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Quercetin Nanocrystal Gel: A Novel Topical Therapeutic Strategy for Androgenetic Alopecia. 槲皮素纳米晶体凝胶:一种新的局部治疗雄激素性脱发的策略。
IF 5.5 3区 医学
Pharmaceutics Pub Date : 2025-09-12 DOI: 10.3390/pharmaceutics17091188
Yaya Su, Yuwen Zhu, Lei Ren, Xiang Deng, Rui Song, Lingling Wu, Zhihui Yang, Hailong Yuan
{"title":"Quercetin Nanocrystal Gel: A Novel Topical Therapeutic Strategy for Androgenetic Alopecia.","authors":"Yaya Su, Yuwen Zhu, Lei Ren, Xiang Deng, Rui Song, Lingling Wu, Zhihui Yang, Hailong Yuan","doi":"10.3390/pharmaceutics17091188","DOIUrl":"10.3390/pharmaceutics17091188","url":null,"abstract":"<p><p><b>Purpose</b>: Androgenetic alopecia (AGA) is a common, chronic, non-cicatricial dermatological condition characterized by progressive miniaturization of hair follicles. Although AGA is a benign disorder, it has a considerable impact on patients' quality of life and psychological health. The current treatment options often demonstrate limited efficacy and are frequently associated with undesirable side effects. This study aimed to co-mill two natural compounds, quercetin (QT) and glycyrrhizic acid (GL), to develop follicle-targeted nanocrystals (NCs), thereby enhancing local accumulation, improving the pathological follicular microenvironment associated with AGA, and promoting hair regrowth. <b>Methods</b>: QT nanocrystals (QT-NCs) were fabricated using a top-down wet media milling technique with GL as a bioactive stabilizer. The resulting QT-NCs were characterized regarding their particle size, crystallinity, morphology, and stability. The skin permeation properties of the QT-NCs were further evaluated in vitro, and their therapeutic efficacy was assessed in a dihydrotestosterone (DHT)-induced AGA mouse model. <b>Results</b>: The QT-NCs exhibited an irregular structure with a particle size ranging from 200 to 300 nm, demonstrating uniform dimensions and excellent storage stability. In vitro permeation studies revealed a 2.27-fold increase in cumulative penetration and a 2.47-fold enhancement in skin retention compared to raw QT. In the DHT-induced AGA mouse model, QT-NCs significantly reduced local DHT levels while concurrently modulating the follicular microenvironment, resulting in markedly improved therapeutic outcomes. Notably, when co-administered, QT and GL demonstrated synergistic pharmacological effects, suggesting potential combinatory benefits. <b>Conclusions</b>: This study presents the first demonstration of QT-NCs for AGA treatment, establishing a novel therapeutic strategy with substantial potential for clinical translation.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 9","pages":""},"PeriodicalIF":5.5,"publicationDate":"2025-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12473781/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177484","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}
引用次数: 0
Optimizing Dose Conversion from IR-Tac to LCP-Tac Formulations in Renal Transplant Recipients: A Population Pharmacokinetic Modeling Study. 肾移植受者从IR-Tac到LCP-Tac的最佳剂量转换:群体药代动力学模型研究。
IF 5.5 3区 医学
Pharmaceutics Pub Date : 2025-09-12 DOI: 10.3390/pharmaceutics17091185
Zeyar Mohammed Ali, Beatriz Fernández-Alarcón, Pere Fontova, Anna Vidal-Alabró, Raul Rigo-Bonnin, Edoardo Melilli, Nuria Montero, Anna Manonelles, Ana Coloma, Alexandre Favà, Josep M Grinyó, Josep M Cruzado, Helena Colom, Nuria Lloberas
{"title":"Optimizing Dose Conversion from IR-Tac to LCP-Tac Formulations in Renal Transplant Recipients: A Population Pharmacokinetic Modeling Study.","authors":"Zeyar Mohammed Ali, Beatriz Fernández-Alarcón, Pere Fontova, Anna Vidal-Alabró, Raul Rigo-Bonnin, Edoardo Melilli, Nuria Montero, Anna Manonelles, Ana Coloma, Alexandre Favà, Josep M Grinyó, Josep M Cruzado, Helena Colom, Nuria Lloberas","doi":"10.3390/pharmaceutics17091185","DOIUrl":"10.3390/pharmaceutics17091185","url":null,"abstract":"<p><p><b>Background/Objectives</b>: Tacrolimus dosing remains challenging due to its narrow therapeutic index and high inter- and intra-patient variability. The extended-release once-daily tacrolimus (LCP-Tac) formulation provides enhanced