Pharmaceutics and Drug Design Commons^™

Subchronic Toxicity Study Of Sterculia Rubiginosa Zoll. Ex Miq. Leaves Extract, Rini Prastiwi, Ester Hidayati, Riska Anggraini, Cut Mauliza, Ita Anggraini, Ema Dewanti

Pharmaceutical Sciences and Research

Ki hampelas (Sterculia rubiginosa Zoll. Ex Miq.) is traditionally used as an antiasthma. It also reported has antioxidant and nephroprotective activity. This study was conducted to evaluate the subchronic toxicity of the leaf extract of ki hampelas. The extract was orally administered to male and female Sprague-Dawley rats at doses of 50, 200, and 400 mg/kg bodyweight (BW) per day for 28 days. The rats were divided into four groups, consist of consist of normal group (Na CMC 0.5%), dose 1 (50 mg/kg BW), dose 2 (200 mg/kg BW), and dose 3 (400 mg/ kg BW) of extract. The …

Colon Targeted Delivery Dosage Forms For Probiotics: A Review, Gede Anom Anjasmara, Pietradewi Hartrianti, Raditya Iswandana

Pharmaceutical Sciences and Research

Encapsulation was a promising method for protecting probiotics from extreme conditions during their passage through the gastrointestinal tract and delivering probiotics to specific sites in the colon for colonization. Various dosage forms have been used in recent years to encapsulate probiotics to maintain cell viability during processing, storage, and through the digestive tract to provide health benefits. However, research related to the encapsulation of probiotics as the dosage forms for colon-targeted delivery systems was still quite limited to conventional dosage forms due to the sensitivity of probiotics to extreme conditions during the process. This review focuses on various types of …

Exploring Rosella (Hibiscus Sabdariffa L.) Calyx Extracts As Natural Dye And Antioxidants In Lip Cream Product: Formulation And Evaluation, Donna Maretta Ariestanti, Abdul Mun'im, Joshita Djajadisastra, Riska Amalia Putri Hutami, Redhalfi Fadhila, Richard Johari James

Pharmaceutical Sciences and Research

Rosella, also known as Hibiscus sabdariffa L., is a plant that contains anthocyanin compounds in its calyx, which are known for their antioxidant properties. These compounds give the plant a captivating red color and can be used as natural dyes. This study aimed to exploit anthocyanins in rosella calyx as natural dyes and antioxidants in lip cream product. The formulations employed extracts from rosella calyx, a viscous extract from maceration in 96% ethanol (F1) and a commercially available powdered rosella extract (F2). Evaluation on the formulations demonstrated that both F1 and F2 effectively maintained the color integrity of the lip …

The Potential Of Herbal Combinations As Adjunctive Therapy For Standard Care Of Covid-19 Patients: A Lesson Learned From Indonesia, Anna Rozaliyani, Satria Pratama, Findra Setianingrum, Fenny Yunita, C. Martin Rumende

Pharmaceutical Sciences and Research

The pandemic of novel coronavirus disease (COVID-19) has become a global disaster that occurred between the end of 2019 and 2023. It caused immeasurable damage to almost all aspects of human life. The disease has opened a lot of new perspectives on Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) origins and pathogenesis, the nature of the virus, the potential for new treatments, and new policies to overcome this pandemic. This review aims to know the potential of plants that are beneficial to combat the diseases, including immunomodulators in the management of COVID-19. Studies reporting COVID-19 with the keywords SARS-CoV-2, COVID-19, …

Antioxidant Activities Of Roja Herbal Tea: Combination Of Rosella Flower (Hibiscus Sabdariffa L.) And Ginger Rhizome (Zingiber Officinale Rosc.), Wahyu Widowati, Teresa Liliana Wargasetia, Teddy Marcus Zakaria, Michael Sebastian Gunadi, Nathanael Halim, Sherly Santiadi, Hanna Sari Widya Kusuma, Nida Firyal Fauziyah

Pharmaceutical Sciences and Research

Herbal teas and plant-based medicines have been widely used worldwide for their therapeutic and healing qualities. Rosella (Hibiscus sabdariffa L.) has various benefits in preventing digestive problems, liver disease, fever, and others. Ginger (Zingiber officinale Rosc.) or known as jahe in Indonesia is believed to benefit numerous clinical conditions linked to oxidative stress, including pancreatitis, hypertension, diabetic kidney disease, Alzheimer’s disease, and tumor development. They have been utilized in traditional medical practice to treat conditions such as fever, nausea, and headaches. In this study, we aimed to determine the antioxidant activities of rosella flower tea, ginger tea, and …

