Pharmaceuticals最新文献

{"title":"Discovering New Tyrosinase Inhibitors by Using In Silico Modelling, Molecular Docking, and Molecular Dynamics.","authors":"Kevin A OréMaldonado, Sebastián A Cuesta, José R Mora, Marcos A Loroño, José L Paz","doi":"10.3390/ph18030418","DOIUrl":"10.3390/ph18030418","url":null,"abstract":"<p><p><b>Background/Objectives:</b> This study was used in silico modelling to search for potential tyrosinase protein inhibitors from a database of different core structures for IC₅₀ prediction. <b>Methods</b>: Four machine learning algorithms and topographical descriptors were tested for model construction. <b>Results</b>: A model based on multiple linear regression was the most robust, with only six descriptors, and validated by the Tropsha test with statistical parameters R² = 0.8687, Q²_LOO = 0.8030, and Q²_ext = 0.9151. From the screening of FDA-approved drugs and natural products, the pIC₅₀ values for 15,424 structures were calculated. The applicability domain analysis covered 100% of the external dataset and 71.22% and 73.26% of the two screening datasets. Fifteen candidates with pIC₅₀ above 7.6 were identified, with five structures proposed as potential tyrosinase enzyme inhibitors, which underwent ADME analysis. <b>Conclusions</b>: The molecular docking analysis was performed for the dataset used in the training-test process and for the fifteen structures from the screening dataset with potential pharmaceutical tyrosinase inhibition, followed by molecular dynamics studies for the top five candidates with the highest predicted pIC₅₀ values. The new use of these five candidates in tyrosinase inhibition is highlighted based on their promising application in melanoma treatment.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 3","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11946302/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143721083","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Enhanced Intranasal Delivery of Atorvastatin via Superparamagnetic Iron-Oxide-Loaded Nanocarriers: Cytotoxicity and Inflammation Evaluation and In Vivo, In Silico, and Network Pharmacology Study for Targeting Glioblastoma Management.","authors":"Kristina Zarif Attalla, Doaa H Hassan, Mahmoud H Teaima, Carol Yousry, Mohamed A El-Nabarawi, Mohamed A Said, Sammar Fathy Elhabal","doi":"10.3390/ph18030421","DOIUrl":"10.3390/ph18030421","url":null,"abstract":"<p><p><b>Objective</b>: This study aims to develop an intranasal (IN) delivery system for glioblastoma multiforme (GBM) management using repurposed superparamagnetic iron-oxide (SPION) loaded with atorvastatin (ATO)-nanostructured lipid carrier (NLC). <b>Methods</b>: Emulsification and ultrasonication were used to formulate ATO-NLCs, and the best formula was loaded with SPION to make the final atorvastatin/superparamagnetic iron oxide-loaded nanostructured lipid carrier (ASN) formulation. Entrapment efficiency (EE%), particle size (PS), zeta potential (ZP), and drug release after 6 h (Q6h) were evaluated for NLCs. ASN was tested for cytotoxicity on T98G cancer cells, and the cell cycle was examined to determine cell death. Furthermore, the ability of the optimal formulation to suppress the levels of inflammatory biomarkers was investigated in Lipopolysaccharide (LPS)-induced inflammation. The brain-targeting behavior of IN-ASN was visualized in rabbits via confocal laser scanning microscopy (CLSM). <b>Results</b>: The optimum NLC exhibited a spherical shape, EE% of 84.0 ± 0.67%, PS of 282.50 ± 0.51 nm, ZP of -18.40 ± 0.15 mV, and Q6h of 89.23%. The cytotoxicity of ASN against cancer cells was 4.4-fold higher than ATO suspension, with a 1.3-fold increment in cell apoptosis. ASN showed significantly reduced pro-inflammatory biomarkers (IL-β, IL-6, TNF-α, TLR4, NF-қB), whereas CLSM revealed enhanced brain delivery with no observed histopathological nasal irritation. The in silico analysis demonstrated enhanced ATO-ADME (absorption, distribution, metabolism, and excretion) properties, while the network pharmacology study identified 10 target GBM genes, among which MAPK3 was the most prominent with a good binding score as elucidated by the simulated docking study. <b>Conclusions</b>: These findings may present ATO/SPION-NLCs as significant evidence for repurposing atorvastatin in the treatment of glioblastoma multiforme.