bioavailability and a sustained pharmacokinetic profile compared to the immediate-release twice-daily tacrolimus (IR-Tac) formulation. Although a general conversion ratio of 1:0.7 is widely recommended when switching between formulations, current guidelines do not account for pharmacogenetic variability. This study aimed to determine whether CYP3A5 genotype influences the conversion ratio in Caucasian renal transplant recipients using population pharmacokinetic (PopPK) modeling. <b>Methods</b>: A PopPK model was developed in NONMEM using full PK profiles (10-18 samples per patient) from 30 stable renal transplant patients treated with both IR-Tac and LCP-Tac. <b>Results</b>: Tacrolimus pharmacokinetics were best described by a two-compartment model with first-order absorption and linear elimination with distinct absorption rate constants and lag times for each formulation. Including circadian rhythm in the apparent clearance (CL/F) and Ka of IR-Tac significantly improved the model. CYP3A5 polymorphism was the most powerful covariate explaining variability on CL/F. <i>CYP3A5*1</i> expressers showed higher clearance and lower exposure requiring a more pronounced dose reduction upon conversion to LCP-Tac. Simulations indicated optimal conversion ratios of 1:0.6 for <i>CYP3A5*1</i> expressers and 1:0.7 for non-expressers. <b>Conclusions</b>: These findings highlight the need to move beyond a one-size-fits-all conversion ratio and adopt genotype-informed strategies. LCP-Tac's enhanced bioavailability requires dose reduction, greater in expressers when switching from IR-Tac. These genotype-specific recommendations provide clinically actionable guidance to complement therapeutic drug monitoring and support more individualized conversion protocols in renal transplantation.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 9","pages":""},"PeriodicalIF":5.5,"publicationDate":"2025-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12473248/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145176683","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}
引用次数: 0
Sprayable Hybrid Gel with Cannabidiol, Hyaluronic Acid, and Colloidal Silver: A Multifunctional Approach for Skin Lesion Therapy. 含有大麻二酚、透明质酸和胶体银的可喷雾混合凝胶:一种用于皮肤病变治疗的多功能方法。
IF 5.5 3区 医学
Pharmaceutics Pub Date : 2025-09-12 DOI: 10.3390/pharmaceutics17091189
Geta-Simona Cîrloiu Boboc, Adina-Elena Segneanu, Ludovic Everard Bejenaru, Marius Ciprian Văruţ, Roxana Maria Bălăşoiu, Daniela Călina, Andreea-Cristina Stoian, Georgiana Băluşescu, Dumitru-Daniel Herea, Maria Viorica Ciocîlteu, Andrei Biţă, George Dan Mogoşanu, Cornelia Bejenaru
{"title":"Sprayable Hybrid Gel with Cannabidiol, Hyaluronic Acid, and Colloidal Silver: A Multifunctional Approach for Skin Lesion Therapy.","authors":"Geta-Simona Cîrloiu Boboc, Adina-Elena Segneanu, Ludovic Everard Bejenaru, Marius Ciprian Văruţ, Roxana Maria Bălăşoiu, Daniela Călina, Andreea-Cristina Stoian, Georgiana Băluşescu, Dumitru-Daniel Herea, Maria Viorica Ciocîlteu, Andrei Biţă, George Dan Mogoşanu, Cornelia Bejenaru","doi":"10.3390/pharmaceutics17091189","DOIUrl":"10.3390/pharmaceutics17091189","url":null,"abstract":"<p><p><b>Background/Objectives</b>: This study presents the development and characterization of a novel thermoresponsive hydrogel composed of hyaluronic acid (HA), poloxamer 407, cannabidiol (CBD), and colloidal silver (Ag), designed for topical antimicrobial therapy. <b>Methods</b>: The Ag-CBD complex was first synthesized and subsequently incorporated into a HA-poloxamer gel matrix to produce a stable, sprayable formulation with suitable physicochemical properties for dermal applications. <b>Results</b>: The HA-Ag-CBD hybrid gel exhibited a physiological pH, a gelation temperature compatible with skin surface conditions, and favorable rheological behavior, including thixotropy and shear thinning-critical for uniform application and retention under dynamic conditions. Release studies confirmed a sustained delivery profile, supporting prolonged local activity of CBD and colloidal Ag. Antimicrobial assays demonstrated that the HA-Ag-CBD hybrid gel retained potent activity against <i>Staphylococcus