Pharmaceutical Development and Technology最新文献_第2页

Development of chondroitin sulfate‑stabilized PLGA microspheres of exenatide via polarity gradient extraction. 极性梯度萃取制备硫酸软骨素稳定艾塞那肽PLGA微球。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-09-18 DOI: 10.1080/10837450.2026.2731988

Ajay J Khopade, Arindam Halder, Vivek Patel, Mehul Joshi, Vinod Burade

{"title":"Development of chondroitin sulfate‑stabilized PLGA microspheres of exenatide via polarity gradient extraction.","authors":"Ajay J Khopade, Arindam Halder, Vivek Patel, Mehul Joshi, Vinod Burade","doi":"10.1080/10837450.2026.2731988","DOIUrl":"10.1080/10837450.2026.2731988","url":null,"abstract":"The present work describes the development and optimization of a poly (lactide-co-glycolide) based sustained release injectable microsphere formulation of exenatide using a coacervation and in oil drying process. The internal phase composition, containing exenatide and stabilizer, was evaluated to identify critical parameters affecting stability, drug loading, particle morphology, and burst release of exenatide. Incorporation of chondroitin sulfate(0.5-2% w/w), formed stable uniform coacervates providing consistent particle size distribution, drug loading up to 4.7% w/w, initial burst (∼1.1%) and impurities, with 'shrunken' microsphere morphology. The secondary emulsification temperature of 2-8 °C produced smaller and more uniform particles. A gradient quenching process for hardening of microspheres using n-heptane: diethyl ether (1:9) to (10:0) provided low porosity and burst release relative to n-heptane alone. The drying and lyophilization conditions reduced residual solvent levels (<5000 ppm or below quantitation) and improved its wetting characteristics. The formulation remained stable for 24 months at 2-8 °C, with minimal loss of assay content. In vitro release showed controlled release for over one month. This translated into approximately 28 days of drug exposure in rat pharmacokinetic studies and sustained glycemic control for 28 days in a db/db mice, thus, correlating microsphere erosion, in vitro release, and in vivo outcomes. This study provides insight into the manufacturing process dynamics.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-22"},"PeriodicalIF":2.9,"publicationDate":"2026-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148913031","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}

引用次数: 0

The design and optimization of a chitosan-based lamotrigine-loaded intranasal mucoadhesive nanomicelle solution using response surface methodology and artificial neural networks. 基于响应面法和人工神经网络的壳聚糖负载拉莫三嗪鼻内黏附纳米胶溶液的设计与优化。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-09-01 Epub Date: 2026-09-04 DOI: 10.1080/10837450.2026.2726934

Siyabonga Melamane, Omobolanle A Omoteso, Sandile M Khamanga, Roderick B Walker

{"title":"The design and optimization of a chitosan-based lamotrigine-loaded intranasal mucoadhesive nanomicelle solution using response surface methodology and artificial neural networks.","authors":"Siyabonga Melamane, Omobolanle A Omoteso, Sandile M Khamanga, Roderick B Walker","doi":"10.1080/10837450.2026.2726934","DOIUrl":"10.1080/10837450.2026.2726934","url":null,"abstract":"The study aimed to develop and optimize chitosan-based mucoadhesive nanomicelles for intranasal delivery of lamotrigine (LTG), to enhance epilepsy treatment, bypass the blood-brain barrier, and potentially improve brain targeting. LTG-loaded nanomicelles were prepared using thin-film hydration and optimized using a central composite design, response surface methodology, and artificial neural networks. The formulation included D-ɑ-tocopheryl polyethylene glycol succinate, Poloxamer 407, chitosan, and glycerol. Critical quality attributes assessed were micelle size (MS), polydispersity index (PDI), Zeta potential (ZP), pH, LTG content, transmittance, in vitro mucoadhesion, LTG release, and 28-day stability. The MS, PDI, ZP, pH, and LTG content of the optimized mucoadhesive nanomicelles was 31.28 ± 0.34 nm, 0.487 ± 0.00, +31.37 ± 1.97 mV, 4.61 ± 0.01, and 2.89 ± 0.01 mg/mL, respectively. The transmittance was 98.50 ± 0.10%, and significant in vitro mucoadhesion, with reduced migration, was observed for mucin-containing gels. LTG release (96.94% at 6 h) followed the Higuchi diffusion model, with sufficient LTG released at 40 min to potentially reach the minimum effective concentration, based on in vitro release data alone. The formulation remained stable for 28 days at 4 °C and 25 °C. Chitosan-based mucoadhesive nanomicelles are a promising intranasal delivery system for LTG, with the potential for brain targeting, controlled LTG release, and improved epilepsy management.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1232-1254"},"PeriodicalIF":2.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148851212","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}

