Pharmaceutics最新文献

{"title":"Intravenous Administration of sRNA Nanoparticles for Treatment of Osteoporosis in Mice.","authors":"Xuemeng Mu, Xinyi Du, Huitian Han, Fei Liu, Zhifa Zheng, Jing Hao, Lijin Liu, Su Liu, Ze Wei, Changfa Huang, Annan Liang, Wei Zou, Lina Zhao, Zhihong Wu, Jia Zhang","doi":"10.3390/pharmaceutics17060789","DOIUrl":"10.3390/pharmaceutics17060789","url":null,"abstract":"<p><p><b>Background</b>: With the intensification of population aging, osteoporosis has become one of the significant public health issues affecting human health. Currently available medications for treating osteoporosis are associated with various adverse effects and resistance issues. Oligonucleotide drugs show great potential. Effective delivery systems are essential to enhance the stability, bioavailability, and targeting of sRNA drugs. Lipid nanoparticles (LNPs) show promise as alternative osteoporosis therapeutics. This study explores the potential of LNPs as an effective delivery system to treat osteoporosis. <b>Methods</b>: LNPs were prepared using microfluidic techniques with varying lipid compositions, and characterized in terms of size, zeta potential, and entrapment efficiency (EE%). Dynamic light scattering (DLS) was employed to determine the size of the LNPs. The zeta potential was measured using electrophoretic light scattering. The pharmacodynamic effects and safety were then evaluated in a mouse model through intravenous administration. <b>Results</b>: Several lipid nanoparticle (LNP) formulations with different nitrogen/phosphorus ratios and different DMG-PEG2000 ratios were examined, and a lead candidate that supports delivery of sRNA in animal models of osteoporosis was identified. In OVX mice, LNP-sRNA significantly improved bone mineral density (BMD), trabecular microstructure, and biomechanical strength. Safety assessments revealed no systemic toxicity. It is shown that the optimized LNPs can serve as a promising delivery system to mediate sRNA delivery to bone tissue. <b>Conclusions</b>: After comparison of in vitro and in vivo properties, the optimized LNPs demonstrated good comprehensive performance as a delivery system for osteoporosis treatment. These results highlight the potential of the optimized LNPs as an ideal delivery system for osteoporosis, offering improved therapeutic efficacy and reduced systemic side effects.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 6","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12196915/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144507370","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":"Development of Ethosomes for the Topical Treatment of Androgenic Alopecia: Ethanol Effect on Dutasteride Targeting to the Hair Follicles.","authors":"Jayanaraian F M Andrade, Rafael V Rocho, Breno N Matos, Geisa N Barbalho, Kariane M Nunes, Marcilio Cunha-Filho, Guilherme M Gelfuso, Tais Gratieri","doi":"10.3390/pharmaceutics17060786","DOIUrl":"10.3390/pharmaceutics17060786","url":null,"abstract":"<p><p><b>Background/Objectives:</b> Treatment options for androgenic alopecia are still very limited and lack long-term efficacy. Dutasteride (DUT) has gained interest as a potent inhibitor of 5α-reductase, allowing for spaced applications, but DUT oral intake can cause serious adverse effects. Herein, we developed, characterized, and assessed the potential of DUT-loaded ethosomes with increasing ethanolic concentrations for hair follicle (HF) targeting to treat androgenic alopecia, hypothesizing that ethanol's interaction with HFs' sebum might increase DUT targeting to the HFs. <b>Methods:</b> Ethosomes were obtained using the water-dropping method. After a hydrodynamic size screening, a 30% ethanol concentration was fixed. Ethosomes with 30% ethanol were also prepared and had their ethanolic content removed by rotary evaporation for the evaluation of ethanol in targeting DUT to the HFs. The targeting factor (Tf) was calculated as the ratio between the DUT amount in HFs and the total DUT amount recovered from all skin layers after in vitro porcine skin penetration tests for 12 and 24 h. <b>Results:</b> The ethanolic concentration affected the vesicles' size and the targeting potential. While the dried ethosomes could not increase DUT accumulation in the HFs at both time points (Tf: 0.27 in 12 h and Tf: 0.28 in 24 h), the presence of 30% ethanol in the vesicles increased the Tf from 0.28 (12 h) to 0.34 (24 h), significantly superior (<i>p</i> < 0.05) than the dried ethosome and control (Tf: 0.24) in 24 h. <b>Conclusion:</b> Ethosomes with a 30% ethanolic concentration were slightly more efficient in targeting HFs for dutasteride delivery.