Study Of Anti-Hyperuricemia, Anti-Inflammatory, And Anti-Nociceptive Effects Of Hylocereus Undatus Stem Bark Extract In Animal Models, Tri Wahyuni, Sartika Harka Putri, Anton Bahtiar

Pharmaceutical Sciences and Research

Dragon fruit, known as Hylocereus undantus (HU), has traditionally been utilized in Banyuwangi, East Java, Indonesia, for addressing gout and rheumatism. Despite its empirical use, there is a lack of reported pharmacological research on this plant. This study aimed to explore the properties of HU extract in treating hyperuricemia, inflammation, and pain. Adenine-potassium oxonate-induced mice were employed to evaluate anti-hyperuricemia activity, measuring uric acid, blood urea nitrogen (BUN), and creatinine serum levels. Carrageenan-induced paw edema in rats was used to assess anti-inflammatory activity, while acetic acid-induced abdominal writhing and hot plate tests were conducted to investigate anti-nociceptive effects. The results …

Functionalized Surface Of Plga Nanoparticles In Thermosensitive Gel To Enhance The Efficacy Of Antibiotics Against Antibiotic Resistant Infections In Endodontics: A Randomized Clinical Trial, Mona Arafa, Hadeel Moussa, Mohamed Medhat Kataia

Pharmacy

Enterococcus faecalis plays the key role in endodontic infections and is responsible for the formation of biofilm on dentin, which causes a resistance against periradicular lesions treatment, consequently the aim of this study is to use nanoparticles entrapping anibacterial agents coated with chitosan that in authors previous study showed a successful in vitro biofilm inhibition, additionally incorporated in thermoresponsive gel.to benefit nanoparticles` small size, and the positive charge of their surfaces that binds with the negatively charged surface of bacterial cell causing its destruction, in addition to the sustained release pattern of the drug based nanoparticles in gel. Therefore, Ciprofloxacin …

Analyzing Functional Interactions Of Designed Peptides By Nmr Spectroscopy, Wonsuk Choi

Pharmaceutical Sciences (MS) Theses

The development of small peptide-based therapeutics can be accelerated by the knowledge of relationships between the peptide structure and its functional interactions. Here, we report the analysis of two groups of synthetic peptides designed for two applications – broad bactericidal action and inhibition of protein-protein interactions in human cells. Novel amphiphilic peptides designed for antibacterial application incorporated arginine as cationic amino acids and non-natural amino acids that have aromatic side chains with similar hydrophobic properties as tryptophan. The interaction of lead cyclic peptides and their linear analogs with a phospholipid bilayer mimicking a bacterial membrane was studied using nuclear magnetic …

Tolfenamic Acid Derivatives: A New Class Of Transcriptional Modulators With Potential Therapeutic Applications For Alzheimer’S Disease And Related Disorders, Juanetta Hill, Karim E. Shalaby, Syed W. Bihaqi, Bothaina H. Alansi, Benjamin Barlock, Keykavous Parang, Richard Thompson, Khalid Ourarhni, Nasser H. Zawia

Pharmacy Faculty Articles and Research

The field of Alzheimer’s disease (AD) has witnessed recent breakthroughs in the development of disease-modifying biologics and diagnostic markers. While immunotherapeutic interventions have provided much-awaited solutions, nucleic acid-based tools represent other avenues of intervention; however, these approaches are costly and invasive, and they have serious side effects. Previously, we have shown in AD animal models that tolfenamic acid (TA) can lower the expression of AD-related genes and their products and subsequently reduce pathological burden and improve cognition. Using TA as a scaffold and the zinc finger domain of SP1 as a pharmacophore, we developed safer and more potent brain-penetrating analogs …

Piperine Encourages Apoptosis In Human Cervical Adenocarcinoma Cells Through Ros Generation, Dna Fragmentation, Caspase-3 Activation And Cell Cycle Arrest, Asif Jafri, Juhi Rais, Sudhir Kumar, Md Arshad

Research Symposium

Background: Cancer is one of the most common destructive diseases and the second leading cause of death in humans. Among cancer, cervical cancer is the second most common malignancy among women globally. Thus, there is a continuous need to search for chemotherapeutic chemicals or naturally occurring drugs to resolve this global health problem. Piperine (1-piperoylpeperdine) is present in the fruits of black pepper (Piper nigrum Linn.) and long pepper (Piper longum Linn.). It possesses several pharmacological properties and in the present study we have evaluated its anti-cancer potential on human cervical adenocarcinoma (HeLa) cells.

