Pharmaceutics and Drug Design Commons^™

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 …

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

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

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 …

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 …

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 …

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

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 …

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 …

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 …

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 …

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% …

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 …

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 …

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 …

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 …

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

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

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

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 …

Chlor-Amidine, A Novel Pad Inhibitor, As An Effective Drug For The Treatment Of Ulcerative Colitis And Prevention Of Colorectal Cancer, Erin Witalison

Theses and Dissertations

Ulcerative colitis (UC) is a chronic inflammatory bowel disease that affects the quality of life of millions of patients worldwide. This disease is associated with inflammation and ulceration of the colonic epithelium, leading to an increased risk for the development of UC-associated colorectal cancer (CRC). Current UC medications are designed to manage the symptoms and induce remission; however, several challenges are faced with current treatment options. 5-aminosalicyclic acid and corticosteroids have few side effects, but have limited efficacy and often the disease becomes refractory. Biologics are introduced after initial treatments fail, but serious side effects are often associated with these …

Calcium Phosphate As A Key Material For Socially Responsible Tissue Engineering, Vuk Uskoković, Victoria M. Wu

Pharmacy Faculty Articles and Research

Socially responsible technologies are designed while taking into consideration the socioeconomic, geopolitical and environmental limitations of regions in which they will be implemented. In the medical context, this involves making therapeutic platforms more accessible and affordable to patients in poor regions of the world wherein a given disease is endemic. This often necessitates going against the reigning trend of making therapeutic nanoparticles ever more structurally complex and expensive. However, studies aimed at simplifying materials and formulations while maintaining the functionality and therapeutic response of their more complex counterparts seldom provoke a significant interest in the scientific community. In this review …

Hiv Vaccines: Progress, Limitations And A Crispr/Cas9 Vaccine, Omar A. Garcia Martinez

Biology: Student Scholarship & Creative Works

ABSTRACT: The HIV-1 pandemic continues to thrive due to ineffective HIV-1 vaccines. Historically, the world’s most infectious diseases, such as polio and smallpox, have been eradicated or have come close to eradication due to the advent of effective vaccines. Highly active antiretroviral therapy is able to delay the onset of AIDS but can neither rid the body of HIV-1 proviral DNA nor prevent further transmission. A prophylactic vaccine that prevents the various mechanisms HIV-1 has to evade and attack our immune system is needed to end the HIV-1 pandemic. Recent advances in engineered nuclease systems, like the CRISPR/Cas9 system, have …

Block Copolymer Based Magnetic Nanoclusters For Cancer-Theranostics: Synthesis, Characterization And In Vitro Evaluation, Hemant M. Vishwasrao

Theses & Dissertations

“There is plenty of room at the bottom”. In this visionary lecture in 1959 Prof. Richard Feynman spoke of the interesting ramifications of working with matter at the atomic scale. Since then, scientists have worked relentlessly towards realizing his vision. The influence of nanobiotechnology on material science and polymer chemistry has given rise to a new field called ‘theranostics’, combining drug delivery and diagnostics within the same nanostructures, thereby enabling simultaneous diagnosis, targeted drug delivery and continued therapy monitoring. Iron oxide nanoparticles (MNPs) are one such class of MRI contrast agents that can be converted into theranostic nanomedicines for cancer …

Stabilization Of Gp120 Outer Domain For Hiv-1-1 Vaccine Immunogen Design, Duoyi Hu

School of Veterinary and Biomedical Sciences: Dissertations, Theses, and Student Research

The sole envelope glycoprotein spike on the surface of Human Immunodeficiency Virus (HIV-1) is composed of two subunits: gp120 and gp41. The gp120 consists of three domains: the inner domain, outer domain and bridging sheet, to which the viral primary receptor CD4 binds and induces a conformational change in gp120 to expose the co-receptor binding site. Previous studies have found that the outer domain of gp120 is relatively more stable than the inner domain and bridging sheet. When superimposed, the co-crystal structures of CD4-gp120 complex and VRC01-gp120 complex revealed that the CD4-binding site (CD4-BS) antibody VRC01 actually mainly bound to …

An Investigation Into Formulation And Therapeutic Effectiveness Of Nanoparticle Drug Delivery For Select Pharmaceutical Agents, Dustin Cooper

