Pharmaceutics and Drug Design Commons^™

Advancing Herbal Medicine: The Role Of Nanosomal Technology In Treating Skin Diseases, Pedro Anugerah Aswan, Baitha Palanggatan Maggadani, Wilzar Fachri, Raditya Iswandana

Pharmaceutical Sciences and Research

Herbal medicine has become popular worldwide, especially in developing countries, with around 80% of the population opting for herbal treatments. The perceived benefits of natural remedies, such as affordability and fewer side effects, drive this trend. Herbal therapies effectively manage skin diseases, infections, and common ailments. However, the absorption of bioactive compounds in herbal extracts is often limited. Recent developments in nano-based herbal delivery systems, like nanosomal, show promise in enhancing the efficacy of herbal remedies for topical applications, providing improved solubility, stability, and skin penetration. This review describes various nanosomal studies developed and successfully used to enhance the topical …

Exploring The Vitronectin Binding Affinity And Cell Viability Effect Of Small Molecule Metabolites From Medicinal Plants For Neuroblastoma, Stephenie C. A Alaribe, Sofia Granados-Aparici, Akolade R. Oladipupo, Isaac Vieco-Marti, Blessing E. Titilayo, Gordon Allen, Rosa Noguera

Pharmaceutical Sciences and Research

High-risk neuroblastoma (HR-NB) is an aggressive form of childhood cancer with a five-year survival rate of less than 50%, underscoring the need for more efficacious and less toxic treatments. The glycoprotein vitronectin (VN) has been linked to poor prognosis in patients with HR-NB, thus inhibitors of VN function represent a promising avenue for molecular mechanotherapy. This study investigated the binding affinity between the somatomedin B (SMB) domain of VN and natural compounds from the medicinal plant, Olax subscorpioidea, targeting the plasminogen activator inhibitor-1 (PAI-1). The therapeutic potential of α-amyrin (AMY), lupeol (LUP), and olax chalcone A (olax CHA) was tested …

Formulation And In Vitro Evaluation Of Kaffir Lime Fruit Peel Extract-Containing Gel For Sunscreen, Antioxidant, And Moisturizing Activity, Farida Lanawati Darsono, Lisa Soegianto

Pharmaceutical Sciences and Research

Kaffir lime peel waste (Citrus hystrix) has antioxidant effects that have the potential to protect the skin from exposure to UV-A and UV-B rays, as well as moisturize the skin. This study aims to determine the effect of increasing the concentration of condensed extract of kaffir lime fruit peel on its effectiveness as an antioxidant, sunscreen activity, and moisturizer. The condensed extract was obtained by maceration using 96% ethanol. In this study, we tested hydrophilic gels consisting of 4 extract concentrations in their formula: F1 (7.5%), F2 (10%), F3 (15%), and F4 (20%). The research phase begins with …

Additive Effects Of N-Acetylcysteine And [R4W4] Combination Treatment On Mycobacterium Avium, Kayvan Sasaninia, Iffat Hasnin Era, Nezam Newman, Jesse Melendez, Wajiha Akif, Eashan Sharma, Omid Nikjeh, Ira Glassman, Cristián Jiménez, Navya Sharma, Ama Xu, Maria Lambros, Miou Zhou, Rakesh Tiwari, Vishwanath Venketaraman

Pharmacy Faculty Articles and Research

Mycobacterium avium is an opportunistic pathogen and a leading contributor to nontuberculous mycobacterial infections in immunocompromised individuals. However, treatment duration, antibiotic toxicity, and resistance present challenges in the management of mycobacterium infections, prompting the need for novel treatment. N-acetylcysteine (NAC) has demonstrated potent antimycobacterial activity, while antimicrobial peptides such as the cyclic [R₄W₄] have shown additive effects when combined with first-line antibiotics. This study aimed to investigate the mechanism and efficacy of NAC and [R₄W₄] combination therapy against M. avium. A membrane depolarization assay was used to evaluate the effects of …

Dual Membrane Receptor Degradation Via Folate Receptor Targeting Chimera, Zhen Wang, Zhixin Li, Jenny Högström, Hiroyuki Inuzuka, Rui Jing, Peiqiang Yan, Tao Hou, Yihang Qi, Daoyuan Huang, Jingchao Wang, Ting Wu, Xiaoying Shi, Bolin Liu, Taru Muranen, Dingpeng Zhang, Wenyi Wei

