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Point Prevalence Survey of Acute Hospital Patients with Difficulty Swallowing Solid Oral Dose Forms Pharmaceutics (IF 5.4) Pub Date : 2024-04-25 Anne Harnett, Stephen Byrne, Jennifer O’Connor, Eimear Burke, Laura South, Declan Lyons, Laura J. Sahm
The safe administration of solid oral dose forms in hospital inpatients with swallowing difficulties is challenging. The aim of this study was to establish the prevalence of difficulties in swallowing solid oral dose forms in acute hospital inpatients. A point prevalence study was completed at three time points. The following data were collected: the prevalence of swallowing difficulties, methods used
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Investigating the Influence of Processing Conditions on Dissolution and Physical Stability of Solid Dispersions with Fenofibrate and Mesoporous Silica Pharmaceutics (IF 5.4) Pub Date : 2024-04-24 Ana Baumgartner, Nina Dobaj, Odon Planinšek
The study aimed to enhance the solubility of the poorly water-soluble drug, fenofibrate, by loading it onto mesoporous silica, forming amorphous solid dispersions. Solid dispersions with 30% fenofibrate were prepared using the solvent evaporation method with three solvents (ethyl acetate, acetone, and isopropanol) at different temperatures (40 °C, boiling point temperature). Various characteristics
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Pharmaceutical Compounding in Veterinary Medicine: Suspension of Itraconazole Pharmaceutics (IF 5.4) Pub Date : 2024-04-24 Gema J. Cabañero-Resta, Bárbara Sánchez-Dengra, Alejandro Ruiz-Picazo, Marival Bermejo, Virginia Merino, Isabel Gonzalez-Alvarez, Marta Gonzalez-Alvarez
Itraconazole is a drug used in veterinary medicine for the treatment of different varieties of dermatophytosis at doses between 3–5 mg/kg/day in cats. Nevertheless, in Spain, it is only available in the market as a 52 mL suspension at 10 mg/mL. The lack of alternative formulations, which provide sufficient formulation to cover the treatment of large animals or allow the treatment of a group of them
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Plant-Derived Bioactive Compounds: Exploring Neuroprotective, Metabolic, and Hepatoprotective Effects for Health Promotion and Disease Prevention Pharmaceutics (IF 5.4) Pub Date : 2024-04-24 Rosa Direito, Sandra Maria Barbalho, Bruno Sepodes, Maria Eduardo Figueira
There is a growing trend among consumers to seek out natural foods and products with natural ingredients. This shift in consumer preferences had a direct impact on both food and pharmaceutical industries, leading to a focus of scientific research and commercial efforts to meet these new demands. The aim of this work is to review recent available scientific data on foods of interest, such as the artichoke
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Characterization of Oil-in-Water Emulsions Prepared with Triblock Copolymer Poloxamer 407 and Low-Molecular-Mass Surfactant Mixtures as Carriers of Grape Pomace Waste Polyphenols Pharmaceutics (IF 5.4) Pub Date : 2024-04-24 Veljko S. Krstonošić, Darija B. Sazdanić, Dejan M. Ćirin, Ivana R. Nikolić, Miroslav S. Hadnađev, Milica T. Atanacković Krstonošić
Background: Natural antioxidants, such as grape pomace polyphenols, can be extracted by a surfactant-based green technology and incorporated into various emulsions. Therefore, this work aimed to investigate the physical stability and rheological characteristics of oil-in-water emulsions stabilized with poloxamer 407 (P407) and its mixtures with the low-molecular-mass surfactants Brij S20 (BS20) and
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Topical Insulin Eye Drops: Stability and Safety of Two Compounded Formulations for Treating Persistent Corneal Epithelial Defects Pharmaceutics (IF 5.4) Pub Date : 2024-04-24 Marta Vicario-de-la-Torre, Virginia Puebla-García, Lidia Ybañez-García, José Javier López-Cano, Miriam Ana González-Cela-Casamayor, Marco Brugnera, Bárbara Burgos-Blasco, David Díaz-Valle, José Antonio Gegúndez-Fernández, José Manuel Benítez-del-Castillo, Rocío Herrero-Vanrell
Compounded insulin eye drops were prepared at 1 IU/mL from commercially available subcutaneous insulin by dilution in saline solution or artificial tears. Physicochemical characterization and in vitro tolerance testing in human and conjunctival cells were followed by a 28-day short-term stability study under various conditions. The formulations were isotonic (280–300 mOsm/L), had a pH close to neutral
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Attempts to Improve Lipophilic Drugs’ Solubility and Bioavailability: A Focus on Fenretinide Pharmaceutics (IF 5.4) Pub Date : 2024-04-24 Silvana Alfei, Guendalina Zuccari
The development of numerous drugs is often arrested at clinical testing stages, due to their unfavorable biopharmaceutical characteristics. It is the case of fenretinide (4-HPR), a second-generation retinoid, that demonstrated promising in vitro cytotoxic activity against several cancer cell lines. Unfortunately, response rates in early clinical trials with 4-HPR did not confirm the in vitro findings
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Vaccination with DC-SIGN-Targeting αGC Liposomes Leads to Tumor Control, Irrespective of Suboptimally Activated T-Cells Pharmaceutics (IF 5.4) Pub Date : 2024-04-24 Aram M. de Haas, Dorian A. Stolk, Sjoerd T. T. Schetters, Laura Goossens-Kruijssen, Eelco Keuning, Martino Ambrosini, Louis Boon, Hakan Kalay, Gert Storm, Hans J. van der Vliet, Tanja D. de Gruijl, Yvette van Kooyk
