AAPS PharmSciTech最新文献

{"title":"Oleic acid Enriched Leciplexes as Novel Mucoadhesive Cationic Nanocarriers of Agomelatine for Glaucoma Treatment","authors":"Mai Ahmed Tawfik,&nbsp;Sadek Ahmed,&nbsp;Rania Moataz El-Dahmy,&nbsp;Diana E. Aziz","doi":"10.1208/s12249-025-03250-0","DOIUrl":"10.1208/s12249-025-03250-0","url":null,"abstract":"<div><p>Agomelatine (AGO) is a dual action drug. Being serotonin receptor antagonist, AGO is orally administered for depression treatment. Here in, AGO was used for intraocular pressure management due to its agonistic activity on the melatonin receptors in the eyes. AGO is a BCS II drug, with low oral bioavailability and massive first-pass metabolism. Oleic acid enriched leciplexes were investigated as novel mucoadhesive cationic nanocarriers to improve AGO’s ocular bioavailability and prolong its pharmacological effect. Twenty-four AGO loaded leciplexes were fabricated by single-step procedure. AGO: lipid ratio, surfactant: phosphatidyl choline ratio, cationic surfactant type, permeation enhancer type were investigated. For optimization; in-vitro assessment of size, homogeneity, surface charge, drug entrapment and in-vitro release was conducted. The optimum system was further examined for crystallinity, compatibility, morphology, pH, refractive index, surface tension and stability. L20 developed at a drug: lipid ratio of 1: 20, cetyltrimethylammonium bromide and phosphatidyl choline at a ratio of 1:5 respectively and 0.25% w/v oleic acid was the optimum system with respect to shape and PS (spherical, 491 nm), PDI (0.29), ZP (31.1 mV), EE (81.8%), in-vitro release (Q_2h; 34.9%, Q_8h; 91.2%), crystallinity, pH (6.3), refractive index (1.24), surface tension (46.2 mN/m) and stability. AGO pharmacodynamic and histopathological studies were conducted in rabbits. Compared to AGO dispersion, elevated maximum IOP reduction (74.2%), prolonged mean residence time (12.88 h), enhanced bioavailability (3 folds) and normal histopathological micrographs proved the potential of L20 leciplex in improving and sustaining the ocular bioavailability of AGO and maintaining its safety.\u0000</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 1","pages":""},"PeriodicalIF":4.0,"publicationDate":"2025-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1208/s12249-025-03250-0.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145352293","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Effect of Surfactants on Oral Delivery of Nanoemulsions Containing Fexofenadine, a Substrate for P-glycoprotein","authors":"Ikki Shibazaki,&nbsp;Yuri Ikeuchi-Takahashi,&nbsp;Mayumi Ikegami-Kawai,&nbsp;Yasuko Obata","doi":"10.1208/s12249-025-03251-z","DOIUrl":"10.1208/s12249-025-03251-z","url":null,"abstract":"<div><p>Nanoemulsions are considered to have an advantage in improving the oral bioavailability of poorly absorbed drugs. However, studies on additives such as surfactants used as emulsifiers, essential for the preparation of nanoemulsions, are relatively limited, and their safety and usefulness require further investigation. In this study, the utility of polyoxyethylene sorbitan monostearate (PS60) and polyglyceryl-10 oleate (PGFE), used as nonionic surfactants, was evaluated by using them as emulsifiers for nanoemulsions containing fexofenadine (FXD), a P-glycoprotein (P-gp) substrate. The median diameter of droplets in FXD nanoemulsions was smaller with PGFE compared with PS60. In the drug release study, all FXD nanoemulsions suppressed the drug release at gastric pH and the cumulative amount of drug released increased at intestinal pH. In an <i>in vivo</i> study, PS60-containing nanoemulsions exhibited a higher area under the plasma concentration–time curve, indicating their potential as an effective formulation for improving the gastrointestinal absorption of FXD. In PS60-containing nanoemulsions, we hypothesize that the absorptive transport of FXD was increased due to the combined effects of improved drug dissolution properties, increased paracellular and/or transcellular transport due to emulsification, and decreased secretory transport due to inhibition of P-gp. In PGFE-containing nanoemulsions, the increased bioavailability of the P-gp substrate drug was lower than PS60-containing nanoemulsions. However, data indicate that PGFE has a weaker P-gp inhibitory potential than PS60 in the cellular transport of digoxin, and it may serve as a surfactant with minimal P-gp interaction in the gastrointestinal tract when used in combination with P-gp substrate drugs.