引用次数: 0

Sustained intravitreal delivery of triamcinolone acetonide via in situ forming lipid liquid crystals: in-vitro and in-vivo evaluations. 曲安奈德通过原位形成脂质液晶的持续玻璃体内传递：体外和体内评估。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-09-01 Epub Date: 2026-09-24 DOI: 10.1080/10837450.2026.2726937

Fatemeh Asgharian Rezae, Malihe Karimi, Mojtaba Abrishami, Hossein Kamali, Bizhan Malaekeh-Nikouei

{"title":"Sustained intravitreal delivery of triamcinolone acetonide via in situ forming lipid liquid crystals: in-vitro and in-vivo evaluations.","authors":"Fatemeh Asgharian Rezae, Malihe Karimi, Mojtaba Abrishami, Hossein Kamali, Bizhan Malaekeh-Nikouei","doi":"10.1080/10837450.2026.2726937","DOIUrl":"10.1080/10837450.2026.2726937","url":null,"abstract":"Posterior segment disorders remain challenging to manage due to limitations in ocular drug delivery. Although intravitreal triamcinolone acetonide (TA) is effective, it requires repeated administration, highlighting the need for sustained-release systems. This study aimed to develop in situ sustained-release formulations of TA using lipid liquid crystals (LLCs). Formulations were prepared with glyceryldioleate (GDO), phosphatidylcholine (PC), and N-methyl pyrrolidone (NMP) at PC:GDO ratios of 50:50, 40:60, and 60:40. A TA-hydroxypropyl-β-cyclodextrin (HPβCD) complex was also prepared. The formulations were characterized for rheological properties, morphology, degradation, and water uptake. In-vitro release was assessed in phosphate-buffered saline (pH 7.4), while in-vivo pharmacokinetics were evaluated in rabbits, comparing a selected LLC formulation with a TA suspension. The F5 formulation (40:60 PC: GDO) achieved sustained release of 35.4% over one month and exhibited superior stability, with 24.9% less degradation compared to F6, which showed undesirable drug crystallization. The TA-HPβCD complex demonstrated an even slower release (28%). F4 (50:50 PC: GDO) was selected as the optimized formulation, demonstrating the lowest water absorption and degradation with a consistent release profile. In-vivo studies confirmed that LLCs provided more controlled and prolonged release compared with conventional TA suspension. In conclusion, LLC-based TA formulations offer a promising strategy for sustained intravitreal drug delivery, with biodegradability, ease of preparation, and prolonged therapeutic levels.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1280-1310"},"PeriodicalIF":2.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148912084","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}

引用次数: 0

Self-assembled ufasomes of unsaturated fatty acids: mechanisms, characterization, and drug delivery potential. 不饱和脂肪酸的自组装ufasome：机制，表征和药物传递潜力。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-09-01 Epub Date: 2026-08-11 DOI: 10.1080/10837450.2026.2713500