Cancer vaccines have emerged as a potent strategy to improve cancer immunity, with or without the combination of checkpoint blockade. In our investigation, liposomal formulations containing synthetic long peptides and α-Galactosylceramide, along with a DC-SIGN-targeting ligand, Lewis Y (LeY), were studied for their anti-tumor potential. The formulated liposomes boosted with anti-CD40 adjuvant demonstrated
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Therapeutic Effects of Essential Oils and Their Bioactive Compounds on Prostate Cancer Treatment Pharmaceutics (IF 5.4) Pub Date : 2024-04-24 Leticia Santos Pimentel, Luciana Machado Bastos, Luiz Ricardo Goulart, Lígia Nunes de Morais Ribeiro
Since prostate cancer (PCa) relies on limited therapies, more effective alternatives are required. Essential oils (EOs) and their bioactive compounds are natural products that have many properties including anticancer activity. This review covers studies published between 2000 and 2023 and discusses the anti-prostate cancer mechanisms of the EOs from several plant species and their main bioactive compounds
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Plant Protease Inhibitors as Emerging Antimicrobial Peptide Agents: A Comprehensive Review Pharmaceutics (IF 5.4) Pub Date : 2024-04-24 Mónica G. Parisi, Brenda Ozón, Sofía M. Vera González, Javier García-Pardo, Walter David Obregón
Antimicrobial peptides (AMPs) are important mediator molecules of the innate defense mechanisms in a wide range of living organisms, including bacteria, mammals, and plants. Among them, peptide protease inhibitors (PPIs) from plants play a central role in their defense mechanisms by directly attacking pathogens or by modulating the plant’s defense response. The growing prevalence of microbial resistance
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Evaluation of the Transport and Binding of Dopamine-Loaded PLGA Nanoparticles for the Treatment of Parkinson’s Disease Using In Vitro Model Systems Pharmaceutics (IF 5.4) Pub Date : 2024-04-23 Karin Danz, Jana Fleddermann, Marcus Koch, Elena Fecioru, Lorenz Maahs, Nicole Kinsinger, Johannes Krämer, Annette Kraegeloh, Sylvia Wagner
The treatment of Parkinson’s disease has been moving into the focus of pharmaceutical development. Yet, the necessity for reliable model systems in the development phase has made research challenging and in vivo models necessary. We have established reliable, reproducible in vitro model systems to evaluate the binding and transport of dopamine-loaded PLGA nanoparticles for the treatment of Parkinson’s
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Physicochemical Stability of Hospital Parenteral Nutrition Solutions: Effect of Changes in Composition and Storage Protocol Pharmaceutics (IF 5.4) Pub Date : 2024-04-23 Luis Otero-Millán, Brais Bea-Mascato, Jose Luis Legido Soto, Noemi Martínez-López-De-Castro, Natividad Lago-Rivero
(1) Background: Parenteral nutrition (PN) is a technique used for the administration of nutrients to patients for whom traditional routes cannot be used. It is performed using solutions with extremely complex compositions, which can give rise to a large number of interactions. These interactions can impact their stability and put the patient’s life at risk. The aim of this study is to determine how
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Exploring the Wound Healing Potential of a Cuscuta chinensis Extract-Loaded Nanoemulsion-Based Gel Pharmaceutics (IF 5.4) Pub Date : 2024-04-23 Nichcha Nitthikan, Weeraya Preedalikit, Kanittapon Supadej, Siripat Chaichit, Pimporn Leelapornpisid, Kanokwan Kiattisin
Cuscuta chinensis (C. chinensis) presents many pharmacological activities, including antidiabetic effects, and antioxidant, anti-inflammatory, and antitumor properties. However, the wound care properties of this plant have not yet been reported. Therefore, this research aimed to evaluate the antioxidant, anti-inflammatory, and antibacterial activities of ethanol and ethyl acetate C. chinensis extracts
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Evaluation of Drug Blood-Brain-Barrier Permeability Using a Microfluidic Chip Pharmaceutics (IF 5.4) Pub Date : 2024-04-23 Jung Yoon Yang, Dae-Seop Shin, Moonkyu Jeong, Seong Soon Kim, Ha Neul Jeong, Byung Hoi Lee, Kyu-Seok Hwang, Yuji Son, Hyeon-Cheol Jeong, Chi-Hoon Choi, Kyeong-Ryoon Lee, Myung Ae Bae
The blood-brain-barrier (BBB) is made up of blood vessels whose permeability enables the passage of some compounds. A predictive model of BBB permeability is important in the early stages of drug development. The predicted BBB permeabilities of drugs have been confirmed using a variety of in vitro methods to reduce the quantities of drug candidates needed in preclinical and clinical trials. Most prior
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Testing S. sonnei GMMA with and without Aluminium Salt-Based Adjuvants in Animal Models Pharmaceutics (IF 5.4) Pub Date : 2024-04-22 Francesca Mancini, Valentina Caradonna, Renzo Alfini, Maria Grazia Aruta, Claudia Giorgina Vitali, Gianmarco Gasperini, Diego Piccioli, Francesco Berlanda Scorza, Omar Rossi, Francesca Micoli
Shigellosis is one of the leading causes of diarrheal disease in low- and middle-income countries, particularly in young children, and is more often associated with antimicrobial resistance. Therefore, a preventive vaccine against shigellosis is an urgent medical need. We have proposed Generalised Modules for Membrane Antigens (GMMA) as an innovative delivery system for Shigella sonnei O-antigen, and
