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Pharmaceutics and Drug Design

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2016

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Full-Text Articles in Pharmacy and Pharmaceutical Sciences

Uji Aktivitas Anti-Inflamasi Minyak Atsiri Daun Kemangi (Ocimum Americanum L.) Pada Tikus Putih Jantan Yang Diinduksi Karagenan, Fadlina Chany Saputri, Rita Zahara Dec 2016

Uji Aktivitas Anti-Inflamasi Minyak Atsiri Daun Kemangi (Ocimum Americanum L.) Pada Tikus Putih Jantan Yang Diinduksi Karagenan, Fadlina Chany Saputri, Rita Zahara

Pharmaceutical Sciences and Research

Kemangi (Ocimum americanum L.) is an aromatic plant that contains citral and known as anti-inflammatory agents. The aim of this study was to determine the anti-inflammatory activity of the essential oil kemangi leaves on carrageenan-induced rat. The male rats were divided into six groups, each consisting of four rats. Group I as negative control was given 0.5% CMC solution, group II as positive control was given diclofenac sodium, group III was given sitral, groups IV, V and VI were given 40 mg/200 g BW, 80 mg/200 g BW, and 160 mg/200 g BW essential oil of Ocimum americanum L., emulsified …


Pengaruh Cara Pengeringan Simplisia Daun Senggani (Melastoma Malabathricum L.) Terhadap Aktivitas Antioksidan Menggunakan Metode Dpph (2,2-Difenil-1-Pikrilhidrazil), Sri Luliana, Nera Umilia Purwanti, Kris Natalia Manihuruk Dec 2016

Pengaruh Cara Pengeringan Simplisia Daun Senggani (Melastoma Malabathricum L.) Terhadap Aktivitas Antioksidan Menggunakan Metode Dpph (2,2-Difenil-1-Pikrilhidrazil), Sri Luliana, Nera Umilia Purwanti, Kris Natalia Manihuruk

Pharmaceutical Sciences and Research

Drying is the most important step to keep the compound stability in simplicia. The objective of this research is to know the effect of drying methods on antioxidant activity in Melastoma malabathricum L. The drying methods tested were oven-drying at 40°C, direct sunlight, indirect sunlight, air-drying at ± 25°C and fresh samples as control. Result revealed that the drying methods of simplicia were significant differences for antioxidant activity in Melastoma malabathricum L. (p < 0,05). Drying method that has the highest antioxidant activity was by air-drying at ± 25°C is 54.60 %.


Efektivitas Snedds Ekstrak Kulit Manggis Terhadap Bakteri P. Mirabilis Dan S. Epidermidis Yang Terdapat Pada Ulkus Diabetik, Rafika Sari, Liza Pratiwi, Pratiwi Apridamayanti Dec 2016

Efektivitas Snedds Ekstrak Kulit Manggis Terhadap Bakteri P. Mirabilis Dan S. Epidermidis Yang Terdapat Pada Ulkus Diabetik, Rafika Sari, Liza Pratiwi, Pratiwi Apridamayanti

Pharmaceutical Sciences and Research

Mangosteen rind possesses the ability to conduct antibacterial activity. Under the development relating to drug delivery system, SNEDDS were known to boost the penetration of active compound. The aim of this research is to compare the effectiveness of the antibacterial activity at both SNEDDS preparation and the ethanol extract of mangosteen rind as the antibacteria against the bacteria that cause diabetic ulcers with the most prevalence whether it was Gram positive or Gram negative bacteria like Proteus mirabilis and Staphylococcus epidermidis. The research started by maceration process with the crude extract as the result continued with the phytochemical screening which …


Perbandingan Efek Larvasida Minyak Atsiri Daun Cengkeh (Syzygium Aromaticum L.) Varietas Zanzibar Dengan Temephos Terhadap Larva Nyamuk Aedes Aegypti, Ridzmullah Wishnu Pamungkas, Neneng Syarifah Syafei, Arto Yuwono Soeroto Dec 2016

Perbandingan Efek Larvasida Minyak Atsiri Daun Cengkeh (Syzygium Aromaticum L.) Varietas Zanzibar Dengan Temephos Terhadap Larva Nyamuk Aedes Aegypti, Ridzmullah Wishnu Pamungkas, Neneng Syarifah Syafei, Arto Yuwono Soeroto

