Journal of Pharmaceutical Innovation最新文献

{"title":"Systematic QbD-Assisted RP-HPLC Method Development for Impurity Analysis of Efonidipine Hydrochloride Ethanolate, Chlorthalidone, and Telmisartan in a Single Pill: A Novel Fixed Dose Combination","authors":"Anil Gadhe,&nbsp;Atmaram Pawar,&nbsp;Vikram Gharge,&nbsp;Balasaheb Jadhav,&nbsp;Vikas Mohite","doi":"10.1007/s12247-026-11042-7","DOIUrl":"10.1007/s12247-026-11042-7","url":null,"abstract":"<div><h3>Purpose</h3><p>Efonidipine Hydrochloride Ethanolate, Chlorthalidone, Telmisartan, and their associated impurities, Efonidipine Related Compound A and Chlorthalidone Related Compound A, in a fixed-dose combination tablet formulation were developed and validated using an RP-HPLC approach.</p><h3>Methods</h3><p>Method development and optimization was done using a Quality by Design methodology supported by Design of Experiments to ensure systematic optimization and dependable chromatographic performance. Buffer pH and mobile phase composition were determined to be crucial technique parameters based on risk assessment, and a central composite design was used to optimize them. They were statistically assessed for their impact on retention durations of the analytes, resolution between Chlorthalidone and Chlorthalidone Related Compound A, and crucial analytical responses between Telmisartan and Efonidipine Related Compound A.</p><h3>Results</h3><p>With correlation coefficients (R²) falling within the range, predictive models demonstrated great reliability. Gradient elution with phosphate buffer, acetonitrile, and methanol utilizing a Photodiode Array detector produced the best separation. Results demonstrated adequate specificity, accuracy, linearity, precision, sensitivity, and robustness after the method was validated in accordance with ICH criteria. Efonidipine Related Compound A and Chlorthalidone Related Compound A were fully validated for their ability to quantify active pharmaceutical ingredients. Resultant separation of degradation products, analyte, and impurity peaks was confirmed by conducting forced degradation studies under various saturation parameters, showing the stability-indicating nature of the method.</p><h3>Conclusion</h3><p>The developed method can serve for stability studies, impurity profiling, and routine quality control of this triple-drug combination.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"22 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2026-09-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149034433","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":"Development and Evaluation of a Hydroxyurea-loaded Invasome Hydrogel for Enhanced Anti-psoriatic Efficacy and Reduced Systemic Exposure","authors":"Taiba Rizvi,&nbsp;Mayank Garhewal,&nbsp;Khusboo Agrawal,&nbsp;Achal Mishra,&nbsp;Yogesh Vaishnav,&nbsp;Shekhar Verma","doi":"10.1007/s12247-026-11028-5","DOIUrl":"10.1007/s12247-026-11028-5","url":null,"abstract":"<div><p>The purpose of this study was to develop and optimize a new invasome hydrogel to deliver hydroxyurea for treating psoriasis topically and with less systemic side effects from oral administration. The optimization of the hydroxyurea loaded invasomes gel was performed using a 2³ factorial design by independently varying the phospholipid, ethanol and terpene concentrations. The optimized formulation (F1) had a particle size of 130 ± 0.16 nm; zeta potential of -28.5 ± 0.045 mV; entrapment efficiency of 92.1 ± 0.15%; viscosity of 10,200 ± 0.17 cP. Morphology was confirmed to be spherical with transmission electron microscopy, drug entrapment and partial amorphization were indicated by Fourier-transform infrared spectroscopy and X-ray diffraction. The hydroxyurea-loaded invasome was then combined with a Carbopol 934 gel base to improve skin compatibility. Stability studies found minimal change in entrapment efficiency and particle size. The in vitro drug release was sustained 99.04 ± 1.29% at 24h, skin permeation and retention studies showed 68.7 ± 5.2%, skin deposition and negligible systemic permeation. In vivo evaluation was performed using a psoriasis rat model induced by imiquimod. Hydroxyurea dramatically reduced erythema, scaling and epidermal thickness, though rejuvenating orthokeratosis compared to clobetasol propionate. Hydroxyurea was not detectable in blood which showed minimal systemic exposure, as measured by HPLC.