlina, Azminah Azminah, Arry Yanuar
Pharmaceutical Sciences and Research
The COVID-19 pandemic has spread to various parts of the world and caused many deaths. The victims are infected by SARS-CoV-2, a new type of coronavirus that has appeared since December 2019 and caused respiratory symptoms, fever, coughing, and shortness of breath. In addition to social distancing, wearing masks and washing hands, diet is important as a defense of the body against SARS-CoV-2. In this review, researchers conducted epigenetic diet studies that could potentially inhibit SARS-CoV-2, and can be consumed and used on a daily basis.
Antagonistic Drug-Herb Interactions Between Clinacanthus Nutans And Cyclophosphamide On Wrl 68 Cell Line,
2020
Faculty of Pharmacy, Universiti Teknologi MARA Cawangan Selangor, 43200, Puncak Alam, Selangor, Malaysia
Antagonistic Drug-Herb Interactions Between Clinacanthus Nutans And Cyclophosphamide On Wrl 68 Cell Line, Nurliana Abd Mutalib, Normala Abd Latip
Pharmaceutical Sciences and Research
Clinacanthus nutans (Acanthaceae), locally known as Sabah snake grass, is popularly taken as prevention as well as treatment for cancer in Malaysia, despite lack of concrete clinical evidence. However, it is crucial to evaluate potential antagonistic, additive, or synergistic interactions that may result from the co-treatment of this plant in chemotherapy. In this study, we demonstrate the drug-herb interaction using combination treatment of C. nutans extracts and cyclophosphamide on the WRL 68 cell line. Materials and Methods: Aqueous and 70% ethanol extract of C. nutans leaves were prepared using decoction and maceration methods. MTT assay was used to test …
A Study On The Formulation Of Plant Matrix Tablets From Coarse Botanical Materials Using Cinnamon Bark And Areca Nut As The Model Botanical Materials,
2020
GEA-NUS Pharmaceutical Processing Research Laboratory, Department of Pharmacy, National University of Singapore, Singapore
A Study On The Formulation Of Plant Matrix Tablets From Coarse Botanical Materials Using Cinnamon Bark And Areca Nut As The Model Botanical Materials, Natalia Veronica, Xiu Hui Ang, Shing Ming Ooi, Celine Valeria Liew, Paul Wan Sia Heng
Pharmaceutical Sciences and Research
Background: There is much interest in formulating botanical materials into tablets due to the compactness and ease of administration. However, tableting of coarse milled botanical materials poses a challenge due to poor tableting properties. Objective: To evaluate the feasibility of wet granulation to produce tablets from coarse milled botanical materials and to assess the effect of formulation on properties of the tablets. Materials and Methods: Cinnamon bark and areca nut were milled to obtain 1–2 mm particle size, which was subsequently used in wet granulation using maltodextrin solution as a granulating liquid. Two diluents were tried; microcrystalline …
Long-Lasting, Patient-Controlled, Procedure-Free Contraception: A Review Of Annovera With A Pharmacist Perspective,
2020
TherapeuticsMD
Long-Lasting, Patient-Controlled, Procedure-Free Contraception: A Review Of Annovera With A Pharmacist Perspective, Jennifer J. Virro, Kathleen Besinque, Christiane E. Carney, Danielle Gross, Brian Bernick, Sebastian Mirkin
Pharmacy Faculty Articles and Research
Annovera (segesterone acetate and ethinyl estradiol vaginal system) is a US Food and Drug Administration FDA-approved long-lasting, reversible contraceptive that is fully administered by the user and does not require a procedure for insertion or removal. The vaginal system is in the shape of a ring and contains low doses of a novel progestin, egesterone acetate, and ethinyl estradiol. It is made of silicone and is fully pliable and flexible. The vaginal system is reusable for 13 cycles, using a 21 days in/7 days out regimen, providing women with the ability to control their fertility. Particularly now during the COVID-19 …
Dermaseptin-Based Antiviral Peptides To Prevent Covid-19 Through In Silico Molecular Docking Studies Against Sars-Cov-2 Spike Protein,
2020
