Pharmaceutics and Drug Design Commons^™

Simultaneous Bactericidal And Osteogenic Effect Of Nanoparticulate Calcium Phosphate Powders Loaded With Clindamycin On Osteoblasts Infected With Staphylococcus Aureus, Vuk Uskoković, Tejal A. Dasai

Pharmacy Faculty Articles and Research

S aureus internalized by bone cells and shielded from the immune system provides a reservoir of bacteria in recurring osteomyelitis. Its targeting by the antibiotic therapy may thus be more relevant for treating chronic bone infection than eliminating only the pathogens colonizing the bone matrix. Assessed was the combined osteogenic and antibacterial effect of clindamycinloaded calcium phosphate nanoparticles of different monophasic compositions on co-cultures comprising osteoblasts infected with S aureus. Antibiotic-carrying particles were internalized by osteoblasts and minimized the concentration of intracellular bacteria. In vitro treatments of the infected cells, however, could not prevent cell necrosis due to the …

Nanoparticulate Drug Delivery Platforms For Advancing Bone Infection Therapies, Vuk Uskoković, Tejal A. Dasai

Pharmacy Faculty Articles and Research

Introduction—The ongoing surge of resistance of bacterial pathogens to antibiotic therapies and the consistently aging median member of the human race signal an impending increase in the incidence of chronic bone infection. Nanotechnological platforms for local and sustained delivery of therapeutics hold the greatest potential for providing minimally invasive and maximally regenerative therapies for this rare but persistent condition.

Areas covered—Shortcomings of the clinically available treatment options, including poly(methyl methacrylate) beads and calcium sulfate cements, are discussed and their transcending using calcium-phosphate/polymeric nanoparticulate composites is foreseen. Bone is a composite wherein the weakness of each component alone is …

Investigating Intermolecular Interactions In Crystalline Aspirin Using Cdft, Nicholas Turner, Tonglei Li, Mingtao Zhang

The Summer Undergraduate Research Fellowship (SURF) Symposium

Drugs today are widely administered in their crystalline form, namely via tablets and capsules. The crystal structure of a drug molecule affects important drug qualities such as solubility, bioavailability, shelf life, and compaction properties. In order to form a basis for crystal structure prediction, it is necessary to first understand how intermolecular interactions cause molecules to pack in certain ways. Being able to predict and perhaps even control a drug molecule’s crystal structure will lead to the development of higher quality drugs that perform more consistently. Scientists and engineers do not fully understand the reasons for a molecule assuming a …

Effects Of Short-Term Portacaval Anastomosis On The Peripheral And Brain Disposition Of The Blood-Brain Barrier Permeability Marker Sodium Fluorescein In Rats, Imam H. Shaik, M. K. Miah, Ulrich Bickel, Reza Mehvar

Pharmacy Faculty Articles and Research

Contradictory results have been reported with regard to the effects of various models of hepatic encephalopathy on the blood-brain barrier (BBB) permeability, which may be due partly to the use of brain concentrations of BBB markers without attention to their peripheral pharmacokinetics. The purpose of the current study was to investigate the effects of short-term portacaval anastomosis (PCA), a type B model of hepatic encephalopathy, on the peripheral pharmacokinetics and brain distribution of sodium fluorescein (FL), which is a small molecule marker of BBB passive permeability. A single 25 mg/kg dose of FL was administered intravenously to 10-day PCA and …

A Standardized Patient Counseling Rubric For A Pharmaceutical Care And Communications Course, Niambi Horton Pharmd, Kenna D. Payne Pharmd, Michelle Jernigan Pharmd, Jill Frost Pharmd, Stephen Wise Pharmd, Mary Klein Pharmd, Joel Epps Mba, H. Glenn Anderson Pharmd

Pharmaceutical Science and Research

Objective. To restructure a required pharmaceutical care and communications course to place greater emphasis on communication skills and include a high-stakes assessment.

Design. A standardized counseling rubric was developed for use throughout the pharmacy curriculum and the counseling laboratory practicals were changed to high-stakes assessments.