Methods: The anti-proliferative effect …

Optimization Of Lubrication And Compression Process Parameters Of Vitamin C Film-Coated Caplets, Ernestine Arianditha Pranasti, Ratna Annisa Utami, Yuda Prasetya Nugraha

Pharmaceutical Sciences and Research

Tablet production is a very intricate process influenced by numerous process variables or parameters. This study aimed to identify the critical processing variables that affect Critical Quality Attributes (CQAs) of vitamin C film-coated caplets utilizing a statistical experimental design. A two-level complete factorial design with two central points was used to examine the process parameters that posed the greatest risk to CQAs. The process variables investigated included mesh size and duration for the lubrication process, as well as speed and main thickness for compression. Statistical results showed that mesh number, lubrication time, and their interaction significantly affect flow rate, Hausner …

Solid Lipid Nanoparticles (Sln): Formulation And Fabrication, Gabriella F. Punu, Yahdiana Harahap, Qonita Kurnia Anjani, Pietradewi Hartrianti, Ryan F. Donnelly, Delly Ramadon

Pharmaceutical Sciences and Research

Solid lipid nanoparticles (SLN) have emerged as a novel drug delivery system and have been utilized for delivering various kinds of drugs since the 1990s. These particles may consist of multiple solid lipids, including glycerides, waxes, and fatty acids, and can be stabilized by a wide range of surfactants. SLN have garnered significant attention from researchers due to its innovative and versatile nature. Moreover, such delivery system has numerous advantages over traditional colloidal carriers, such as liposomes, polymeric nanoparticles, and emulsions. Several research groups have been developing SLN formulations and fabrication techniques based on their intended purpose, and this research …

Optimization Of 3,4-Dimethoxychalcone And Rutin Containing Gel With Simplex Lattice Design And In Vitro-In Vivo Test As A Sunscreen, Hana Anisa Fatimi, Abdul Karim Zulkarnain, Marlyn Dian Laksitorini

Pharmaceutical Sciences and Research

3,4-Dimethoxychalcone and rutin, a flavonoid that contains chromophore groups, can absorb UV light and thus can be developed as a sunscreen. The objective of this study was to determine the optimum formula of 3,4-dimethoxychalcone and rutin containing gel, evaluate its physical stability, and activity of 3,4-dimethoxychalcone and rutin gel as a sunscreen through in vitro and in vivo tests. HPMC, CMC-Na, and methylcellulose were formulated into a gel base to obtain good adhesion and a clear appearance gel. Simplex Lattice Design (SLD) with Design Expert software version 10 was utilized to determine the optimum gel formulation. UVA-PF protection, photostability with …

Evaluation Of Anti-Vegf And Pan-Retinal Photocoagulation Laser Therapies In Proliferative Diabetic Retinopathy Patients: A Systematic Review, Senyum Indrakila, Namira Putri Imani, Aiman Hilmi Asaduddin, Muzakiya Lailatul Karima, Lygia Angelica Widjaja

Pharmaceutical Sciences and Research

Diabetic retinopathy is a complication of diabetes that is one of the top five causes of blindness in those over 50. The standard treatment is pan-retinal photocoagulation, which is effective but has established side effects. Anti-vascular endothelial growth factor (anti-VEGF) therapy becomes an alternative to avoid the side effects caused by laser therapy. This systematic review aims to know the effectiveness of anti-VEGF therapy compared to the pan-retinal photocoagulation laser therapy in patients with proliferative diabetic retinopathy. This review was carried out using a systematic review checklist on PRISMA (Preferred Reporting Items for Systematic Reviews and Meta-Analyses). The articles reviewed …