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 6","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12196546/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144507384","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":"DNA Tweezers with Replaceable Clamps for the Targeted Degradation of Cell Membrane Proteins.","authors":"Yang Sun, Yichen Huang, Daiquan Chen, Shangjiu Hu, Tao Pan, Yuanding Liu, Ruowen Wang, Weihong Tan","doi":"10.3390/pharmaceutics17060785","DOIUrl":"10.3390/pharmaceutics17060785","url":null,"abstract":"<p><p><b>Background</b>: Cell membrane proteins play crucial roles in signal transduction and nutrient transport. Many membrane proteins are reportedly overexpressed in cancer cells, which is closely related to cancer progression. The targeted degradation of these membrane proteins has been demonstrated to be a promising strategy for tumor treatment. Several strategies using aptamers to mediate membrane protein lysis, such as lysosomal-mediated lysis and proteasome-mediated lysis, have been reported, but their efficiency is limited by the binding affinity of the aptamer to a single target. <b>Methods</b>: We constructed DNA tweezers with replaceable clamps, which can lyse different proteins upon clamp replacement. Moreover, the clamp improved the degradation efficiency of the target proteins by enhancing the specificity and improving the binding affinity. <b>Results</b>: Lysis was verified in different tumor cell lines and the antitumor activity was confirmed in zebrafish. <b>Conclusions</b>: Overall, these DNA tweezers improve the efficiency of the targeted delivery of functional nucleic acids, provide an efficient and versatile strategy for the degradation of disease-causing proteins, and expand the approach to antitumor therapy.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 6","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12197088/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144507385","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":"Incorporation of Mometasone Furoate into a Cyclodextrin Metal-Organic Framework to Optimize Nasal Administration.","authors":"Jie Li, Yuhua Guo, Yan Liu, Qingfang Gao, Siwen Wang, Li Wu, Caifen Wang, Xiaohong Ren, Jiwen Zhang","doi":"10.3390/pharmaceutics17060788","DOIUrl":"10.3390/pharmaceutics17060788","url":null,"abstract":"<p><p><b>Background/Objectives:</b> Mometasone furoate (MF) is a topical corticosteroid used to reduce allergic and inflammation symptoms. In this study, MF was incorporated into the hydrophobic cavities of γ-cyclodextrin metal-organic frameworks (CD-MOFs) to prepare MF@MOF powders for nasal delivery. <b>Methods</b>: MF@MOF particles were characterized by scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), and thermogravimetry. A transparent biomimetic model of the human nasal cavity was produced by 3D printing and used to evaluate intra-nasal depositions patterns. <b>Results</b>: Drug loading was optimized by incubating MF with a CD-MOF at a ratio of 4% for 1 h at 40 °C, and the cubic morphology and particle size of the nanoparticles were not altered using an incubation method. PXRD and FTIR analyses confirmed the successful loading of MF into the CD-MOF. Using a 3D biomimetic nasal cavity model, a 30° administration angle was found to result in reduced drug accumulation in the nasal vestibule and enhanced deposition in the respiratory and olfactory regions, compared with administration at 45°. Approximately 51% of the drug reached the respiratory zone in the model of the nasal cavity from male subjects, while almost 60% of the drug reached this zone in the model associated with female subjects. Compared with nasal sprays, nasal powder sprays had less deposition in the nasal vestibule and more deposits in the middle and inferior nasal concha. <b>Conclusions</b>: MF@MOF is suitable for intranasal administration. Delivery of MF as a nasal powder shows potential in the treatment of chronic rhinosinusitis.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 6","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12197233/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144507367","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":"Metronidazole Suspension for Paediatric Use in Developing Countries: Formulation, Quality, and Stability.","authors":"Francesca Baratta, Chiara Zingarelli, Federica Fanton, Editson Lamy, Gaetano Di Lascio, Paola Brusa","doi":"10.3390/pharmaceutics17060787","DOIUrl":"10.3390/pharmaceutics17060787","url":null,"abstract":"<p><p><b>Background/Objectives.