Drug Development and Industrial Pharmacy最新文献

{"title":"pH-responsive chitosan-alginate hydrogel beads: for enhanced bioavailability and controlled release of omeprazole.","authors":"Anil K Philip, Betty Annie Samuel, Yagub Salem Saleh, Bassim I Mohammad, Hayder A Al-Aubaidy","doi":"10.1080/03639045.2025.2536620","DOIUrl":"10.1080/03639045.2025.2536620","url":null,"abstract":"<p><strong>Objective: </strong>To develop a pH-responsive drug delivery using chitosan-alginate hydrogel beads for enhanced therapeutic efficacy of omeprazole.</p><p><strong>Significance: </strong>The developed system offers improved drug entrapment, release profiles, and enhanced bioavailability for omeprazole compared to commercial formulation.</p><p><strong>Methods: </strong>pH-responsive chitosan-alginate hydrogel beads were prepared using a modified ionotropic gelation technique. The process was optimized <i>via</i> a two-level factorial design. Characterization involved drug entrapment efficiency determination, molecular dynamic simulations, <i>in vitro</i> drug release studies, and Caco-2 cell monolayer permeability assessments. Stability was evaluated under accelerated conditions, and <i>in vivo</i> efficacy was tested in rats with indomethacin-induced peptic ulcer disease.</p><p><strong>Results: </strong>The optimized formulation achieved 82.70 ± 2.02% drug entrapment efficiency. <i>In vitro</i> release studies demonstrated superior pH-dependent behavior, with minimal release (<20%) at pH 1.2 and sustained release (>92%) at pH 7.4 over 24 h. Molecular modeling revealed high entrapment efficiency. The Caco-2 cell study showed a 2-fold increase in drug permeability (2.8 × 10^-6cm/s) compared with that of free omeprazole (4.5 × 10^-6cm/s) and a commercial formulation (3.7 × 10^-6cm/s), with no significant cytotoxicity (cell viability > 95%). <i>In vivo</i> studies demonstrated significant ulcer healing, reducing the ulcer index from 3.96 to 1.20. Accelerated stability studies indicated a 24-month shelf-life under normal conditions.</p><p><strong>Conclusions: </strong>The novel chitosan-alginate hydrogel system offers a promising solution for improving omeprazole delivery, with significant enhancements in drug entrapment, release profile, bioavailability, and stability.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-16"},"PeriodicalIF":2.4,"publicationDate":"2025-07-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144648829","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":"<i>Ehretia microphylla</i> Lam.: unveiling pharmacognostic, physicochemical, phytochemical and toxicity insights.","authors":"Surya Suresh, Karthiyayini Ramaswamy, Yangchen Dolma Kom","doi":"10.1080/03639045.2025.2532139","DOIUrl":"10.1080/03639045.2025.2532139","url":null,"abstract":"<p><strong>Objective: </strong>To establish a comprehensive pharmacognostic, physicochemical, phytochemical characteristics analysis and toxicity potential of <i>Ehretia microphylla</i> leaves.</p><p><strong>Significance: </strong>The phytochemical profile of medicinal plants varies with environmental and climatic factors making the preliminary analysis essential. This study is the first to report the GC-MS profile and toxicity using brine shrimp lethality assay of <i>E. microphylla</i> leaves contributing new data on its phytochemical profile and toxicity profile supporting its safety and potential for herbal drug development.</p><p><strong>Methods: </strong>Organoleptic and fluorescence analyses were conducted to determine sensory and chemical properties. Physicochemical parameters such as ash values, extractable values and moisture content were measured. Phytochemical profiling was carried out using Gas Chromatography-Mass Spectrometry. Toxicity was evaluated using brine shrimp lethality assay and the IC₅₀ was determined.</p><p><strong>Results: </strong>The sample exhibited army green color, characteristic odor, bitter taste and coarse texture in organoleptic analysis. Fluorescence analysis showed the sample with changes from green to pink on UV and visible light. The physicochemical evaluation also established the standard values of ash content, extractive values and moisture content. GC-MS revealed 32 bioactive compounds. The brine shrimp lethality assay indicated moderate toxic activity with an IC₅₀ of 472.24 µg/mL according Meyer's cytotoxicity index.</p><p><strong>Conclusion: </strong>This study presents a detailed scientific profile of <i>E. microphylla</i> leaves, which gives evidence for their potency as potential therapeutic agents. The findings validate the traditional medicinal applications and provide a basis for drug development studies in the future.