Medicinal Chemistry and Pharmaceutics Commons^™

A Micro-Nano Particle System For Sustained Drug Release In Lung Cancer Therapy, Heta N. Jadhav

USF Tampa Graduate Theses and Dissertations

Lung cancer remains the leading cause of cancer-related mortality in men and women worldwide (National Comprehensive Cancer Network). Hence, developing an effective new therapy to treat lung cancer is under intense investigation. Specifically, the sustained release of a drug in lung tumors is critically important. Previous studies at the USF have shown that telmisartan exhibits synergistic properties when combined with Actinomycin-D for lung cancer treatment. The objective of this study is to develop a novel micro/nano system consisting of lipids and chitosan polymers that would be able to deliver Tel directly to the lungs and release its payloads in a …

Sunitinib-Loaded Mpeg-Pcl Micelles For The Treatment Of Age-Related Macular Degeneration, Jarriaun D. Streets

USF Tampa Graduate Theses and Dissertations

Age-related Macular Degeneration, or AMD will be responsible for the vision impairment of more than 5 million late-aged adults in the next 30 years. Current treatment options include frequent intravitreal injections which report high levels of pain resulting in a low patient compliance. However, there are methods of drug delivery that can decrease the amount of intravitreal injections by sustaining drug release. Polymeric micelles, specifically MPEG-PCL have reported superb biocompatibility and more efficient ways of delivering anti-VEGF drugs such as Sunitinib to the posterior segment of the eye. In this study, the novel micellar formulation exhibited an average DLS particle …

Synthesis Of A Targeted Ph Responsive Nanoparticle For Controlled Release Of Actinomycin D, Alejandro Jesus Gonzalez

USF Tampa Graduate Theses and Dissertations

Out of all cancer diagnosis’s, lung cancer has the highest mortality in both sexes making it the leading cause of cancer deaths. Current therapeutic and clinical methods fail to successfully treat the disease, contributed to the development of multi-drug resistance (MDR). Hence, new therapies are needed that can exploit the tumor microenvironment (TME) to target Cancer Stem Cells (CSC). CSCs constitute a key population of the TME, promoting hypoxia, low intracellular pH, and angiogenesis. Actinomycin D (ACD) is a potent CSC inhibitor, but due to its high toxicity and lack of specificity towards cancer cells presents a need for a …

To Compare Cyclosporine A Nanoformulations For Their Effectiveness In Reducing Nephrotoxicity, Ilkin Nasirli

USF Tampa Graduate Theses and Dissertations

Cyclosporine (CsA) is one of the main immune-suppressant agents which has been used widely in organ transplantation against graft rejection. However, the low oral bioavailability and the associated adverse effects such as nephrotoxicity are the main drawbacks of current usage of this drug. Thus, purpose of this research is to formulate PLGA nanoparticles of CsA to improve its effectiveness and to reduce the nephrotoxicity induced by the plain drug. CsA-loaded PLGA nanoparticles were prepared by the nanoprecipitation method. Particle size and zeta potential of the formulation was determined and percent drug entrapment were also determined. Quantitative estimation was carried out …

Pazopanib Loaded Plga Nanoparticles For The Treatment Of Age-Related Macular Degeneration, Gulimirerouzi Fnu

USF Tampa Graduate Theses and Dissertations

Age-related macular degeneration (AMD) is a reason of severe vision loss worldwide. Pazopanib is a multitargeted tyrosine kinase inhibitor drug that can reduce neovascularization by mainly acting on vascular endothelial growth factor receptor (VEGFR). An intraocular injection to posterior segment of eye of anti-VEGF agent at present represents the cornerstone of therapies for AMD. However, challenges in targeting and delivering drug to eye’s posterior segment well as difficulties arising from repetitive frequent intraocular injections, which requires novel drug delivery method. In this study, pazopanib loaded PLGA‐NPs were prepared and the studied formulation had particle size of 132.1 ± 1.4 nm …

Nanoparticle Synthesis For Glucose-Loaded Mesoporous Silica And Sucrose Hydrolysis Strategies For Bioanalyte Detection Applications Using A Personal Glucose Meter, Xiomar Emauel Bustos Perez

USF Tampa Graduate Theses and Dissertations

Point-of-care (POC) tests are a reliable, portable, easy to use, and more affordable alternative to regular laboratory diagnostic tests. They bypass the necessity of expensive equipment, human labor, and technical expertise. The personal glucose meter (PGM) is a POC device that measures glucose levels in blood. Lately, the PGM have been used as a tool to detect other bioanalytes in different applications. There are two analytes which POC detection would be beneficial for patients: creatinine and tacrolimus. Creatinine is used to calculate glomerular filtration rate, a measurement of kidneys function that can help to diagnose kidney failure, and other nephropathies. …

A New Approach To The Development Of An Rsv Anti-Viral Targeted Nanocarrier For Dual Inhibition Of Viral Infection And Replication, Anthony N. Singer

USF Tampa Graduate Theses and Dissertations

Respiratory Syncytial Virus (RSV) is a potentially life-threatening respiratory pathogen that infects approximately 64 million children and immunocompromised adults globally per year. Currently, there is a need for prophylactic and therapeutic approaches effective against primary and secondary RSV infections. This project focuses on the development of a simple, smart, and scalable anti-RSV nanotherapeutic that combines novel cellular antiviral defense mechanisms targeting the inhibition of viral fusion and replication. An ICAM-1 targeted liposomal nanocarrier will be synthesized and coated with a layer of chitosan containing the anti-fusion HR2-D peptide as an extracellular defense mechanism. Additionally, chitosan complexed to dual expressing short …

Signal Detection Of Adverse Drug Reaction Using The Adverse Event Reporting System: Literature Review And Novel Methods, Minh H. Pham

USF Tampa Graduate Theses and Dissertations

One of the objectives of the U.S. Food and Drug Administration is to protect the public health through post-marketing drug safety surveillance, also known as Pharmacovigilance. An inexpensive and efficient method to inspect post-marketing drug safety is to use data mining algorithms on electronic health records to discover associations between drugs and adverse events.