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"22 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2026-09-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149034921","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":"In Vitro-In Vivo Correlation (IVIVC) of Satranidazole HCl-Loaded Polymeric Nanoparticles for Colon Targeting: A Comprehensive Evaluation","authors":"Debgopal Ganguly,&nbsp;Ananta Choudhury,&nbsp;Subhabrota Majumdar","doi":"10.1007/s12247-026-11070-3","DOIUrl":"10.1007/s12247-026-11070-3","url":null,"abstract":"<div><h3>Background</h3><p>Colon-targeted drug delivery systems are critical for treating inflammatory bowel disease (IBD) and associated colon cancer. Satranidazole (STZ), a second-generation nitroimidazole, offers therapeutic potential but suffers from poor solubility and early absorption in the upper gastrointestinal tract. This study aimed to develop STZ-loaded polymeric nanoparticles (STZ-Nps) and establish a Level A <i>in vitro</i>-<i>in vivo</i> correlation (IVIVC).</p><h3>Methods</h3><p>STZ-Nps were fabricated using Eudragit RS100 and RL100 via a modified solvent evaporation method. Nine formulations (F1-F9) were evaluated for particle size, zeta potential, polydispersity index (PDI), entrapment efficiency (EE%), and<i> in vitro</i> drug release. The optimized formulation (F3) was administered orally to male Wistar rats (30 mg/kg), and pharmacokinetic parameters were determined using a validated RP-HPLC method. IVIVC was established by correlating <i>in vitro</i> cumulative drug release with <i>in vivo</i> fraction absorbed.</p><h3>Results</h3><p>F3 demonstrated optimal characteristics: particle size 193 nm, zeta potential − 34.25 mV, PDI 0.125, and EE% 83.5 ± 0.5%. <i>In vitro</i> release showed 95.85% cumulative release over 16 h following zero-order kinetics (R² = 0.9529). Pharmacokinetic evaluation revealed Cmax of 10.33 ± 2.15 µg/mL at Tmax of 4.0 h, with AUC0-12 h of 59.48 ± 13.34 µg·h/mL. A strong linear correlation (R² = 0.9714) was established between <i>in vitro</i> release and<i> in vivo</i> absorption.</p><h3>Conclusion</h3><p>The F3 formulation demonstrated significant systemic absorption following oral administration, as confirmed by comparison with IP reference data. The robust IVIVC supports the predictive utility of <i>in vitro</i> release data for <i>in vi</i>v<i>o</i> performance, facilitating formulation optimization for IBD and colon cancer therapy.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"22 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2026-09-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149034932","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":"Effect of Cuprous Oxide Nanoparticles Green-synthesized Using Artemisia dracunculus Extract on Cell-cycle Progression and Apoptosis in Bladder Cancer Cells","authors":"Junqing Gu,&nbsp;Qiang Zhang,&nbsp;Chunlin Tan,&nbsp;Zhongbo Du","doi":"10.1007/s12247-026-11035-6","DOIUrl":"10.1007/s12247-026-11035-6","url":null,"abstract":"<div><p>Biogenically mediated cuprous oxide nanoparticles using herbal extracts possess potent anticancer properties across different cancer cell models. These biocompatible particles induce apoptosis while minimizing toxicity, suiting nanomedicine applications. In this research, the generated cuprous oxide nanoparticles were stabilized effectively by the <i>Artemisia dracunculus</i> aqueous extract. FT-IR, EDX, TEM, XRD, UV-Vis, and FE-SEM methods were used to characterize the produced Cu₂O NPs@<i>Artemisia dracunculus</i>. Peaks at 2θ angles of 36°, 42°, and 61° depict the crystal planes (111), (200), and (220), respectively. In this investigation, the resulting particles (10–20 nm) were observed. The anti-bladder cancer potentials of the Cu₂O NPs@<i>Artemisia dracunculus</i> may eradicate remarkably bladder cancer cells through the MTT examination. The bladder cancer cells viability has been