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 3","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11944838/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143720360","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Unraveling the Neuropharmacological Properties of <i>Lippia alba:</i> A Scientometric Approach.","authors":"Pedro I C Silva, Lucas V P S Pantoja, Brenda C Conceição, Marta E O Barbosa, Luiza F R Soares, Rui Daniel Prediger, Enéas A Fontes-Júnior, Jofre J S Freitas, Cristiane S F Maia","doi":"10.3390/ph18030420","DOIUrl":"10.3390/ph18030420","url":null,"abstract":"<p><p><i>Lippia alba</i> (Verbenaceae) is popularly known as lemon balm or false melissa and is one of the most widely used plants in traditional medicine in the Amazon region. In this study, we conducted a comprehensive bibliometric analysis, with conventional metrics associated with a critical review based on the neuropharmacological activities, to identify potential medical applications and also gaps in knowledge that require further investigation. Fifty-two articles were included according to the eligibility criteria. In the country analysis, Brazil emerged as the main contributor to research with the highest number of publications and citations. Notably, nine of the ten main research institutions are Brazilian, with the Universidade Federal de Santa Maria standing out with 761 citations. The keywords \"anesthesia\", \"<i>Lippia alba</i>\", and \"essential oil\" were the most frequent, highlighting their importance in this field. Essential oils are the most common type of extraction, which linalool, citral, geraniol, carvone, and limonene were the main constituents identified. According to the type of study, preclinical studies presented the highest frequency, primarily through fish experimental models. The main neuropharmacological activities identified were sedative-anesthetic, anxiolytic, anticonvulsant, and analgesic, with mechanisms of action via the GABAergic pathway. This bibliometric review provided new evidence reinforcing the potential of <i>L. alba</i> as a promising alternative for the treatment of neuropsychiatric disorders. It also highlighted existing knowledge gaps, mainly related to the comparison of the actions of the different chemotypes of the species and the investigation of the mechanisms underlying their neuropharmacological properties. Additionally, there is a lack of knowledge in other emerging areas related to the central nervous system, such as mood and cognitive disorders.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 3","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11945933/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143721208","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Assessing the Antibacterial Potential and Biofilm Inhibition Capability of Atorvastatin-Loaded Nanostructured Lipid Carriers via Crystal Violet Assay.","authors":"Njoud Altuwaijri, Rawan Fitaihi, Fai A Alkathiri, Sarah I Bukhari, Alanoud M Altalal, Alyaa Alsalhi, Lama Alsulaiman, Aljawhara O Alomran, Noura S Aldosari, Safa A Alqhafi, Majd Alhamdan, Rihaf Alfaraj","doi":"10.3390/ph18030417","DOIUrl":"10.3390/ph18030417","url":null,"abstract":"<p><p><b>Background/Objectives</b>: Atorvastatin (ATR), an antihyperlipidemic drug with a potential antibacterial effect, was investigated in this study. Like other statins, ATR has been repurposed for several uses, ranging from anti-inflammatory to antimicrobial applications, and has demonstrated successful results. However, the efficacy of ATR is limited by its low solubility, indicating an opportunity for its encapsulation in a nanotechnology-based drug delivery system. <b>Methods</b>: Nanostructured lipid carrier (NLC) formulations were prepared using high-pressure homogenization and ultrasonication. The formulations were characterized, including their particle size, polydispersity index, zeta potential, encapsulation efficiency, and in vitro release. Antibacterial activity against methicillin-resistant <i>Staphylococcus aureus</i> (MRSA), <i>Escherichia coli</i> (<i>E. coli</i>), and <i>Staphylococcus aureus</i> (<i>S. aureus</i>) was evaluated using the growth curve (bacterial growth over time) and well diffusion methods (zone of inhibition and minimum inhibitory concentration (MIC) determination). The crystal violet assay was employed to assess biofilm inhibition. <b>Results</b>: The NLC formulations were optimized, and the size and zeta potential of the blank nanoparticles were 130 ± 8.39 nm and -35 ± 0.5 mV, respectively. In comparison, the encapsulated NLCs had a size of 142 ± 52.20 nm and a zeta potential of -31 ± 1.41 mV. The average encapsulation efficiency was 94%, and 70% of the drug was released after 24 h. The ATR-loaded NLCs showed significantly enhanced antibacterial activity by reducing the minimum inhibitory concentration by 2.5-fold for <i>E. coli</i>, 1.8-fold for <i>S. aureus</i>, and 1.4-fold for MRSA, and promoting more effective bacterial growth inhibition. Notably, biofilm inhibition was significantly improved with ATR-NLCs, achieving 80% inhibition for <i>S. aureus</i>, 40% for <i>E. coli</i>, and 30% for MRSA, compared to free ATR (<i>p</i> < 0.001). These findings suggest that NLC encapsulation enhances ATR's antimicrobial efficacy and biofilm suppression. <b>Conclusions</b>: This study identified NLCs as successful carriers of ATR, significantly enhancing its antibacterial efficacy and biofilm inhibition capabilities. This formulation, which shows antimicrobial potential against both Gram-positive and Gram-negative bacteria, should be further studied and developed against different resistant microbial strains.