aureus</i> and <i>Candida albicans</i>, with minimum inhibitory and bactericidal concentrations (MIC/MBC) statistically comparable to those of the unencapsulated Ag-CBD complex. Against <i>E. coli</i>, the HA-Ag-CBD hydrogel exhibited primarily bacteriostatic activity, with a low MIC (9.24 μg/mL) but a substantially higher MBC (387.35 μg/mL), consistent with the intrinsic structural resistance of Gram-negative bacteria. In contrast, bactericidal activity was more pronounced against Gram-positive strains, reflecting differential susceptibility related to bacterial envelope properties. CBD consistently demonstrated superior antimicrobial efficacy to colloidal Ag, while the Ag-CBD combination produced slightly enhanced, mainly additive effects, likely due to complementary membrane disruption and intracellular Ag<sup>+</sup> ion activity. Cytotoxicity assays on normal human dermal fibroblasts confirmed that the HA-Ag-CBD hybrid gel maintained >70% cell viability at therapeutically relevant concentrations, in accordance with ISO 10993-5:2009 guidelines, and effectively mitigated the inherent cytotoxicity of the Ag-CBD complex. <b>Conclusions</b>: The HA-Ag-CBD hybrid gel demonstrates strong potential as a biocompatible, multifunctional topical formulation for the treatment of infected wounds and skin lesions. Future work will focus on in vivo evaluation, assessment of skin permeation, and further development to support translational applications.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 9","pages":""},"PeriodicalIF":5.5,"publicationDate":"2025-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12473813/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177551","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}
引用次数: 0
Liposomal Encapsulation of Pine Green Cone Essential Oil: The Influence of the Carrier on the Enhancement of Anti-Inflammatory Activity. 松青精油脂质体包封:载体对增强其抗炎活性的影响。
IF 5.5 3区 医学
Pharmaceutics Pub Date : 2025-09-11 DOI: 10.3390/pharmaceutics17091182
Snježana Mirković, Vanja Tadić, Marina Tomović, Anica Petrović, Marijana Andjić, Jovana Bradić, Sanja Perać, Aleksandar Radojković, Jelena Jovanović, Ana Žugić
{"title":"Liposomal Encapsulation of Pine Green Cone Essential Oil: The Influence of the Carrier on the Enhancement of Anti-Inflammatory Activity.","authors":"Snježana Mirković, Vanja Tadić, Marina Tomović, Anica Petrović, Marijana Andjić, Jovana Bradić, Sanja Perać, Aleksandar Radojković, Jelena Jovanović, Ana Žugić","doi":"10.3390/pharmaceutics17091182","DOIUrl":"10.3390/pharmaceutics17091182","url":null,"abstract":"<p><p><b>Background/Objectives:</b> This study aimed to investigate the traditionally claimed anti-inflammatory effect of essential oil (EO) derived from pine green cones per se and after encapsulation into liposomes, which is expected to enhance its bioactivity and stability. <b>Methods</b>: The chemical profiling of EO was conducted using GC/GC-MS. The physico-chemical characterization of the liposomal formulation (LEO) included encapsulation efficiency, FTIR spectroscopy, and AFM imaging. Additionally, parameters such as mean particle diameter, polydispersity index, zeta potential, pH, and electrical conductivity were evaluated and reassessed after 30 days and 1 year to determine formulation stability. The in vivo anti-inflammatory effect of the EO and LEO was examined using a carrageenan-induced rat paw edema model. <b>Results</b>: The <i>Pinus halepensis</i> EO contained 14 components, mainly, α-pinene, myrcene, and (E)-caryophyllene. Encapsulation efficiency was 97.35%. AFM analyses confirmed the nanoscale dimensions and spherical shape of liposomes, while FTIR indicated successful encapsulation through overlapping functional groups. The droplet size of blank liposomes (L) ranged from 197.4 to 217 nm, while adding the EO decreased the droplet size and electrical conductivity. The polydispersity index (PDI) remained below 0.2. The zeta potential of the liposomes was between -35.61 and -49.43 mV, while the pH value was in the range of 4.35 to 5.01. These results indicate satisfactory stability across repeated measurements. Administration of LEO