Assessment. An annual mid-semester and end-of-semester high-stakes patient-counseling objective structured clinical examination (OSCE) conducted prior to and after revision of the course and counseling rubric documented improvements in students’ scores. Performance on the post-course annual assessment patient counseling OSCE improved compared to that on the pre-course (p,0.001).

Conclusion. The 2010 course revision improved …

Controlling The Size And Shape Of Polypeptide Colloidal Particles: Temperature Dependence Of Particle Formation, John P. Gavin, Nolan B. Holland, Kiril A. Streletzky

Undergraduate Research Posters 2013

A promising approach for developing new drug delivery vehicles is by using stimuli responsive hydrogel nanoparticles. Polypeptide surfactants designed in our lab have been shown to form micellar particles of varying sizes and shapes depending on the solution salt concentration. These responsive polypeptide surfactants consist of a small charged protein domain (foldon) with three elastin-like polypeptide (ELP) chains forming a three-armed star polymer. The size and shape of the micelles they form is dependent on the ratio of total ELP volume to head group area. By introducing linear ELP into the ELP-foldon solution, the total volume of ELP in the …

Development Of Hif-1Α/Hif-1Β Heterodimerization Inhibitors Using A Novel Bioluminescence Reporter Assay System For In Vitro High Throughput Screening And In Vivo Imaging, Yun-Chen Chiang

Dissertations & Theses (Open Access)

Tumor growth often outpaces its vascularization, leading to development of a hypoxic tumor microenvironment. In response, an intracellular hypoxia survival pathway is initiated by heterodimerization of hypoxia-inducible factor (HIF)-1α and HIF-1β, which subsequently upregulates the expression of several hypoxia-inducible genes, promotes cell survival and stimulates angiogenesis in the oxygen-deprived environment. Hypoxic tumor regions are often associated with resistance to various classes of radio- or chemotherapeutic agents. Therefore, development of HIF-1α/β heterodimerization inhibitors may provide a novel approach to anti-cancer therapy. To this end, a novel approach for imaging HIF-1α/β heterodimerization in vitro and in vivo was developed in this study …

Combination Of Sirna-Directed Gene Silencing With Cisplatin Reverses Drug Resistance In Human Non-Small Cell Lung Cancer, Shanthi Ganesh, Arun K. Iyer, Jan Weller, David V. Morrissey, Mansoor M. Amiji

Pharmaceutical Sciences Faculty Publications

One of the most challenging aspects of lung cancer therapy is the rapid acquisition of multidrug-resistant (MDR) phenotype. One effective approach would be to identify and downregulate resistance-causing genes in tumors using small interfering RNAs (siRNAs) to increase the sensitivity of tumor cells to chemotherapeutic challenge. After identifying the overexpressed resistance-related antiapoptotic genes (survivin and bcl-2) in cisplatin-resistant cells, the siRNA sequences were designed and screened to select the most efficacious candidates. Modifications were introduced in them to minimize off-target effects. Subsequently, the combination of siRNA and cisplatin that gave the maximum synergy was identified in resistant cells. We then …

Microspheres For Liver Radiomicrospheres Therapy And Planning, Alejandro Amor-Coarasa

FIU Electronic Theses and Dissertations

Liver cancer accounts for nearly 10% of all cancers in the US. Intrahepatic Arterial Radiomicrosphere Therapy (RMT), also known as Selective Internal Radiation Treatment (SIRT), is one of the evolving treatment modalities. Successful patient clinical outcomes require suitable treatment planning followed by delivery of the microspheres for therapy. The production and in vitro evaluation of various polymers (PGCD, CHS and CHSg) microspheres for a RMT and RMT planning are described. Microparticles with a 30±10 µm size distribution were prepared by emulsion method. The in vitro half-life of the particles was determined in PBS buffer and porcine plasma and their potential …