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 1","pages":""},"PeriodicalIF":4.0,"publicationDate":"2025-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145352291","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Novel Quercetin-Ascorbic Acid Nano Cocrystals: A Carrier-free Strategy for Enhancement of Solubility, Topical Anti-oxidant Activity and Cytotoxicity","authors":"Najam ul Hassan Jawa,&nbsp;Nasir Abbas,&nbsp;Hafiza Nasreen Aslam,&nbsp;Hafsa Afzal,&nbsp;Misbah Hameed,&nbsp;Nadeem Irfan Bukhari,&nbsp;Sumera Latif","doi":"10.1208/s12249-025-03239-9","DOIUrl":"10.1208/s12249-025-03239-9","url":null,"abstract":"<div><p>Quercetin (QUC), an extensively investigated nutraceutical, demonstrates various clinical and therapeutic effects such as anti-oxidant, anti-inflammatory, anti-malarial, anti-viral, anti-carcinogenic and cytoprotective properties. However, the effectiveness of QUC is off-set by its poor solubility, stability, permeability, and absorption. In current research, a cocrystal nanonization strategy, integrating the cocrystallization and nanosizing techniques, has been tested to address intrinsic issues of QUC. A cocrystal of QUC with ascorbic acid (as co-former) synthesized by solvent evaporation was transformed into nano-cocrystal (NCC) by top-down homogenization technique using 0.045% Poloxamer 188 (as stabilizer). NCC was characterized by SEM and Zetasizer and appeared to be blocked-shaped with mean particle size of 300 ± 80 nm. Further characterization was undertaken using powder X-ray diffraction, differential scanning calorimetry and Fourier transform infrared spectroscopy. The properties of cocrystal and NCC were explored by solubility, <i>In-vitro</i> dissolution, anti-oxidant, and cytotoxicity studies against Vero and MCF-7 cells. NCC presented 17 and 5 times enhanced solubility and dissolution of QUC in distilled water and 1.6 times enhanced anti-oxidant activity compared to free QUC, and substantial mortality against MCF-7 cells. NCC remained stable in gel for six months at 4 ± 2ºC and 30 ± 2ºC/60 ± 5%RH. The gel released 98.91% QUC after 5 h. Hence, the topical formulation by combining the advantages of cocrystals and nanonization (nano-cocrystals) might be a promising strategy in treating various skin ailments by virtue of ameliorated physicochemical profile, anti-oxidant activity and stability.\u0000</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 1","pages":""},"PeriodicalIF":4.0,"publicationDate":"2025-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145352292","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Enhanced Ocular Delivery of Itraconazole via a Self-Emulsifying Drug Delivery System: Improved Antifungal Activity and Cellular Uptake","authors":"Sukannika Tubtimsri,&nbsp;Yotsanan Weerapol","doi":"10.1208/s12249-025-03254-w","DOIUrl":"10.1208/s12249-025-03254-w","url":null,"abstract":"<div><p>Corneal fungal infections are a leading cause of blindness worldwide; however, poor ocular drug absorption limits current topical antifungal treatments. Itraconazole (ICZ), a potent antifungal agent, exhibits low aqueous solubility and limited permeability. This study aimed to develop self-emulsifying drug delivery systems (SEDDS) to enhance the solubility, permeability, and ocular cell uptake of ICZ, providing a more effective topical therapy. ICZ solubility was evaluated in various vehicles (Tween 80, Tween 60, Span 20, coconut oil, and olive oil). Ten optimized SEDDS formulations were prepared, with particle sizes ranging from 514 to 1,384 nm (tenfold dilution). <i>In vitro</i> drug permeation was assessed using Franz diffusion cells with a parallel artificial membrane permeability assay. Cellular uptake was evaluated in ocular cell lines, and drug diffusion kinetics were analyzed using the Higuchi model. Formulation stability was assessed over a 6-month period. Formulation F1 achieved the highest permeation (96.71% ± 1.99%), followed by F3 (96.33% ± 3.24%) and F2 (80.98% ± 2.85%), whereas ICZ-PEG showed minimal permeation (11.55% ± 2.80%). The Higuchi model indicated diffusion-controlled transport. Cellular uptake was highest for F3, followed by F1 and F2, with approximately 50.3-, 38.6-, and 12.3-fold higher uptake than ICZ-PEG, respectively. All ICZ-SEDDS formulations remained stable for &gt; 6 months. ICZ-SEDDS markedly improved the solubility, permeability, and ocular cell uptake of ICZ compared with ICZ-PEG. The superior performance of formulation F3 highlights the potential of SEDDS as an effective strategy for overcoming limitations in topical antifungal therapy for corneal fungal infections.