significantly inhibited paw edema relative to the controls, with a percentage inhibition of approximately 69%, which does not significantly differ from the effect of hydrocortisone, which was used as a positive control. <b>Conclusions</b>: This is the first study to report liposomal encapsulation and in vivo anti-inflammatory activity of an EO derived specifically from green cones of <i>P. halepensis</i>. Our findings demonstrate that EO-loaded liposomes exhibited favorable physico-chemical properties and notable anti-inflammatory activity, comparable to that of hydrocortisone. These results support their potential application in the development of effective topical anti-inflammatory formulations.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 9","pages":""},"PeriodicalIF":5.5,"publicationDate":"2025-09-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12473864/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177547","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}
引用次数: 0
Formulation of Recombinant Therapeutic Proteins: Technological Innovation, Regulations, and Evolution Towards Buffer-Free Formulations. 重组治疗蛋白的配方:技术创新,法规和向无缓冲配方的演变。
IF 5.5 3区 医学
Pharmaceutics Pub Date : 2025-09-11 DOI: 10.3390/pharmaceutics17091183
Tomas Gabriel Bas
{"title":"Formulation of Recombinant Therapeutic Proteins: Technological Innovation, Regulations, and Evolution Towards Buffer-Free Formulations.","authors":"Tomas Gabriel Bas","doi":"10.3390/pharmaceutics17091183","DOIUrl":"10.3390/pharmaceutics17091183","url":null,"abstract":"<p><p><b>Background/Objectives</b>: Formulating recombinant therapeutic proteins is essential to ensure their safety, efficacy, and stability. A growing trend in biopharmaceutical development is the move toward buffer-free formulations, which aim to reduce immunogenicity, improve tolerability, and simplify production. This review explores technological advances, regulatory perspectives, and safety considerations related to this shift. <b>Methods</b>: A systematic documentary review was conducted using the PSALSAR framework. Scientific publications, patents, and regulatory documents (2020-2025) were retrieved from PubMed, Scopus, Web of Science, and regulatory databases (FDA, EMA). Inclusion criteria focused on recombinant proteins, buffer-free formulations, and regulatory alignment. <b>Results</b>: The findings reveal an increasing adoption of self-buffering strategies in high-concentration subcutaneous biologics. Technologies such as Fc-fusion, PASylation, and XTENylation enhance stability without conventional buffers. Regulatory bodies are progressively accepting minimalist formulations, provided safety and biosimilarity are demonstrated. However, intellectual property barriers limit formulation transparency. A synthesis of recent FDA and EMA approvals illustrates this formulation evolution. <b>Conclusions</b>: Buffer-free formulations offer a promising alternative for therapeutic protein development by improving patient experience and reducing formulation complexity. They align with biosimilar goals and regulatory trends, although long-term transparency and safety assessments remain critical for widespread adoption.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 9","pages":""},"PeriodicalIF":5.5,"publicationDate":"2025-09-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12473750/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145176629","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}
引用次数: 0
Evaluation of Permeation Enhancers for Vaginal Delivery of Buserelin Acetate Using a Validated Chromatographic Method and Ex Vivo Porcine Model. 用有效的色谱法和离体猪模型评价醋酸布瑟林阴道给药的渗透促进剂。
IF 5.5 3区 医学
Pharmaceutics Pub Date : 2025-09-11 DOI: 10.3390/pharmaceutics17091181
Ahm Musleh Uddin, Roy N Kirkwood, Kiro R Petrovski, Souha H Youssef, Baljinder Singh, Songhita Mukhopadhyay, Yunmei Song, Sanjay Garg