Research Fatigue Among Injecting Drug Users In Karachi, Pakistan, Aysha Zahidie, Arshad Altaf, Adeel Ahsan, Tanzil Jamali

Community Health Sciences

Background

Karachi is the largest metropolis of Pakistan and its economic hub attracting domestic migrants for economic opportunities. It is also the epicenter of HIV epidemic in the country. Since 2004, one pilot study and four behavioral and biological surveillance rounds have been conducted in Karachi. In addition many student research projects have also focused on key risk groups including injection drug users (IDUs). As a result of this extra ordinary exposure of same kind of questions, IDUs know how to respond to high value questions related to sharing of needles or unsafe sexual practices. The purpose of the study …

Hollow Fiber Membrane-Based Air Gap Membrane Distillation, Xuan Wang

Theses

Membrane Distillation (MD) is a thermally-driven separation process. In this research, desalination of 1 % NaCl solution is achieved by one type of MD namely, Air Gap Membrane Distillation (AGMD). The characteristics of AGMD are evaluated by using a hollow-fiber-set-based compact device. Hot brine solution and cold water are passed through two different fiber sets separately: porous hydrophobic polyvinylidene fluoride hollow fibers of the E type (PVDF E) and solid polypropylene (PP) hollow fibers. Vapor from the hot brine crosses the membrane pores of the PVDF fibers and the air gap, and finally condenses over the surface of solid hollow …

Dissolution Of Different Commercial Aspirin Tablets Using A Novel Off-Center Paddle Impeller (Opi) Dissolution Testing System, Yang Qu

Theses

Dissolution testing is routinely conducted in the pharmaceutical industry to provide in vitro drug release information for quality control purposes. The most common dissolution testing system for solid dosage forms is the United States Pharmacopeia (USP) Dissolution Testing Apparatus 2. In this work, a modified Apparatus 2, termed "OPI" System for "off-center paddle impeller," in which the impeller is placed 8 mm off center in the vessel is tested to determine its sensitivity to differentiate between the dissolution profiles of differently formulated and manufactured tablets. Dissolution tests are conducted with both the OPI System and the Standard System using three …

Hydrodynamic Effects Of A Cannula In A Usp Dissolution Testing Apparatus 2, Qianqian Liu

Theses

Dissolution testing is routinely used in the pharmaceutical industry to provide in vitro drug release information for drug development and quality control purposes. The USP Testing Apparatus 2 is the most common dissolution testing system for solid dosage forms. Usually, sampling cannulas are used to take samples manually from the dissolution medium. However, the inserted cannula can alter the normal fluid flow within the vessel and produce different dissolution testing results.

The hydrodynamic effects introduced by a permanently inserted cannula in a USP Dissolution Testing Apparatus 2 were evaluated by two approaches. Firstly, the dissolution tests were conducted with two …

Engineering Spores To Display G Protein-Coupled Receptors For Directed Evolution, Alyssa Misoo Kim

Theses

All human cells are surrounded by a plasma membrane made from a phospholipid bilayer, which is responsible for maintaining a biologically active species, while stopping entry of deleterious substances from the outside. G protein-coupled receptors (GPCRs) are the membrane proteins, which transmit signals across the cell membrane. GPCRs are involved in almost every physiological process, and irregular control leads to pathological conditions. Therefore, they are major drug targets. Crystal structure determination is required to understand the molecular details of activation/deactivation. However, GPCRs are difficult to crystallize because of stability issues. An efficient protein engineering system needs to be developed. The …

Effect Of Tablet Compression On The Dissolution Of Aspirin Tablets Using A Novel Off-Center Paddle Impeller (Opi) Dissolution Testing System, Chuan Sun

Theses

In the pharmaceutical industry, dissolution testing is routinely carried out to determine the dissolution rate of oral solid dosage forms. Among several testing devices, the USP Dissolution Apparatus 2 is the device most commonly used. However, despite its widespread use, this apparatus has been shown to produce test failures and to be very sensitive to a number of small geometry changes.