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Enhancing the Bioavailability of Resveratrol: Combine It, Derivatize It, or Encapsulate It? Pharmaceutics (IF 5.4) Pub Date : 2024-04-22 Mohamed Salla, Nadine Karaki, Belal El Kaderi, Abeer J. Ayoub, Samar Younes, Maya N. Abou Chahla, Shairaz Baksh, Sami El Khatib
Overcoming the limited bioavailability and extensive metabolism of effective in vitro drugs remains a challenge that limits the translation of promising drugs into clinical trials. Resveratrol, despite its well-reported therapeutic benefits, is not metabolically stable and thus has not been utilized as an effective clinical drug. This is because it needs to be consumed in large amounts to overcome
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Combination of miR159 Mimics and Irinotecan Utilizing Lipid Nanoparticles for Enhanced Treatment of Colorectal Cancer Pharmaceutics (IF 5.4) Pub Date : 2024-04-22 Rulei Yang, Yiran Liu, Ning Yang, Tian Zhang, Jiazhen Hou, Zongyan He, Yutong Wang, Xujie Sun, Jingshan Shen, Hualiang Jiang, Yuanchao Xie, Tianqun Lang
Colorectal cancer (CRC) ranks as the third most prevalent global malignancy, marked by significant metastasis and post-surgical recurrence, posing formidable challenges to treatment efficacy. The integration of oligonucleotides with chemotherapeutic drugs emerges as a promising strategy for synergistic CRC therapy. The nanoformulation, lipid nanoparticle (LNP), presents the capability to achieve co-delivery
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Nucleolin-Targeting AS1411 Aptamer-Conjugated Nanospheres for Targeted Treatment of Glioblastoma Pharmaceutics (IF 5.4) Pub Date : 2024-04-21 Kyeongjin Seo, Kihwan Hwang, Kyung Mi Nam, Min Ju Kim, Yoon-Kyu Song, Chae-Yong Kim
Post-operative chemotherapy is still required for the treatment of glioblastoma (GBM), for which nanocarrier-based drug delivery has been identified as one of the most effective methods. However, the blood-brain barrier (BBB) and non-specific delivery to non-tumor tissues can significantly limit drug accumulation in tumor tissues and cause damage to nearby normal tissues. This study describes a targeted
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Unveiling the Potential of Extracellular Vesicles as Biomarkers and Therapeutic Nanotools for Gastrointestinal Diseases Pharmaceutics (IF 5.4) Pub Date : 2024-04-21 Valentina Arrè, Rita Mastrogiacomo, Francesco Balestra, Grazia Serino, Federica Viti, Federica Rizzi, Maria Lucia Curri, Gianluigi Giannelli, Nicoletta Depalo, Maria Principia Scavo
Extracellular vesicles (EVs), acting as inherent nanocarriers adept at transporting a range of different biological molecules such as proteins, lipids, and genetic material, exhibit diverse functions within the gastroenteric tract. In states of normal health, they participate in the upkeep of systemic and organ homeostasis. Conversely, in pathological conditions, they significantly contribute to the
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Development of Mechanistic In Vitro–In Vivo Extrapolation to Support Bioequivalence Assessment of Long-Acting Injectables Pharmaceutics (IF 5.4) Pub Date : 2024-04-19 Daniela Amaral Silva, Maxime Le Merdy, Khondoker Dedarul Alam, Yan Wang, Quanying Bao, Nilesh Malavia, Diane Burgess, Viera Lukacova
Long-acting injectable (LAI) formulations provide sustained drug release over an extended period ranging from weeks to several months to improve efficacy, safety, and compliance. Nevertheless, many challenges arise in the development and regulatory assessment of LAI drug products due to a limited understanding of the tissue response to injected particles (e.g., inflammation) impacting in vivo performance
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Ponatinib Induces a Procoagulant Phenotype in Human Coronary Endothelial Cells via Inducing Apoptosis Pharmaceutics (IF 5.4) Pub Date : 2024-04-19 Bálint Krajcsir, Marianna Pócsi, Zsolt Fejes, Béla Nagy, János Kappelmayer, Ildikó Beke Debreceni
BCR-ABL tyrosine kinase inhibitors (TKIs) are effective drugs in the treatment of patients with chronic myeloid leukemia. However, based on clinical studies, ponatinib was associated with the development of thrombotic complications. Since endothelial cells (ECs) regulate blood coagulation, their abnormal phenotype may play a role in the development of thrombotic events. We here aimed to investigate
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Amount of Dentifrice and Fluoride Concentration Affect the pH and Inorganic Composition of Dual-Species Biofilms of Streptococcus mutans and Candida albicans Pharmaceutics (IF 5.4) Pub Date : 2024-04-20 Caio Sampaio, Alberto Carlos Botazzo Delbem, Thayse Yumi Hosida, Ana Vitória Pereira Fernandes, Bruna do Amaral, Leonardo Antônio de Morais, Douglas Roberto Monteiro, Juliano Pelim Pessan
This work assessed the influence of the amount of dentifrice and fluoride (F) concentration in the product on the pH and inorganic components of Streptococcus mutans and Candida albicans dual-species biofilms. The biofilms were treated with suspensions of fluoride dentifrices containing 550 or 1100 ppm of F (550 F or 1100 F, respectively) administered at comparable intensities: (i-1) 550 F/0.08 g or
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Modulating the Nature of Ionizable Lipids and Number of Layers in Hyaluronan-Decorated Lipid Nanoparticles for In Vitro Delivery of RNAi Pharmaceutics (IF 5.4) Pub Date : 2024-04-20 Victor Passos Gibson, Houda Tahiri, Claudia Gilbert, Chun Yang, Quoc Thang Phan, Xavier Banquy, Pierre Hardy