</b> The paediatric population is a heterogenous group that is known to be a therapeutic orphan despite the recent incentives to promote the development of children's formulations. Especially in low and middle-income countries, there is still a worldwide shortfall for the treatment and prevention of a variety of paediatric conditions. In this context, we developed a formulation specifically intended to administer metronidazole to paediatric patients using basic and low-cost excipients and with a simple set-up method. <b>Methods</b>. Various mixtures of excipients were prepared to obtain a suitable metronidazole liquid formulation at a concentration of 250 mg/5 mL. The best formula was tested for its quality and stability, assessing the uniformity of content, the pH, and the dispersion quality. We evaluated the stability of the preparation for 180 days at room temperature (25 +/- 2 °C), in a thermostatic oven (40 +/- 2 °C), and in a fridge (4 +/- 2 °C). <b>Results.</b> The tests performed gave excellent results. No variation greater than 10% was detected in the metronidazole concentration or in pH values after 180 days regardless of the temperature conditions during storage. Moreover, the microscope analysis confirmed the absence of significant differences over time. <b>Conclusions.</b> The results were consistent in different environmental conditions, ensuring the possibility of using the formulation even in those tropical countries where is not always possible to guarantee the conservation of medicines in controlled conditions. Moreover, the simple composition and easy preparation procedure make it possible to produce the suspension in any context, ensuring the quality of the finished product.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 6","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12196289/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144507424","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":"Exploring a Novel Anti-Inflammatory Therapy for Diabetic Retinopathy Based on Glyco-Zeolitic-Imidazolate Frameworks.","authors":"Elena Díaz-Paredes, Francisco Martín-Loro, Rocío Rodríguez-Marín, Laura Gómez-Jaramillo, Elena M Sánchez-Fernández, Carolina Carrillo-Carrión, Ana I Arroba","doi":"10.3390/pharmaceutics17060791","DOIUrl":"10.3390/pharmaceutics17060791","url":null,"abstract":"<p><p><b>Background/Objectives:</b> Diabetic retinopathy is an ocular disease caused by changes in the expression of inflammatory mediators and increased oxidative stress in the retina and is the leading cause of vision loss in diabetic patients. Currently, there is no treatment capable of reversing retinal damage, which represents a significant burden on the quality of life of patients. (1<i>R</i>)-1-Dodecylsulfonyl-5<i>N</i>,6<i>O</i>-oxomethylidenenojirimycin stands outs as a prototype of the sp²-iminoglycolipids family for its beneficial neuroprotective effect against this chronic eye disease. Critical issues related to the low solubility and bioavailability of this glycolipid in biological settings are overcome by its encapsulation in a Zeolitic-Imidazolate Framework (ZIF) structure, resulting in homogeneous and biocompatible GlycoZIF nanoparticles. Cell studies show an enhanced cellular uptake compared with the free glycolipid, and importantly, its bioactivity is preserved once released inside cells. <b>Methods:</b> Extensive in vitro and ex vivo assays with diabetic retinopathy models unveil the mechanistic pathways of the designed GlycoZIF. <b>Results:</b> A reduction in proinflammatory mediators, increased heme oxygenase-1 level, inhibition of NLRP3 inflammasome, and reduced reactive gliosis is shown. <b>Conclusions:</b> These findings demonstrate for the first time the potential of Glyco-modified ZIFs for the treatment of diabetes-related ocular problems by controlling the immune-mediated inflammatory response.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 6","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12196511/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144507390","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":"Hydroxypropyl Methylcellulose-A Key Excipient in Pharmaceutical Drug Delivery Systems.","authors":"Robert-Alexandru Vlad, Andrada Pintea, Cezara Pintea, Emőke-Margit Rédai, Paula Antonoaea, Magdalena Bîrsan, Adriana Ciurba","doi":"10.3390/pharmaceutics17060784","DOIUrl":"10.3390/pharmaceutics17060784","url":null,"abstract":"<p><p>Hydroxypropyl methylcellulose (Hypromellose, HPMC) is a well-known excipient used in the pharmaceutical and nutraceutical fields due to its versatile physicochemical properties. HPMC (derived from cellulose and obtained through etherification) varies in polymerization