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 1","pages":""},"PeriodicalIF":4.0,"publicationDate":"2025-10-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145341164","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Fabrication of Gastroretentive and Extended-Release Famotidine Floating Tablets via Fused Deposition Modeling","authors":"Esraa Al Shawakri,&nbsp;Eman A. Ashour,&nbsp;Rasha M. Elkanayati,&nbsp;Mashan Almutairi,&nbsp;Sundus Omari,&nbsp;Nouf AlShammari,&nbsp;Michael A. Repka","doi":"10.1208/s12249-025-03237-x","DOIUrl":"10.1208/s12249-025-03237-x","url":null,"abstract":"<div><p>Famotidine suffers from low oral bioavailability due to poor aqueous solubility, short half-life, and limited gastric retention. This study aimed to develop gastro-retentive floating tablets of famotidine using hot-melt extrusion (HME) and fused deposition modeling (FDM) 3D printing approach to enhance its solubility, prolong gastric residence, and achieve extended drug release. Famotidine was incorporated into various polymeric carriers, including hydroxypropyl cellulose (HPC LF) and hydroxypropyl methylcellulose (HPMC E5), to produce drug-loaded filaments using an 11 mm twin-screw co-rotating extruder. The filaments were subsequently 3D-printed into low-density, hollow tablets to achieve prolonged gastric floatation. The solid-state characterization by differential scanning calorimetry (DSC) revealed the absence of famotidine’s crystalline melting peak in both filaments and 3D-printed tablets, suggesting amorphization within the polymer matrix. FTIR spectroscopy indicated hydrogen bonding interactions between famotidine and polymer hydroxyl groups, supporting the stabilization of the solid dispersion. The lead formulation demonstrated excellent buoyancy of about nine hours and extended drug release in 0.1 N HCl, confirming the potential of the system for extended gastric retention. This work highlights the utility of HME-FDM 3D printing for developing tailored, gastro-retentive dosage forms that enhance the performance of poorly soluble drugs like famotidine through amorphous solid dispersion and formulation-driven design.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 8","pages":""},"PeriodicalIF":4.0,"publicationDate":"2025-10-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1208/s12249-025-03237-x.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145290611","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Investigations on the Spatial Dust Distribution for Emission Site Localization in Containment","authors":"Hendrik Küllmar,&nbsp;Martin Schöler,&nbsp;Jonas Brügmann,&nbsp;Claudia S. Leopold","doi":"10.1208/s12249-025-03236-y","DOIUrl":"10.1208/s12249-025-03236-y","url":null,"abstract":"<div><p>Dustiness and the spatial distribution of dust are major problems when working with highly active pharmaceutical ingredients. Therefore, the aim of this study was to develop a chamber setup that allows a reproducible atomization of small powder quantities and the detection of not only dustiness but also the spatial distribution of airborne dust at extremely low concentrations, to prove that an emission site may be localized with stationary sampling even in a confined space. For this purpose, the time required for evacuation of the chamber setup was determined with fuming sulfuric acid. In subsequent atomization experiments, the safe surrogate acetaminophen was used. The spatial distribution of the surrogate was detected with nine IOM samplers (Institute of Occupational Medicine) and its quantification was carried out via HPLC. A linear tendency of the quantity of aerosol formed in dependence of the sample mass was demonstrated. In addition, significant differences between individual spots of detection and thus a spatial distribution in the detection chamber was observed. These results indicated a strong convective mass transport within the chamber setup. To verify these results, the airflow used for atomization was simulated using Computational Fluid Dynamics, confirming the convective mass transport and the spatial distribution of the airborne acetaminophen dust. In summary, it was shown that an emission site may be localized based on stationary exposure data even at concentrations as low as those mandatory in the contained manufacture of HPAPI-containing pharmaceuticals.\u0000</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 8","pages":""},"PeriodicalIF":4.0,"publicationDate":"2025-10-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1208/s12249-025-03236-y.