shown to be impacted by Cu₂O NPs@<i>Artemisia dracunculus</i>. The cytotoxicity value of Cu₂O NPs@<i>Artemisia dracunculus</i> against the HUVEC (Normal) cells was so low and less than IC₅₀. The IC₅₀ value of Cu₂O NPs@<i>Artemisia dracunculus</i> was 17 µg/mL against the UM-UC-3 bladder cancer cells. Recent Cu₂O NPs@<i>Artemisia dracunculus</i> suggests anti-human bladder cancer potential without high toxicity against the normal cells. The IC₅₀ value of Cu₂O NPs@<i>Artemisia dracunculus</i> was 33 µg/mL against the DPPH free radicals, while the IC₅₀ value of BHT (as a drug control) was 18 µg/mL. The flow cytometry examination of the UM-UC-3 cancer cells indicated the reduction of G0/G1 and G2/M phases and progression the S phase. Cu₂O NPs@<i>Artemisia dracunculus</i> reduced the level of colony formation and mRNA expression of Bcl2, while increased the levels of apoptosis, LDH release, and ROS and mRNA expression of Bax and P53. The research data showed the employing Cu₂O NPs@<i>Artemisia dracunculus</i> benefits to treat bladder cancer in the in vitro condition.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"22 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2026-09-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149034933","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":"Engineered Lipid–Polymer Hybrid Nanoparticles of Delafloxacin for Dry Powder Inhaler: Box-Behnken Design-Based Optimization, Physicochemical Characterization, and In Vitro Lung Deposition Study","authors":"Priti Bagade,&nbsp;Achal Kuranjekar,&nbsp;Purushottam Gangane,&nbsp;Md Ali Mujtaba,&nbsp;Gamal Osman Elhassan,&nbsp;Siham Abdoun,&nbsp;Turky Omar Asar,&nbsp;Ameeduzzafar Zafar","doi":"10.1007/s12247-026-11067-y","DOIUrl":"10.1007/s12247-026-11067-y","url":null,"abstract":"<div><h3>Background and Aim</h3><p>Delafloxacin (DLF) is a broad-spectrum fluoroquinolone antibiotic with activity against both Gram-positive and Gram-negative bacteria and potential application in the treatment of non-nosocomial pneumonia. This study aimed to develop and characterize DLF-loaded lipid–polymer hybrid nanoparticles (LPHNPs) formulated as a dry powder inhaler (DPI) for pulmonary delivery. </p><h3>Methods and Results</h3><p>LPHNPs were prepared using a single-emulsion solvent evaporation method and optimized through a three-factor, three-level Box–Behnken design. The optimized nanoparticles exhibited a particle size of 166 ± 1.98 nm, polydispersity index of 0.259 ± 0.006, zeta potential of -23.7 ± 2.4 mV, entrapment efficiency of 89 ± 1.02%, and drug loading of 20 ± 0.37%. The optimized LPHNPs were converted into dry powder formulations using spray drying and lyophilization techniques for enhanced aerosolization and pulmonary delivery performance. Solid-state characterization using Fourier transform infrared spectroscopy and differential scanning calorimetry confirmed drug encapsulation and compatibility with excipients, while X-ray diffraction indicated an amorphous nature of the formulations. Morphological analysis revealed smooth, spherical particles. In vitro release studies demonstrated an initial burst followed by sustained drug release. The DPI formulations showed excellent aerodynamic properties, including high fine particle fraction, low moisture content, and good flowability. Brunauer–Emmett–Teller analysis indicated high drug loading with low surface area, and accelerated stability studies confirmed formulation robustness over six months. </p><h3>Conclusion</h3><p>Overall, the developed DPI-based LPHNP system offers enhanced stability, sustained release, and improved lung deposition, indicating its promise as an effective and patient-friendly pulmonary delivery system for DLF.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"22 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2026-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149034815","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":"Intellectual Property Landscape of Soft Gelatin Capsule Dosage Forms: Patents, Limitations, and Strategies for Non-Infringing Formulation Development","authors":"Senthilraja Kaliyamoorthy,&nbsp;A. T. Rajasekhar","doi":"10.1007/s12247-026-11059-y","DOIUrl":"10.1007/s12247-026-11059-y","url":null,"abstract":"<div><h3>Purpose</h3><p>This review comprehensively examines the patent landscape for soft gelatin capsule (softgel) dosage forms, critically analyzes key patent claims and their inherent limitations, and proposes evidence-based strategies for developing non-infringing formulations.