Pharmaceutics and Drug Design Commons^™

Solid Dispersion Technology For Improving The Solubility Of Antiviral Drugs, Maria Elvina Tresia Butar-Butar, Nasrul Wathoni, Hestiary Ratih, Yoga Windhu Wardhana

Pharmaceutical Sciences and Research

Most drugs, including antiviral drugs, show low solubility in water, which affects dissolution, bioavailability, and therapeutic effectiveness. Therefore, many antiviral drugs are given in very large doses. One of the efforts to overcome these problems is the application of solid dispersions in which polymers and surfactants can trap drug molecules that are in the amorphous phase. Drugs in a hydrophilic carrier will increase wettability, water absorption capacity, and porosity of particles, so that the drug is released better. This review article will discuss the development of technology in solid-state, how solid dispersion overcomes the lack of solubility and the rate …

Beyond Use Date (Bud) Determination Of Ambroxol Hydrochloride Syrup By High-Performance Liquid Chromatography – Uv/Vis Detector, Catur Jatmika, Raditya Iswandana, Indah Dewi Lestari

Pharmaceutical Sciences and Research

Ambroxol HCl is a mucolytic agent often used to treat respiratory disorders associated with excess mucus secretion. This study aims to determine the beyond-use date (BUD) of ambroxol HCl syrup on the market based on analysis of the decrease in drug content using High-Performance Liquid Chromatography (HPLC) – UV/Vis detector. The HPLC conditions were reversed-phase with a C18 column, mobile phase containing acetonitrile - phosphate buffer 0.05 M pH 4.5 (60:40) at a flow rate of 1.0 ml/min using UV detection at 248 nm. To determine BUD, five syrup preparations (brands) obtained from the Jakarta area were analyzed in triplicate. …

The Application Of Continuous Stationary Phase Gradients To High-Performance Liquid Chromatography And Its Potential To Improve Pharmacological Research, Hannah Klose

Senior Honors Theses

The separation of mixtures into different components is integral to experimentation and analysis in a multitude of fields. Chromatography is one of the most popular, well-developed, and well-studied methods used to examine the makeup of a mixture. Thus, the improvement of chromatographic procedures directly benefits research across many scientific disciplines. The application of a continuous stationary phase gradient to High-Performance Liquid Chromatography (HPLC) methods has been proposed to improve the separation of complex mixtures that are difficult to achieve with existing separation techniques. By incorporating a gradient stationary phase, analysts will create a more selective mode of separation to improve …

Development, Optimization, And In Vitro/In Vivo Evaluation Of Azelaic Acid Transethosomal Gel For Antidermatophyte Activity, Ali Nasr, Noha Badawi, Yasmine Tartor, Nader Sobhy, Ali Nasr

Pharmacy

Treatment of dermatophytosis is quite challenging. This work aims to investigate the antidermatophyte action of Azelaic acid (AzA) and evaluate its efficacy upon entrapment into transethosomes (TEs) and incorporation into a gel to enhance its application. Optimization of formulation variables of TEs was carried out after preparation using the thin film hydration technique. The antidermatophyte activity of AzA-TEs was first evaluated in vitro. In addition, two guinea pig infection models with Trichophyton (T.) mentagrophytes and Microsporum (M.) canis were established for the in vivo assessment. The optimized formula showed a mean particle size of 219.8 ± 4.7 nm and a …

Computational Evaluation Of Bioactive Compounds From Vaccinium Vitis-Idaea L (Ligonberry) For Treating Kras-Associated Lung Cancer, Ayooluwa Ilesanmi, Gbenga Dairo, Toheeb Balogun, Bibiire Awoyale

Undergraduate Research Conference

Lung cancer is the cancer of the lung's epithelial cells typically characterized by difficult breathing, chest pain, blood-stained coughs, headache, and weight loss. If left unmanaged, lung cancer can spread to other body parts. While several treatment methods exist for managing lung cancer, exploring natural plant sources for developing therapeutics offers great potential in complementing different treatment approaches. In this study, we concentrated on inhibiting the mutated Kirsten rat sarcoma viral oncogene homolog (KRAS) by targeting an associated protein (Phosphodiesterase 6δ) to which KRAS form complexes. We evaluated bioactive compounds from Lingonberry (Vaccinium vitis-idaea L), adopting computational approaches such as …

Virtual And In Vitro Screening Of Natural Products Identifies Indole And Benzene Derivatives As Inhibitors Of Sars-Cov-2 Main Protease (MPro), Dony Ang, Riley Kendall, Hagop S. Atamian

Biology, Chemistry, and Environmental Sciences Faculty Articles and Research

The rapid spread of the coronavirus disease 2019 (COVID-19) resulted in serious health, social, and economic consequences. While the development of effective vaccines substantially reduced the severity of symptoms and the associated deaths, we still urgently need effective drugs to further reduce the number of casualties associated with SARS-CoV-2 infections. Machine learning methods both improved and sped up all the different stages of the drug discovery processes by performing complex analyses with enormous datasets. Natural products (NPs) have been used for treating diseases and infections for thousands of years and represent a valuable resource for drug discovery when combined with …

Effectiveness And Safety Of Apixaban Vs Warfarin In Patients With Venous Thromboembolism With Risk Factors For Bleeding Or For Recurrences, Alexander T. Cohen, Janvi Sah, Amol D. Dhamane, Dionne M. Hines, Theodore Lee, Lisa Rosenblatt, Birol Emir, Allison Keshishian, Huseyin Yuce, Xuemei Luo

Publications and Research

Introduction

Patients at increased risk of bleeding and recurrent VTE who develop venous thromboembolism (VTE) present challenges for clinical management. This study evaluated the effectiveness and safety of apixaban vs warfarin in patients with VTE who have risk factors for bleeding or recurrences.