School of Medicine Faculty Publications

Cancer drug resistance poses a significant challenge in oncology, often driven by intricate cross-talk among membrane-bound receptors that compromise mono-targeted therapies. We develop a dual membrane receptor degradation strategy leveraging Folate Receptor α (FRα) to address this issue. Folate Receptor α Targeting Chimeras-dual (FolTAC-dual) are engineered degraders designed to selectively and simultaneously degrade distinct receptor pairs: (1) EGFR/HER2 and (2) PD-L1/VISTA. Through modular optimization of modality configurations and geometries, we identify the “string” format as the most effective construct. Mechanistic studies demonstrate an ~85% increase in EGFR-binding affinity compared to the conventional knob-into-hole design, likely contributing to the improved efficiency …

Predictive Gene Expression Signatures For Alzheimer's Disease Using Post-Mortem Brain Tissue, Ashley Duche, Oliver Tan, Andrius Baskys, Rachita K. Sumbria, Moom R. Roosan

Pharmacy Faculty Articles and Research

Background: Alzheimer’s Disease (AD) is a progressive neurodegenerative disorder characterized by amyloid-beta (Aβ) plaques and tau protein aggregates in the brain. These pathological features manifest in specific regions, but mechanisms rendering some areas more susceptible to early AD-related changes remain poorly understood. To address this, we developed predictive gene expression signatures to explore molecular mechanisms underlying regional vulnerability to AD pathology.

Methods: Post-mortem brain tissues from participants of the Religious Orders Study and Memory and Aging Project (ROSMAP), Mayo Clinic, and Mount Sinai Brain Bank (MSBB) were used to derive gene expression signatures from six brain regions affected at varying …

Editorial: Molecular Mechanisms Of Ion Channel Activation And Modulation, Meng Cui, Miao Zhang

Pharmacy Faculty Articles and Research

"Ion channels are integral membrane proteins that regulate the passage of ions across cell membranes, thereby shaping processes as diverse as neuronal signaling, muscle contraction, and hormone secretion. Channel activation is typically initiated by a stimulus such as voltage, ligand binding, or mechanical stress that induces conformational changes and opens the channel pore. Beyond activation, channels are subject to fine-tuned modulation by a wide range of endogenous and exogenous agents, from lipids and neurotransmitters to pharmacological drugs. Modulators can stabilize the open, closed, or inactivated states, shift ligand affinities, or alter gating kinetics. Dissecting the structural and dynamic basis of …

Smart Dressings Accelerating Wound Healing With Tranexamic Acid-Infused Aligned Electrospun Nanofibers: In Vitro And In Vivo Assessments, Samar A. Salim, Abdullah Elbadry, Eman Gomaa, Mennatullah Faisal, Elbadawy A. Kamoun

Nanotechnology Research Centre

The development of advanced wound dressings capable of accelerating healing and achieving effective hemostasis remains a critical challenge in managing traumatic and surgical wounds. This study reports the fabrication and comprehensive evaluation of a novel multilayered, sandwich-structured nanofiber scaffold composed of Tranexamic acid (TXA), chitosan (CS), polyvinyl alcohol (PVA), L-arginine, and polylactic acid (PLA) for biodegradable wound dressing applications. Using sequential electrospinning, a four-layered scaffold was developed as a smart wound dressing, comprising an immediate-release TXA-CS-PVA layer for rapid clotting, a hydrophobic PLA barrier layer for protection, a sustained-release L-arginine-PVA layer to promote tissue regeneration, and a final PLA protective …

Peptide-Based Inorganic Nanoparticles As Efficient Intracellular Delivery Systems, Amir Nasrolahi Shirazi, Rajesh Vadlapatla, Ajoy Koomer, Anthony Nguyen, Vian Khoury, Keykavous Parang

Pharmacy Faculty Articles and Research

Background/Objectives: Peptide-based inorganic nanoparticles (PINPs) have emerged as promising candidates for intracellular delivery due to their unique structural and functional attributes. These hybrid nanostructures combine the high surface area and tunable optical/magnetic properties of metal cores (e.g., Au, Ag, Fe3O4) with the biocompatibility, targeting specificity, and responsive behavior of peptides. In particular, peptides with amphipathic or cell-penetrating features could facilitate efficient transport of molecular cargos across cellular membranes while enabling stimulus-responsive drug release in target tissues. Methods: We review key synthesis methods (especially green, peptide-mediated one-pot approaches), functionalization strategies (e.g., thiol-gold bonds, click chemistries), and characterization techniques (TEM, …

The 9th Annual Lafora Science Symposium: A Rare Epilepsy Community Makes Progress Towards Clinical Readiness, Meredith I. Williams, Katherine J. Donahue, Pascual Sanz, Souad Messahel, Jose M. Serratosa, Jordi Duran, Roberto Michelucci, Lorenzo Muccioli, Antonio Delgado-Escueta, Viet-Hong Nguyen, Berge A. Minassian, Matthew S. Gentry