</p><h3>Methods</h3><p>A systematic search of the USPTO, EPO (Espacenet), and WIPO PatentScope databases was conducted for the period 1990–2025. More than 3,200 patent records were initially retrieved; approximately 950 were screened on title and abstract, and more than 420 were analyzed in full. Structured search terminology included IPC/CPC codes A61K, A61J, and B65D. Only granted patents and published applications with clearly defined claims were included for detailed analysis. FDA Orange Book listings and European Medicines Agency (EMA) Supplementary Protection Certificate (SPC) registers were reviewed as complementary regulatory sources. Patent status was verified using the USPTO Patent Full-Text Database, EPO Espacenet Register, and WIPO PatentScope as of March 2026.</p><h3>Results</h3><p>The softgel IP landscape contains multiple expired foundational patents and numerous active patents with narrow, specific claims. Key technical limitations — hydrophilic drug incompatibility, moisture sensitivity, gelatin crosslinking, and temperature-constrained processing — naturally restrict enforceable claim breadth. Strategic design-around approaches including excipient substitution, alternative non-gelatin shell polymers, seamless encapsulation technology, and novel LBDDS fill systems provide potential pathways toward FTO, subject to pharmaceutical and legal validation.</p><h3>Conclusion</h3><p>Generic and innovation-driven manufacturers may develop non-infringing softgel formulations through systematic patent landscaping combined with rational formulation design. Emerging technologies in nanotechnology, 3D printing, and bio-based shell materials offer substantial unclaimed IP space for proactive patent filing. All design-around strategies discussed herein represent scientific frameworks; independent legal counsel is essential before commercial implementation.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"22 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2026-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149034907","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":"Micellar Systems with Hydrophobic Core-Stabilized Polyethyleneimine Enabling Time-Dependent Positive Zeta Potential Transformation for Enhanced Intestinal Mucopermeation and Cellular Uptake","authors":"Ahmad Saleh Malkawi","doi":"10.1007/s12247-026-11052-5","DOIUrl":"10.1007/s12247-026-11052-5","url":null,"abstract":"<div><h3>Objective</h3><p>This study aimed to develop micelles (M) bearing polyethyleneimine (PEI)–stearic acid (SA) hydrophobic ionic complex (PEISA) loads with a zeta potential-changing property for effective intestinal mucopermeation and cellular uptake.</p><h3>Methods</h3><p>The ionic complex PEISA was formed at 3:1, 3:2, and 3:4 SA-to-PEI charge ratios and dissolved in Cremophor RH 40, Cremophor EL, and Labrasol. The resultant homogenous micellar mixtures were reconstituted in DMSO, diluted in physiological media, and examined regarding the nanosize, polydispersity index (PDI), and zeta potential using dynamic light scattering (DLS). Micellar biocompatibility using a resazurin assay and cellular uptake were checked over Caco-2 cells, whereas mucopermeation was evaluated using in vitro Transwell diffusion.</p><h3>Results</h3><p>The ionic complex PEISA significantly improved PEI solubility from 0 up to ~ 1.5 (<i>p</i> ≤ 0.01), ~ 4.5 (<i>p</i> ≤ 0.001), and ~ 5.5 (<i>p</i> ≤ 0.001) mg/mL in the lipophilic core of Labrasol, Cremophor EL, and Cremophor RH 40, respectively. DLS measured an average droplet size of ~ 16 nm with &lt; 0.3 PDI, proving uniformity and stability. At 1:200 and 1:100, micellar dilutions preserving &gt; 90% cell viability after 24 h proved biocompatibility. At 3:100 dilution, MPEISA (3:1) observed cell viability (20.74 ± 1.83%) significantly (<i>p</i> ≤ 0.001) lower than MPEISA (3:2) (65.35 ± 3.91%) and MPEISA (3:4) (75.92 ± 1.75%). The gradual zeta potential changes depicted over 180 min from − 7.90 mV up to + 1.80 mV for MPEISA (3:4), MPEISA (3:2), and MPEISA (3:1) showed a significant improvement in micellar mucopermeation (<i>p</i> ≤ 0.001) to 46 ± 3.96%, 56.90 ± 4%, and 62.16 ± 4.06% and micellar cellular uptake (<i>p</i> ≤ 0.001) to 70.69 ± 5.63%, 62.72 ± 1.57%, and 57.46 ± 0.76% after 4–5 h, respectively.