Pharmaceutical Sciences and Research

The use of temephos as larvicides in disease prevention Dengue Hemorrhagic Fever (DHF) in Indonesia has been going on for 40 years. Larviciding very long led the resistance to temephos. Cloves, one of native Indonesia plant contains eugenol that are toxic to the insect’s body. This study aims to examine the effectiveness of Zanzibar clove leaf essential oil compared to temephos in killing the larvae of Aedes aegypti. This study uses experimental laboratory research design. The samples are larvae of Aedes aegypti stage III. The mosquito larvae were classified into six groups, each given a clove leaf essential oil with …


Assessment Of Achieved Systolic Blood Pressure In Newly Treated Hypertensive Patients Aged 60-79 Years Before And After Eighth Joint National Committee Recommendations, Michael S. Kelly, Joseph J. Saseen, Joel C. Marrs Dec 2016

Assessment Of Achieved Systolic Blood Pressure In Newly Treated Hypertensive Patients Aged 60-79 Years Before And After Eighth Joint National Committee Recommendations, Michael S. Kelly, Joseph J. Saseen, Joel C. Marrs

Pharmacy Faculty Articles and Research

Objective:

To determine whether patients who were newly prescribed antihypertensive therapy after the Eighth Joint National Committee (JNC 8) update were treated to a relaxed systolic blood pressure (SBP) goal compared with patients treated before the update.

Methods:

A retrospective cohort study approved by the Colorado Multiple Institutional Review Board. Patients aged 60–79 years, without diabetes or chronic kidney disease (CKD), newly treated for hypertension at a University of Colorado primary care clinics were included. The mean first-achieved and last-stable SBPs of patients newly prescribed antihypertensive medications from 1 January 2012 to 31 December 31 2013 (before cohort) were compared …


Comparison Of Outcomes Following A Switch From A Brand To An Authorized Vs. Independent Generic Drug, Richard Hansen, Jingjing Qian, Richard L. Berg, James G. Linneman, Enrique Seoane-Vazquez, Sarah Dutcher, Saeid Raofi, C. David Page, Peggy L. Peissig Dec 2016

Comparison Of Outcomes Following A Switch From A Brand To An Authorized Vs. Independent Generic Drug, Richard Hansen, Jingjing Qian, Richard L. Berg, James G. Linneman, Enrique Seoane-Vazquez, Sarah Dutcher, Saeid Raofi, C. David Page, Peggy L. Peissig

Pharmacy Faculty Articles and Research

Authorized generics are identical in formulation to brand drugs, manufactured by the brand company but marketed as a generic. Generics, marketed by generic manufacturers, are required to demonstrate pharmaceutical and bioequivalence to the brand drug, but repetition of clinical trials is not required. This retrospective cohort study compared outcomes for generics and authorized generics, which serves as a generic vs. brand proxy that minimizes bias against generics. For the seven drugs studied between 1999-2014, 5,234 unique patients were on brand drug prior to generic entry and 4,900 (93.6%) switched to a generic. During the 12-months following the brand-to-generic switch, patients …


Polymeric Nanocarriers For Delivery Of Small Molecules And Mirnas For The Treatment Of Liver Fibrosis And Pancreatic Cancer, Virender Kumar Dec 2016

Polymeric Nanocarriers For Delivery Of Small Molecules And Mirnas For The Treatment Of Liver Fibrosis And Pancreatic Cancer, Virender Kumar

Theses & Dissertations

The aim of this thesis is to develop combination therapy of small molecules and miRNAs for treating liver fibrosis and pancreatic cancer. New amphiphilic biodegradable polymers capable of carrying small hydrophobic molecules and hydrophilic anionic nucleic acids were synthesized, characterized and evaluated in vitro and in vivo liver fibrosis and pancreatic cancer mouse models.

