Pharmacy and Pharmaceutical Sciences Commons^™

Evaluation Of Antipsychotic Activity Of Ethanolic Bark Extract Of Myrica Esculenta In Rats, Biswash Sapkota, Ankit Acharya, Bishal Dangi, Annegowda Hv

Pharmaceutical Sciences and Research

The antipsychotic properties of Myrica esculenta stem bark were evaluated. The stem bark was collected, shade dried, and pulverized. Extraction was carried out with 70% ethanol by occasional shaking. Preliminary phytochemical screening of the extract was investigated in this study. Antipsychotic activity was evaluated against apomorphine-induced stereotypy using cook’s pole climbing apparatus and haloperidol-induced catalepsy models. Bioamine determination of noradrenaline and dopamine was also performed. The extract contains phytochemicals, including glycosides, flavonoids, volatile oils, proteins, saponins, phenolics, and tannins. The result showed decreased apomorphine-induced stereotyped behavior. This study reported significant dose-dependent potentiation of haloperidol-induced catalepsy in rats and a longer …

Antifungal Activity Of Polyscias Scutellaria Fosberg Leaves Against Candida Albicans, Nada Marcha Putri, Jasmine Regita Putri, Berna Elya, Robiatul Adawiyah

Pharmaceutical Sciences and Research

Polyscias scutellaria Fosberg is one of the indigenous plants from Indonesia that widely used as folk medicines for several illnesses. The leaves of P. scutellaria were previously studied as an antimicrobial agent. Nonetheless, this theory of antifungal activity has never been scientifically verified. This study aimed to evaluate the antifungal activity of P. scutellaria against Candida albicans. The leaves of P. scutellaria were macerated using an ethanol solvent. Then, the extract was evaporated and dissolved by 1% DMSO into different concentrations (100 μg/mL, 200 μg/mL, 400 μg/mL, 800 μg/mL, 1600 μg/mL, 3200 μg/mL, and 6400 μg/mL). Fluconazole, as a …

The Anti-Proliferation Effect Of An Isolated Butanol Fraction Of Tampa Badak (Voacanga Foetida (Bl.) K. Schum) Leaves On Leukemia, Lung, And Cervical Cancer, Adriani Susanty, Dachriyanus Dachriyanus, Yanwirasti Yanwirasti, Fatma Sri Wahyuni, Andisyah Putri Sekar, Nur Alimin, Magdazaleni Magdazaleni, Sri Esky Sofia, Citra Kartika Dewi

Pharmaceutical Sciences and Research

Voacanga foetida (Bl.) K.Schum leaves are known to have cytotoxic activity against blood cancer cells. This study was aimed to determine the potential of an isolated butanol fraction of Voacanga foetida (Bl.) K.Schum leaves (Tb3 compound) in inhibiting the proliferation of several cancer cells, including leukemia (K562), lung cancer (A549), and cervical cancer (He-La) using the dye exclusion method. We found that the percentage of anti-proliferation of the Tb3 compound was increased in a dose-dependent manner, where it showed 83% (K562), 72.3% (He-La), and 70.7% (A549) inhibition at higher concentration. These values were relatively higher compared to doxorubicin as a …

Potential Of Jamu In Nanotechnology Perspective As An Alternative Treatment For Covid-19, Dhadhang Wahyu Kurniawan, Azis Ikhsanudin

Pharmaceutical Sciences and Research

The world seems to be recovering at this time, especially because of the 2019 global coronavirus disease pandemic (COVID-19) caused by the Coronavirus 2 virus (SARS-CoV-2). This virus is similar to other β-coronaviruses through several steps to enter and bind angiotensin-converting enzyme 2 (ACE2) as the main receptor. This binding, particularly in the respiratory epithelium and alveoli of the lungs, affects harmony in human host cells. No specific vaccines and antivirals are available to date as drug investigations are still ongoing. However, many Indonesians consume herbal medicine, especially 'empon-empon' containing the Zingiberaceae family, to protect their health from COVID-19. So …

Inhibitory And Anti-Biofilm Effects Of Orthoshipon Aristatus Against Candida Albicans, Ratika Rahmasari, Ananda Hanny Chairunissa, Marina Ika Irianti, Roshamur Cahyan Forestrania, Ayun Erwina Arifianti, Herman Suryadi, Juliann Nzembi Makau, Ibrahim Jantan, Berna Elya