Electronic Theses and Dissertations

Drug based nanoparticle (NP) formulations have gained considerable attention over the past decade for their use in various drug delivery systems. NPs have been shown to increase bioavailability, decrease side effects of highly toxic drugs, and prolong drug release. Furthermore, polymer based, biodegradable nanodelivery has become increasing popular in the field of NP formulation because of their high degree of compatibility and low rate of toxicity. Due to their popularity, commercially available polymers such as poly lactic acid (PLA), poly glycolic acid (PGA) and polylactic-co-glycolic acid (PLGA) are commonly used in the development and design of new nano based delivery …

Hit Identification For Pkcζ Inhibitors: Structure-Based Optimization, Virtual Screening, And Biological Evaluation, Xiaoxin Wu

Theses and Dissertations (ETD)

Protein kinase C ζ (PKCζ) is believed to be a promising target for the treatment of some diseases, including inflammatory diseases, obesity and diabetes. Hit identification of PKCζ inhibitors was conducted by structure-based modification, virtual screening and biological evaluation. Among all the compounds selected and synthesized, compound JW-1-60A showed moderate activity against PKCζ at 30 μM and 100 μM. The molecular modeling studies showed that the binding mode of JW-1-61A was very close to the binding mode of JP-3-149, a reported PKCζ inhibitor with very potent activity, which might partially explain the moderate activity of JW-1-61A. Based on the structure …

Engineering A Mutation In The Heparin Binding Pocket Of The Human Fibroblast Growth Factor, Roshni Patel

Chemistry & Biochemistry Undergraduate Honors Theses

Fibroblast growth factors (FGFs) are family of proteins that belong to a group of growth factors that are found in mammals and play an important role in angiogenesis, differentiation, organogenesis, and tissue repair. In summary, their main functionality is involved in cell division and proliferation. Because FGFs plays such a vital role in cell proliferation, they are mainly involved in the process of wound healing and injuries. FGF binds to its ligand, heparin—a heavily sulfated glycosaminoglycan. The binding of heparin to FGF occurs through electrostatic interactions, specifically between the negatively charged sulfate groups on heparin and positively charged residues such …

Uji Aktivitas Penghambatan Xantin Oksidase Secara In-Vitro Oleh Isolat 6,4’-Dihidroksi-4-Metoksibenzofenon-2-O-Β-D Glukopiranosida(C20h22o10) Yang Diisolasi Dari Mahkota Dewa (Phaleria Macrocarpa (Scheff.) Boerl), Aprilita Rina Yanti Eff, Sri Teguh Rahayu, Resta Dwi Syachfitri

Pharmaceutical Sciences and Research

Hyperuricemia is a condition in which an increasing in uric acid levels abovenormal. Hyperuricemia is a major factor in the development of gout. Gout is adisease caused by the accumulation of monosodium urate crystals in the tissues dueto elevated levels of uric acid. Crown gods (Phaleria macrocarpa (Scheff.) Boerl) is Indonesia native medicinal that has effect such as lowering blood pressure, diabetes mellitus drugand lowering uric acid levels. One of the chemical constituents of this plant is abenzopheneon compound that is 6,4’-dihydroxy-4-metoksi benzofenon-2-O-β-D-glukopiranosida (C20H22O10). Research was conducted to determine the activity of 6,4’-dihydroxy -4-metoksi benzofenon-2-O-β-D-glukopiranosida (C20H22O10) that isolated from Crown …

Uji Penghambatan Xantin Oksidase Secara In Vitro Ekstrak Kulit Rambutan, Nurul Eka Putri, Rissyelly Rissyelly, Marista Gilang Mauldina

Pharmaceutical Sciences and Research

Hyperuricemia is a condition have higher uric acid levels that can cause a cumulation uric acid crystals in the tissues. Xanthine oxidase is an enzyme which catalyze the oxidation of hypoxanthine into xanthine and into uric acid.Therefore, the inhibition of xanthine oxidase will reduce ammount of uric acid. This research aims to determine xanthine oxidase inhibition activity and also to identify chemical constituent group of extract rambutan (Nephelium lappaceum Linn.) skin. Rambutan fruit skin was extracted by graded maceration using a three solvent, based on polarity the solvent are n-hexane, ethyl acetate and methanol. The test of inhibition xanthine oxidase …