Lipid nanoparticles (LNPs) have established their position as nonviral vectors for gene therapy. Tremendous efforts have been made to modulate the properties of LNPs to unleash their full clinical potential. Among the strategies being pursued, the layer-by-layer (LbL) technique has gained considerable attention in the biomedical field. Illuminated by our previous work, here we investigate if the LbL
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Exploring the Impact of Hepatic Impairment on Pralsetinib Pharmacokinetics Pharmaceutics (IF 5.4) Pub Date : 2024-04-20 Kit Wun Kathy Cheung, Yang Tang, Doreen Anders, Teresa Barata, Astrid Scalori, Priya Agarwal, Rucha Sane, Sravanthi Cheeti
Pralsetinib is a kinase inhibitor indicated for the treatment of metastatic rearranged during transfection (RET) fusion-positive non-small cell lung cancer. Pralsetinib is primarily eliminated by the liver and hence hepatic impairment (HI) is likely alter its pharmacokinetics (PK). Mild HI has been shown to have minimal impact on the PK of pralsetinib. This hepatic impairment study aimed to determine
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Performance Characterisation of the Airvo2TM Nebuliser Adapter in Combination with the Aerogen SoloTM Vibrating Mesh Nebuliser for in Line Aerosol Therapy during High Flow Nasal Oxygen Therapy Pharmaceutics (IF 5.4) Pub Date : 2024-04-20 Ronan MacLoughlin, Marc Mac Giolla Eain
High flow oxygen (HFO) therapy is a well-established treatment in respiratory disease. Concurrent aerosol delivery can greatly expediate their recovery. The aim of this work was to complete a comprehensive characterisation of one such HFO therapy system, the Airvo2TM, used in combination with the Aerogen SoloTM vibrating mesh nebuliser. Representative adult, infant, and paediatric head models were
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Polymeric Amorphous Solid Dispersions of Dasatinib: Formulation and Ecotoxicological Assessment Pharmaceutics (IF 5.4) Pub Date : 2024-04-18 Katarina Sokač, Martina Miloloža, Dajana Kučić Grgić, Krunoslav Žižek
Dasatinib (DAS), a potent anticancer drug, has been subjected to formulation enhancements due to challenges such as significant first-pass metabolism, poor absorption, and limited oral bioavailability. To improve its release profile, DAS was embedded in a matrix of the hydrophilic polymer polyvinylpyrrolidone (PVP). Drug amorphization was induced in a planetary ball mill by solvent-free co-grinding
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Evaluation of Printability of PVA-Based Tablets from Powder and Assessment of Critical Rheological Parameters Pharmaceutics (IF 5.4) Pub Date : 2024-04-19 Jonas Lenhart, Florian Pöstges, Karl G. Wagner, Dominique J. Lunter
Fused deposition modeling (FDM) is a rather new technology in the production of personalized dosage forms. The melting and printing of polymer–active pharmaceutical ingredient (API)—mixtures can be used to produce oral dosage forms with different dosage as well as release behavior. This process is utilized to increase the bioavailability of pharmaceutically relevant active ingredients that are poorly
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Microemulsions and Nanoemulsions for Topical Delivery of Tripeptide-3: From Design of Experiment to Anti-Sebum Efficacy on Facial Skin Pharmaceutics (IF 5.4) Pub Date : 2024-04-19 Nontachai Magrode, Worrapan Poomanee, Kanokwan Kiattisin, Chadarat Ampasavate
The targeted delivery of a hydrophilic Tripeptide-3 to the skin using microemulsions or nanoemulsions for facial oil reduction was the focus of this study. The impact factors affecting oil/water transparent dispersion formation, such as the surfactant system, HLB value, and co-solvent, were identified through the water titration method and pseudoternary phase diagram plots. The interfacial tension
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Darunavir Nanoformulation Suppresses HIV Pathogenesis in Macrophages and Improves Drug Delivery to the Brain in Mice Pharmaceutics (IF 5.4) Pub Date : 2024-04-19 Lina Zhou, Sandip Godse, Namita Sinha, Sunitha Kodidela, Udai Singh, Santosh Kumar
Although antiretroviral therapy (ART) can suppress peripheral HIV, patients still suffer from neuroHIV due to insufficient levels of ART drugs in the brain. Hence, this study focuses on developing a poly lactic-co-glycolic acid (PLGA) nanoparticle-based ART drug delivery system for darunavir (DRV) using an intranasal route that can overcome the limitation of drug metabolic stability and blood–brain
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High Manganese Content of Lipid NanoMn (LNM) by Microfluidic Technology for Enhancing Anti-Tumor Immunity Pharmaceutics (IF 5.4) Pub Date : 2024-04-19 Jiawei Sun, Jingjing Gong, Lidong Gong, Chuanda Zhu, Longhao Li-Yang, Jingya Wang, Yuanyuan Yang, Shiming Zhang, Silu Liu, Ji-Jun Fu, Pengcheng Xu
Immunotherapy is a clinically effective method for treating tumors. Manganese can activate the cGAS-STING signaling pathway and induce an anti-tumor immune response. However, its efficacy is hindered by non-specific distribution and low uptake rates. In this study, we employed microfluidic technology to design and develop an innovative preparation process, resulting in the creation of a novel manganese
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Hypoxia-Activated Theragnostic Prodrugs (HATPs): Current State and Future Perspectives Pharmaceutics (IF 5.4) Pub Date : 2024-04-19 Sankarprasad Bhuniya, Eirinaios I. Vrettos