Pharmacy Faculty Articles and Research

Lafora disease (LD) is a fatal childhood progressive myoclonus epilepsy and glycogen storage disease that is caused by recessive mutations in either EPM2A or EPM2B. The hallmarks of LD are cytoplasmic, aberrant glycogen-like aggregates, called Lafora bodies (LBs), that drive disease progression. The 9th Annual Lafora Science Symposium was held in San Diego, California and brought together over 70 researchers, clinicians, academic trainees, and friends and family members of patients with LD and 80 attendees joined virtually. This symposium focused primarily on international collaborations for therapeutic development and biomarker identification and strategies for preparing the Lafora community for upcoming …

Cbl Regulation Of C-Met Signaling In Corneal Epithelial Cells., Kate Elise Tarvestad Laise

Electronic Theses and Dissertations

The cornea is the most anterior portion of the eye and permits light passage through to retina, allowing formation of a clear image as long as it remains healthy. If the cornea sustains damage, it creates and entrance for foreign body invasion, infection, and ultimately blindness in the immunocompromised eye. Healing the corneal tissue is critical for vision restoration and pain alleviation, as it is the most densely innervated tissue in the body. Growth factors and their cognate receptors are currently under investigation as tools to restore proper corneal physiology. We hypothesize that manipulating the hepatocyte growth factor (HGF) /c-Met …

In Vitro Α-Glucosidase Enzyme Inhibition Activity Test Of Water Extract From Sintok (Cinnamomum Sintoc Blume) Bark, Astrella Amanda Putri Saksono, Inana Ratu Soripada Simanjuntak, Mariana Wahjudi, Marisca Evalina Gondokesumo

Pharmaceutical Sciences and Research

Diabetes mellitus is a condition characterized by elevated blood glucose levels beyond the normal limits. One therapeutic approach for managing diabetes mellitus involves inhibiting the α-glucosidase enzyme, which plays a role in glucose absorption in the body. However, the use of oral antidiabetic drugs from the α-glucosidase inhibitor class often causes gastrointestinal side effects. Therefore, exploring natural materials as alternative treatments is a promising option. In Indonesia, one plant with potential as an alternative treatment is sintok (Cinnamomum sintoc Blume), a member of the Cinnamomum genus, which is widely utilized in traditional medicine for chronic diseases such as …

Potential Of Legume Seeds From The Leguminosae Family As Material Source Of Food And Medicine : A Literature Review, Ni Made Ayu Gangga Dewi, Nina Dewi Oktaviyanti, Aurapa Sakulpanich, Kartini Kartini

Pharmaceutical Sciences and Research

Leguminosae, also known as Fabaceae, is the third largest plant family after Orchidaceae and Asteraceae. This review aimed to explore the potential of several legume species indigenous to Indonesia, from the Leguminosae family, as sources of food and medicine. The data used for the analysis were collected from various online databases such as PubMed, ScienceDirect, and Google Scholar. The results showed that there were 13 species of Leguminosae family plants found easily in Indonesia including Cajanus cajan, Canavalia ensiformis, Mucuna pruriens, Arachis hypogaea, Vigna subterranea, Glycine max, Phaseolus vulgaris, Phaseolus lunatus, Vigna radiata, Vigna unguiculata subsp. unguiculata, Vigna angularis, Vigna …

Optimization Of Formula, Stability Testing, And Antioxidant Activity Of Clay Masks As Skin Moisturizers, Naniek Widyaningrum, Agung Dwi Anggoro Bhakti, Alghafiqy Harya Evan Maulana, Amalia Safitri, Adinda Fajrah Ramadhani, Anisa Febriani, Anggit Naufal Hanafi, Thendi Abdul Arief

Pharmaceutical Sciences and Research

Clay masks are cosmetic formulations designed to adhere closely to the skin, effectively lifting contaminants, cleansing the face, and absorbing impurities. We made a clay mask containing active ingredients such as niacinamide, alpha arbutin, ceramide, and hyaluronic acid. A careful selection of ingredients is essential for ensuring safety and mitigating potential dermatological issues. This study aimed to evaluate the physical characteristics, stability, primary irritation potential, and moisturizing efficacy of this clay mask formulation. Kaolin and bentonite are the primary base materials. The research included formulation optimization and physical stability testing using a cycling test, where each cycle was conducted over …

Surface Keratin 1, A Tumor-Selective Peptide Target In Human Triple-Negative Breast Cancer, Shih-Jing Yao, Farideh Amirrad, Elmira Ziaei, Azam Saghaeidehkordi, Moom R. Roosan, Kiumars Shamloo, Ajay Sharma, Rachita K. Sumbria, Surya M. Nauli, Christopher G. Bunick, Kamaljit Kaur