degree and viscosity, factors that both influence its functional applications. Usually, an increased polymerization degree implies a higher viscosity, depending also on the amount of polymer used. Hypromellose plays a crucial role in solid dosage forms, serving as a binder in the case of controlled-release tablets, a film-forming agent in the case of orodispersible films and mucoadhesive films, and a release modifier due to its presence in different polymerization degrees in the case of extended or modified release tablets. However, its compatibility with other excipients and the active ingredient must be carefully evaluated to prevent formulation challenges via several analytical methods such as differential scanned calorimetry (DSC), Fourier Transformed Infrared spectroscopy (FT-IR), X-Ray Particle Diffraction (XRPD), and Scanning Electron Microscopy (SEM). This review explores the physicochemical characteristics, and diverse applications of HPMC, emphasizing its significance in modern drug delivery systems.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 6","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12196896/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144507421","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":"Innovative Approaches in Cancer Treatment: Emphasizing the Role of Nanomaterials in Tyrosine Kinase Inhibition.","authors":"Antónia Kurillová, Libor Kvítek, Aleš Panáček","doi":"10.3390/pharmaceutics17060783","DOIUrl":"10.3390/pharmaceutics17060783","url":null,"abstract":"<p><p>Medical research is at the forefront of addressing pressing global challenges, including preventing and treating cardiovascular, autoimmune, and oncological diseases, neurodegenerative disorders, and the growing resistance of pathogens to antibiotics. Understanding the molecular mechanisms underlying these diseases, using advanced medical approaches and cutting-edge technologies, structure-based drug design, and personalized medicine, is critical for developing effective therapies, specifically anticancer treatments. <b>Background/Objectives</b>: One of the key drivers of cancer at the cellular level is the abnormal activity of protein enzymes, specifically serine, threonine, or tyrosine residues, through a process known as phosphorylation. While tyrosine kinase-mediated phosphorylation constitutes a minor fraction of total cellular phosphorylation, its dysregulation is critically linked to carcinogenesis and tumor progression. <b>Methods</b>: Small-molecule inhibitors, such as imatinib or erlotinib, are designed to halt this process, restoring cellular equilibrium and offering targeted therapeutic approaches. However, challenges persist, including frequent drug resistance and severe side effects associated with these therapies. Nanomedicine offers a transformative potential to overcome these limitations. <b>Results</b>: By leveraging the unique properties of nanomaterials, it is possible to achieve precise drug delivery, enhance accumulation at target sites, and improve therapeutic efficacy. Examples include nanoparticle-based delivery systems for TKIs and the combination of nanomaterials with photothermal or photodynamic therapies to enhance treatment effectiveness. Combining nanomedicine with traditional treatments holds promise and perspective for synergistic and more effective cancer management. <b>Conclusions</b>: This review delves into recent advances in understanding tyrosine kinase activity, the mechanisms of their inhibition, and the innovative integration of nanomedicine to revolutionize cancer treatment strategies.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 6","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12196280/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144507368","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":"Anxiolytic and Antidepressant Effects of Organic Polysulfide, Dimethyl Trisulfide Are Partly Mediated by the Transient Receptor Potential Ankyrin 1 Ion Channel in Mice.","authors":"Kitti Göntér, Viktória Kormos, Erika Pintér, Gábor Pozsgai","doi":"10.3390/pharmaceutics17060781","DOIUrl":"10.3390/pharmaceutics17060781","url":null,"abstract":"<p><p><b>Background/Objectives</b>: Dimethyl trisulfide (DMTS) is a naturally occurring polysulfide with known antioxidant and neuroprotective properties. DMTS is a lipophilic transient receptor potential ankyrin 1 (TRPA1) ligand that reaches the central nervous system (CNS). Its role in the CNS, particularly regarding depression-like behaviour, has yet to be explored. This study investigates the influence of DMTS on stress responses and whether this effect is mediated through the