In Chapter 1, an overview of liver fibrosis, current treatments and the role of miRNAs in liver fibrosis as well as the design of their delivery systems is given. Further, a general introduction to pancreatic cancer and role of miRNAs in pancreatic cancer is given. In …


Development Of Cxcr4-Inhibiting Nanoparticles For The Treatment Of Metastatic Cancer, Yan Wang Dec 2016

Development Of Cxcr4-Inhibiting Nanoparticles For The Treatment Of Metastatic Cancer, Yan Wang

Theses & Dissertations

Metastasis is the main cause of cancer mortality and morbidity, leading to several million deaths every year. Less than 20% of pancreatic cancer (PC) patients are candidates for surgery due to spread beyond the pancreas. Desmoplasia presents substantial barriers to perfusion, diffusion, and convection of antitumor therapeutics into the PC tissues. We focus on developing novel therapies that regulates tumor microenvironment, chemosensitizing tumor to therapeutics and preventing metastasis.

Gene therapy is emerging as a promising new therapeutic agents for cancer treatment. A targeted, systemic, effective and safe gene delivery system should be developed. CXCR4/SDF-1 axis plays a crucial role in …


Carriers For The Tunable Release Of Therapeutics: Etymological Classification And Examples, Vuk Uskoković, Shreya Ghosh Dec 2016

Carriers For The Tunable Release Of Therapeutics: Etymological Classification And Examples, Vuk Uskoković, Shreya Ghosh

Pharmacy Faculty Articles and Research

Introduction—Physiological processes at the molecular level take place at precise spatiotemporal scales, which vary from tissue to tissue and from one patient to another, implying the need for the carriers that enable tunable release of therapeutics.

Areas Covered—Classification of all drug release to intrinsic and extrinsic is proposed, followed by the etymological clarification of the term “tunable” and its distinction from the term “tailorable”. Tunability is defined as analogous to tuning a guitar string or a radio receiver to the right frequency using a single knob. It implies changing a structural parameter along a continuous quantitative scale and …


Mechanism Of Interaction Of Peptide Modified Nanoparticles With Porphyromonas Gingivalis., Ankita Jain Dec 2016

Mechanism Of Interaction Of Peptide Modified Nanoparticles With Porphyromonas Gingivalis., Ankita Jain

Electronic Theses and Dissertations

Studies suggest that P. gingivalis functions as a keystone pathogen and interacts with primary colonizers in the supragingival biofilm such as S. gordonii. This interaction contributes to the initial colonization of the oral cavity by P. gingivalis and thus represents a potential target for therapeutic intervention. We have identified a peptide (BAR) derived from the streptococcal SspB protein that functions to inhibit P. gingivalis adherence to S. gordonii. In addition, we showed that nanoparticles (NPs) functionalized with BAR inhibit this interaction more potently than free soluble peptide, possibly by promoting interaction with P. gingivalis at higher valency than …


Reactive Oxygen Species Modulation Of Na/K-Atpase Regulates Fibrosis And Renal Proximal Tubular Sodium Handling, Jiang Liu, David J. Kennedy, Yanling Yan, Joseph I. Shapiro Md Nov 2016

Reactive Oxygen Species Modulation Of Na/K-Atpase Regulates Fibrosis And Renal Proximal Tubular Sodium Handling, Jiang Liu, David J. Kennedy, Yanling Yan, Joseph I. Shapiro Md

Yanling Yan

The Na/K-ATPase is the primary force regulating renal sodium handling and plays a key role in both ion homeostasis and blood pressure regulation. Recently, cardiotonic steroids (CTS)-mediated Na/K-ATPase signaling has been shown to regulate fibrosis, renal proximal tubule (RPT) sodium reabsorption, and experimental Dahl salt-sensitive hypertension in response to a high-salt diet. Reactive oxygen species (ROS) are an important modulator of nephron ion transport. As there is limited knowledge regarding the role of ROS-mediated fibrosis and RPT sodium reabsorption through the Na/K-ATPase, the focus of this review is to examine the possible role of ROS in the regulation of Na/K-ATPase …


Lack Of Cross-Reactivity Allergy Following A Switch From Alirocumab To Evolocumab, Matthew D. Stryker, Michael Kane, Robert Busch Oct 2016

Lack Of Cross-Reactivity Allergy Following A Switch From Alirocumab To Evolocumab, Matthew D. Stryker, Michael Kane, Robert Busch