Pharmaceutical Sciences and Research

There are increasing number of reports on Candida albicans developing resistance to available anti-fungal drugs. Thus, there is an urgent need to discover new agents for treatment of candidiasis. The alcoholic extracts of Orthoshipon aristatus have been shown to exhibit antifungal activity against C. albicans by using the agar diffusion and broth microdilution methods. However, the underlying mechanisms of anti-C. albicans effect of O. aristatus have not been well understood. This study was aimed to evaluate the cytotoxic and anti-biofilm effects of the n-hexane and ethanol extracts of purple and white varieties of O. aristatus leaves …

Fractionation Of Citronella Oil And Identification Of Compounds By Gas Chromatography-Mass Spectrometry, Yelfi Anwar, Victor S. Siringoringo

Pharmaceutical Sciences and Research

Citronella oil is one of the most important essential oils and is widely used in the pharmaceutical, cosmetic and food industries. However, the selling price of citronella oil is still low, so efforts are needed to increase its added value by isolating the active components such as citronellal, citronellol and geraniol. This study aims to isolate the active ingredients of citronella oil that have higher economic added value. Citronella oil was obtained by the process of distillation of Cymbopogon nardus (L.) Rendle leaves. The essential oil was then fractionated by a vacuum fractionation process. The essential oil fraction was identified …

Antioxidant And Antiaging Assays Of Ageratum Conyzoides (L.) Ethanolic Extract, Afifah B. Sutjiatmo, Novi Edriayani, Tira Endang Mulyasari, Faizal Hermanto, M. Fahrauk, Elin Y. Sukandar, Hanna Sari Widya Kusuma, Rizal Rizal, Wahyu Widowati

Pharmaceutical Sciences and Research

The declining ability of tissues to repair or replace themselves and maintain their structure and normal function is called aging. Aging is caused by free radical that can induce the activation of elastase and collagenase. Ageratum conyzoides (L.) or known as Babadotan is a medicinal plant that has been reported to be a good source of antioxidants that also inhibit aging process. The purpose of this research is to evaluate the antioxidant and antiaging properties of Babadotan Ethanolic Extract (BEE). Franswoth method was used to determine the phytochemical assay of BEE. Measurement of 2,2-diphenyl 1-picrylhydrazyl (DPPH) scavenger was used for …

Pharmacological Characterization Of Novel Serotonin Transporter Inhibitors Identified Through Computational Structure-Based Virtual Screening, Michael Wasko

Electronic Theses and Dissertations

Depression is a mental health disorder affecting greater than 350 million people worldwide with roughly 7% of the United States population diagnosed as of 2017. The selective serotonin reuptake inhibitors (SSRIs) have been the mainstay of pharmacotherapies for depression for the last 40 years. The SSRIs target the serotonin transporter (SERT), a monoamine transporter (MAT) responsible for terminating serotonergic neurotransmission. The SSRIs are not perfect therapeutics and suffer from delayed response times, inconsistent efficacy among patients, and often produce intolerable side effects. Therefore, a strong need exists to develop new antidepressants that are more efficacious and have fewer adverse effects. …

Rilpivirine-Associated Aggregation-Induced Emission Enables Cell-Based Nanoparticle Tracking, Insiya Mukadam

Theses & Dissertations

Antiretroviral therapy (ART) has improved the quality and duration of life for people living with human immunodeficiency virus (HIV) infection. However, limitations in drug efficacy, the emergence of viral mutations and the paucity of cell-tissue targeting remain. We posit that to maximize ART potency and therapeutic outcomes newer drug formulations that reach HIV cellular reservoirs need to be created. In a step towards achieving this goal we discovered the aggregation-induced emission (AIE) property of the non-nucleoside reverse transcriptase inhibitor Rilpivirine (RPV) and used it as a platform for drug cell and subcellular tracking. RPV nanocrystals were created with endogenous AIE …

Anti-Muc4Β Antibodies As A Novel Therapeutic Modality For The Treatment Of Pancreatic Cancer, Catherine Orzechowski