TRPA1 ion channel, known for its role in stress adaptation. Using a mouse model involving three-week exposure, we examined the impact of DMTS on depression-like behaviour and anxiety and identified the involved brain regions. <b>Methods</b>: Our methods involved testing both <i>Trpa1</i>-wild-type and gene-knockout mice under CUMS conditions and DMTS treatment. DMTS was administered intraperitoneally at a dose of 30 mg/kg on days 16 and 20 of the 21-day CUMS protocol-in hourly injections seven times to ensure sustained exposure. Various behavioural assessments-including the open field, marble burying, tail suspension, forced swim, and sucrose preference tests-were performed to evaluate anxiety and depression-like behaviour. Additionally, we measured body weight changes and the relative weights of the thymus and adrenal glands, while serum levels of corticosterone and adrenocorticotropic hormone were quantified via ELISA. FOSB (FBJ murine osteosarcoma viral oncogene homolog B) immunohistochemistry was utilised to assess chronic neuronal activation in stress-relevant brain areas. <b>Results</b>: Results showed that CUMS induces depression-like behaviour, with the response being modulated by the TRPA1 status and that DMTS treatment significantly reduced these effects when TRPA1 channels were functional. DMTS also mitigated thymus involution due to hypothalamic-pituitary-adrenal (HPA) axis dysregulation. <b>Conclusions</b>: Overall, DMTS appears to relieve depressive and anxiety symptoms through TRPA1-mediated pathways, suggesting its potential as a dietary supplement or adjunct therapy for depression and anxiety.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 6","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12196134/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144507377","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":"<i>Cenostigma bracteosum</i> Hydroethanolic Extract: Chemical Profile, Antibacterial Activity, Cytotoxicity, and Gel Formulation Development.","authors":"Addison R Almeida, Francisco A S D Pinheiro, Marília G M Fideles, Roberto B L Cunha, Vitor P P Confessor, Kátia N Matsui, Weslley S Paiva, Hugo A O Rocha, Gislene Ganade, Laila S Espindola, Waldenice A Morais, Leandro S Ferreira","doi":"10.3390/pharmaceutics17060780","DOIUrl":"10.3390/pharmaceutics17060780","url":null,"abstract":"<p><p><b>Background:</b><i>Cenostigma bracteosum</i> (Tul.) Gagnon & G.P. Lewis (Fabaceae), popularly known as \"catingueira\", is a plant widely distributed in the Caatinga biome, which comprises 11% of the Brazilian territory. While this species is of interest given local knowledge, formal reports are lacking in the literature, warranting targeted investigation. This study aimed to prepare and characterize a hydroethanolic extract of <i>C. bracteosum</i> leaves, prepare carbopol gels containing the extract, and evaluate their cytotoxicity and antibacterial activity against <i>Staphylococcus aureus</i> and <i>Escherichia coli</i>. <b>Methods</b>: The initial extract was prepared in an ultrasonic bath using ethanol/water (70:30, <i>v</i>/<i>v</i>). The extract (1 mg/mL) was analyzed by liquid chromatography coupled with mass spectrometry (UHPLC-MS/MS). Carbopol-based gels containing 1% and 3% of <i>C. bracteosum</i> extract were prepared and characterized in terms of pH, conductivity, spreadability, and rheology. The cytotoxicity was determined by the MTT method using MC3T3-E1 pre-osteoblast cells and L929-CCL1 fibroblast cells. The antibacterial activity of the extract and gels was evaluated using the agar diffusion method against <i>S. aureus</i> and <i>E. coli</i>. <b>Results</b>: The <i>C. bracteosum</i> leaves extract demonstrated antibacterial activity against <i>S. aureus</i> and <i>E. coli</i>, were not cytotoxic for the assessed cells at concentrations up to 100 μg/mL, and its analysis by UHPLC-MS/MS allowed the annotation of 18 metabolites, mainly of the phenolic acid and flavonoids glycoside classes, together with a biflavonoid. The prepared gels remained stable over the 30-day post-production analysis period. <b>Conclusions</b>: These findings provide a better understanding of the chemical diversity of the secondary metabolites of a common Caatinga biome species-<i>C. bracteosum</i>-specifically present in leaves hydroethanolic extract and gel formulation adapted for skin application with activity against <i>S. aureus.</i></p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 6","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12196441/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144507356","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}