European Journal of Pharmaceutics and Biopharmaceutics最新文献

{"title":"In vivo systemic evaluation of nasal drug absorption from powder formulations in rats","authors":"Ryosuke Tatsuta ,&nbsp;Akiko Tanaka ,&nbsp;Ken-ichi Ogawara ,&nbsp;Kazutaka Higaki ,&nbsp;Tomoyuki Furubayashi ,&nbsp;Toshiyasu Sakane","doi":"10.1016/j.ejpb.2024.114612","DOIUrl":"10.1016/j.ejpb.2024.114612","url":null,"abstract":"<div><div>Despite the potential benefits of nasal drug delivery, there is a need for a systematic evaluation of the efficacy of powder formulations adhering to the nasal mucosa. This study aims to establish a systematic evaluation method for nasal drug absorption from powder formulations. We selected three model compounds—antipyrine, griseofulvin, and acyclovir—and analyzed their pharmacokinetics following nasal administration of powder formulations under physiological conditions. Our experimental design incorporated assessments of the drug absorption patterns. Antipyrine demonstrated rapid absorption exclusively from the nasal cavity. In contrast, griseofulvin exhibited absorption from the nasal cavity and the gastrointestinal tract. This phenomenon could be attributed to the rapid nasal clearance of the drug with an initial half-life of 5 min. To further establish the physiological validity of our method, we conducted an experiment to investigate the impact of changing the mucociliary clearance (MC) on nasal absorption that resulted in a 1.2-fold increase in the bioavailability of acyclovir upon prolonged MC. Our findings support the utility of established methods in evaluating nasal absorption and their behavior in the nasal cavity. This study holds a promising advancement toward effective drug delivery via nasal administration, potentially leading to targeted delivery and improved therapeutic outcomes.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114612"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142817541","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Stearic acid-capped mesoporous silica microparticles as novel needle-like-structured drug delivery carriers","authors":"Mohamad Anas Al Tahan ,&nbsp;Ali Al-Khattawi ,&nbsp;Craig Russell","doi":"10.1016/j.ejpb.2024.114619","DOIUrl":"10.1016/j.ejpb.2024.114619","url":null,"abstract":"<div><div>Mesoporous silica are widely utilised as drug carriers due to their large pore volume and surface area, which facilitate effective loading. Additionally, they can be used to enhance drugs stability and protect against enzymatic degradation due to their silica framework. However, without the addition of a capping material, the loaded cargo may be prematurely released before reaching the target site. This work reports the functionalisation of a commercially available silica microparticle (SYLOID XDP 3050) with stearic acid at various stearic acid loading concentrations (20–120 % w/w). Scanning electron microscopy (SEM) analysis revealed that the pores were capped with stearic acid, with the filling ratio increasing proportionally to the loading concentration. Notably, needle-like structures appeared when the stearic acid amount exceeded 80 % w/w, surpassing the calculated theoretical maximum pore filling ratio (64.32 %). The molecular interactions were highlighted using Fourier-transform infrared spectroscopy (FTIR), as the intensity of the CH₃ increased with increased stearic acid loading concentrations. The needle-structures phenomenon was corroborated by 3D confocal imaging. It utilised the autofluorescence properties of stearic acid to demonstrate its presence within the carrier, with fluorescence intensity increasing alongside the stearic acid concentration. Differential scanning calorimetry (DSC) indicated the crystalline nature of these needle structures, which was further confirmed by X-ray diffraction (XRD) analysis, validating the crystallisation of the stearic acid needles. Moreover, nitrogen porosimetry was employed to assess the pore volume and surface area, where the formulation containing 120 % stearic acid exhibited the lowest pore volume (0.59 cc). This value was smaller than unloaded SYLOID (2.1 cc), indicating near-complete filling of the carrier. This newly developed SYLOID-stearic acid carrier will now be used to enhance formulation development as a platform to enhance protein oral drug delivery.