Hypoxia is a significant feature of solid tumors and frequently poses a challenge to the effectiveness of tumor-targeted chemotherapeutics, thereby limiting their anticancer activity. Hypoxia-activated prodrugs represent a class of bio-reductive agents that can be selectively activated in hypoxic compartments to unleash the toxic warhead and thus, eliminate malignant tumor cells. However, their applicability
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ABCG2 Transports the Flukicide Nitroxynil and Affects Its Biodistribution and Secretion into Milk Pharmaceutics (IF 5.4) Pub Date : 2024-04-19 Laura Álvarez-Fernández, Esther Blanco-Paniagua, Gracia Merino
The ABCG2 transporter plays a key role in pharmacological and toxicological processes, affecting bioavailability, tissue accumulation and milk secretion of its substrates. This protein is expressed in several biological barriers acting as a protective mechanism against xenobiotic exposure by pumping out a broad range of compounds. However, its induced expression during lactation in alveolar cells of
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Host–Guest Complexation of Itraconazole with Cyclodextrins for Bioavailability Enhancement Pharmaceutics (IF 5.4) Pub Date : 2024-04-19 Lenuţa-Maria Şuta, Amalia Ridichie, Adriana Ledeţi, Claudia Temereancă, Ionuţ Ledeţi, Delia Muntean, Matilda Rădulescu, Renata-Maria Văruţ, Claudia Watz, Florentin Crăineanu, Denisa Ivan, Gabriela Vlase, Lavinia Stelea
Itraconazole is an antifungal agent included in the triazole pharmacological classification that belongs to the BCS class II, characterized by a low solubility in an aqueous medium (of 1 ng/mL, at neutral pH), which is frequently translated in a low oral bioavailability but with a high permeability. In this sense, it is necessary to find solutions to increase/improve the solubility of itraconazole
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Assessing the Occurrence and Influence of Cancer Chemotherapy-Related Pharmacogenetic Alleles in the Chilean Population Pharmaceutics (IF 5.4) Pub Date : 2024-04-19 Gareth I. Owen, Miguel Cordova-Delgado, Bernabé I. Bustos, Leslie C. Cerpa, Pamela Gonzalez, Sebastián Morales-Pison, Benjamín Garcia-Bloj, Marcelo Garrido, Juan Francisco Miquel, Luis A. Quiñones
Background: Pharmacogenomic knowledge as a biomarker for cancer care has transformed clinical practice, however, as current guidelines are primarily derived from Eurocentric populations, this limits their application in Latin America, particularly among Hispanic or Latino groups. Despite advancements, systemic chemotherapy still poses challenges in drug toxicity and suboptimal response. This study
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LDLR-Mediated Targeting and Productive Uptake of siRNA-Peptide Ligand Conjugates In Vitro and In Vivo Pharmaceutics (IF 5.4) Pub Date : 2024-04-17 Baptiste Broc, Karine Varini, Rose Sonnette, Belinda Pecqueux, Florian Benoist, Maxime Masse, Yasmine Mechioukhi, Géraldine Ferracci, Jamal Temsamani, Michel Khrestchatisky, Guillaume Jacquot, Pascaline Lécorché
Small RNA molecules such as microRNA and small interfering RNA (siRNA) have become promising therapeutic agents because of their specificity and their potential to modulate gene expression. Any gene of interest can be potentially up- or down-regulated, making RNA-based technology the healthcare breakthrough of our era. However, the functional and specific delivery of siRNAs into tissues of interest
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Transport of Non-Steroidal Anti-Inflammatory Drugs across an Oral Mucosa Epithelium In Vitro Model Pharmaceutics (IF 5.4) Pub Date : 2024-04-15 Grace C. Lin, Heinz-Peter Friedl, Sarah Grabner, Anna Gerhartl, Winfried Neuhaus
Non-steroidal anti-inflammatory drugs (NSAIDs) are one of the most prescribed drugs to treat pain or fever. However, oral administration of NSAIDs is frequently associated with adverse effects due to their inhibitory effect on the constitutively expressed cyclooxygenase enzyme 1 (COX-1) in, for instance, the gastrointestinal tract. A systemic delivery, such as a buccal delivery, of NSAIDs would be
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Cryo-Milled β-Glucan Nanoparticles for Oral Drug Delivery Pharmaceutics (IF 5.4) Pub Date : 2024-04-16 Guanyu Chen, Yi Liu, Darren Svirskis, Hongyu Li, Man Ying, Weiyue Lu, Jingyuan Wen
Gemcitabine is a nucleoside analog effective against a number of cancers. However, it has an oral bioavailability of less than 10%, due to its high hydrophilicity and low permeability through the intestinal epithelium. Therefore, the aim of this project was to develop a novel nanoparticulate drug delivery system for the oral delivery of gemcitabine to improve its oral bioavailability. In this study
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Enhancing In Vivo Electroporation Efficiency through Hyaluronidase: Insights into Plasmid Distribution and Optimization Strategies Pharmaceutics (IF 5.4) Pub Date : 2024-04-17 Debnath Maji, Verónica Miguela, Andrew D. Cameron, Delcora A. Campbell, Linda Sasset, Xin Yao, Andy T. Thompson, Carleigh Sussman, David Yang, Robert Miller, Marek M. Drozdz, Rachel A. Liberatore
Electroporation (EP) stands out as a promising non-viral plasmid delivery strategy, although achieving optimal transfection efficiency in vivo remains a challenge. A noteworthy advancement in the field of in vivo EP is the application of hyaluronidase, an enzyme with the capacity to degrade hyaluronic acid in the extracellular matrix, which thereby enhances DNA transfer efficiency by 2- to 3-fold.