Methods

Adult patients with VTE initiating apixaban or warfarin were identified from five claims databases. Stabilized inverse probability treatment weighting (IPTW) was used to balance characteristics between cohorts for the main analysis. Subgroup interaction analyses were conducted to evaluate treatment effects among patients with and without each of the conditions that increased the risk of bleeding (thrombocytopenia …

The Science Of Oral Carbapenems, Landon Olsen, Daniel J. Yang, Aiyi Chen, Thahn-Liem Vu, H. Stephen Lee

Annual Research Symposium

No abstract provided.

A Ligand-Based Approach To Identifying Commercially Available Inhibitors Of Human Galactokinase (Galk), Tyler Rose

Annual Research Symposium

The purpose of this project was to find inhibitors of the human galactokinase (GALK) enzyme. GALK is responsible for catalyzing the conversion of galactose to galactose 1-phosphate, the first step in galactose metabolism. Galactose 1-phosphate builds up in the cells of patients with type 1 galactosemia due a genetic disorder. It has been proposed that inhibiting galactose 1-phosphate production by GALK may prevent many of the major complications of type 1 galactosemia. In this study, a ligand-based approach was used to identify commercially available inhibitors of GALK, starting from galactose-bearing natural products. Candidate inhibitors were screened for their ability to …

Tech Note 2023-1 Nih Contribution To Phased Clinical Development Of Drugs Approved From 2010-2019, Edward Zhou, Matthew Jackson, Fred Ledley

CISI Publication

This report describes the methods and preliminary results for the manuscript titled, “Spending on Phased Clinical Development of Approved Drugs by the US National Institutes of Health Compared With Industry.”

Characterization, Antibacterial, Antioxidant, Antidiabetic, And Anti-Inflammatory Activities Of Green Synthesized Silver Nanoparticles Using Phragmanthera Austroarabica A. G. Mill And J. A. Nyberg Extract, Shady Swidan, Dina Khodeer, Sarah Shabayek, Ali Nasr, Roaa Khinkar, Mohammed Aldurdunji, Maryam Ramadan, Jihan Badr

Pharmacy

Introduction: Diabetes mellitus is a chronic metabolic disorder that exhibited great expansion all over the world. It is becoming an epidemic disease adding a major burden to the health care system, particularly in developing countries.

Methods: The plant under investigation in the current study Phragmanthera austroarabica A. G. Mill and J. A. Nyberg is traditionally used in Saudi Arabia for the treatment of diabetes mellitus. The methanolic extract (200 mg/kg) of the plant and pure gallic acid (40 mg/kg), a major metabolite of the plant, as well as their silver nanoparticle formulae (AgNPs) were evaluated for their antidiabetic activity.

Results …

Pharmacology Of Disulfiram As An Antibacterial Agent, Yogesh Meka

Theses, Dissertations and Capstones

Disulfiram (Antabuse®) is an oral prescription drug used to treat alcohol abuse disorder (AUD). Disulfiram (DSF) and its metabolites act on the body by inhibiting multiple enzymes involved in alcohol metabolism. This study aims to understand the pharmacology of disulfiram as an antibacterial medication. Previous studies on DSF showed antibiotic activity against multidrug-resistant Staphylococcus aureus strains (MRSA). The initial aim of this study was to decipher the mechanisms involved in inhibiting bacterial growth by DSF, which was done by performing biochemical studies. The studies revealed that DSF had antagonistic effects on redox buffering and energy production. Another aim of this …

Role Of Histone Deacetylase (Hdac) In Epithelial To Mesenchymal Transition (Emt) In A Human Cholangiocyte Model Of Ischemic Cholangiopathy, Priyanshi Pragnesh Parikh

Theses and Dissertations

Organ transplants are a vital intervention for many diseases that result in end stage organ failure. Currently, the donation pool is not meeting the demands of the transplant list. Expanding this pool to include donation after cardiac death (DCD) is highly sought-after. However, the use of DCD livers can lead to increased odds of graft failure and ischemic cholangiopathy. The loss of epithelialization and fibrosis that occurs during ischemic cholangiopathy is characteristic of these cells undergoing epithelial-to-mesenchymal transition (EMT). The biological changes the cell experiences enhance migratory capacity, invasiveness, and increased resistance to apoptosis. Our earlier studies have shown differential …

Testing The Efficacy And Synergistic Components Of Sesamol And Black Rice Extract On Human Colon Cancer Cells, Sera Lim, Philip M. Gerk