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114619"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142881221","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Inhibition of naproxen crystallization by polymers: The role of topology and chain length of polyvinylpyrrolidone macromolecules","authors":"Luiza Orszulak ,&nbsp;Patryk Włodarczyk ,&nbsp;Barbara Hachuła ,&nbsp;Taoufik Lamrani ,&nbsp;Karolina Jurkiewicz ,&nbsp;Magdalena Tarnacka ,&nbsp;Marek Hreczka ,&nbsp;Kamil Kamiński ,&nbsp;Ewa Kamińska","doi":"10.1016/j.ejpb.2024.114581","DOIUrl":"10.1016/j.ejpb.2024.114581","url":null,"abstract":"<div><div>This paper presents an innovative approach that utilizes self-synthesized homopolymers of polyvinylpyrrolidone (PVP) with different architectures as effective matrices for inhibiting the crystallization of naproxen (NAP). We have thoroughly investigated amorphous solid dispersions containing NAP and (<em>i</em>) self-synthesized linear PVP, (<em>ii</em>) self-synthesized three-armed star-shaped PVP, and (<em>iii</em>) self-synthesized linear PVP with a mass (M_n) corresponding to the length of one arm of the star polymer, as well as (<em>iv</em>) commercial linear PVP K30 as a reference. Differential scanning calorimetry, X-ray diffraction, and infrared spectroscopy studies, as well as molecular dynamics simulations were conducted to gain comprehensive insights into the thermal and structural properties, as well as intermolecular interactions in the NAP-PVP systems. The main purpose of all experiments was to assess the impact of macromolecule structure (topology, molecular weight) on the kinetics of the crystallization of NAP – a drug that is very difficult to vitrify. Our studies clearly showed that the most effective matrix in inhibiting the NAP crystallization is linear, self-synthesized PVP with higher molecular weight (M_n) similar to that of the commercial PVP K30, but lower, strictly controlled dispersity. We also found that crystallization of API proceeds at a similar pace for the binary mixture composed of a star-shaped PVP and linear polymer with M_n corresponding to M_n of one arm of the star-shaped macromolecule in the vicinity of the <em>T</em>_g. The obtained data highlight the key role of polymer structure in designing new pharmaceutical formulations.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114581"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142750493","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Fishroesomes show intrinsic anti-inflammatory bioactivity and ability as celecoxib carriers in vivo","authors":"Marta Guedes ,&nbsp;Joana Vieira de Castro ,&nbsp;Ana Cláudia Lima ,&nbsp;Virgínia M. F. Gonçalves ,&nbsp;Maria Elizabeth Tiritan ,&nbsp;Rui L. Reis ,&nbsp;Helena Ferreira ,&nbsp;Nuno M. Neves","doi":"10.1016/j.ejpb.2024.114587","DOIUrl":"10.1016/j.ejpb.2024.114587","url":null,"abstract":"<div><div>According to the World Health Organization (WHO), chronic inflammatory-related diseases represent the greatest threat to human health. Indeed, failure in the resolution of inflammation leads to serious pathological conditions, such as cardiovascular diseases, arthritis, cancer, diabetes, autoimmune diseases, and neurodegenerative disorders that are often associated with extremely high human suffering and societal and economic burdens. Despite the number and efficacy of available therapeutic agents have been increased, the serious side effects associated with some of them often create a very high risk/benefit ratio for patients. Therefore, herein, a drug delivery system was engineered to overcome important drawbacks of conventional therapies and to have a synergistic action with the incorporated drug. Indeed, it will have an added beneficial role in controlling inflammation. For that, sardine (<em>Sardina pilchardus</em>) roe was used as the lipidic source to produce bioactive liposomes, namely fishroesomes. These spherical vesicles with ≈326 nm in size and a significant negative surface charge (≈-31 mV) were able to encapsulate and control the release of the anti-inflammatory drug celecoxib. Moreover, fishroesomes were cytocompatible for different cell types (chondrocytes and macrophages), at concentrations in which they present anti-inflammatory properties. Importantly, fishroesomes were more effective in reducing pro-inflammatory mediators than the free drug. We also demonstrated that a single intra-articular injection of the fishroesomes encapsulating or not celecoxib in an experimental rat model of inflammatory arthritis was safe and more effective in controlling the pain and reducing the synovial inflammation compared to the free drug. Notably, as the celecoxib concentration in the sardine roe-derived liposomes was less than half of the amount of free drug, this study demonstrates the value of fishroesomes in counteracting inflammation. Therefore, the developed formulations may be considered a promising therapeutic option for inflammatory conditions.