{"title":"Evaluation of Permeation Enhancers for Vaginal Delivery of Buserelin Acetate Using a Validated Chromatographic Method and Ex Vivo Porcine Model.","authors":"Ahm Musleh Uddin, Roy N Kirkwood, Kiro R Petrovski, Souha H Youssef, Baljinder Singh, Songhita Mukhopadhyay, Yunmei Song, Sanjay Garg","doi":"10.3390/pharmaceutics17091181","DOIUrl":"10.3390/pharmaceutics17091181","url":null,"abstract":"<p><p><b>Background/Objectives</b>: This study aimed to enhance the vaginal permeation of buserelin acetate (BA), a synthetic gonadotropin-releasing hormone (GnRH) analogue, by evaluating various permeation enhancers (PEs) using a validated reversed-phase high-performance liquid chromatography (RP-HPLC) method and an ex vivo porcine vaginal model. <b>Methods</b>: A robust RP-HPLC method was developed and validated according to ICH Q2 (R2) guidelines to enable accurate quantification of BA in permeation samples. The analytical method demonstrated high specificity, linearity (R<sup>2</sup> = 0.9999), accuracy (98-102%), precision (%RSD < 2%), robustness, and stability. Using this method, ex vivo permeation studies were conducted with six different PEs: 2-hydroxypropyl-β-cyclodextrin, sodium dodecyl sulfate, poloxamer 188, Span 80, Tween 80, and chitosan. <b>Results</b>: Among all tested PEs, chitosan demonstrated the best enhancement of BA permeation. It achieved the highest flux (J) (0.64 ± 0.03 × 10<sup>-2</sup> µg/cm<sup>2</sup>·h) and apparent permeability coefficient (P<sub>app</sub>) (16.20 ± 0.84 × 10<sup>-5</sup> cm/h), both of which were statistically significantly higher (<i>p</i> < 0.05) than those of all other enhancer groups. Kinetic modelling indicated a non-Fickian, biphasic permeation mechanism best described by the Makoid-Banakar model. <b>Conclusions</b>: These findings highlight chitosan's potential as an effective intravaginal delivery vehicle for peptide therapeutics and establish the validated HPLC method as a reliable platform for future formulation development and translational studies in mucosal drug delivery.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 9","pages":""},"PeriodicalIF":5.5,"publicationDate":"2025-09-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12473407/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177444","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}
引用次数: 0
Nanoencapsulation of Biotics: Feasibility to Enhance Stability and Delivery for Improved Gut Health. 生物制剂的纳米胶囊化:提高稳定性和改善肠道健康的可行性。
IF 5.5 3区 医学
Pharmaceutics Pub Date : 2025-09-11 DOI: 10.3390/pharmaceutics17091180
Pedro Brivaldo Viana da Silva, Thiécla Katiane Osvaldt Rosales, João Paulo Fabi
{"title":"Nanoencapsulation of Biotics: Feasibility to Enhance Stability and Delivery for Improved Gut Health.","authors":"Pedro Brivaldo Viana da Silva, Thiécla Katiane Osvaldt Rosales, João Paulo Fabi","doi":"10.3390/pharmaceutics17091180","DOIUrl":"10.3390/pharmaceutics17091180","url":null,"abstract":"<p><p>The human gastrointestinal tract contains a complex and diverse community of microorganisms, referred to as the gut microbiota. Due to their close proximity to human cells, these microorganisms play a crucial role in maintaining the host's health, influencing various metabolic processes, and providing protection against potentially harmful agents and pathogens. The disruption in this microbial ecosystem, known as dysbiosis, is associated with inflammatory and metabolic diseases, as well as certain types of cancer. Strategies to modulate the microbiota toward a state of homeostasis through the use of \"biotics\" (probiotics, prebiotics, synbiotics, and postbiotics) have increased. However, challenges such as low stability, loss of microbial viability, and difficulties in delivery to the intestine significantly decrease the progress of their clinical and nutritional applications. Microencapsulation and nanoencapsulation technologies offer potential solutions to enhance the stability, bioavailability, and controlled release of microorganisms and/or bioactive compounds within the gastrointestinal tract. Considering these aspects, this review provides a comprehensive overview of recent advances in nanoencapsulation techniques for biotics, highlighting their mechanisms of action, potential health benefits, and applications in functional foods and targeted therapies. Furthermore, it addresses existing limitations, evaluates feasibility, and discusses the future potential of these technologies in promoting gut health and disease prevention. Further research, especially through clinical studies, is mandatory to verify the safety and effectiveness of nanoencapsulated biotics and to obtain regulatory approval.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 9","pages":""},"PeriodicalIF":5.5,"publicationDate":"2025-09-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12473147/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177500","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}