Pharmacy Faculty Articles and Research

Targeting drugs to cancer cells via overexpressed cell-surface receptors has emerged as an effective therapeutic strategy for several cancers. However, identifying cell-surface receptors that allow selective uptake of targeting ligands by cancer cells—while sparing normal cells—remains a challenge, especially for triple-negative breast cancer (TNBC), which lacks a well-defined receptor for targeted delivery. In this study, immunohistochemical (IHC) analysis revealed that human TNBC patient tissues have significantly higher levels of keratin 1 (K1) compared to normal breast tissues. Among TNBC tissues, grade 3 tumors showed significantly higher (threefold) K1 expression compared to grade 2 tumors. We analyzed human TNBC and normal …

Targeting Obesity: The Role Of Glp-1 Receptor Agonists In Achieving Sustainable Weight Loss, Brad Vamplew

Lynchburg Journal of Medical Science

This review critically evaluates the effectiveness of glucagon-like peptide-1 receptor agonist pharmacotherapy in managing obesity. Obesity is a health epidemic that affects 100 million Americans, and it puts individuals at higher risk for numerous health comorbidities over a lifetime. A comprehensive literature review was completed by utilizing PubMed and its clinical queries function to locate relevant research. The research information was narrowed down with a focus on obesity management and glucagon-like peptide-1 receptor agonists for therapy. Numerous current clinical studies and trials were incorporated into this review. Many clinical trials substantiated the benefits of this pharmacotherapy for the management of …

Engineering Cxcr2-Ligand-Based Fusion Proteins To Modulate Myeloid Cell Trafficking In Pancreatic Cancer, Benjamin N. Christopher

MUSC Theses and Dissertations

Pancreatic ductal adenocarcinoma (PDAC) has one of the lowest 5-year survival rates of all cancers, and limited treatment options exist. Immunotherapy is effective in some cancer types, but the immunosuppressive tumor microenvironment (TME) of PDAC is a barrier to effective immunotherapy. CXCR2+ myeloid-derived suppressor cells (MDSCs) are abundant in PDAC tumors in humans and in mouse models. MDSCs suppress effector cell function, making them attractive targets for restoring anti-tumor immunity. The studies outlined in this dissertation (1) link tumor-intrinsic oncogenic signaling to dysregulated myeloid activity in PDAC, (2) describe a rationally designed fusion protein and potent inhibitor of CXCR2+ myeloid …

Multidrug Resistance: Are We Still Afraid Of The Big Bad Wolf, Abdulelah Alhazza, Adenike Oyegbesan, Emira Bousoik, Hamidreza Montazeri Aliabadi

Pharmacy Faculty Articles and Research

After the era of multidrug resistance (MDR) against cytotoxic chemotherapy, the development of resistance against newly developed molecularly targeted drugs also seems inevitable. While the mechanisms involved in resistance against these two categories of anticancer drugs are different, the principles are similar: inherent resistance (also known as primary resistance) is a result of heterogeneity in cancer cells where a subpopulation of the cells do not show a favorable initial response to the drug, while acquired resistance (or secondary resistance), as the name suggests, is developed after repeated treatments due to the plasticity of cancer cells. Despite the introduction of a …

Fda Approves Lecanemab-Irmb Maintenance Dosing For Early Alzheimer’S Disease Treatment, Jordyn Linfield, Giang Nguyen, Ashley Jacob, Andrew Johnson, Maria Nguyen, Sara Ha, Joshua Honaker, Samantha Mccord, Kelly Kroustos

Pharmacy and Wellness Review

Alzheimer’s disease (AD) is the most prevalent neurodegenerative disorder and is associated with progressive and irreversible cognitive decline that begins with memory lapses leading to physical and functional impairment. The conventional therapies that have been used for the treatment from Alzheimer's Disease include acetylcholinesterase inhibitors and memantine, but additional therapy options are being developed. Lecanemab, brand name Lequembi, is currently a Food and Drug Administration (FDA) approved humanized monoclonal antibody for the treatment of Alzheimer’s disease and indicated for mild cognitive impairment (MCI) or mild dementia. While there is impactful aid for treatment, lecanemab has three significant adverse reactions, which …

The Endocannabinoid System's Influence And Modulation Of Nociception, Doreen M. Flannery

Honors Thesis

The anatomy and physiology of pain is a well-defined pathway where noxious stimuli is processed by different systems in the brain. The central research question of this review is how can we better understand the neurobiological effects pain has, and assess if there is therapeutic potential in using endocannabinoids to modulate these effects. Endocannabinoids are signaling molecules that play a key role at both the cellular and molecular level in modulating both acute and chronic pain by influencing different processes within each level that affect how the body responds to both internal and external stimuli. The endocannabinoid system is a …