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 3","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-03-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11944405/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143721091","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis, Molecular Simulation, DFT, and Kinetic Study of Imidazotriazole-Based Thiazolidinone as Dual Inhibitor of Acetylcholinesterase and Butyrylcholinesterase Enzymes.","authors":"Manal M Khowdiary, Shoaib Khan, Tayyiaba Iqbal, Wajid Rehman, Muhammad Bilal Khan, Mujaddad Ur Rehman, Zanib Fiaz, Hakimullah","doi":"10.3390/ph18030415","DOIUrl":"10.3390/ph18030415","url":null,"abstract":"<p><p><b>Background:</b> Alzheimer's disease is a complex and multifactorial brain disorder characterized by gradual memory impairment, cognitive disturbance, and severe dementia, and, ultimately, its progression leads to patient death. This research work presents the design, synthesis, and characterization of novel imidazotriazole-based thiazolidinone derivatives (<b>1</b>-<b>14</b>), displaying promising anti-Alzheimer's activity. <b>Methods:</b> These derivatives were synthesized by using 1<i>H</i>-imidazole-2-thiol as a starting reagent. Structural characterization was accomplished by ¹³C-NMR and ¹H-NMR, while the molecular weight was confirmed by HREI-MS. These compounds were investigated for their anti-Alzheimer's potential under an in vitro analysis. <b>Results:</b> These compounds showed a significant to moderate biological potential against AChE and BChE in comparison to donepezil (IC₅₀ = 8.50 µM and 8.90 µM against AChE and BuChE), used as a reference drug. Among these compounds, analog <b>10</b> with IC₅₀ values of 6.70 µM and 7.10 µM against AChE and BuChE emerged as the lead compound of the series with promising biological efficacy against targeted enzymes. Molecular docking revealed the interactive nature of active ligands against target enzymes. These compounds were also assessed under dynamic conditions to examine the structural deviation and conformational changes in a protein complex structure. DFT calculations provided the relative stability and reactivity of the lead compounds. An ADMET analysis showed that these compounds have no toxicological profile. <b>Conclusions:</b> This research study paves the way for the further development and optimization of novel and selective imidazotriazole-based thiazolidinone inhibitors as potent anti-Alzheimer's agents.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 3","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-03-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11944621/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143721244","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Mixture Containing 5% Polysaccharide Extract of <i>Cerioporus squamosus</i> (Huds.) Quélet, 5% Dexpanthenol, and 0.2% Hyaluronic Acid Shows In Vitro and In Vivo Wound Healing Properties.","authors":"Jovana D Petrović, Tamara A Carević Milićević, Jasmina M Glamočlija, Jelena B Kulaš, Ivana I Mirkov","doi":"10.3390/ph18030416","DOIUrl":"10.3390/ph18030416","url":null,"abstract":"<p><p><b>Background:</b> This study explores wound healing and the antimicrobial potential of a natural formulation containing a polysaccharide extract from <i>Cerioporus squamosus</i>, hyaluronic acid, and dexpanthenol. <b>Methods:</b> Wound healing effects were assessed using HaCaT keratinocytes, while antimicrobial activity was evaluated against human skin pathogens using a microdilution assay. In vitro cytotoxicity tests ensured formulation safety, whereas in vivo wound healing was further investigated using an animal model. Gene expression analysis was performed to assess the molecular mechanisms involved. <b>Results:</b> The unique glucan composition of <i>C. squamosus</i> (15.38% α-glucans and 7.91% β-glucans) deviated from typical mushroom polysaccharide profiles, warranting further exploration of its bioactivity. In vitro mushroom polysaccharides promoted 25.35% wound closure after 24 hours, while the three-component formulation achieved 35.81% closure. Antibacterial activity showed a minimum inhibitory concentration (MIC) of 0.44-1.75 mg/mL and minimum bactericidal concentration (MBCs) of 0.88-3.50 mg/mL, while antifungal activity ranged from 0.22 to 0.44 mg/mL (MICs) and 0.44 to 0.88 mg/mL (minimum fungicidal concentration-MFC). In vivo data showed that 60% of treated wounds fully closed by day 11, despite no statistically significant difference from the control. However, gene expression analysis highlighted VEGF and collagen upregulation, indicating an enhancement of wound healing on a molecular level. <b>Conclusions:</b> The novel three-component formulation demonstrated consistent wound healing and antimicrobial properties, supporting its potential as a safe and effective treatment for chronic and acute wounds.