</p><h3>Conclusion</h3><p>The gradual PEI cationic charge exposure from the micellar complex PEISA enabled a time-dependent shift in micellar zeta potential toward a positive value, leading to improved mucus permeation and enhanced cellular uptake.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"22 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2026-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148987108","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":"Pharmaceutical Import Forecasting for Supply-Chain Decision Support: A Comparative Evaluation of Fuzzy, Statistical, and Machine-Learning Models","authors":"Ramiz Alekperov,&nbsp;Rahib Imamguluyev","doi":"10.1007/s12247-026-11057-0","DOIUrl":"10.1007/s12247-026-11057-0","url":null,"abstract":"<div><h3>Purpose</h3><p>Pharmaceutical supply-chain planning in import-dependent economies is sensitive to macroeconomic shocks, currency volatility, and global supply disruptions. This study evaluates a Dynamic Fuzzy Time Series (DFTS) candidate together with statistical and machine-learning benchmarks for annual pharmaceutical-import forecasting.</p><h3>Methods</h3><p>Azerbaijan’s annual pharmaceutical-import observations for 2012–2023 are used for model development; the 2024 observation (USD 507.50 million) is reserved as an untouched external holdout. Model comparison uses a common rolling-origin/expanding-window protocol beginning with a 2012–2017 initial training window. RMSE is pre-specified as the primary loss, with MAE and sMAPE as complementary measures. The DFTS recency parameter rho is selected from {0.70, 0.80, 0.90, 1.00}, and an optional log-space long-term blending weight alpha is selected from {0, 0.25, 0.50, 0.75, 1.00}, using pre-2024 rolling-origin RMSE only.</p><h3>Results</h3><p>Among the reproduced benchmarks, the naive forecast achieved the lowest rolling-origin RMSE (95.84 million USD). The best DFTS setting was rho = 0.70 with RMSE = 120.17 million USD; adding the long-term log-trend component did not reduce RMSE, so the selected alpha was 0 and the hybrid candidate collapsed to the DFTS component. Its frozen 2024 forecast was USD 591.91 million, corresponding to a 16.63% absolute percentage error, compared with 10.51% for the naive benchmark.</p><h3>Conclusion</h3><p>The revised evidence does not support a claim that the hybrid/DFTS candidate outperforms simple benchmarks on this short annual series. Its value is instead methodological and scenario-oriented: the framework provides a transparent shock-aware evaluation structure, while the empirical results show the importance of benchmark discipline, leakage-free validation, and cautious operational interpretation.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"22 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2026-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148986389","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":"RGD-Conjugated Silica Nanoparticles for Potentially Targeted Delivery of Quercetin to HeLa Cancer Cells","authors":"Mais Fuad Bulbul,&nbsp;Areen M Khattabi,&nbsp;Fabian Rios","doi":"10.1007/s12247-026-11044-5","DOIUrl":"10.1007/s12247-026-11044-5","url":null,"abstract":"<div><h3>Purpose</h3><p>To overcome the main limitation of Quercetin (QUR), such as its poor water solubility, low bioavailability, and instability which affect its therapeutic use. QUR was encapsulated into commercially available silica nanoparticles (SNs) and subsequently surface-conjugated with the Arg-Gly-Asp (RGD) peptide to obtain SNs-QUR and SNs-QUR-RGD, respectively.