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Early Detection of Myeloid-Derived Suppressor Cells in the Lung Pre-Metastatic Niche by Shortwave Infrared Nanoprobes Pharmaceutics (IF 5.4) Pub Date : 2024-04-17 Jake N. Siebert, Jay V. Shah, Mei Chee Tan, Richard E. Riman, Mark C. Pierce, Edmund C. Lattime, Vidya Ganapathy, Prabhas V. Moghe
Metastatic breast cancer remains a significant source of mortality amongst breast cancer patients and is generally considered incurable in part due to the difficulty in detection of early micro-metastases. The pre-metastatic niche (PMN) is a tissue microenvironment that has undergone changes to support the colonization and growth of circulating tumor cells, a key component of which is the myeloid-derived
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Preparation and Characterization of Polymeric Microparticles Based on Poly(ethylene brassylate-co-squaric Acid) Loaded with Norfloxacin Pharmaceutics (IF 5.4) Pub Date : 2024-04-17 Alexandru-Mihail Șerban, Isabella Nacu, Irina Rosca, Alina Ghilan, Alina Gabriela Rusu, Loredana Elena Niță, Raluca Nicoleta Darie-Niță, Aurica P. Chiriac
In recent years, increasing interest has been accorded to polyester-based polymer microstructures, driven by their promising potential as advanced drug delivery systems. This study presents the preparation and characterization of new polymeric microparticles based on poly(ethylene brassylate-co-squaric acid) loaded with norfloxacin, a broad-spectrum antibiotic. Polymacrolactone was synthesised in mild
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In Vivo Imaging of Acute Hindlimb Ischaemia in Rat Model: A Pre-Clinical PET Study Pharmaceutics (IF 5.4) Pub Date : 2024-04-15 Gergely Farkasinszky, Judit Szabó Péliné, Péter Károlyi, Szilvia Rácz, Noémi Dénes, Tamás Papp, József Király, Zsuzsanna Szabo, István Kertész, Gábor Mező, Gabor Halmos, Zita Képes, György Trencsényi
Background: To better understand ischaemia-related molecular alterations, temporal changes in angiogenic Aminopeptidase N (APN/CD13) expression and glucose metabolism were assessed with PET using a rat model of peripheral arterial disease (PAD). Methods: The mechanical occlusion of the base of the left hindlimb triggered using a tourniquet was applied to establish the ischaemia/reperfusion injury model
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Transcription Factor Binding Site in Promoter Determines the Pattern of Plasmid-Based Transgene Expression In Vivo Pharmaceutics (IF 5.4) Pub Date : 2024-04-15 Chunbo Zhang, Dexi Liu
Understanding the regulation of transgene expression is critical for the success of plasmid-based gene therapy and vaccine development. In this study, we used two sets of plasmid vectors containing secreted embryonic alkaline phosphatase or the mouse IL-10 gene as a reporter and investigated the role of promoter elements in regulating transgene expression in vivo. We demonstrated in mice that hydrodynamic
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Drug Release from Lipid Microparticles—Insights into Drug Incorporation and the Influence of Physiological Factors Pharmaceutics (IF 5.4) Pub Date : 2024-04-15 Eliza Wolska, Karolina Sadowska
The aim of this study was to assess the impact of physiological factors, namely tear fluid and lysozyme enzyme, as well as surfactant polysorbate, on the release profile from solid lipid microparticles (SLM), in the form of dispersion intended for ocular application. Indomethacin (Ind) was used as a model drug substance and a release study was performed by applying the dialysis bag method. Conducting
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Comprehensive Therapeutic Approaches to Tuberculous Meningitis: Pharmacokinetics, Combined Dosing, and Advanced Intrathecal Therapies Pharmaceutics (IF 5.4) Pub Date : 2024-04-14 Ahmad Khalid Madadi, Moon-Jun Sohn
Tuberculous meningitis (TBM) presents a critical neurologic emergency characterized by high mortality and morbidity rates, necessitating immediate therapeutic intervention, often ahead of definitive microbiological and molecular diagnoses. The primary hurdle in effective TBM treatment is the blood–brain barrier (BBB), which significantly restricts the delivery of anti-tuberculous medications to the
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Aptamers for the Delivery of Plant-Based Compounds: A Review Pharmaceutics (IF 5.4) Pub Date : 2024-04-14 Joana Gamboa, Pedro Lourenço, Carla Cruz, Eugenia Gallardo
Natural compounds have a high potential for the treatment of various conditions, including infections, inflammatory diseases, and cancer. However, they usually present poor pharmacokinetics, low specificity, and even toxicity, which limits their use. Therefore, targeted drug delivery systems, typically composed of a carrier and a targeting ligand, can enhance natural product selectivity and effectiveness
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68Ga-DOTA-D-Alanine-BoroPro Radiotracer for Imaging of the Fibroblast Activation Protein in Malignant and Non-Malignant Diseases Pharmaceutics (IF 5.4) Pub Date : 2024-04-12 Diana Trujillo-Benítez, Myrna Luna-Gutiérrez, José G. Aguirre-De Paz, Pedro Cruz-Nova, Gerardo Bravo-Villegas, Joel E. Vargas-Ahumada, Paola Vallejo-Armenta, Enrique Morales-Avila, Nallely Jiménez-Mancilla, Rigoberto Oros-Pantoja, Clara Santos-Cuevas, Erika Azorín-Vega, Blanca Ocampo-García, Guillermina Ferro-Flores