Undergraduate Research Posters

Purpose: Systemic treatment of colorectal cancer involves chemotherapeutic agents which elicit serious and negative side effects from the toxicity of the drug. To address this issue, we are testing dietary supplements for their efficacy against human colon cancer cell lines and also their potential synergistic effects when combined with conventional chemotherapy. Dietary supplements (specifically sesamol and black rice extract) exhibit anticancer, anti-inflammatory, and chemo-preventive properties. Meanwhile, one of the cancer resistance mechanisms is the upregulation of drug elimination mechanisms, leading to multi-drug resistance. We hypothesize that dietary compounds will act as chemo-enhancers, thus enhancing potency of the chemotherapy drug(s) on …

Cultivating Health, Not Wealth In The United States' Healthcare System: Comprehensive Revisions For The Orphan Drug Act Of 1983, Kayla Smith

Regis University Student Publications (comprehensive collection)

This thesis explores the way in which the Orphan Drug Act of 1983, originally instituted in response to a lack of treatments for rare diseases in the United States of America, has failed to achieve its initial objectives in the 40 years since its implementation. In evaluating various successful examples of government subsidization programs designed to intervene in private industry, this thesis composes the criterion required for funding-based legislation which maximize market outcomes while minimizing tax-payer burden. An analysis of the synthetic organic chemistry industry – and a case study into the production of a particular orphan treatment for a …

Self-Assembled Ternary Polypeptide Nanoparticles With Improved Biostability For Drug Delivery In Cancer Therapy, Preye Mike Agbana

Theses and Dissertations--Pharmacy

Cancer remains a real and present threat to global health. In the United States, according to cancer statistics, almost 40% of people will be diagnosed with cancer at some point in their lifetime. Conventional chemotherapy has become the mainstay for cancer treatment option. However, chemotherapeutic agents are plagued with problems such as poor aqueous solubility, chemical degradation, Bio instability, and off-site toxicity due to non-specificity. New drug modalities are needed to tackle the ever-growing burden on cancer. In recent times, the promise of nanotechnology has aided to develop drug delivery vehicles to facilitate the administration of potent chemotherapeutics. Nanoformulations such …

Public Health Product Hops, Michael S. Sinha

All Faculty Scholarship

Pharmaceutical product hops are anticompetitive maneuvers that often represent a last-ditch effort by brand manufacturers to preserve market share in the face of generic competition. An integral part of product life cycle management strategies, product hops may offer marginal benefits to patients but can substantially increase costs to payers and patients alike. Yet industry advocates maintain that this is essential follow-on research and development, resulting in the development of novel products that would otherwise never reach the market.

Is there a middle ground between these two diametrically opposed views? Might certain product hops be considered beneficial, perhaps if they furthered …

Right Treatment Wrong Time: Immunotherapy Administration Post-Radiotherapy Decreases Tumor Burden In A Preclinical Model Of Brain Metastasis, Kathryn Elizabeth Blethen

Graduate Theses, Dissertations, and Problem Reports

This dissertation (a) provided an in-depth literature review of methods to modulate the blood-brain and blood-tumor barriers to increase drug delivery and efficacy in brain metastases, (b) evaluated the effects of whole-brain radiation therapy on the blood-brain barrier in immunocompetent and immunocompromised mouse models and proposed a mechanism by which the immune response to radiation disrupts the blood-brain barrier, and (c) developed a syngeneic lung cancer brain metastasis model to determine the impact of coordinated immunotherapy administration with radiotherapy. The blood-brain barrier is an impediment to drug delivery to the brain. The inherent leakiness of the blood-tumor barrier does not …

Physiologically-Based Pharmacokinetic (Pbpk) Modeling For The Preclinical Development Of Spectinamide Antibiotics, Keyur R. Parmar

Theses and Dissertations (ETD)

Despite being an ancient disease caused by Mycobacterium tuberculosis (Mtb) and after decades of research, tuberculosis (TB) still affects millions of people every year worldwide. In 2018, the World Health Organization (WHO) reported that 10 million people developed tuberculosis and 1.5 million died of the disease. With the increase in the multidrug-resistant (MDR) and extensively drug-resistant (XDR) cases, the treatment for TB with the standard first and second-line therapy is becoming increasingly difficult. Therefore, there is an urgent need to find new anti-TB drugs as combination partners of existing and experimental classes of antimicrobial agents to shorten and simplify the …

Assessing Drug Development Proporties Of Antithrombotic And Anti - Cancer Agents, Elsamani I. Abdelfadiel

Theses and Dissertations

The current GAG anticoagulants such as heparin, heparin derivatives, and vitamin K antagonists, such as warfarin continue to be the backbone of anticoagulant therapy. These drugs act through an indirect mechanism to convey inhibition of several coagulation enzymes. However, xv their use leads to several serious adverse effects, such as excessive bleeding risk and unpredictability of patient response. Regardless of their clinical achievement, every individual agent is accompanied by several side effects, particularly major/minor bleeding, thrombocytopenia, drug-food or drug-drug interactions, or absence of antidote. Of all these side effects, bleeding, and a lack of an effective antidote to reverse excessive …