Individual And Combined Effect Of Eudragit® Rs 100 And Eudragit® Rl 100 On Sustained Release Characteristics Of Ropinirole Hcl-Loaded Microparticles, Aamir Hayyat, Nabeel Siddique

Pharmaceutical Sciences and Research

Ropinirole HCl is a non-ergoline dopamine agonist which is recommended for the treatment of both Parkinson’s disease and Restless Legs Syndrome (RLS). Its half-life is about 6 hours and it is metabolized in the liver primarily by CYP1A2. Its metabolites are water-soluble and rapidly excreted from the body in urine. However, its oral bioavailability is low. Therefore, this current project aimed to produce and evaluate sustained release ropinirole microparticles coated with Eudragit^® RS 100 and RL 100 by varying polymer types and concentrations. Ropinirole microparticles were prepared by oil in oil emulsion solvent evaporation technique. Emulsifier concentration was constantly …

Targeting Breast Cancer: The Familiar, The Emerging, And The Uncharted Territories, Hamidreza Montazeri Aliabadi, Arthur Manda, Riya Sidgal, Co Chung

Pharmacy Faculty Articles and Research

Breast cancer became the most diagnosed cancer in the world in 2020. Chemotherapy is still the leading clinical strategy in breast cancer treatment, followed by hormone therapy (mostly used in hormone receptor-positive types). However, with our ever-expanding knowledge of signaling pathways in cancer biology, new molecular targets are identified for potential novel molecularly targeted drugs in breast cancer treatment. While this has resulted in the approval of a few molecularly targeted drugs by the FDA (including drugs targeting immune checkpoints), a wide array of signaling pathways seem to be still underexplored. Also, while combinatorial treatments have become common practice in …

Cyclic Peptides With Antifungal Properties Derived From Bacteria, Fungi, Plants, And Synthetic Sources, Naiera M. Helmy, Keykavous Parang

Pharmacy Faculty Articles and Research

Fungal infections remain a significant concern for human health. The emergence of microbial resistance, the improper use of antimicrobial drugs, and the need for fewer toxic antifungal treatments in immunocompromised patients have sparked substantial interest in antifungal research. Cyclic peptides, classified as antifungal peptides, have been in development as potential antifungal agents since 1948. In recent years, there has been growing attention from the scientific community to explore cyclic peptides as a promising strategy for combating antifungal infections caused by pathogenic fungi. The identification of antifungal cyclic peptides from various sources has been possible due to the widespread interest in …

The Opioid Epidemic: How Genetics Play A Role In Addiction And Treatment, Kirsten Houston

Honors College Theses

The opioid epidemic is an issue within the pharmaceutical industry in the United States of America due to prescription and non-prescription substances being made available to the population. Opioids include chemical substances that affect the body and brain through opioid receptors, including the mu, kappa, and delta receptors. These substances are derived and synthesized from the poppy plant. Multiple causes have been linked to opioid abuse disorder, including but not limited to employment, income, housing, nutrition, mental health disorders, and genetics. By gathering information from previous literature, genetics may be the main cause of narcotic analgesic tolerance and abuse. Specific …

A New Method For Investigating Bioequivalence Of Inhaled Formulations: A Pilot Study On Salbutamol, Homa Razaei, Maryam Khoubnasabjafari, Vahid Jouyban-Gharamaleki, Hamed Hamishehkar, Mohammad Reza Afshar Mogaddam, Elaheh Rahimpour, Reza Mehvar, Abolghasem Jouyban

Pharmacy Faculty Articles and Research

Purpose: An efficient, cost-effective and non-invasive test is required to overcome the challenges faced in the process of bioequivalence (BE) studies of various orally inhaled drug formulations. Two different types of pressurized meter dose inhalers (MDI-1 and MDI-2) were used in this study to test the practical applicability of a previously proposed hypothesis on the BE of inhaled salbutamol formulations.