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114587"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142791338","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Nanomedicine for pediatric healthcare: A review of the current state and future prospectives","authors":"Jiayi Chen,&nbsp;Zhifeng Zhao,&nbsp;Doaa Alantary,&nbsp;Jingjun Huang","doi":"10.1016/j.ejpb.2024.114597","DOIUrl":"10.1016/j.ejpb.2024.114597","url":null,"abstract":"<div><div>Nanomedicine has emerged as a valuable treatment and diagnosis option, due to its ability not only to address formulation challenges associated with new therapeutic moieties, but also to improve the existing drugs efficacy. Nanomedicine provides appealing advantages such as increased drug payload, enhanced stability, tailored drug release profile, improved bioavailability and targeted drug delivery, etc. Tremendous research and regulatory efforts have been made in the past decades to advance nanomedicine from the benchtop to clinic. Numerous nanotechnology-based formulation approaches have been seen succeeding in commercialization. Despite the progress in nanomedicine use in adults, the advancement in pediatric population has been much slower. Clearly the treatment of disease in children cannot be simplified by dose adjustment based on body weight or surface, due to the significant differences in physiology thus the drug absorption, distribution, metabolism, excretion and transport (ADMET), between children and adults. This inherent variable among others poses much more challenges when developing pediatric-specific nanomedicine or translating adult nanodrug to pediatric indication. This review therefore intends to highlight the physiological differences between children and adult, and the common pediatric diseases which are good candidates for nanomedicine. The formulation approaches utilized in the marketed nanomedicine with pediatric indications, including liposomes, nanocrystals, polymeric nanoparticles and lipid nanoemulsions are elaborated. Finally, the challenges and gaps in pediatric nanomedicine development and commercialization, and the future prospectives are discussed.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114597"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142794402","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Human milk improves the oral bioavailability of the poorly water-soluble drug clofazimine","authors":"Ellie Ponsonby-Thomas ,&nbsp;Anna C. Pham ,&nbsp;Shouyuan Huang ,&nbsp;Malinda Salim ,&nbsp;Laura D. Klein ,&nbsp;Simone Margaard Offersen ,&nbsp;Thomas Thymann ,&nbsp;Ben J. Boyd","doi":"10.1016/j.ejpb.2024.114604","DOIUrl":"10.1016/j.ejpb.2024.114604","url":null,"abstract":"<div><div>Clofazimine is an emerging drug for the treatment of cryptosporidiosis in infants. As a poorly water-soluble drug, the formulation of clofazimine in age-appropriate vehicles is challenging and often results in the use of off-label formulations. Milk-based vehicles such as human milk and bovine milk have been investigated as age-appropriate formulations and shown to increase the solubilisation of poorly water-soluble drugs <em>via</em> enhanced solubility in lipid digestion products <em>in vitro</em>. We hypothesised that administration of clofazimine within a milk-based vehicle would enhance bioavailability for infant patients. Towards this objective, suspensions of clofazimine in human and bovine milk were orally administered separately to piglets and rats and the subsequent plasma concentrations were compared to those after administration of an aqueous drug suspension. Initial investigations with a rodent model showed a significant increase (258%) in the oral bioavailability of clofazimine when administered with human milk. Similarly, the oral bioavailability of clofazimine was significantly higher when administered in both human (154%) and bovine milk (175%) using a neonatal piglet model, suggesting comparable enhancement in oral bioavailability could be achieved with human or bovine milk. These findings demonstrate the potential of human milk in particular to provide an effective administration vehicle for clofazimine administration to infants without the need for additional excipients.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114604"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142827981","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Co-assembled supramolecular hydrogel of asiaticoside and Panax notoginseng saponins for enhanced wound healing","authors":"Hanmei Huang ,&nbsp;Xiaohong Yang ,&nbsp;Xueying Qin ,&nbsp;Yingyan Shen ,&nbsp;Yu Luo ,&nbsp;Liu Yang ,&nbsp;Xiumei Ke ,&nbsp;Rongping Yang","doi":"10.1016/j.ejpb.2024.114617","DOIUrl":"10.1016/j.ejpb.2024.114617","url":null,"abstract":"<div><div>Self-assembling natural drug hydrogels have emerged as promising biomaterials for scalable and customizable drug delivery systems attributed to their inherent biocompatibility and biodegradability. Asiaticoside (AS), a bioactive compound derived from <em>Centella asiatica (L.) Urb.