The objective of this study was to determine whether a novel dissolution system termed “OPI” for “off-center paddle impeller” was sensitive enough to determine differences in tablet dissolution profiles caused by different compression pressure during the tablet manufacturing process. …

Qsar Modeling Of Chemical Penetration Enhancers Using Novel Replacement Algorithms, Hui Qiu

Theses

The applications of transdermal delivery are limited because of the resistance of the skin to drug diffusion. Only potent drugs, with molecular weight less than 500 Da, are suitable to cross the skin barrier. Chemical Penetration Enhancers (CPEs) are used to promote the absorption of solutes across the dermal layers. In this investigation, a Quantitative Structure-Activity Relationship (QSAR) model is applied to relate chemical penetration enhancer structures with the flux enhancement ratio through a statistical approach.

A database, consisting of 61 non-polar CPEs, is selected for the study. Each compound is represented by 777 QSAR descriptors, which encode the physical …

Shots For Tots?, Eric A. Feldman

All Faculty Scholarship

By endorsing the use of a vaccine that makes the experience of puffing on a cigarette deeply distasteful, Lieber and Millum have taken the first few tentative steps into a future filled with medical interventions that manipulate individual preferences. It is tempting to embrace the careful arguments of “Preventing Sin” and celebrate the possibility that the profound individual and social costs of smoking will finally be tamed. Yet there is something unsettling about the possibility that parental discretion may be on the cusp of a radical expansion, one that involves a new and unexplored approach to behavior modification.

A Series Of Pharmaceutical Technology Concepts Applied To Pediatric Formulations, Hao Lou

Theses and Dissertations (ETD)

Pediatric formulations have received great attention from regulatory agencies in the United States and Europe. Since solid dosage forms such as tablets and capsules will not be able to improve pediatric patients’ compliance, customized pediatric formulations are needed. In response, formulators in the pharmaceutical industry have made significant effort into developing various pediatric formulations. However, developing satisfactory pediatric formulations is a process that is guided by case by case basis. The objective of this current study was to apply the scientific pharmaceutical technology concepts into developing modern pediatric formulations. We have shown that the drug delivery design will be affected …

In Vitro Characterization Of Avian Influenza Virus Isolates With A Truncated Ns1 Gene Segment, Aaron Dick

Honors Scholar Theses

Avian Influenza Virus represents a significant threat to the world poultry population, and is a potential threat to humans due to the possibility of cross-species AIV infection. Our approach is to characterize a number of avian virus populations with respect to their content of biologically active particles that include hemagglutinating particles (HAP), plaque forming particles (PFP), interferon inducing particles (IFP), interferon induction-suppressing particles (ISP), defective-interfering particles (DIP), cell-killing particles (CKP) and non-infectious cell killing particles (niCKP) using unique in vitro assays developed for avian influenza virus in the Marcus-Sekellick Laboratory. Specifically, we will use a strain of Avian influenza virus, …

Liposomal Fasudil, A Rho-Kinase Inhibitor, For Prolonged Pulmonary Preferential Vasodilation In Pulmonary Arterial Hypertension, Vivek Gupta, Nilesh Gupta, Imam H. Shaik, Reza Mehvar, Ivan F. Mcmurty, Masahiko Osa, Eva Nozik-Grayck, Fakhrul Ahsan

Pharmacy Faculty Articles and Research

Current pharmacological interventions for pulmonary arterial hypertension (PAH) require continuous infusions, multiple inhalations, or oral administration of drugs that act on various pathways involved in the pathogenesis of PAH. However, invasive methods of administration, short duration of action, and lack of pulmonary selectivity result in noncompliance and poor patient outcomes. In this study, we tested the hypothesis that encapsulation of an investigational anti-PAH molecule fasudil (HA-1077), a Rho-kinase inhibitor, into liposomal vesicles results in prolonged vasodilation in distal pulmonary arterioles. Liposomes were prepared by hydration and extrusion method and fasudil was loaded by ammonium sulfate-induced transmembrane electrochemical gradient. Liposomes were …