Methods: Salbutamol concentration profiles of the exhaled breath condensate (EBC) samples collected from volunteers receiving two inhaled formulations were compared employing BE criteria. In addition, the aerodynamic particle size distribution of the inhalers was determined by employing next generation impactor. …

Genetic Mutations Of KCa2.3 And KCa3.1 Channels Affect Ca2+ Sensitivity, Razan Orfali

Pharmaceutical Sciences (PhD) Dissertations

The Ca²⁺-activated potassium channels K_Ca channels are a unique family of potassium channels activated by intracellular calcium. K_Ca channels are critical for maintaining K⁺ homeostasis and modulate several physiological processes, from the firing properties of neurons to the control of the transmitter release. The Ca²⁺ sensitivity of these channels allows intracellular Ca²⁺ to regulate the electrical activity of the cell membrane. Increased Ca²⁺ sensitivity of K_Ca channels caused by gain of function mutations (GOF) in the KCNN genes results in a broad spectrum of human channelopathies, including Zimmermann- Laband syndrome (ZLS), …

Solid Dispersion Technology For Improving The Solubility Of Antiviral Drugs, Maria Elvina Tresia Butar-Butar, Nasrul Wathoni, Hestiary Ratih, Yoga Windhu Wardhana

Pharmaceutical Sciences and Research

Most drugs, including antiviral drugs, show low solubility in water, which affects dissolution, bioavailability, and therapeutic effectiveness. Therefore, many antiviral drugs are given in very large doses. One of the efforts to overcome these problems is the application of solid dispersions in which polymers and surfactants can trap drug molecules that are in the amorphous phase. Drugs in a hydrophilic carrier will increase wettability, water absorption capacity, and porosity of particles, so that the drug is released better. This review article will discuss the development of technology in solid-state, how solid dispersion overcomes the lack of solubility and the rate …

Beyond Use Date (Bud) Determination Of Ambroxol Hydrochloride Syrup By High-Performance Liquid Chromatography – Uv/Vis Detector, Catur Jatmika, Raditya Iswandana, Indah Dewi Lestari

Pharmaceutical Sciences and Research

Ambroxol HCl is a mucolytic agent often used to treat respiratory disorders associated with excess mucus secretion. This study aims to determine the beyond-use date (BUD) of ambroxol HCl syrup on the market based on analysis of the decrease in drug content using High-Performance Liquid Chromatography (HPLC) – UV/Vis detector. The HPLC conditions were reversed-phase with a C18 column, mobile phase containing acetonitrile - phosphate buffer 0.05 M pH 4.5 (60:40) at a flow rate of 1.0 ml/min using UV detection at 248 nm. To determine BUD, five syrup preparations (brands) obtained from the Jakarta area were analyzed in triplicate. …

Antibody-Drug Conjugates For Multiple Myeloma: Just The Beginning, Or The Beginning Of The End?, Upasana Ray, Robert Z Orlowski

Faculty, Staff and Student Publications

Multiple myeloma is a malignancy of immunoglobulin-secreting plasma cells that is now often treated in the newly diagnosed and relapsed and/or refractory settings with monoclonal antibodies targeting lineage-specific markers used either alone or in rationally designed combination regimens. Among these are the anti-CD38 antibodies daratumumab and isatuximab, and the anti-Signaling lymphocytic activation molecule family member 7 antibody elotuzumab, all of which are used in their unconjugated formats. Single-chain variable fragments from antibodies also form a key element of the chimeric antigen receptors (CARs) in the B-cell maturation antigen (BCMA)-targeted CAR T-cell products idecabtagene vicleucel and ciltacabtagene autoleucel, which are approved …

The Science Of Oral Carbapenems, Landon Olsen, Daniel J. Yang, Aiyi Chen, Thahn-Liem Vu, H. Stephen Lee

Annual Research Symposium

No abstract provided.

Characterization, Antibacterial, Antioxidant, Antidiabetic, And Anti-Inflammatory Activities Of Green Synthesized Silver Nanoparticles Using Phragmanthera Austroarabica A. G. Mill And J. A. Nyberg Extract, Shady Swidan, Dina Khodeer, Sarah Shabayek, Ali Nasr, Roaa Khinkar, Mohammed Aldurdunji, Maryam Ramadan, Jihan Badr

Pharmacy

Introduction: Diabetes mellitus is a chronic metabolic disorder that exhibited great expansion all over the world. It is becoming an epidemic disease adding a major burden to the health care system, particularly in developing countries.

Methods: The plant under investigation in the current study Phragmanthera austroarabica A. G. Mill and J. A. Nyberg is traditionally used in Saudi Arabia for the treatment of diabetes mellitus. The methanolic extract (200 mg/kg) of the plant and pure gallic acid (40 mg/kg), a major metabolite of the plant, as well as their silver nanoparticle formulae (AgNPs) were evaluated for their antidiabetic activity.