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 3","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-03-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11946009/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143721145","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"From Traditional Efficacy to Drug Design: A Review of Astragali Radix.","authors":"Xiaojie Jin, Huijuan Zhang, Xiaorong Xie, Min Zhang, Ruifeng Wang, Hao Liu, Xinyu Wang, Jiao Wang, Dangui Li, Yaling Li, Weiwei Xue, Jintian Li, Jianxin He, Yongqi Liu, Juan Yao","doi":"10.3390/ph18030413","DOIUrl":"10.3390/ph18030413","url":null,"abstract":"<p><p>Astragali Radix (AR), a traditional Chinese herbal medicine, is derived from the dried roots of <i>Astragalus membranaceus</i> (Fisch.) Bge. var. <i>mongholicus</i> (Bge.) Hsiao (<i>A. membranaceus</i> var. mongholicus, AMM) or <i>Astragalus membranaceus</i> (Fisch.) Bge (A. <i>membranaceus</i>, AM). According to traditional Chinese medicine (TCM) theory, AR is believed to tonify qi, elevate yang, consolidate the body's surface to reduce sweating, promote diuresis and reduce swelling, generate body fluids, and nourish the blood. It has been widely used to treat general weakness and chronic illnesses and to improve overall vitality. Extensive research has identified various medicinal properties of AR, including anti-tumor, antioxidant, cardiovascular-protective, immunomodulatory, anti-inflammatory, anti-diabetic, and neuroprotective effects. With advancements in technology, methods such as computer-aided drug design (CADD) and artificial intelligence (AI) are increasingly being applied to the development of TCM. This review summarizes the progress of research on AR over the past decades, providing a comprehensive overview of its traditional efficacy, botanical characteristics, drug design and distribution, chemical constituents, and phytochemistry. This review aims to enhance researchers' understanding of AR and its pharmaceutical potential, thereby facilitating further development and utilization.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 3","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-03-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11945149/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143721093","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Evaluating the Use of Inhaled Budesonide and Ipratropium Bromide Combination in Patients at High Risk of Acute Respiratory Distress Syndrome Development: A Randomized Controlled Trial.","authors":"Hebatallah Ahmed Mohamed Moustafa, Faten H Elbery, Ahmad Z Al Meslamani, Sherouk M Okda, Bshra A Alsfouk, Amira B Kassem","doi":"10.3390/ph18030412","DOIUrl":"10.3390/ph18030412","url":null,"abstract":"<p><p><b>Objectives:</b> There is a scarcity of pharmacological treatments that efficiently address lung injury in individuals experiencing acute respiratory distress syndrome (ARDS). Early inhaled corticosteroids and ipratropium may reduce pulmonary inflammation and injury of the lungs, minimizing the risk of ARDS. <b>Method:</b> This is a double-blinded randomized control trial conducted on patients at risk of ARDS. Patients were randomly allocated into two groups; the intervention group (63 patients) were administered aerosolized budesonide and ipratropium bromide, and the control group (56) were administered a placebo every eight hours for five days. Alteration in oxygen saturation divided by inspired oxygen (Fio2) (S/F) after five days was the primary outcome. Secondary outcomes included ARDS occurrence, mechanical ventilation (MV) requirement, hospital stay duration, and mortality rates. <b>Results:</b> Of the 604 screened, only 119 patients were included. The intervention group (63 patients) S/F ratio recovered versus the fall of the control group. Both groups had similar organ dysfunction and 28-day mortality. The intervention group had significantly (<i>p</i> < 0.001) fewer cases developing ARDS (9.5%) and MV (9.5%) than the control group (46.4% and 35.7%, respectively). <b>Conclusions:</b> The administration of inhaled budesonide and ipratropium bromide improved oxygenation, as assessed by the S/F ratio, and significantly reduced the rate of ARDS development and the requirement of MV versus the control group. Larger multi-center trials including diverse patient populations are needed to validate these results.