Excerpts in Pharmacy Research Journal

The proprotein convertase subtilisin/kexin type 9 (PCSK9) gene and gain-of-function mutations were first described in 2003. The gain-of-function mutations observed were associated with low-density lipoprotein-cholesterol (LDL-C) levels in the 400’s, in addition to premature cardiovascular disease. Subsequent loss-of-function experiments conducted in mice demonstrated marked reductions in plasma cholesterol levels in the absence of PCSK9. Physiologically, PCSK9 serves as a chaperone protein and functions to reduce low-density lipoprotein (LDL) receptor recycling; consequently, less LDL-C is removed from circulation and serum lipid concentrations become elevated. Inhibition of PCSK9 prevents LDL receptor degradation and preserves receptor recycling to the hepatocyte surface; this in …


Modeling With Medicinal Chemistry: Practical Innovative Technology-Based Activity To Enhance Student’S Learning Through Inter-Departmental Collaboration: Part I, Miriam Ansong, Denise Simpson, Nicole K. Stute Oct 2016

Modeling With Medicinal Chemistry: Practical Innovative Technology-Based Activity To Enhance Student’S Learning Through Inter-Departmental Collaboration: Part I, Miriam Ansong, Denise Simpson, Nicole K. Stute

Excerpts in Pharmacy Research Journal

Background: Concepts of formulary management and its applications in clinical practice is a challenge faced by many first professional year pharmacy students. This challenge may be attributed to a lack of foundational knowledge and practical skills at this level. Preparing students for lifelong learning mandates early exposure to practical application of concepts. This warrants the need for students to integrate knowledge, skills, abilities, and attitudes in clinical practice. As a result, a state-of-the-art one stop shopping structure of the day (SOD) activity was created for P1 pharmacy students to enable the authors to assess their skill sets.

Objective: The objective …


Research And Publication Highlights, Miriam Ansong Oct 2016

Research And Publication Highlights, Miriam Ansong

Excerpts in Pharmacy Research Journal

Bibliography of completed research and book chapters


The Changing Landscape Of Biosimilars In Rheumatology, Thomas Dorner, Vibeke Strand, Paul Cornes, Joao Goncalves, Laszlo Gulacsi, Jonathan Kay, Tore K. Kvien, Josef S. Smolen, Yoshiya Tanaka, Gerd R. Burmester Sep 2016

The Changing Landscape Of Biosimilars In Rheumatology, Thomas Dorner, Vibeke Strand, Paul Cornes, Joao Goncalves, Laszlo Gulacsi, Jonathan Kay, Tore K. Kvien, Josef S. Smolen, Yoshiya Tanaka, Gerd R. Burmester

Jonathan Kay

Biosimilars remain a hot topic in rheumatology, and some physicians are cautious about their application in the real world. With many products coming to market and a wealth of guidelines and recommendations concerning their use, there is a need to understand the changing landscape and the real clinical and health-economic potential offered by these agents. Notably, rheumatologists will be at the forefront of the use of biosimilar monoclonal antibodies/soluble receptors. Biosimilars offer cost savings and health gains for our patients and will play an important role in treating rheumatic diseases. We hope that these lower costs will compensate for inequities …


Which Drugs Cause Cancer?, Andrew Knight, Jarrod Bailey, Jonathan Balcombe Sep 2016

Which Drugs Cause Cancer?, Andrew Knight, Jarrod Bailey, Jonathan Balcombe

Jarrod Bailey, PhD

Animal tests yield misleading results.


Effect Of Standard Treatment Guidelines With Or Without Prescription Audit On Prescribing For Acute Respiratory Tract Infection (Ari) And Diarrhoea In Some Thana Health Complexes (Thcs) Of Bangladesh, M. O. Faruk Khan, A.K. Azad Chowdhury, M. A. Matin, K. Begum, M. A. Galib Sep 2016

Effect Of Standard Treatment Guidelines With Or Without Prescription Audit On Prescribing For Acute Respiratory Tract Infection (Ari) And Diarrhoea In Some Thana Health Complexes (Thcs) Of Bangladesh, M. O. Faruk Khan, A.K. Azad Chowdhury, M. A. Matin, K. Begum, M. A. Galib

M. O. Faruk Khan

Inappropriate prescribing for ARI and diarrhoea is a serious health problem in many developing countries including Bangladesh. A baseline retrospective prescribing survey for ARI and diarrhoea have been conducted in randomly selected 60 thana health complexes (THCs) of Dhaka division of Bangladesh. In the 38 of 60 THCs, the prescribers did not comply with the standard treatment guidelines (STG) for ARI. They are marked as 'unsatisfactory performers'. In these THCs unnecessary antibiotics were prescribed in more than 50% of the encounters. The study further revealed that in 26 THCs, comprising 41.6% of the 38 THCs, the situation was even worse …