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-16"},"PeriodicalIF":2.4,"publicationDate":"2025-07-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144607801","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":"Investigation on the protective effect of Ganoderma Lucidum spore oil on pustular acne based on molecular dynamics simulation and experimental validation.","authors":"Chunyu Wang, Hanxiao You, Yuting Yan, Yue Zhou, Xinxin Liu","doi":"10.1080/03639045.2025.2531403","DOIUrl":"10.1080/03639045.2025.2531403","url":null,"abstract":"<p><p>Ganoderma lucidum spore oil (GLSO), a bioactive natural product, demonstrates notable antioxidant, anti-inflammatory, and immunomodulatory properties, suggesting therapeutic potential. Pustular acne, characterized by intrafollicular pus accumulation, is primarily mediated by oxidative stress. This study investigated the antioxidative and therapeutic effects of GLSO on pustular acne through integrated computational and experimental approaches. Network pharmacological analysis revealed eight core targets associated with pustular acne pathogenesis. Molecular docking and dynamics simulations demonstrated stable binding of lucidone A and Cerevisterol to key targets (PTPN6/KDR), suggesting their role in modulating oxidative signaling pathways. <i>In vitro</i> experiments demonstrated that GLSO (25-100 mg/L) significantly improved the viability of H₂O₂-treated human keratinocytes and attenuated intracellular ROS levels, achieving efficacy comparable to that of vitamin C (positive control). Western blot and RT-PCR analyses confirmed that GLSO upregulates mRNA and protein expression of PTPN6 and KDR. Additionally, GLSO exhibited potent total antioxidant capacity (ABTS: 2.88 mmol/g; FRAP: 0.126 mmol/g). These findings suggest that GLSO alleviates pustular acne by targeting oxidative stress <i>via</i> active components such as lucidone A and Cerevisterol, which modulate PTPN6 and KDR signaling. This study provides mechanistic insights and preclinical evidence to support further clinical development of Ganoderma-derived therapeutics.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-13"},"PeriodicalIF":2.4,"publicationDate":"2025-07-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144616770","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":"<i>Terminalia arjuna</i> gum as a novel biopolymer for microbead formulation in pH-sensitive drug delivery.","authors":"Maryam Basharat, Sobia Noreen, Amjid Khan, Farooq Anwar, Bushra Ijaz, Khurram Shahzad Munawar, Mudeera Anwar, M Abdullah","doi":"10.1080/03639045.2025.2531402","DOIUrl":"10.1080/03639045.2025.2531402","url":null,"abstract":"<p><strong>Objective: </strong>Biocompatible drug delivery systems that endure stomach acidity while enabling controlled release in the colon are essential for enhancing bioavailability.</p><p><strong>Significance: </strong>This study presents <i>Terminalia arjuna</i> (<i>T. arjuna</i>) gum, a plant-based substitute for synthetic excipients and a natural, biodegradable polymer for controlled drug delivery. It helps create safer, more efficient oral formulations with more stability of acid-labile drugs.</p><p><strong>Method: </strong><i>T. arjuna</i> gum was utilized to create plain, blended (<i>T. arjuna</i> gum and sodium alginate were used in a blended formulation to increase stability, drug entrapment, and controlled release), and coated (Propylene glycol and gum mixture was used as the coating material) microbeads <i>via</i> the ionic gelation method.</p><p><strong>Result: </strong>Characterization showed that the size of plain microbeads was 645.67 ± 7.74 μm, while the size of coated microbeads was 586.23 ± 7.18 μm. Drug entrapment efficiency ranged from 67.06% to 88.12%. Swelling studies in pH 7.4 buffer revealed that coated microbeads had a higher swelling index (1.47 ± 0.09) than blended microbeads (1.18 ± 0.06). <i>In vitro</i> release studies demonstrated sustained release, as predicted by the Korsmeyer-Peppas model, indicating non-Fickian diffusion. Scanning Electron Microscopy (SEM) results revealed spherical microbeads with varying surface morphologies, including rough, porous, and smooth textures, depending on the formulation. Thermogravimetric Analysis (TGA) and Differential Scanning Calorimetry (DSC) confirm the stability of microbeads. Powder X-ray Diffraction (PXRD) confirmed the amorphous form of P-Na within the microbeads, and Fourier-Transform Infrared Spectroscopy (FTIR) validated successful drug entrapment without significant interactions with the polymer. Acute toxicity studies on Swiss albino mice showed no adverse effects, and <i>in vivo</i> pharmacokinetic studies in rabbits demonstrated a prolonged P-Na half-life, increasing from 1.12 to 2.24 hrs with a C_max of 2264.8 ng/mL.</p><p><strong>Conclusion: </strong>These findings suggest that <i>T. arjuna</i> gum-based microbeads are promising candidates for sustained drug delivery applications. Future research should focus on optimizing these formulations for various drugs, exploring additional therapeutic applications, and investigating the long-term stability of <i>T. arjuna</i> gum-based systems for potential clinical use.