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 3","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-03-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11945358/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143720571","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Green Tea: A Novel Perspective on the Traditional Plant's Potential in Managing Periodontal Diseases.","authors":"Magdalena Paczkowska-Walendowska, Jan Grzegorzewski, Jakub Kwiatek, Marta Leśna, Judyta Cielecka-Piontek","doi":"10.3390/ph18030409","DOIUrl":"10.3390/ph18030409","url":null,"abstract":"<p><p>Green tea (<i>Camellia sinensis</i>) exhibits significant potential in oral health due to its antioxidant, anti-inflammatory, and antimicrobial properties. This review explores its role in managing periodontal disease, a common condition characterized by inflammation, microbial imbalances, and tissue destruction. The primary bioactive components, particularly epigallocatechin-3-gallate (EGCG), contribute to green tea's therapeutic effects by inhibiting bacterial adhesion, modulating inflammatory pathways, and reducing oxidative stress. Clinical studies suggest green tea improves periodontal health by reducing pocket depth, inflammation, and bleeding. It can serve as an adjunct to conventional therapies, including scaling and root planing, and be incorporated into oral care products such as mouthwashes and dentifrices. Furthermore, green tea presents a natural alternative to chemical agents like chlorhexidine, potentially mitigating side effects and addressing concerns about antibiotic resistance. However, its efficacy remains moderate compared to established treatments, highlighting the need for further research to optimize its formulation and therapeutic applications. Green tea represents a sustainable and biocompatible approach to periodontal therapy, supporting its integration into preventive and therapeutic oral health strategies.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 3","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-03-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11946246/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143721061","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Ceftriaxone-Loaded Liposomal Nanoparticles for Pulmonary Delivery Against Lower Respiratory Tract Infections: Development and Characterization.","authors":"Vijay Kumar Panthi, Kathryn E Fairfull-Smith, Timothy J Wells, Tony Wang, Nazrul Islam","doi":"10.3390/ph18030414","DOIUrl":"10.3390/ph18030414","url":null,"abstract":"<p><p><b>Background/Objectives:</b> Herein, we demonstrate the development and characterization of ceftriaxone (CTX)-loaded liposomal nanoparticles (NPs) intended to be applicable to the management of lower respiratory tract infections (LRTIs) associated with resistant bacteria. <b>Methods:</b> The CTX-loaded liposomal NPs were fabricated by a thin film hydration approach. <b>Results:</b> The particle size of the NPs, determined by a Zetasizer, was within the range of 90-536 nm. Microscopic examination by transmission electron microscopy (TEM) and scanning electron microscopy (SEM) revealed that particles are spherical in shape and have retained their original morphology even after freeze-drying. Attenuated total reflection-Fourier transform infrared (ATR-FTIR), differential scanning calorimetry (DSC), thermogravimetric (TG), and powder X-ray diffraction (PXRD) spectra exhibited that CTX is incorporated into the liposomes with no possible interaction between drug and excipients. The formation of the CTX-loaded liposomal NPs was dependent on the concentrations of phospholipids, cholesterol and mannitol; however, no considerable differences were observed in entrapment efficiency and loading capacity of CTX formulations (F6-F10). Using a twin-stage impinger (TSI), the in vitro aerosolization of the formulations were carried out at a flow rate of 60 ± 5 L/min and CTX was determined by a validated HPLC method and the prepared liposomal formulations produced promising fine particle fraction (FPF) between 47 and 62%. The prepared formulation (F6) showed prolonged CTX release of 94.0% ± 5.7 and 95.9% ± 3.9 at 24 h and 48 h, respectively. The drug release followed the Hixon-Crowell model, with CTX being transported through Fickian diffusion. <b>Conclusions:</b> These results highlight the prepared CTX-loaded inhaled liposomal formulation would be suitable for pulmonary delivery and extend the successful antibiotic delivery strategies for the effective management of LRTIs.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 3","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-03-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11945751/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143721130","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}