引用次数: 0
Invasomes and Nanostructured Lipid Carriers for Targeted Delivery of Ceftazidime Combined with N-Acetylcysteine: A Novel Approach to Treat Pseudomonas aeruginosa-Induced Keratitis. 侵袭体和纳米结构脂质载体靶向递送头孢他啶联合n -乙酰半胱氨酸:治疗铜绿假单胞菌诱导的角膜炎的新方法。
IF 5.5 3区 医学
Pharmaceutics Pub Date : 2025-09-11 DOI: 10.3390/pharmaceutics17091184
Mina Josef, Menna M Abdellatif, Rehab Abdelmonem, Mohamed A El-Nabarawi, Mahmoud Teaima, Hadeer M Bedair, Alshaimaa Attia
{"title":"Invasomes and Nanostructured Lipid Carriers for Targeted Delivery of Ceftazidime Combined with N-Acetylcysteine: A Novel Approach to Treat <i>Pseudomonas aeruginosa</i>-Induced Keratitis.","authors":"Mina Josef, Menna M Abdellatif, Rehab Abdelmonem, Mohamed A El-Nabarawi, Mahmoud Teaima, Hadeer M Bedair, Alshaimaa Attia","doi":"10.3390/pharmaceutics17091184","DOIUrl":"10.3390/pharmaceutics17091184","url":null,"abstract":"<p><p><b>Objectives</b>: This study was designed to optimize a ceftazidime (CTZ)-loaded nanocarrier that could efficiently permeate across corneal tissues. Moreover, N-acetylcysteine (NAC) was combined with an optimized CTZ-loaded formula to augment the antimicrobial activity and facilitate the efficient healing of <i>Pseudomonas aeruginosa</i>-induced keratitis. <b>Methods</b>: Different CTZ-loaded invasomes (INVs) and CTZ-loaded nanostructured lipid carriers (NLC) were fabricated and fully characterized via the determination of the entrapment efficiency (EE%), particle size (PS), surface charge, and percentage of CTZ release. Next, NAC was added to the optimized formulae from each nanocarrier, which were further assessed through ex vivo corneal permeation and in vitro antimicrobial activity studies. Finally, an in vivo evaluation of the optimal nanocarrier in the presence of NAC was performed. <b>Results</b>: Both nanocarriers showed nanoscale PS with sufficient surface charges. CTZ-loaded NLC formulae showed a higher EE% range with a sustained drug release profile. Both optimized formulae showed a spherical shape and excellent stability. Moreover, the antibacterial activity and biofilm inhibition assessments confirmed the synergistic effects of NAC when combined with different CTZ-loaded nanocarriers. However, the optimized CTZ-loaded INV formula achieved higher corneal permeation and deposition compared to the optimized CTZ-loaded NLC formula. Finally, the in vivo assessment confirmed the dominance of the optimized CTZ-loaded INV formula combined with NAC, where the microbiological, histopathological, and immunohistopathological examinations showed the rapid eradication of keratitis. <b>Conclusions</b>: Recent strategies for the incorporation of antibiotics into nanocarriers, combined with mucolytic agents, can offer a promising platform to boost the therapeutic efficiency of antibiotics and prevent antimicrobial resistance.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 9","pages":""},"PeriodicalIF":5.5,"publicationDate":"2025-09-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12473240/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177563","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}
引用次数: 0
Recent Advances in Nose-to-Brain Gene Delivery for Central Nervous System Disorders. 中枢神经系统疾病鼻-脑基因传递研究进展
IF 5.5 3区 医学
Pharmaceutics Pub Date : 2025-09-10 DOI: 10.3390/pharmaceutics17091177
Flávia Nathiely Silveira Fachel, Angélica Salatino-Oliveira, Willian da Silva Carniel, Rafaela Zimmermann, Ursula Matte, Helder Ferreira Teixeira, Guilherme Baldo, Roselena Silvestri Schuh