Results …

Investigating The Use Of Mpges-1 Inhibitors For The Treatment Of Abdominal Aortic Aneurysms, Lauren M. Weaver

Theses and Dissertations--Pharmacy

The cardiovascular field is still searching for a treatment for abdominal aortic aneurysms (AAA). This inflammatory disease is a deadly, permanent ballooning of the aortic artery. It often goes undiagnosed until a late stage where associated rupture has a high mortality rate. Surgery is the only option available to patients, but it is risky. There are currently no FDA-approved pharmacological treatments for AAA available. Historically, drugs that have been examined in interventional clinical trials for treatment of AAA were repurposed therapeutics. Novel treatments have been unable to reach the clinic, stalling out in pre-clinical studies. Exceedingly few murine studies have …

The Impact Of Hiv-1 Tat And Morphine On Spatial Distribution Of Drugs In The Brain., Austin M. Jones

Theses and Dissertations

Despite combination antiretroviral therapy effectively suppressing HIV within the periphery, the central nervous system (CNS) remains affected by the virus. Approximately half of people living with HIV will experience HIV-associated neurocognitive disorders (HAND) or neuroHIV. Concurrent opioid use exacerbates neuroHIV by promoting neuroinflammation, viral replication, and potentially altering the antiretroviral concentrations within the brain.

Using a transgenic mouse that expresses the HIV-1 Tat protein, we examined the effects of Tat and morphine on antiretroviral accumulation and distribution and the effects of Tat on morphine accumulation within the brain using infrared matrix-assisted laser desorption electrospray ionization with mass spectrometry imaging (IR-MALDESI-MSI). …

Physiologically-Based Pharmacokinetic (Pbpk) Modeling For The Preclinical Development Of Spectinamide Antibiotics, Keyur R. Parmar

Theses and Dissertations (ETD)

Despite being an ancient disease caused by Mycobacterium tuberculosis (Mtb) and after decades of research, tuberculosis (TB) still affects millions of people every year worldwide. In 2018, the World Health Organization (WHO) reported that 10 million people developed tuberculosis and 1.5 million died of the disease. With the increase in the multidrug-resistant (MDR) and extensively drug-resistant (XDR) cases, the treatment for TB with the standard first and second-line therapy is becoming increasingly difficult. Therefore, there is an urgent need to find new anti-TB drugs as combination partners of existing and experimental classes of antimicrobial agents to shorten and simplify the …

Right Treatment Wrong Time: Immunotherapy Administration Post-Radiotherapy Decreases Tumor Burden In A Preclinical Model Of Brain Metastasis, Kathryn Elizabeth Blethen

Graduate Theses, Dissertations, and Problem Reports (ETD)

This dissertation (a) provided an in-depth literature review of methods to modulate the blood-brain and blood-tumor barriers to increase drug delivery and efficacy in brain metastases, (b) evaluated the effects of whole-brain radiation therapy on the blood-brain barrier in immunocompetent and immunocompromised mouse models and proposed a mechanism by which the immune response to radiation disrupts the blood-brain barrier, and (c) developed a syngeneic lung cancer brain metastasis model to determine the impact of coordinated immunotherapy administration with radiotherapy. The blood-brain barrier is an impediment to drug delivery to the brain. The inherent leakiness of the blood-tumor barrier does not …

Characterisation And Antibacterial Activity Of Green Tea Extract-Enriched Solid Goat’S Milk Soap, Uswatun Chasanah, Dian Ermawati, Dwi Putri Utami, Angela Nora Hayati

Pharmaceutical Sciences and Research

Solid goat’s milk soap is organic and beneficial for the health and appearance of the skin. One of the components in green tea known to display antibacterial activities is epigallocatechin gallate (ECGC). In this study, the effects of solid goat’s milk soap containing 1%, 2%, and 4% green tea extract on the growth of Propionibacterium acnes, Staphylococcus aureus, and Staphylococcus epidermidis were examined. The soap was characterized for its organoleptic, pH, free fatty acid, alkalinity, water content, foam stability, and hardness. In addition, an in vitro antimicrobial test was performed utilising the well-diffusion method. The findings revealed that all the …