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-19"},"PeriodicalIF":2.4,"publicationDate":"2025-07-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144616766","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 Photoprotection with <i>Rheum ribes</i>-Loaded Solid Lipid Nanoparticles: A Novel Sunscreen Gel Formulation.","authors":"Pedram Ebrahimnejad, Seyyed Mobin Rahimnia, Toktam Najafi, Amirhossein Babaei, Taha Monadi, Sayedeh Zohre Vaziri, Mahdie Taheri, Mohammad Azadbakht, Ali Nokhodchi","doi":"10.1080/03639045.2025.2534815","DOIUrl":"https://doi.org/10.1080/03639045.2025.2534815","url":null,"abstract":"<p><strong>Purposes: </strong>The limitations of current sunscreens in protecting against skin cancer and aging have been acknowledged. The use of <i>Rheum ribes</i> extract, rich in phenolic compounds and with strong antioxidant activity, for sunscreen applications has not been extensively studied. This study aims to develop a sunscreen gel containing <i>Rheum ribes</i> (Rhubarb) root extract-loaded solid lipid nanoparticles (SLNs) and evaluate its sun protection factor (SPF) through <i>in vitro</i> testing.</p><p><strong>Methods: </strong><i>Rheum ribes</i> extract-loaded SLNs were manufactured by an emulsification-solvent evaporation method. The impact of glyceryl monostearate (GMS) concentration on SLN size, polydispersity index (PDI), entrapment efficiency (EE), and <i>in vitro</i> drug release was investigated. The optimized formulation was incorporated into a gel base, and its SPF was determined using spectrophotometric techniques. Skin permeation and retention studies, as well as skin irritation and cytotoxicity assessments, were conducted.</p><p><strong>Results: </strong>The optimized extract-loaded SLN formulation exhibited a nano-sized diameter (298.07 ± 14.54 nm), uniform distribution (PDI = 0.308 ± 0.001), high entrapment efficiency (69.18 ± 2.60%), and significant skin permeation (32.03 ± 1.44% after 24 hours) and retention (6.42 ± 0.39 mg/cm² after 24 hours). This formulation demonstrated a substantially higher SPF (17.435) than the simple extract gel (SPF = 1.913). All gel preparations were found to be non-irritating and non-cytotoxic.</p><p><strong>Conclusion: </strong>This study demonstrates the potential of <i>Rheum ribes</i> extract-loaded SLNs for developing effective and safe sunscreen gels. The optimized nanogel formulation achieved significant SPF enhancement while maintaining skin compatibility, highlighting its promising application in cosmetic sun protection.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-18"},"PeriodicalIF":2.4,"publicationDate":"2025-07-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144641981","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":"Engineering pH-responsive niosomes with ergosterol and CHEMS for controlled carfilzomib release: insights from <i>in vitro</i> and <i>in vivo</i> studies.","authors":"Mohammad Reza Hajinezhad, Sonia Fathi-Karkan, Maryam Roostaee, Sara Sargazi, Shekoufeh Mirinejad, Roghayeh Sheervalilou, Saman Sargazi, Mahmood Barani","doi":"10.1080/03639045.2025.2530161","DOIUrl":"10.1080/03639045.2025.2530161","url":null,"abstract":"<p><strong>Objective: </strong>Carfilzomib (CFZ), a selective proteasome inhibitor, was encapsulated in pH-responsive niosomes to enhance its stability and targeted delivery.</p><p><strong>Significance: </strong>This formulation aims to improve the controlled release and therapeutic efficacy of CFZ while minimizing systemic toxicity.</p><p><strong>Methods: </strong>Niosomes were prepared via thin-film hydration using ergosterol, CHEMS, Span 60, and Tween 60. The lipid film was hydrated with PBS (pH 7.4) containing CFZ in DMSO at 60 °C, followed by sonication to form unilamellar vesicles. The formulation was characterized for encapsulation efficiency, particle size, drug release, cytotoxicity, and <i>in vivo</i> toxicity.</p><p><strong>Results: </strong>Encapsulation efficiency reached 89.82%, with particle size increasing slightly from 323 nm (empty niosomes) to 334 nm (CFZ-loaded). In vitro release was pH-dependent, with 74.39% of CFZ released at pH 5.4 versus 54.55% at pH 7.4. CFZ-loaded niosomes exhibited enhanced cytotoxicity against breast cancer cells (IC₅。 = 0.0415 µM) compared to free CFZ (IC₅。 = 0.0714 µM). A synergistic effect with doxorubicin was observed (combination index <1). <i>In vivo</i> studies showed no significant toxicity at 1 and 2 mg/kg doses. However, 4 mg/kg caused elevations in liver enzymes, BUN, and creatinine, with histopathological signs of liver and kidney damage.</p><p><strong>Conclusions: </strong>The CFZ-loaded niosomal system demonstrated optimal size, pH-responsive release, and superior anticancer activity. These findings highlight its potential as an effective carrier for controlled proteasome inhibitor delivery.