Why Patients Need Protection From The Sun, M. O. Faruk Khan, W. Steve Pray Sep 2016

Why Patients Need Protection From The Sun, M. O. Faruk Khan, W. Steve Pray

M. O. Faruk Khan

Sunlight has been thought to be beneficial in recent decades, a time in which widespread tanning has become the norm. However, some patients’ quest for the perfect tan may lead them to permanent disfigurement and early death due to the damaging effects of ultraviolet (UV) radiation.


Antibiotic Sensitivity In Pseudomonas Aeruginosa Of Diabeticpatient’S Foot Ulcer, Pratiwi Apridamayanti, Khairunnisa Azani Meilinasary, Rafika Sari Aug 2016

Antibiotic Sensitivity In Pseudomonas Aeruginosa Of Diabeticpatient’S Foot Ulcer, Pratiwi Apridamayanti, Khairunnisa Azani Meilinasary, Rafika Sari

Pharmaceutical Sciences and Research

Diabetes Mellitus (DM) patients are at risk to have the diabetic ulcer. The main reason for DM’s patient with ulcer complication to be treated and healed in hospital is bacterial infection. One of many bacteria that infects diabetic ulcer is Pseudomonas aeruginosa. The effort to treat this infection is by using antibiotic. The use of antibiotic unfortunately, is often found inaccurate causing the microbe resistance to occur. To choose the right antibiotic, it needs to test the antibiotic’s sensitivity towards Pseudomonas aeruginosa. The aim of this study is to determine the sensitivity of antibiotics against Pseudomonas aeruginosa. Sample used was …


Skrining Aktivitas Antibakteri Bakteriosin Dari Minumance Hun Tiau, Rafika Sari, Lia Deslianri, Pratiwi Apridamayanti Aug 2016

Skrining Aktivitas Antibakteri Bakteriosin Dari Minumance Hun Tiau, Rafika Sari, Lia Deslianri, Pratiwi Apridamayanti

Pharmaceutical Sciences and Research

Lactic acid bacteria is one of the beneficial bacteria because it can produce an antimicrobial peptide called bacteriocin. Bacteriocin has been applied as a natural food preservative because it effectively prevents the growth of pathogenic bacteria in food or drink. This study aims to identify the lactic acid bacteria as producers of bacteriocin from Ce hun tiau which have inhibitory activity againts pathogenic bacteria such as Escherichia coli, Staphylococus aureus and Salmonella typhi. In this study, Lactic acid bacteria were isolated from Ce Hun Tiau using streak plate method on media deMan Rogose Sharpe. Screening bacteriocin using disc diffusion method …


Validasi Metode Analisis Ofloksasin Dalam Plasma In Vitro Secara Kromatografi Cair Kinerja Tinggi-Fluoresensi Mengacu Pada European Medicines Agency Guideline, Letitia Tania, Eme Stepani Sitepu, Yahdiana Harahap Aug 2016

Validasi Metode Analisis Ofloksasin Dalam Plasma In Vitro Secara Kromatografi Cair Kinerja Tinggi-Fluoresensi Mengacu Pada European Medicines Agency Guideline, Letitia Tania, Eme Stepani Sitepu, Yahdiana Harahap

Pharmaceutical Sciences and Research

Ofloxacin is an antibiotic from second generation of fluoroquinolones group. Concentration of ofloxacin in human plasma is in low level, and due to that fact, it requires a selective, accurate, sensitive method of analysis. In this study, the optimization and validation of ofloxacin analysis in human plasma using high performance liquid chromatography-fluorescence with ciprofloxacin-HCl as an internal standard were carried out. Separation of ofloxacin was performed using C18 (Waters, SunfireTM 5 µm; 250 x 4.6 mm) column with an isocratic mobile phase consisted of triethylamine 1% in water pH 3.0–acetonitrile (84:16) in the flow rate of 1.0 mL/min, 40oC column …