Theses & Dissertations

The deregulation of cell surface glycoproteins, such as mucins, is a hallmark of many tumors of epithelial origin. The transmembrane mucin MUC4, is differentially overexpressed in several malignancies, including pancreatic, breast, ovarian, lung, cervical, and head and neck cancers. Of all the aforementioned cancers, the role of MUC4 has been the most thoroughly in pancreatic cancer (PC), which is the 4th leading cause of cancer-related deaths in the United States. While MUC4 is undetectable in the normal or inflamed pancreas (pancreatitis), its expression progressively increases during PC progression and its higher expression correlates with poor survival. The role of MUC4 …

Polymeric Drug Delivery Systems For Cancer Therapy And Radionuclide Decorporation, Sameer A. Alshehri

Theses & Dissertations

The main objective of this body of work is to develop polymeric drug delivery systems for cancer radiotherapy and the decorporation of radiological materials. The polymeric systems for radiotherapy were evaluated in vitro and in vivo (in normal, prostate, and ovarian cancer mice models). The polymeric system for radionuclide decorporation was also evaluated in vitro and in a normal mouse model. Due to its attractive properties, the N-(2-Hydroxypropyl) methacrylamide (HPMA) copolymer was utilized as the main carrier for the developed systems.

Chapter 1 provides an overview of prostate and ovarian cancer, targeted radiopharmaceuticals, nanomedicine-based drug delivery for cancer, HPMA copolymers, …

Long-Acting Nanoformulated Antivirals For The Treatment And Prevention Of Hiv-1 And Hbv Infections, Dhruvkumar M. Soni Dr.

Theses & Dissertations

While antiretroviral therapy (ART) has revolutionized treatment and prevention of human immunodeficiency virus type one (HIV-1) infection, regimen adherence, viral mutations, drug toxicities, stigma and pill fatigue are limitations. These have led to the development of long acting (LA) ART. These include, but are not limited to, implantable devices, new chemical entities, prodrug modifications and nanoformulations. To these ends, this thesis focues on the transformation of nucleoside reverse transcriptase inhibitors (NRTIs) into LA parenterals, While elusive, data from our laboratories demonstrated that modifications to the PROdrug and nucleoTide technology (ProTide) enables improvements in drug apparent half-life and tissue and cell …

Honey Vs. Silver Sulfadiazine In The Reepithelialization Of Partial-Thickness Burn Wounds, Andi Diamond, Monica Bowler

Physician Assistant Capstones, 2020-current

Objective: To determine whether silver sulfadiazine (SSD) should remain the gold standard of initial burn wound treatment or if it should be replaced with an alternative treatment that allows for faster skin cell regrowth. Methods: Database search of PubMed and Google Scholar were used to evaluate patient clinical trials with the search terms “burn”, “honey”, and “silver”. Results: Three trials met inclusion criteria. All three of the studies found significant improvement in their primary endpoint with the use of honey. The first study showed the honey group to have healing time of 13.47 ± 4.06 days and …

Great Expectations: Phosph(On)Ate Prodrugs In Drug Design—Opportunities And Limitations, Victoria Yan

Dissertations and Theses (Open Access)

Phosphate and phosphonates are chemical moieties with historical precedence in anticancer and antiviral nucleotide analogues. Synchronous to modern efforts identifying novel therapeutic targets in cancer, such chemical moieties are being investigated in the design of novel inhibitors with antineoplastic potential. A central challenge to the delivery of phosph(on)ate-containing drugs is their anionic character at physiological pH, which portends poor membrane permeability. This limitation has been successfully overcome through the use of prodrugs. When attached to the phosph(on)ate moiety, prodrugs mask the negative charge and easily enable cell permeability. Upon cellular entry, the promoieties are enzymatically or environmentally cleaved to unveil …

Celecoxib Loaded In-Situ Provesicular Powder And Its In-Vitro Cytotoxic Effect For Cancer Therapy: Fabrication, Characterization, Optimization And Pharmacokinetic Evaluation, Shady Swidan, Ali Nasr, Sameh Elhady, Noha Badawi