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-16"},"PeriodicalIF":2.4,"publicationDate":"2025-07-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144599692","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 novel data-driven approach to assess the chewability and grittiness of the chewable tablets using a texture analysis.","authors":"Yu Zhang, Hongyue Liu, Jitong Wang, Fan Zhao, Jinru Hu, Zhidan Liu, Ruixiang Li, Minchen Liu, Jia Zeng, Li Qin, Ruofei Du","doi":"10.1080/03639045.2025.2523547","DOIUrl":"10.1080/03639045.2025.2523547","url":null,"abstract":"<p><strong>Context: </strong>Chewable tablet palatability significantly impacts patient compliance, but current pharmacopeias have no standardized evaluation methods. This requires developing an objective system for assessing the palatability of chewable dosage forms, which will aid in setting quality control standards.</p><p><strong>Objective: </strong>Using a texture analyzer, this study aimed to develop an objective, data-driven approach to evaluate chewability and grittiness in chewable tablets.</p><p><strong>Methods: </strong>10 commercially available chewable tablet formulations were assessed, with subjective sensory evaluations supplemented by texture analysis-based measurements to quantify attributes of chewability and grittiness. To evaluate chewability, measurements of axial compression force, work, and adhesion were conducted, establishing optimal conditions of 400 N, 3 mm, and 50% strain to simulate oral chewing. For grittiness, a correlation between particle size and linear distance value was demonstrated, with Calcium carbonate used as a reference material to establish a standardized evaluation scale.</p><p><strong>Results: </strong>Results indicated a strong correlation between tablet formulations and their sensory and texture analysis scores, with stickiness largely influenced by formulation ingredients such as milk powder and cacao powder. And the particle size of the insoluble material in the tablets largely influences the grit sensation.</p><p><strong>Conclusion: </strong>We developed a novel data-driven approach that offers a standardized assessment system to evaluate palatability characteristics in chewable tablets, facilitating more consistent formulation comparisons and potential optimization for consumer acceptability. This approach highlights the utility of texture analysis in transitioning empirical palatability assessments to objective, quantifiable methods, which may extend to other oral dosage forms.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-15"},"PeriodicalIF":2.4,"publicationDate":"2025-07-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144607802","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":"Impact of Actuation Force on the Quality Assessment of Pressurized Metered- Dose Inhalers.","authors":"Yaru Zhou, Bo Yang, Wentao Pan","doi":"10.1080/03639045.2025.2533523","DOIUrl":"https://doi.org/10.1080/03639045.2025.2533523","url":null,"abstract":"<p><strong>Objective: </strong>To investigate the influence of varied actuation forces on the quality assessment of pressurized metered-dose inhalers(pMDIs).</p><p><strong>Methods: </strong>Both manual and automatic methods were employed to assess the effects of manual actuation and automatic actuation (with different set actuation forces) on the delivered dose uniformity(DDU), emitted dose per actuation(EDPA), and aerodynamic particle size distribution(APSD) results of pMDIs.</p><p><strong>Results: </strong>When manual actuation was performed, the discrepancies in the DDU were observed, whereas differences in the EDPA and APSD results were not evident. When utilizing automatic actuation, the results for DDU, EDPA, and APSD all exhibited good uniformity. However, it was observed that inadequate actuation force, insufficient to fully open the valve, resulted in lower outcomes for all the aforementioned parameters. And when the actuation speed is excessively low, it results in a decline in the FPF value.</p><p><strong>Conclusions: </strong>The process of routine manual testing for DDU in inhalation aerosols, as well as methodology transfer in this field, necessitates meticulous attention to the standardization of operation techniques and actuation forces among diverse experimenters. Furthermore, using automated actuation can avoid variations due to manual operation and achieve good uniformity of results. However, when employing automatic actuation, it is crucial to select an actuation force that effectively ensures complete valve opening, thereby safeguarding the accuracy and reliability of the inhalation aerosol product. This suggests that attention should be paid to patients with limited hand strength (such as children and the elderly) when using aerosols.