Department of Pharmacy, Faculty of Mathematics and Natural Sciences, Universitas Islam Bandung, Indonesia
Dermaseptin-Based Antiviral Peptides To Prevent Covid-19 Through In Silico Molecular Docking Studies Against Sars-Cov-2 Spike Protein, Taufik Muhammad Fakih
Pharmaceutical Sciences and Research
A pandemic coronavirus disease of 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has now been declared a global pandemic by the World Health Organization. The search for new drugs, especially by utilizing antiviral peptides is a very potential area. Through this study, protein-peptide docking and protein-protein docking simulations were conducted using in silico methods to identify, evaluate, and explore the molecular affinity and interaction of dermaseptin peptide molecules produced by frogs of the genus Phyllomedusa against the SARS-CoV-2 spike protein macromolecule, and its effect on attachment to the surface of the ACE-2 (Angiotensin Converting Enzyme-2) receptor. …
A Mini Review : Clinically Significant Potential Drug-Drug Interactions In Covid-19 And Comorbid Therapy,
2020
Study Program of Pharmacy, Faculty of Medicine, Hang Tuah University, Surabaya, Indonesia
A Mini Review : Clinically Significant Potential Drug-Drug Interactions In Covid-19 And Comorbid Therapy, Ana Khusnul Faizah, Nani Wijayanti Dyah Nurrahman, Oki Nugraha Putra
Pharmaceutical Sciences and Research
Coronavirus disease 2019 (COVID-19) is a disease caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and can be aggravated by comorbid diseases. In administering COVID-19 therapy, we need to consider potential drug-drug interactions (pDDIs) with comorbid drugs. Most patients with comorbid diseases get polypharmacy, therefore the risk of pDDIs increases. Potential drug-drug interactions can cause unwanted effects such as toxicity to death. There is no on-label therapy for COVID-19 but FDA has Emergency Use Authorization (EUA) for hydroxychloroquine, chloroquine, azithromycin, remdesivir, ritonavir, and lopinavir. Some COVID-19 treatment potential drug-drug interactions have a level of severity C and D, so …
Prediction Of Asiatic Acid Derivatives Affinity Against Sars-Cov-2 Main Protease Using Molecular Docking,
2020
Faculty of Pharmacy, Universitas Padjadjaran, Bandung, Indonesia
Prediction Of Asiatic Acid Derivatives Affinity Against Sars-Cov-2 Main Protease Using Molecular Docking, Ida Musfiroh, Alia Resti Azura, Driyanti Rahayu
Pharmaceutical Sciences and Research
COVID-19 is a pandemic that currently occurs in almost all parts of the world, caused by a new coronavirus species that can infect humans, namely SARS-CoV-2. To date, there is no effective drug to treat COVID-19. There are studies proving that the secondary metabolites of pentacyclic triterpenes have antiviral activity, one of which is asiatic acid. The aims of this study are to obtain the affinity and interactions of asiatic acid derivative structures in inhibiting the main protease of SARS-CoV-2. The research method was molecular docking of asiatic acid and its derivatives against the main protease of SARS-CoV-2 (6LU7) consisting …
The Potential Roles Of Jamu For Covid-19: A Learn From The Traditional Chinese Medicine,
2020
Faculty of Pharmacy, Universitas Muhammadiyah Purwokerto, Indonesia
The Potential Roles Of Jamu For Covid-19: A Learn From The Traditional Chinese Medicine, Dwi Hartanti, Binar Asrining Dhiani, Shintia Lintang Charisma, Retno Wahyuningrum
Pharmaceutical Sciences and Research
As the pandemic of the coronavirus disease 2019 (COVID-19) continues while there is no drug and vaccine available, every effort to discover one should be considered. This review aimed to discuss the potential use of jamu, the Indonesian traditional herbal medicine, to deal with COVID-19 by following those of more-established traditional Chinese medicine (TCM). The online literature search using the PubMed database, as well as the circulars from the Indonesian Ministry of Health, were carried out to collect data up to June 07, 2020. The use of TCM for the treatment and prevention of COVID-19 has been officiated in the …