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145256118","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Enhanced Tumor Treatment Outcomes of PEGylated Liposomal Gefitinib in Non-Small Cell Lung Cancer: A Comprehensive Preclinical Evaluation with Superior Therapeutic Efficacy","authors":"Rajeshkumar S. Palva,&nbsp;Jolly R. Parikh,&nbsp;Rajnikant M. Suthar,&nbsp;Musaratafrin Saiyed,&nbsp;Mitali Patel,&nbsp;Prajesh Prajapati,&nbsp;Umang H. Shah","doi":"10.1208/s12249-025-03235-z","DOIUrl":"10.1208/s12249-025-03235-z","url":null,"abstract":"<div><p>This study developed PEGylated liposomal gefitinib (GTL) to overcome clinical limitations of gefitinib therapy in NSCLC, including poor tumor targeting and suboptimal therapeutic outcomes. GTL was formulated using DPPC:cholesterol:mPEG-2000-DSPE (8:7:1) and comprehensively evaluated for tumor treatment efficacy. GTL achieved optimal physicochemical properties (87.7 ± 4.81 nm, EE 60.15%) with polymer relaxation-controlled release kinetics (Super Case II transport, <i>n</i> = 1.0789) providing sustained therapeutic exposure. The GTL demonstrated superior tumor treatment outcomes with threefold enhanced cytotoxicity (IC₅₀: 4.93 <i>vs</i> 15.03 μg/mL) and remarkable <i>in vivo</i> efficacy including 57% tumor volume reduction versus control and 32% superiority over free gefitinib. Comprehensive tumor treatment evaluation revealed enhanced apoptotic activity (68.35% caspase 3/7 activation), near-complete restoration of normal lung architecture, and significant tumor clearance confirmed by histopathological analysis. The controlled release mechanism enabled sustained therapeutic levels while minimizing systemic toxicity. GTL maintained stability for 12 months under ICH conditions, supporting clinical development. This work represents the comprehensive tumor treatment evaluation of gefitinib nanoformulation, demonstrating clinically relevant therapeutic superiority for improved NSCLC patient outcomes.\u0000</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 8","pages":""},"PeriodicalIF":4.0,"publicationDate":"2025-10-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145249249","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Dissolution Amelioration by Small Amounts of HPMC in the Difficult-to-solve Drug Combination Baicalein-imperatorin Co-Amorphous System: Dispersion and Crystallization Inhibition","authors":"Tong Su,&nbsp;Xinli Liang,&nbsp;Qieying Jiang,&nbsp;Yu Tong,&nbsp;Mubarak G. Bello,&nbsp;Gonglong Li,&nbsp;Zhenggen Liao","doi":"10.1208/s12249-025-03245-x","DOIUrl":"10.1208/s12249-025-03245-x","url":null,"abstract":"<div><p>Drug-drug co-amorphous systems (CAS) represent an emerging co-delivery strategy for combination therapy. Current research primarily explores combinations of poorly water-soluble drugs with water-soluble counterparts, while CAS comprising exclusively poorly water-soluble drugs remains underexplored. Such systems may exhibit unique dissolution behaviors due to the absence of hydrophilic components. In prior work, we developed a co-amorphous system of two poorly water-soluble drugs, baicalin (Bai) and imperatorin (Imp). However, this system demonstrated significant agglomeration during dissolution and limited dissolution enhancement. To address this, we incorporated trace hydroxypropyl methylcellulose (HPMC) into the Bai-Imp-CAS via spray drying. This study investigates HPMC’s impact on dissolution behavior and underlying mechanisms through comprehensive analyses of supersaturation dissolution, dispersion kinetics, agglomeration rate, contact angle, surface free energy, nucleation time, and crystal growth rate. Results indicate that trace HPMC significantly enhances dissolution performance by reducing contact angles and increasing surface free energy, thereby improving dispersibility and inhibiting recrystallization. Additionally, HPMC elevates the glass transition temperature (<i>Tg</i>), improving physical stability. These findings provide a novel theoretical framework for optimizing poorly soluble drug combinations and offer practical solutions for co-delivery system development.Finally, it is also important to note that the degree of improvement of HPMC on the dissolution of the two drugs in the difficult-to-dissolve drug combination is also related to the solubility of the drugs themselves, their crystallization properties and the ratio of the two drugs.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 8","pages":""},"PeriodicalIF":4.0,"publicationDate":"2025-10-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145237677","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Comparative Study of the Influence of Lipid Composition on Stability, In Vitro Release, and Antioxidant Activity of Quercetin-loaded Ceramide-containing Liposomes for Topical Delivery","authors":"Ioannis Tsichlis,&nbsp;Veatriki-Despoina Koufonikola,&nbsp;Chrysi Chaikali,&nbsp;Sophia Hatziantoniou,&nbsp;Costas Demetzos","doi":"10.1208/s12249-025-03226-0","DOIUrl":"10.1208/s12249-025-03226-0","url":null,"abstract":"<div><p>This study investigates the influence of phospholipid saturation by comparing hydrogenated soy phosphatidylcholine (HSPC) and egg yolk phosphatidylcholine (EPC) on the physicochemical characteristics, colloidal