{"title":"Recent Advances in Nose-to-Brain Gene Delivery for Central Nervous System Disorders.","authors":"Flávia Nathiely Silveira Fachel, Angélica Salatino-Oliveira, Willian da Silva Carniel, Rafaela Zimmermann, Ursula Matte, Helder Ferreira Teixeira, Guilherme Baldo, Roselena Silvestri Schuh","doi":"10.3390/pharmaceutics17091177","DOIUrl":"10.3390/pharmaceutics17091177","url":null,"abstract":"<p><p>The nasal route represents a promising non-invasive technique for the direct delivery of nucleic acids to the central nervous system (CNS) disorders, effectively bypassing the blood-brain barrier. This route offers several advantages, including ease of administration, enhanced patient compliance, rapid therapeutic onset, and increased availability. Nonetheless, challenges such as mucociliary clearance, enzymatic degradation, and the low permeability of cell membranes to large molecules remain obstacles to the effectiveness of this approach. To address these limitations and achieve targeted nose-to-brain delivery with optimized therapeutic outcomes, various technological solutions have been explored, such as nanotechnology-based delivery systems and mucoadhesive formulations. These innovations aim to enhance the permeability of the nasal mucosa, extend the residence time of therapeutic agents in the nasal cavity, and improve overall treatment effectiveness. While the nasal gene delivery to the brain is still relatively new, it holds considerable potential for expanding treatment options for a range of CNS disorders. In this context, this review examines the anatomy and physiology of the nasal route, the mechanisms of biomolecule transport from nose to brain, the potential of gene delivery vectors, key preclinical advancements, and clinical perspectives for the nasal delivery of nucleic acids in CNS disorders.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 9","pages":""},"PeriodicalIF":5.5,"publicationDate":"2025-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12473560/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177550","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}
引用次数: 0
Advances in Second Near-Infrared Window Photothermal Agents and Photothermal Therapy for Tumors in Interdisciplinary Medical Research. 二次近红外窗口光热剂及肿瘤光热治疗在跨学科医学研究中的进展。
IF 5.5 3区 医学
Pharmaceutics Pub Date : 2025-09-10 DOI: 10.3390/pharmaceutics17091178
Runxuan Zhou, Yufei Chen, Shuxi Yao, Weiyun Zhang, Dawei Ye
{"title":"Advances in Second Near-Infrared Window Photothermal Agents and Photothermal Therapy for Tumors in Interdisciplinary Medical Research.","authors":"Runxuan Zhou, Yufei Chen, Shuxi Yao, Weiyun Zhang, Dawei Ye","doi":"10.3390/pharmaceutics17091178","DOIUrl":"10.3390/pharmaceutics17091178","url":null,"abstract":"<p><p>Cancer continues to pose a significant threat to human health. While early diagnosis has improved survival rates for many cancer patients, a substantial number still do not achieve the desired treatment outcomes. Therefore, it is imperative to develop novel therapeutic approaches for tumor management. Second near-infrared window photothermal therapy has garnered considerable attention from researchers due to its effective tumor-killing capabilities and minimal side effects. This review commences by summarizing the advancements in second near-infrared photothermal agents, alongside an evaluation of the advantages and disadvantages of various photothermal agents. Subsequently, we highlight the benefits of combining photothermal therapy with other treatment modalities. Finally, we present a compilation of reports detailing the application of photothermal therapy in the treatment of various tumor types in clinical settings. In the conclusion, we underscore the challenges and potential research directions associated with photothermal therapy. Our article aims to facilitate interdisciplinary research in the fields of nanomedicine and clinical medicine.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"17 9","pages":""},"PeriodicalIF":5.5,"publicationDate":"2025-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12473562/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177468","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}
引用次数: 0
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