</p><h3>Methods</h3><p>Encapsulation efficiency, loading capacity, and in vitro drug release were determined by UV spectroscopy, while successful RGD conjugation was verified by FT-IR analysis. Particle size, zeta potential, and polydispersity index (PDI) were evaluated using dynamic light scattering (DLS) to assess the physicochemical properties and colloidal stability of the formulations. The cytotoxic activity of free QUR, SNs-QUR, and SNs-QUR-RGD against HeLa cervical cancer cells was investigated using the MTT assay.</p><h3>Results</h3><p>The encapsulation efficiency and loading capacity of QUR in SNs were approximately 55.7% and 0.11%, respectively. FT-IR spectra confirmed the successful attachment of RGD to the nanoparticle surface. DLS results revealed an increase in mean particle size following QUR loading and further enlargement after RGD conjugation, while zeta potential and PDI values indicated good stability and moderate size uniformity. In Vitro Release studies demonstrated a sustained release pattern for SNs-QUR-RGD, which was slower than that of SNs-QUR, whereas free QUR showed the fastest release. Moreover, SNs-QUR-RGD exhibited enhanced cytotoxicity compared with SNs-QUR and free QUR, highlighting its potential as an efficient targeted nanocarrier for hydrophobic anticancer drugs.</p><h3>Conclusion</h3><p>The SNs-QUR-RGD exhibited efficient drug encapsulation, sustained release and enhanced cytotoxicity against HeLa cells, highlighting its potential as a promising targeted nanocarrier for the delivery of QUR and other hydrophobic anticancer agents.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"22 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2026-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148986928","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":"Long-Term In-Vitro Aerosol Performance and Drug Retention of a Cardboard-Based Spacer (MDI PLUS®) Compared with Conventional Spacer Designs","authors":"Ahmed H.M. Sobh,&nbsp;Marina E. Boules,&nbsp;Mohammed A. Amin,&nbsp;Mohamed E. A. Abdelrahim,&nbsp;Mina Nicola","doi":"10.1007/s12247-026-11039-2","DOIUrl":"10.1007/s12247-026-11039-2","url":null,"abstract":"<div><h3>Background</h3><p>Spacers and valved holding chambers improve drug delivery. However, plastic versions are bulky, costly, and susceptible to electrostatic effects. Newer cardboard or portable designs are affordable and convenient, though evidence regarding long-term aerosol performance remains limited.</p><h3>Methods</h3><p>This study assessed the durability, drug retention, and aerosol emission performance of a cardboard-based spacer (MDI PLUS®) over 200 repeated actuations. Aerosol emission of salbutamol (Ventolin®, 100 µg/actuation) and beclometasone (Clenil Forte®, 250 µg/actuation) was measured at set intervals using an Andersen cascade impactor (28.3 L/min), determining total emitted dose (TED) and aerodynamic particle size characteristics. Single-puff deposition within the MDI PLUS®, on the pressurized metered dose inhaler (pMDI), and on a user’s hand was also compared with two commercial plastic spacers, AeroChamber Plus® and AeroChamber2go™.</p><h3>Results</h3><p>Over 200 uses, MDI PLUS® maintained a stable delivered dose for salbutamol (TED 221–198 µg) and beclometasone (506–532 µg), without significant change in mass median aerodynamic diameter (≈ 3.97–4.45 μm). Salbutamol fine particle dose (FPD) and fraction (FPF) declined non-significantly, from 165 µg/75% to 119 µg/60%, while beclometasone FPD (307–393 µg) and FPF (61–75%) remained largely unchanged. Drug retention within the spacer increased with repeated use across all devices but was significantly lower for MDI PLUS® (p &lt; 0.05) than for either AeroChamber device. Deposition on the pMDI and on the hand was negligible for all devices.</p><h3>Conclusion</h3><p>MDI PLUS® showed durable, consistent aerosol performance across repeated use, with lower drug retention supporting its suitability as a reliable long-term spacer.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"22 1","pages":""},"PeriodicalIF":2.6,"publicationDate":"2026-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148986929","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}