Potensi Ekstrak Etanol Daun Petai (Parkia Speciosa Hassk.) Terhadap Kadar Superoksida Dismutase (Sod) Pada Plasma Tikus Yang Mengalami Stres Oksidatif, Ruth Haryati Butarbutar, Robiyanto Robiyanto, Eka Kartika Untari Aug 2016

Potensi Ekstrak Etanol Daun Petai (Parkia Speciosa Hassk.) Terhadap Kadar Superoksida Dismutase (Sod) Pada Plasma Tikus Yang Mengalami Stres Oksidatif, Ruth Haryati Butarbutar, Robiyanto Robiyanto, Eka Kartika Untari

Pharmaceutical Sciences and Research

Cigarette smoke is free radicals superoxide resources that contains, hydrogen peroxide, hidrosil and peroksil. Superoxide dismutase (SOD) is an enzymatic antioxidants that protect cells from oxidative stress by catalyzing superoxide dismutase (O2 *) into O2 and H2O2 . This study aims to determine the potential of ethanolic extract petai leaves against plasma SOD enzyme activity in animals exposed by cigarette smoke. The simplicia extracted by maseration using ethanol 96%. Thirty-six rats Sprague Dawley strain were divided into six groups: normal group was not given treatment, negative group received 10% CMC-Na, positive control group received vitamin E, and treatment group received …


Optimasi Kombinasi Karbopol 940 Dan Hpmc Terhadap Sifat Fisik Gel Ekstrak Dan Fraksi Metanol Daun Kesum (Polygonum Minus Huds.) Dengan Metode Simplex Lattice Design, Rafika Sari, Siti Nani Nurbaeti, Liza Pratiwi Aug 2016

Optimasi Kombinasi Karbopol 940 Dan Hpmc Terhadap Sifat Fisik Gel Ekstrak Dan Fraksi Metanol Daun Kesum (Polygonum Minus Huds.) Dengan Metode Simplex Lattice Design, Rafika Sari, Siti Nani Nurbaeti, Liza Pratiwi

Pharmaceutical Sciences and Research

Indonesia especially Kalimantan Barat well known by its biodiversity, one of the potential resource is Kesum leaves. Kesum leaves are potential by its antibacterial effect, so that it can be formulated into pharmaceutical dosage form, especially gel. This research aims to know the best comparison between Carbopol 940 and Hydroxypropyl methylcellulose (HPMC) gel base affecting the physical stability of methanol extract and fraction of kesum leaves gel by Simplex Lattice Design (SLD) method. Gels were prepared into three variation base such as gel A (100% Carbopol - 0% HPMC); gel B (0% Carbopol - 100% HPMC); and gel C (50% …


An Update On Braf Inhibitors And Other New Molecular Targets For The Treatment Of Malignant Melanoma Of The Skin, M. O. Faruk Khan, Carroll L. Ramos Aug 2016

An Update On Braf Inhibitors And Other New Molecular Targets For The Treatment Of Malignant Melanoma Of The Skin, M. O. Faruk Khan, Carroll L. Ramos

M. O. Faruk Khan

Malignant melanoma of the skin originates from mutations in melanocytes and can be lethal if unrecognized or untreated in its earlier stages. Deaths from melanoma are increasing in the United States and around the world every year. The available treatments produce low rates of response with modest survival impact. Among potential molecular targets under investigation, which are mostly in the tyrosine kinase pathway, the BRAF (V-raf murine sarcoma viral oncogene homolog B1) gene is the best studied and most frequently reported mutation in melanoma. The molecular targets for melanoma treatment, promising drugs for future melanoma treatment as well as the …


Long-Acting Antiretroviral Nanoformulation Development And Subcellular Trafficking, Dongwei Guo Aug 2016

Long-Acting Antiretroviral Nanoformulation Development And Subcellular Trafficking, Dongwei Guo

Theses & Dissertations

The introduction of nanoformulated antiretroviral therapeutic regimens is a promising alternative to standard once a day oral treatment of HIV infection. Our lab has pioneered this effort and was successful in harnessing mononuclear phagocytes (monocytes, dendritic cells and macrophages) as nanoformulated drug carriers. The approach was developed as Trojan horses for drug transport, delivery and distribution to sites of viral replication in order to facilitate microbial elimination in HIV sanctuaries. However, the remaining challenges for current antiretroviral nanoformulations include to formulate a broad range of hydrophilic short-acting drugs, and to elucidate the mechanism of sequestered nanoparticles in macrophages at the …