Recently, we reported a new fibroblast activation protein (FAP) inhibitor radiopharmaceutical based on the 99mTc-((R)-1-((6-hydrazinylnicotinoyl)-D-alanyl) pyrrolidin-2-yl) boronic acid (99mTc-HYNIC-D-Alanine-BoroPro)(99mTc-HYNIC-iFAP) structure for tumor microenvironment SPECT imaging. This research aimed to synthesize 68Ga-[2,2’,2’’,2’’’-(2-(4-(2-(5-(((S)-1-((S)-2-boronopyrrolidin-1-yl)-1-oxopro
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Investigation of Photodynamic Therapy Promoted by Cherenkov Light Activated Photosensitizers—New Aspects and Revelations Pharmaceutics (IF 5.4) Pub Date : 2024-04-13 Lisa Hübinger, Kerstin Wetzig, Roswitha Runge, Holger Hartmann, Falk Tillner, Katja Tietze, Marc Pretze, David Kästner, Robert Freudenberg, Claudia Brogsitter, Jörg Kotzerke
This work investigates the proposed enhanced efficacy of photodynamic therapy (PDT) by activating photosensitizers (PSs) with Cherenkov light (CL). The approaches of Yoon et al. to test the effect of CL with external radiation were taken up and refined. The results were used to transfer the applied scheme from external radiation therapy to radionuclide therapy in nuclear medicine. Here, the CL for
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Delivery of DNA-Based Therapeutics for Treatment of Chronic Diseases Pharmaceutics (IF 5.4) Pub Date : 2024-04-13 Carleigh Sussman, Rachel A. Liberatore, Marek M. Drozdz
Gene therapy and its role in the medical field have evolved drastically in recent decades. Studies aim to define DNA-based medicine as well as encourage innovation and the further development of novel approaches. Gene therapy has been established as an alternative approach to treat a variety of diseases. Its range of mechanistic applicability is wide; gene therapy has the capacity to address the symptoms
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A Novel Class of Human ADAM8 Inhibitory Antibodies for Treatment of Triple-Negative Breast Cancer Pharmaceutics (IF 5.4) Pub Date : 2024-04-13 Nora D. Mineva, Stefania Pianetti, Sonia G. Das, Srimathi Srinivasan, Nicolas M. Billiald, Gail E. Sonenshein
New targeted treatments are urgently needed to improve triple-negative breast cancer (TNBC) patient survival. Previously, we identified the cell surface protein A Disintegrin And Metalloprotease 8 (ADAM8) as a driver of TNBC tumor growth and spread via its metalloproteinase and disintegrin (MP and DI) domains. In proof-of-concept studies, we demonstrated that a monoclonal antibody (mAb) that simultaneously
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First Generic Teriparatide: Structural and Biological Sameness to Its Reference Medicinal Product Pharmaceutics (IF 5.4) Pub Date : 2024-04-13 Jimena Fernández-Carneado, Mariona Vallès-Miret, Sílvia Arrastia-Casado, Ana Almazán-Moga, Maria J. Macias, Pau Martin-Malpartida, Marta Vilaseca, Mireia Díaz-Lobo, Mayte Vazquez, Rosa M. Sanahuja, Gemma Gambús, Berta Ponsati
Teriparatide is an anabolic peptide drug indicated for the treatment of osteoporosis. Recombinant teriparatide was first approved in 2002 and has since been followed by patent-free alternatives under biosimilar or hybrid regulatory application. The aim of this study is to demonstrate the essential similarity between synthetic teriparatide BGW and the reference medicinal product (RMP), and thus to ensure
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In Situ Preparation of Tannic Acid-Modified Poly(N-isopropylacrylamide) Hydrogel Coatings for Boosting Cell Response Pharmaceutics (IF 5.4) Pub Date : 2024-04-13 Jufei Xu, Xiangzhe Liu, Pengpeng Liang, Hailong Yuan, Tianyou Yang
The improvement of the capability of poly(N-isopropylacrylamide) (PNIPAAm) hydrogel coating in cell adhesion and detachment is critical to efficiently prepare cell sheets applied in cellular therapies and tissue engineering. To enhance cell response on the surface, the amine group-modified PNIPAAm (PNIPAAm-APTES) nanohydrogels were synthesized and deposited spontaneously on tannic acid (TA)-modified
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Non-Invasive Delivery of Negatively Charged Nanobodies by Anodal Iontophoresis: When Electroosmosis Dominates Electromigration Pharmaceutics (IF 5.4) Pub Date : 2024-04-13 Phedra Firdaws Sahraoui, Oscar Vadas, Yogeshvar N. Kalia
Iontophoresis enables the non-invasive transdermal delivery of moderately-sized proteins and the needle-free cutaneous delivery of antibodies. However, simple descriptors of protein characteristics cannot accurately predict the feasibility of iontophoretic transport. This study investigated the cathodal and anodal iontophoretic transport of the negatively charged M7D12H nanobody and a series of negatively
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An Integrative Study of Scrophularia takesimensis Nakai in an Ovalbumin-Induced Murine Model of Asthma: The Effect on T Helper 2 Cell Activation Pharmaceutics (IF 5.4) Pub Date : 2024-04-12 Yun-Soo Seo, Jun-Ho Song, Hyo Seon Kim, Hyeon Hwa Nam, Sungyu Yang, Goya Choi, Sung-Wook Chae, Jeongmin Lee, Bokyung Jung, Joong-Sun Kim, Inkyu Park