Pharmacy

Introduction: Several recent studies have shown that the role of cyclooxygenase 2 (COX-2) in carcinogenesis has become more evident. It affects angiogenesis, apoptosis, and invasion, and plays a key role in the production of carcinogens. It has also been reported that COX-2 inhibitors such as celecoxib (CLX) might play an effective role in preventing cancer formation and progression. Formulation of CLX into nanovesicles is a promising technique to improve its bioavailability and anticancer efficacy. Aim: The aim of this study is to optimize and evaluate the anticancer efficacy of CLX-loaded in-situ provesicular powder composed of surfactants and fatty alcohol-based novel …

Development And Characterization Of Glimepiride Novel Solid Nanodispersion For Improving Its Oral Bioavailability, Shady Swidan, Mona Qushawy, Ali Nasr, Yasmin Mortagi

Pharmacy

Glimepiride is an antidiabetic drug which is one of the third generation sulfonylureas. It belongs to class II, according to the BCS (Biopharmaceutical Classification System), which is characterized by low solubility and high permeability. The aim of this work was to formulate glimepiride as solid dispersion using water-soluble carriers to enhance its aqueous solubility and thus enhance its bioavailability. Nine formulations of glimepiride solid dispersion were prepared by a solvent evaporation technique using three different carriers (mannitol, polyethylene glycol 6000, and β-cyclodextrin) with three different drug carrier ratio (1:1, 1:3, and 1:6). Formulation variables were optimized using 32 full factorial …

Veru-111 As An Oral Tubulin Inhibitor Suppressing Triple-Negative Breast Cancer And Evaluation Of Novel Tubulin Inhibitors For Cancer Therapy, Shanshan Deng

Theses and Dissertations (ETD)

Triple negative breast cancer (TNBC) has aggressive clinical features strongly associated with poorer overall prognosis and higher mortality rates relative to other molecular subtypes. FDA-approved drugs, such as paclitaxel, are effective in treating TNBC. Yet, treatment failure is commonly observed due to the development of acquired chemoresistance, which remains a clinical challenge for TNBC therapy.

Model-Based Dose-Exposure-Response Assessment For Lead And Backup Spectinamide In A Mouse Model Of Tuberculosis, Santosh Janardan Wagh

Theses and Dissertations (ETD)

Despite decades of research, tuberculosis remains the oldest pathogen-based disease that is the leading cause of death from a single infectious agent. Among many anti-tubercular therapies under investigation, the semisynthetic compounds spectinamides are a promising novel class of anti-tuberculosis agents. One such lead candidate, spectinamide 1810, and backup spectinamide 1599 have demonstrated excellent efficacy, safety, and drug-like properties in various in vitro and in vivo assessments. The dose-ranging and dose fractionation studies were designed to characterize the dose-exposure-response relationship for lead and backup spectinamide in a mouse model of Mycobacterium tuberculosis infection. In this current study, we used 26 and …

Contraceptive Methods In The United States: The Question Of Abortive Mechanisms, Tara Ferenczy

Senior Honors Theses

This thesis reviews the many methods of contraception available in the United States. Although society’s understanding of women’s health has become a major topic, there is still a significant deficit of information regarding how the accessible methods affect women’s bodies, specifically reproductive tissue. The thesis analyzes numerous contraceptive options focusing specifically on the mechanisms of action to determine whether options have abortifacient properties so that readers may develop educated opinions regarding medical and ethical uses. Information involving strengths and limitations of each technique and the effects on both the female body and the reproductive material assist in understanding the process …

Validation And Application Of A Novel Target-Based Whole-Cell Screen To Identify Antifungal Compounds, Christian Alexander Dejarnette

Theses and Dissertations (ETD)

Traditional approaches to drug discovery are inefficient and have several key limitations that constrain our capacity to rapidly identify and develop novel experimental therapeutics. To address this, we have devised a second-generation target-based whole-cell screening assay based on the principles of competitive fitness, which can rapidly identify target-specific and physiologically-active compounds. Briefly, strains expressing high, intermediate, and low levels of a preselected target protein were constructed, tagged with spectrally distinct fluorescent proteins (FPs), and mixed together. The pooled strains were then grown in the presence of various small molecules, and the relative growth of each strain within the mixed culture …