The purpose of this study is two-fold. First, we review the methods and algorithms proposed in the literature for identifying association drug interactions to an adverse event and discuss their advantages and drawbacks. Second, we attempt to adapt some novel methods that have been used in …

Chemical Investigation Of Antarctic Marine Organisms & Their Role In Modern Drug Discovery, Jacqueline Lee Fries

USF Tampa Graduate Theses and Dissertations

The chemicals produced by biological systems, whether proteins, peptides, or terpenes, will always provide an intriguing topic for researchers. Invisibly controlling every aspect of nature, these molecules are responsible for life, evolution, and death. Specifically, here is described the secondary metabolites produced by Antarctic marine organisms as well as others, and how they are used to defend or attract other animals while potentially providing health benefits to mankind. This is done through collection, extraction, and separation of individual specimens. The respective mixtures of compounds after isolation are then analyzed via spectroscopic methods such as nuclear magnetic resonance spectroscopy, mass spectrometry, …

Statistical Analysis, Modeling, And Algorithms For Pharmaceutical And Cancer Systems, Bong-Jin Choi

USF Tampa Graduate Theses and Dissertations

The aim of the present study is to develop a statistical algorithm and model associ- ated with breast and lung cancer patients. In this study, we developed several statistical softwares, R packages, and models using our new statistical approach.

In the present study, we used the five parameters logistic model for determining the optimal doses of a pharmaceutical drugs, including dynamic initial points, an automatic process for outlier detection and an algorithm that develops a graphic user interface(GUI) program. The developed statistical procedure assists medical scientists by reducing their time in determining the optimal dose of new drugs, and can …

Computational Approaches For Structure Based Drug Design And Protein Structure-Function Prediction, Sai Lakshmana Kumar Vankayala

USF Tampa Graduate Theses and Dissertations

This dissertation thesis consists of a series of chapters that are interwoven by solving interesting biological problems, employing various computational methodologies. These techniques provide meaningful physical insights to promote the scientific fields of interest. Focus of chapter 1 concerns, the importance of computational tools like docking studies in advancing structure based drug design processes. This chapter also addresses the prime concerns like scoring functions, sampling algorithms and flexible docking studies that hamper the docking successes. Information about the different kinds of flexible dockings in terms of accuracy, time limitations and success studies are presented. Later the importance of Induced fit …

Cure From The Cave: Volcanic Cave Actinomycetes And Their Potential In Drug Discovery, Naowarat (Ann) Cheeptham Dr., Tara Sadoway, Devon Rule, Kent Watson, Paul Moote, Laiel C. Soliman, Nicholas Azad, Kingsley Donkor, Derrick Horne

International Journal of Speleology

Volcanic caves have been little studied for their potential as sources of novel microbial species and bioactive compounds with new scaffolds. We present the first study of volcanic cave microbiology from Canada and suggest that this habitat has great potential for the isolation of novel bioactive substances. Sample locations were plot ted on a contour map that was compiled in ArcView 3.2. Over 400 bacterial isolates were obtained from the Helmcken Falls cave in Wells Gray Provincial Park, British Columbia. From our preliminary screen, of 400 isolates tested, 1% showed activity against extended spectrum ß-lactamase E. coli, 1.75% against Escherichia …

N-Glycosylation Dictates Proper Processing Of Organic Anion Transporting Polypeptide 1b1, Juan Yao, Weifang Hong, Jiujiu Huang, Kai Zhan, Hong Huang, Mei Hong

School of Information Faculty Publications

Organic anion transporting polypeptides (OATPs) have been extensively recognized as key determinants of absorption, distribution, metabolism and excretion (ADME) of various drugs, xenobiotics and toxins. Putative N-glycosylation sites located in the extracellular loops 2 and 5 is considered a common feature of all OATPs and some members have been demonstrated to be glycosylated proteins. However, experimental evidence is still lacking on how such a post-translational modification affect the transport activity of OATPs and which of the putative glycosylation sites are utilized in these transporter proteins. In the present study, we substituted asparagine residues that are possibly involved in N-glycosylation with …

Modulating The Pharmacokinetics Of Bioflavonoids, Adam John Smith

USF Tampa Graduate Theses and Dissertations

One of the largest obstacles in drug development is to overcome solubility and bioavailability problems. Preformulation strategies such as nanoparticle formation are often employed but sometimes create new issues and are limited in their effectiveness and applications. Since the majority of drugs are marketed and sold as solid forms, drug delivery systems are not always desirable. This is where solid-state chemistry becomes important. Traditional solid-state chemistry approaches are often successful but are sometimes too restrictive and cannot be applied to certain compounds. Cocrystals have emerged as an alternative solid-state technique that can be applied to a broad range of compounds. …