Scrophularia have traditionally been used as herbal medicines to treat neuritis, sore throats, and laryngitis. In particular, S. takesimensis, a Korean endemic species with restricted distribution on Ulleung Island, holds significant resource and genetic value. However, its pharmacological properties have not been thoroughly evaluated. Thus, we provide detailed morphological characteristics and genomic
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Technological Functionalisation of Microencapsulated Genistein and Daidzein Delivery Systems Soluble in the Stomach and Intestines Pharmaceutics (IF 5.4) Pub Date : 2024-04-12 Jurga Andreja Kazlauskaite, Inga Matulyte, Mindaugas Marksa, Jurga Bernatoniene
Encapsulating antioxidant-rich plant extracts, such as those found in red clover, within microcapsules helps protect them from degradation, thus improving stability, shelf life, and effectiveness. This study aimed to develop a microencapsulation delivery system using chitosan and alginate for microcapsules that dissolve in both the stomach and intestines, with the use of natural and synthetic emulsifiers
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Cell Membrane-Coated Biomimetic Nanoparticles in Cancer Treatment Pharmaceutics (IF 5.4) Pub Date : 2024-04-12 Shu Zhang, Xiaojuan Zhang, Huan Gao, Xiaoqin Zhang, Lidan Sun, Yueyan Huang, Jie Zhang, Baoyue Ding
Nanoparticle-based drug delivery systems hold promise for cancer treatment by enhancing the solubility and stability of anti-tumor drugs. Nonetheless, the challenges of inadequate targeting and limited biocompatibility persist. In recent years, cell membrane nano-biomimetic drug delivery systems have emerged as a focal point of research and development, due to their exceptional traits, including precise
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Molecular Ballet: Investigating the Complex Interaction between Self-Assembling Dendrimers and Human Serum Albumin via Computational and Experimental Methods Pharmaceutics (IF 5.4) Pub Date : 2024-04-12 Gabriele Cavalieri, Domenico Marson, Nicoletta Giurgevich, Rachele Valeri, Fulvia Felluga, Erik Laurini, Sabrina Pricl
Dendrimers, intricate macromolecules with highly branched nanostructures, offer unique attributes including precise control over size, shape, and functionality, making them promising candidates for a wide range of biomedical applications. The exploration of their interaction with biological environments, particularly human serum albumin (HSA), holds significant importance for biomedical utilization
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Iron Oxide Nanoparticles: Selectively Targeting Melanoma Cells In Vitro by Inducing DNA Damage via H2AX Phosphorylation and Hindering Proliferation through ERK Dephosphorylation Pharmaceutics (IF 5.4) Pub Date : 2024-04-11 Danai E. Prokopiou, Anastasia Chillà, Francesca Margheri, Gabriella Fibbi, Anna Laurenzana, Eleni K. Efthimiadou
This study investigates the distinctive characteristics of iron oxide magnetic nanoparticles (mNPs) and their potential application in cancer therapy, focusing on melanoma. Three types of mNPs, pre-validated for safety, underwent molecular analysis to uncover the activated signaling pathways in melanoma cells. Using the Western blot technique, the study revealed that mNPs induce cytotoxicity, hinder
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Mirk/Dyrk1B Kinase Inhibitors in Targeted Cancer Therapy Pharmaceutics (IF 5.4) Pub Date : 2024-04-11 Nikolaos Kokkorakis, Marios Zouridakis, Maria Gaitanou
During the last years, there has been an increased effort in the discovery of selective and potent kinase inhibitors for targeted cancer therapy. Kinase inhibitors exhibit less toxicity compared to conventional chemotherapy, and several have entered the market. Mirk/Dyrk1B kinase is a promising pharmacological target in cancer since it is overexpressed in many tumors, and its overexpression is correlated
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Progress in the Use of Hydrogels for Antioxidant Delivery in Skin Wounds Pharmaceutics (IF 5.4) Pub Date : 2024-04-10 Lidia Maeso, Pablo Edmundo Antezana, Ailen Gala Hvozda Arana, Pablo Andrés Evelson, Gorka Orive, Martín Federico Desimone
The skin is the largest organ of the body, and it acts as a protective barrier against external factors. Chronic wounds affect millions of people worldwide and are associated with significant morbidity and reduced quality of life. One of the main factors involved in delayed wound healing is oxidative injury, which is triggered by the overproduction of reactive oxygen species. Oxidative stress has been
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The Antimicrobial Potency of Mesoporous Silica Nanoparticles Loaded with Melissa officinalis Extract Pharmaceutics (IF 5.4) Pub Date : 2024-04-10 Gabriela Petrișor, Ludmila Motelica, Roxana Doina Trușcǎ, Andreea-Luiza Mȋrț, Gabriel Vasilievici, Justinian-Andrei Tomescu, Cristina Manea, Andreea Ștefania Dumbravǎ, Viorica Maria Corbu, Irina Gheorghe-Barbu, Denisa Ficai, Ovidiu-Cristian Oprea, Bogdan-Ștefan Vasile, Anton Ficai, Anca Daniela Raiciu
Melissa officinalis is an important medicinal plant that is used and studied intensively due to its numerous pharmacological effects. This plant has numerous active compounds with biomedical potential; some are volatile, while others are sensitive to heat or oxygen. Therefore, to increase stability and prolong biological activities, the natural extract can be loaded into various nanostructured systems