Click-Free Synthesis Of A Multivalent Tricyclic Peptide As A Molecular Transporter, Sumit Kumar, Dindyal Mandal, Shaima Ahmed El-Mowafi, Saghar Mozaffari, Rakesh Kumar Tiwari, Keykavous Parang

Pharmacy Faculty Articles and Research

The cellular delivery of cell-impermeable and water-insoluble molecules remains an ongoing challenge to overcome. Previously, we reported amphipathic cyclic peptides c[WR]₄ and c[WR]₅ consisting of alternate arginine and tryptophan residues as nuclear-targeting molecular transporters. These peptides contain an optimal balance of positive charge and hydrophobicity, which is required for interactions with the phospholipid bilayer to facilitate their application as a drug delivery system. To further optimize them, we synthesized and evaluated a multivalent tricyclic peptide as an efficient molecular transporter. The monomeric cyclic peptide building blocks were synthesized using Fmoc/tBu solid-phase chemistry and cyclization in the …

Epigenetic Diet To Modulate Immune Response Against Sars-Cov-2, Andika Andika, Risa Ahdyani, Linda Erlina, Azminah Azminah, Arry Yanuar

Pharmaceutical Sciences and Research

The COVID-19 pandemic has spread to various parts of the world and caused many deaths. The victims are infected by SARS-CoV-2, a new type of coronavirus that has appeared since December 2019 and caused respiratory symptoms, fever, coughing, and shortness of breath. In addition to social distancing, wearing masks and washing hands, diet is important as a defense of the body against SARS-CoV-2. In this review, researchers conducted epigenetic diet studies that could potentially inhibit SARS-CoV-2, and can be consumed and used on a daily basis.

Antioxidant And Elastase Inhibitor Potential Of Petals And Receptacle Of Rose Flower (Rosa Damascena), Evi Mawarni, Chrismis Novalinda Ginting, Linda Chiuman, Ermi Girsang, Rr. Anisa Siwianti Handayani, Wahyu Widowati

Pharmaceutical Sciences and Research

Free radicals can cause damage to cells or tissues, autoimmune diseases, degenerative diseases, or cancer. Therefore, the body needs important substances, namely antioxidants that can help protect the body by reducing negative effect from free radicals. Rose flower (Rosa damascena) has anthocyanin pigment which belongs to flavonoid group which has a function as antioxidant or free radical scavenger. This study aims to determine antioxidant and anti-elastase potentials of rose petals and receptacles. The method used in this study was a qualitative phytochemical test to determine the compounds contained in the Rose Petal Extract (RPE) and Rose Receptacle Extract (RRE), ABTS …

Potential Risk Factors For Mortality Due To Cardiovascular Disease Among Hemodialysed Patients In Indonesia, Diana Laila Ramatillah, Syed Azhar Syed Sulaiman, Kashif Ullah Khan

Pharmaceutical Sciences and Research

Severe vascular calcifications, alterations in cardiovascular structure and function, immune dysfunction, and anemia are adverse effects of parathyroid hormone (PTH), which may contribute to increase risk factors of cardiovascular morbidity and mortality among renal failure patients. To evaluate the potential risk factors for mortality due to cardiovascular disease among hemodialysed patients in Indonesia, this cohort study was conducted. This study included 178 patients on hemodialysis who had been followed up two times a week for nine months (prospective cohort) and 185 patients who died in the last five years (retrospective cohort). Universal sampling technique were used to select the study …

A Study On The Formulation Of Plant Matrix Tablets From Coarse Botanical Materials Using Cinnamon Bark And Areca Nut As The Model Botanical Materials, Natalia Veronica, Xiu Hui Ang, Shing Ming Ooi, Celine Valeria Liew, Paul Wan Sia Heng

Pharmaceutical Sciences and Research

Background: There is much interest in formulating botanical materials into tablets due to the compactness and ease of administration. However, tableting of coarse milled botanical materials poses a challenge due to poor tableting properties. Objective: To evaluate the feasibility of wet granulation to produce tablets from coarse milled botanical materials and to assess the effect of formulation on properties of the tablets. Materials and Methods: Cinnamon bark and areca nut were milled to obtain 1–2 mm particle size, which was subsequently used in wet granulation using maltodextrin solution as a granulating liquid. Two diluents were tried; microcrystalline …