</em>, is known for its antioxidant, antifibrotic, and anti-inflammatory properties, primarily accelerating wound healing through the promotion of collagen synthesis. However, its low water solubility leads to poor transdermal absorption and reduced bioavailability when applied topically. <em>Panax notoginseng</em> saponins (PNS), active compounds derived from the stems of <em>Panax notoginseng (Burk.) F.H. Chen</em>, exhibit amphiphilic and surfactant properties, rendering them effective stabilizers. Our research has demonstrated that the co-assembly of AS and PNS forms a hydrogel, termed AS&amp;PNS hydrogel, which significantly enhances wound healing by reducing interleukin-6 (IL-6) levels and promoting the production of vascular endothelial growth factor (VEGF). Treatment with AS&amp;PNS hydrogel also tended to normalize epidermal thickness and improve collagen fiber organization at the wound site. This novel hydrogel material presents a straightforward and effective approach to managing skin wounds.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114617"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142863771","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Green synthesis of gold nano-particles using Madhuca indica flower extract and their anticancer activity on head and neck cancer: Characterization and mechanistic study","authors":"Depanwita Saha ,&nbsp;Debojit Talukdar ,&nbsp;Poulami Mukherjee ,&nbsp;Debarpan Mitra ,&nbsp;Rimi Mukherjee ,&nbsp;Subhabrata Guha ,&nbsp;Aritri Bhattacharjee ,&nbsp;Rahul Naskar ,&nbsp;Sumanta Kumar Sahu ,&nbsp;Neyaz Alam ,&nbsp;Gaurav Das ,&nbsp;Nabendu Murmu","doi":"10.1016/j.ejpb.2025.114625","DOIUrl":"10.1016/j.ejpb.2025.114625","url":null,"abstract":"<div><div>Complete eradication of aggressive head and neck squamous cell carcinoma (HNSCC) still remains a major challenging problem due to numerous resistance properties of cancer stem cells (CSC) which is crucially responsible for tumor recurrence and metastasis. This challenge causes a high demand for the emergence of novel targeted treatment modalities for improved therapeutic efficacies. Phytochemicals derived from plants proves to be a wide reservoir of important drug candidates which have the potential to impede multiple aspects of malignant growth and progression.</div><div>In the present study, we aimed to synthesize gold nanoparticles in a rapid and cost-effective manner by utilizing <em>Madhuca indica</em> flower extract and to evaluate its anticancer efficacy on head and neck cancer model via targeting cancer stemness and EMT.</div><div>The phytochemicals present in the <em>Madhuca indica</em> flower extract acted as an effective reducing agent helping in the green synthesis of gold nanoparticles. The generated AuNPs were characterized by UV–Vis spectroscopy, XRD, FTIR, TEM, FE-SEM, DLS, EDX. Anti cancer potential of synthesized AuNPs were evaluated by in vitro and <em>ex vivo</em> HNSCC model. In vivo toxicity was assessed in Swiss albino mice model.</div><div>The gold nanoparticles were characterized using UV–Vis spectroscopy which revealed unique wavelength maxima at 550 nm and its crystalline nature was confirmed by XRD. AuNPs were observed to be spherical in shape with the mean diameter of 20.34 ± 4.36 nm and zeta potential of nearly −50 mV. The FTIR spectral shift indicated the incorporation of various functional groups. MI-AuNP depicted strong anticancer attributes against HNSCC cell lines SCC154 and FaDu through significant inhibition of cancer stemness and EMT as evident from decreased tumor sphere forming efficiency and CD44+/CD24- subpopulation along with dose dependent downregulated expression of relevant CSC markers and EMT markers both in vitro and <em>ex vivo</em> HNSCC model. Additionally, no evidence of <em>in vivo</em> toxicity has been observed with MI-AuNP administration.</div><div>In conclusion, this study reported for the first time that the MI-AuNP synthesized by novel green chemistry can efficiently prevent the self-renewal capability of HNSCC by targeting Cancer stemness. The scientific significance of this study lies in the fact that MI-AuNP might be a novel and potential therapeutic candidate against aggressive and metastatic HNSCC. The findings in this study unravels the way for developing a novel therapeutic candidate against aggressive and metastatic HNSCC with a much higher prognostic potential and significantly reduced off target toxicity.