Sars-Cov-2: Virology And Drug Repurposing Approaches,
2020
Faculty of Pharmacy, Universitas Indonesia, Depok, Indonesia
Sars-Cov-2: Virology And Drug Repurposing Approaches, Ratika Rahmasari, Heri Setiawan, Rezi Riadhi Syahdi, Ayun Arifianti, Marina Ika Irianti, Rani Sauriasari, Juliann Nzembi Makau, Muhareva Raekiansyah
Pharmaceutical Sciences and Research
An emerging coronavirus, SARS-CoV-2, is the causative agent for the ongoing pandemic of coronavirus disease 2019 (COVID-19), which has caused a worldwide social and economic disruption. Currently, no antiviral drugs with proven clinical efficacy, or vaccines for its prevention. Therefore, to combat the pandemic of this novel coronavirus, new effective treatments are urgently needed. In the process of traditional drug development, developing new drugs from scratch is a time- consuming process, requires high-investment, and is a high-risk process, which is impractical to face the immediate global challenge of the SARS-CoV-2 pandemic. Drug repurposing strategy is one of the effective ways …
Remdesivir: Mechanism And Effectiveness For Coronavirus Disease 2019 (Covid-19),
2020
Faculty of Pharmacy, Universitas Airlangga, Surabaya, Indonesia
Remdesivir: Mechanism And Effectiveness For Coronavirus Disease 2019 (Covid-19), Vina Neldi, Suharjono Suharjono
Pharmaceutical Sciences and Research
Currently, coronavirus disease 2019 (COVID-19) is a very serious health problem. The World Health Organization (WHO) has characterized this disease as a pandemic. Recommendations related to vaccines and drugs are not available yet because they are still in the clinical trial phase, and one of the superior drugs is remdesivir which has an antiviral activity. Several clinical trials of this drug are being carried out with the aim of evaluating its safety and efficacy in COVID-19 patients. There are two clinical trials with completed recruitment status, which are NCT04257656 and NCT04280705. NCT04257656 showed that remdesivir had faster time for clinical …
Chloroquine: An Old To Be Repurposed Drug For Covid-19 Infection (Risk And Benefit),
2020
Study Program of Pharmacy, Faculty of Medicine, Hang Tuah University, Surabaya, Indonesia
Chloroquine: An Old To Be Repurposed Drug For Covid-19 Infection (Risk And Benefit), Oki Nugraha Putra, Ana Khusnul Faizah, Nani Wijayanti Dyah Nurrahman, Hardiyono Hardiyono
Pharmaceutical Sciences and Research
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) causes Coronavirus Disease 2019 (COVID-19) with a high rate of mortality. Chloroquine and hydroxychloroquine have been used for antimalarial and autoimmune diseases for many years. Due to low toxicity and well tolerability as well as immunomodulatory properties, these drugs are proposed to treat viral infection. Some studies, both in vitro and in a clinical setting, have been evaluated for their ability to treat SARS- CoV-2 as promising therapies. Although The National Agency of Drugs and Food Control of The Republic of Indonesia issued emergency authorization for chloroquine and hydroxychloroquine to be used against …
Hybrid Cyclic/Linear Peptides In A Multi-Component Lipid Structure As A Sirna Delivery System,
2020
Chapman University
Hybrid Cyclic/Linear Peptides In A Multi-Component Lipid Structure As A Sirna Delivery System, Abdulaziz Alasmari
Pharmaceutical Sciences (MS) Theses
Delivering siRNA is challenging due to many obstacles, such as extremely short in vivo half-life, rapid elimination via glomerular filtration, and inability to cross cell membranes due to the hydrophilic and negatively-charged nature. Thus, a delivery system is needed to deliver the siRNA into the cells by crossing the negatively-charged phospholipid cell membrane. The goal of this project was to design hybrid cyclic-linear peptides as siRNA delivery system. We designed and synthesized hybrid cyclic-linear peptides [R5K]W5, [R6K]W6, and [R5K]W7 containing positively-charged arginine residues attached to hydrophobic tryptophan chains for more efficient interaction with siRNA and to improve siRNA internalization into …