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-14"},"PeriodicalIF":2.4,"publicationDate":"2025-07-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144616769","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":"Comparative study between pH, time and colonic bacterial enzyme triggered polymers for colonic delivery of coated ketoprofen multi-particulates.","authors":"Debaprasad Ghosh, Ashu Mittal, Mandeep Kumar Arora","doi":"10.1080/03639045.2025.2525951","DOIUrl":"https://doi.org/10.1080/03639045.2025.2525951","url":null,"abstract":"<p><strong>Background: </strong>In this study, we aimed to prepare, evaluate, and compare drug-loaded pellets of ketoprofen coated with different triggering mechanisms for colonic delivery.</p><p><strong>Objective: </strong>The purpose of this study was to compare Eudragit S100 and Eudragit L100 based pH-dependent, hydroxypropyl cellulose and ethyl cellulose-based time-dependent and high methoxylated pectin and ethyl cellulose-based colonic bacterial enzymatic degradation-dependent coatings over drug-loaded pellets for most efficient colon targeting.</p><p><strong>Methods: </strong>Any possible drug-polymer interactions were analyzed using Fourier-transform infrared spectroscopy and differential scanning calorimetry. Drug-loaded pellets were prepared using powder layering technology. Different batches of coated pellets were prepared for <i>in vitro</i> evaluation, and optimized batches were selected. These optimized batches were investigated for surface topography by scanning electron microscopy and for colon targeting efficiency by <i>in vivo</i> X-ray roentgenography and gamma scintigraphy studies in white New Zealand rabbits.</p><p><strong>Results: </strong>The drug and polymers were found to be compatible. The prepared coated multi-particulates exhibited favorable micrometric properties. In vitro dissolution studies showed that the polysaccharide pectin high methoxylated and ethyl cellulose-coated optimized batch limited drug release to 16.724 ± 1.124% in the upper gastrointestinal tract and released up to 91.556 ± 3.144% in the colon following zero-order Korsmeyer-peppas super case-II transport (mean dissolution time 36.1779 h). Scanning electron microscopy analysis confirmed the surface characteristics of the pellets before and after dissolution. <i>In vivo</i> studies in New Zealand white rabbits using X-ray roentgenography and gamma scintigraphy demonstrated the optimized batch's gastrointestinal transit and colon targeting efficiency.</p><p><strong>Conclusion: </strong>Statistically, the polysaccharide-based formulation showed promising results for targeted drug release in the colon.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-14"},"PeriodicalIF":2.4,"publicationDate":"2025-07-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144590676","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":"Quality by design (QbD)-driven formulation of sildenafil citrate microparticles using quasi-emulsion technique for pulmonary delivery: an <i>in vitro</i> study.","authors":"Ashwini K Diwate, Vaishali Y Londhe","doi":"10.1080/03639045.2025.2525957","DOIUrl":"10.1080/03639045.2025.2525957","url":null,"abstract":"<p><strong>Objective: </strong>The goal of this research was to create inhalable microparticles to ensure the continuous delivery of sildenafil citrate (SC) to treat pulmonary arterial hypertension (PAH). This was done to address the limitations of SC, including its short half-life and systemic side effects.</p><p><strong>Methods: </strong>To create the inhalable microparticles, a particle engineering method called the quasi-emulsion solvent diffusion method was utilized. The study employed quality by design (QbD), a regulatory-based approach, to enhance the final product's quality. The optimization of microparticles was achieved using central composite design to enhance micromeritics properties and sustain drug release profiles. Characterization studies, including FTIR, differential scanning calorimetry (DSC), scanning electron microscopy, XRD, and surface morphology analysis, were conducted to evaluate the microparticles. Aerodynamic properties were measured to predict where particles will be deposited in the respiratory tract.</p><p><strong>Results: </strong>The optimized formulated microparticles had an acceptable mean particle size and an entrapment efficiency greater than 90%. The optimized microparticles demonstrated a sustained drug release of 80.42 ± 0.23% over 24 h. Aerodynamic properties showed a mass median aerodynamic diameter of 3.45 ± 0.0 µm, a fine particle fraction of 21%, and 77.29 ± 2.9% of the dose recovered from the inhaler. Modified tapped density measurements indicated improved flow properties of the microparticles.</p><p><strong>Conclusion: </strong>The QbD approach was successfully employed to formulate inhalable microparticles for sustained pulmonary delivery. The optimized microparticles exhibited enhanced micromeritics properties and sustained drug release profiles, making them a promising option for the treatment of PAH.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-12"},"PeriodicalIF":2.4,"publicationDate":"2025-07-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144539515","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}