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114625"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142931097","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Bupivacaine multivesicular liposomes/meloxicam nanocrystals in a thermosensitive gel adapted to the “microenvironment” for long-term analgesia","authors":"Dongxu Gao ,&nbsp;Yuan Zhao ,&nbsp;Junfeng Liu ,&nbsp;Runxuan Chu ,&nbsp;Junji Wang ,&nbsp;Wei Bian ,&nbsp;Xuejie Liu ,&nbsp;Weigen Lu ,&nbsp;Jun He","doi":"10.1016/j.ejpb.2025.114630","DOIUrl":"10.1016/j.ejpb.2025.114630","url":null,"abstract":"<div><div>Current analgesics on the market exhibit a short duration of action and induce the production of inflammatory factors in tissues damaged by surgical procedures. Inflammatory factor production can create acidic environments, limiting drug delivery. In this study, we developed a novel injectable formulation comprising bupivacaine multivesicular liposomes of high osmotic pressure (H-MVL) and meloxicam nanocrystals (MLX) in a thermosensitive gel (H-MVL/MLX@GEL) adapted to the microenvironment for long-term postoperative analgesia. To achieve formulation stability, H-MVL were prepared by regulating the osmotic pressure of the gel system. Moreover, the inclusion of MLX serves to not only attenuate local inflammatory factors, regulating the acidic microenvironment, but also to prolong the duration of action of meloxicam (MEL). The increased absorption of bupivacaine (BUP) and the prolongation of the half-life of BUP release in H-MVL/MLX@GEL were demonstrated through pharmacokinetic experiments. Sciatic nerve block models and hot plate analgesia tests demonstrated that H-MVL/MLX@GEL effectively alleviated pain for at least five days. The immunohistochemical results showed that the addition of MLX reduced the production of the local inflammatory factors interleukin-6 (IL-6) and tumour necrosis factor-α (TNF-α), thereby improving the analgesic effect by regulating the local acidic environment and alleviating local irritation.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114630"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142970236","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Patches containing quercetin microcapsules to ameliorate dermal herpes simplex virus injuries in mice","authors":"Jéssica Bassetto Carra ,&nbsp;Maria Laura Goussain Darido ,&nbsp;Camila Felix Vecchi ,&nbsp;Mariana Carla de Oliveira ,&nbsp;Ricardo Luís Nascimento de Matos ,&nbsp;Pietra Mitiko Tateyama Pattini ,&nbsp;Bianca Larissa Masquetti ,&nbsp;Beatriz da Silva Tavares ,&nbsp;Marcos Luciano Bruschi ,&nbsp;Ana Paula Frederico Rodrigues Loureiro Bracarense ,&nbsp;Renê Oliveira do Couto ,&nbsp;Rubia Casagrande ,&nbsp;Sandra Regina Georgetti ,&nbsp;Waldiceu A. Verri Jr ,&nbsp;Ligia Carla Faccin Faccin-Galhardi ,&nbsp;Marcela Maria Baracat","doi":"10.1016/j.ejpb.2025.114631","DOIUrl":"10.1016/j.ejpb.2025.114631","url":null,"abstract":"<div><div>This study aimed to develop patches containing quercetin-loaded microcapsules and to evaluate their <em>in vitro</em> and <em>in vivo</em> safety and efficacy in preclinical surveys. A set of <em>in vitro</em> experiments evidenced the virucidal activity of quercetin against the HSV-1-KOS (sensitive to acyclovir) and HSV-1-AR (resistant to acyclovir) strains, with improved outcomes upon the first. The patches presented a homogeneous aspect, were easily handled, had a suitable bioadhesion, and possessed mechanical properties of soft and weak material, besides a pH compatible with human skin. The <em>in vitro</em> release profile of quercetin showed an initial burst release, followed by a controlled release rate, which was best described by Gompertz kinetics (R² of 0.93). Using quercetin-loaded patches for treating HSV-1-KOS-induced injuries was feasible since they were well tolerated in the <em>in vivo</em> skin irritation test and significantly decreased the injury scores until the fourth out of eight days of treatment in mice compared to acyclovir cream (50 mg/g). Altogether, the <em>in vitro</em> and <em>in vivo</em> antiviral assays indicate that this flavonol acts in the earlier stage of the infection, likely impairing the HSV-1 adsorption to the cell. The anti-inflammatory capacity of the quercetin-loaded patches was noteworthy as evidenced by histological analysis. These findings bring prospects for safer and more effective management of mucocutaneous HSV-1 injuries.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114631"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142982938","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}