stability, drug release behavior and antioxidant activity of quercetin-loaded ceramide-containing liposomes for topical delivery. Liposomes composed of EPC:Cer:Que and HSPC:Cer:Que were prepared by thin-film hydration followed by sonication. The nanosystems were studied for particle size, polydispersity index, ζ-potential, and entrapment efficiency. Colloidal stability was evaluated under mechanical stress, accelerated aging, and long-term storage, while <i>in vitro</i> drug release, drug retention, and antioxidant activity were assessed under simulated skin conditions. Incorporation of ceramides into EPC bilayer reduced stability issues associated with unsaturated phospholipids and maintained a fluid structure, promoting drug release. Both formulations exhibited enhanced colloidal stability with EPC-based liposomes maintaining their properties at all conditions, whereas HSPC-based liposomes showed increased particle size following mechanical stress. HSPC-based liposomes demonstrated higher quercetin entrapment efficiency (63 ± 5%), improved retention over time (75% at 90 days), and a more sustained release (45% at 480 min). EPC-based ceramide-containing liposomes exhibited faster release (50% at 240 min), resulting in greater antioxidant activity as indicated by DPPH assay (0.474 ascorbic acid equivalents), while FRAP assay results were comparable for both formulations (0.012 Fe²⁺ equivalents), indicating consistent ferric reducing potential after release. These findings highlight the significance of phospholipid composition in liposome behavior and provide insights into the design of stable and effective ceramide-containing nanosystems for topical delivery of poorly water-soluble compounds such as quercetin, with potential applications in managing photoaging, inflammation, and wound healing.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 8","pages":""},"PeriodicalIF":4.0,"publicationDate":"2025-10-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1208/s12249-025-03226-0.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145237631","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Road to Precision Nanomedicine: An Insight on Drug Repurposing and Advances in Nanoformulations for Treatment of Cancer","authors":"Yasmina Elmahboub,&nbsp;Rofida Albash,&nbsp;Sadek Ahmed,&nbsp;Salwa Salah","doi":"10.1208/s12249-025-03233-1","DOIUrl":"10.1208/s12249-025-03233-1","url":null,"abstract":"<div><p>Cancer remains one of the most significant global health challenges, with its burden continuing to rise. The limitations of conventional anticancer therapies caused by the lack of tissue selectivity, demands urgent development of safer and more selective therapies to target tumors. Identifying the fundamental cancer hallmarks provided a comprehensive understanding of cancer biology for effective tumor targeting, encompassing tumor-promoting inflammation, metabolic reprogramming, immune evasion, genomic instability, phenotypic plasticity, epigenetic reprogramming, and polymorphic microbiomes. Moreover, drug repurposing is a cost-effective and time-saving method for cancer therapy that accelerates the drug discovery process by reusing drugs for new indications. Current research is focusing on combining drug repurposing with nanocarriers that enhance tumor targeting, reduce the side effects, and improve the bioavailability of the drug in a single nanoformulation. This article analyzes various types of nanoparticles encapsulating different classes of drugs, such as phenelzine, fexofenadine, telmisartan, losartan, metformin, canagliflozin, atorvastatin, and fenbendazole, highlighting their anticancer effects and the influence of nanocarriers on the drug’s therapeutic effect. Results revealed that drug-encapsulated nanoparticles enhanced antitumor effects compared to the free drug solutions. This is attributed to the synergism from the nanocarrier’s functionalization, sustained drug release, and improved cellular uptake within tumors that leads to targeting multiple cancer hallmarks. Additionally, this review highlights the present challenges in the clinical translation of nanoformulation and demonstrates how artificial intelligence may facilitate drug screening and identification, therapeutic optimization, and large-scale manufacture. Finally, using these technologies in combination with drug repurposing presents a promising direction for advancing cancer treatment.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 8","pages":""},"PeriodicalIF":4.0,"publicationDate":"2025-10-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1208/s12249-025-03233-1.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145237662","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}