In Vitro Metabolic Stability Study Of New Cyclen Based Antimalarial Drug Leads Using Rp-Hplc And Lc-Ms/Ms, Apoorva V. Rudraraju, Mohammad F. Hossain, Anjuli Shrestha, Prince N.A. Amoyaw, Babu L. Tekwani, M. O. Faruk Khan Aug 2016

In Vitro Metabolic Stability Study Of New Cyclen Based Antimalarial Drug Leads Using Rp-Hplc And Lc-Ms/Ms, Apoorva V. Rudraraju, Mohammad F. Hossain, Anjuli Shrestha, Prince N.A. Amoyaw, Babu L. Tekwani, M. O. Faruk Khan

M. O. Faruk Khan

Metabolic stability of the new antimalarial drug leads is determined using Human Liver Microsome (HLM) and specific cytochrome P450 enzyme (CYP2C8) taking the clinically used antimalarial drug chloroquine as a positive control. Experiment is done using standard methods. All the assays were conducted in 0.5 M phosphate buffer at pH 7.4. In general the metabolic reaction was initiated by adding 1 mM NADPH and 0.5 mg of enzyme. Incubations were done with time frequency of 0 hr, 1 hr, and 2 hrs at 37°C and the reactions were terminated by adding acetonitrile in the equal amounts of the assay mixture …


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 Aug 2016

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 …


Rnai Nanotechnology: A Platform For Sirna Screening And Cancer Gene Therapy, Mayurbhai Ravikant Patel Aug 2016

Rnai Nanotechnology: A Platform For Sirna Screening And Cancer Gene Therapy, Mayurbhai Ravikant Patel

Seton Hall University Dissertations and Theses (ETDs)

Over the past two decades, advances in RNA structural biology have improved our understanding of the structures and folding properties of naturally occurring RNAs. RNA sequences and structures participate in many specific biological functions, such as those performed by messenger RNA (mRNA), ribosomal RNA (rRNA), transfer RNA (tRNA), micro RNA (miRNA), short-interfering RNA (siRNA), small nuclear RNA (snRNA) and many others. The noncoding RNAs, such as siRNA, do not express proteins but have been utilized in a wide range of applications, including RNA interference (RNAi) and the regulation of mRNA expression. These important biological functions have been implemented in gene …


Discoveries Of Targets And Novel Agents For The Treatment Of Ischemic Retinopathy And Neovascular Disease, Jordan Javad Toutounchian Aug 2016

Discoveries Of Targets And Novel Agents For The Treatment Of Ischemic Retinopathy And Neovascular Disease, Jordan Javad Toutounchian

Theses and Dissertations (ETD)

Diabetic retinopathy (DR) and age-related macular degeneration (AMD) are among the most common causes of blindness in adults. Vision loss can occur during the advanced stages of DR and AMD as a consequence of unregulated and dysfunctional growth of new blood vessels, or neovascularization (NV) in the retina or choroid. NV can also be triggered by numerous other ocular insults and diseases including radiation retinopathy (RR) and retinal vein occlusion. These latter cases are generally less common but, like DR and AMD, they are characterized by an initial injury, chronic inflammation, and ischemia which perpetuates episodes of retinal neovascularization (RNV). …


A Mechanical Study Of Cancer Drug-Receptor Interactions, Specifically In G-Quadruplex Dna And Topoisomerase I Enzymes, Kelly Ann Mulholland Jul 2016

A Mechanical Study Of Cancer Drug-Receptor Interactions, Specifically In G-Quadruplex Dna And Topoisomerase I Enzymes, Kelly Ann Mulholland

Theses and Dissertations

Computational methods are becoming essential in drug discovery as they provide information that traditional drug development methods lack. Using these methods to understand drug-receptor interactions in detail, researchers are able to efficiently design promising drug candidates. In this study, extra precision Glide docking, molecular dynamics simulations and MMGBSA binding energy calculations provided information about the binding behavior of small molecules to two specific targets for current cancer therapeutics: G-quadruplex DNA and Topoisomerase I enzyme. The first study focuses on the compound Telomestatin, which induces apoptosis of various cancer cells with a relatively low effect on somatic cells due to its …