Antagonistic Drug-Herb Interactions Between Clinacanthus Nutans And Cyclophosphamide On Wrl 68 Cell Line, Nurliana Abd Mutalib, Normala Abd Latip

Pharmaceutical Sciences and Research

Clinacanthus nutans (Acanthaceae), locally known as Sabah snake grass, is popularly taken as prevention as well as treatment for cancer in Malaysia, despite lack of concrete clinical evidence. However, it is crucial to evaluate potential antagonistic, additive, or synergistic interactions that may result from the co-treatment of this plant in chemotherapy. In this study, we demonstrate the drug-herb interaction using combination treatment of C. nutans extracts and cyclophosphamide on the WRL 68 cell line. Materials and Methods: Aqueous and 70% ethanol extract of C. nutans leaves were prepared using decoction and maceration methods. MTT assay was used to test …

Long-Lasting, Patient-Controlled, Procedure-Free Contraception: A Review Of Annovera With A Pharmacist Perspective, Jennifer J. Virro, Kathleen Besinque, Christiane E. Carney, Danielle Gross, Brian Bernick, Sebastian Mirkin

Pharmacy Faculty Articles and Research

Annovera (segesterone acetate and ethinyl estradiol vaginal system) is a US Food and Drug Administration FDA-approved long-lasting, reversible contraceptive that is fully administered by the user and does not require a procedure for insertion or removal. The vaginal system is in the shape of a ring and contains low doses of a novel progestin, egesterone acetate, and ethinyl estradiol. It is made of silicone and is fully pliable and flexible. The vaginal system is reusable for 13 cycles, using a 21 days in/7 days out regimen, providing women with the ability to control their fertility. Particularly now during the COVID-19 …

The Potential Roles Of Jamu For Covid-19: A Learn From The Traditional Chinese Medicine, Dwi Hartanti, Binar Asrining Dhiani, Shintia Lintang Charisma, Retno Wahyuningrum

Pharmaceutical Sciences and Research

As the pandemic of the coronavirus disease 2019 (COVID-19) continues while there is no drug and vaccine available, every effort to discover one should be considered. This review aimed to discuss the potential use of jamu, the Indonesian traditional herbal medicine, to deal with COVID-19 by following those of more-established traditional Chinese medicine (TCM). The online literature search using the PubMed database, as well as the circulars from the Indonesian Ministry of Health, were carried out to collect data up to June 07, 2020. The use of TCM for the treatment and prevention of COVID-19 has been officiated in the …

Sars-Cov-2: Virology And Drug Repurposing Approaches, Ratika Rahmasari, Heri Setiawan, Rezi Riadhi Syahdi, Ayun Arifianti, Marina Ika Irianti, Rani Sauriasari, Juliann Nzembi Makau, Muhareva Raekiansyah

Pharmaceutical Sciences and Research

An emerging coronavirus, SARS-CoV-2, is the causative agent for the ongoing pandemic of coronavirus disease 2019 (COVID-19), which has caused a worldwide social and economic disruption. Currently, no antiviral drugs with proven clinical efficacy, or vaccines for its prevention. Therefore, to combat the pandemic of this novel coronavirus, new effective treatments are urgently needed. In the process of traditional drug development, developing new drugs from scratch is a time- consuming process, requires high-investment, and is a high-risk process, which is impractical to face the immediate global challenge of the SARS-CoV-2 pandemic. Drug repurposing strategy is one of the effective ways …

Dermaseptin-Based Antiviral Peptides To Prevent Covid-19 Through In Silico Molecular Docking Studies Against Sars-Cov-2 Spike Protein, Taufik Muhammad Fakih

Pharmaceutical Sciences and Research

A pandemic coronavirus disease of 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has now been declared a global pandemic by the World Health Organization. The search for new drugs, especially by utilizing antiviral peptides is a very potential area. Through this study, protein-peptide docking and protein-protein docking simulations were conducted using in silico methods to identify, evaluate, and explore the molecular affinity and interaction of dermaseptin peptide molecules produced by frogs of the genus Phyllomedusa against the SARS-CoV-2 spike protein macromolecule, and its effect on attachment to the surface of the ACE-2 (Angiotensin Converting Enzyme-2) receptor. …