Raghavi Bansal, Deepanshi Baloni, Manoj Kumar Mishra

{"title":"Self-assembled ufasomes of unsaturated fatty acids: mechanisms, characterization, and drug delivery potential.","authors":"Raghavi Bansal, Deepanshi Baloni, Manoj Kumar Mishra","doi":"10.1080/10837450.2026.2713500","DOIUrl":"10.1080/10837450.2026.2713500","url":null,"abstract":"Ufasomes-vesicular systems formed from long-chain unsaturated fatty acids such as oleic acid-have re-emerged as cost-effective, biocompatible alternatives to phospholipid liposomes. These bilayered assemblies self-organize at specific pH conditions and efficiently encapsulate both hydrophilic and lipophilic drugs. Their highly fluid membranes, attributed to cis-double-bond-induced structural disorder, enhance interaction with biological barriers, particularly the stratum corneum, making them valuable for topical and transdermal delivery. This review outlines the chemistry and self-assembly of ufasomes, followed by a critical appraisal of preparation techniques-including thin-film hydration and reverse-phase evaporation-and their influence on vesicle size, stability and encapsulation efficiency. Advantages such as biocompatibility, biodegradability and pH-responsive release are highlighted alongside limitations including pH-dependent instability and oxidative susceptibility. Key characterization approaches are summarized, and the therapeutic scope of ufasomes is examined, encompassing enhanced dermal delivery of antifungals and antidepressants, targeted cancer therapy, and improved oral bioavailability of nutraceuticals like oleuropein. The review concludes with emerging strategies to overcome current constraints and perspectives on advancing ufasomes toward clinical translation as versatile drug-delivery systems.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1137-1171"},"PeriodicalIF":2.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148670593","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}

引用次数: 0

Light source-dependent photooxidation of therapeutic monoclonal antibodies: a comparative study of light-emitting diode (LED) and fluorescent exposure. 光源依赖的治疗性单克隆抗体的光氧化：发光二极管（LED）和荧光暴露的比较研究。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-09-01 Epub Date: 2026-09-04 DOI: 10.1080/10837450.2026.2725579

Eva-Maria Baur, Lukas Bollenbach, Torsten Schultz-Fademrecht, Dariush Hinderberger, Michaela Blech, Patrick Garidel

{"title":"Light source-dependent photooxidation of therapeutic monoclonal antibodies: a comparative study of light-emitting diode (LED) and fluorescent exposure.","authors":"Eva-Maria Baur, Lukas Bollenbach, Torsten Schultz-Fademrecht, Dariush Hinderberger, Michaela Blech, Patrick Garidel","doi":"10.1080/10837450.2026.2725579","DOIUrl":"10.1080/10837450.2026.2725579","url":null,"abstract":"Although therapeutic proteins are susceptible to visible light-induced photooxidation, the underlying mechanisms remain unclear because amino acid residues do not directly absorb light above 400 nm. To evaluate the role of light source characteristics, three monoclonal antibodies formulated in water were exposed to spectrally distinct fluorescent and light-emitting diode (LED) sources, eliminating excipient-related effects. Following exposure to visible light (400-800 nm), degradation was assessed by size-exclusion, Protein A, and ion-exchange chromatography, together with mass spectrometry. The LED spectrum displayed a pronounced emission at 451 nm and a broad band between 480 and 800 nm, whereas the fluorescent lamp exhibited prominent emissions at 436, 545, and 612 nm, with additional blue-light contributions overlapping antibody absorption. Both light sources induced dose- and antibody-dependent photodegradation, characterized by increased high molecular weight species, Fc-oxidation, acidic and basic charge variants, and methionine and tryptophan oxidation, without detectable fragmentation. Monomer content decreased by 1-4 %, Fc-oxidized variants increased by 5-20 %, and the ion-exchange main peak decreased by 2-8 %. LED-induced degradation was less pronounced than that induced by fluorescent light, reflecting reduced short-wavelength emission. These findings support photosensitizer-mediated oxidation at 400-450 nm and highlight the importance of controlling light exposure during bioprocessing.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1197-1216"},"PeriodicalIF":2.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148851194","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}

引用次数: 0

Development and preclinical evaluation of a copper-based acidic hydrogel for atopic dermatitis. 铜基酸性水凝胶治疗特应性皮炎的研制及临床前评价。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-09-01 Epub Date: 2026-08-10 DOI: 10.1080/10837450.2026.2708938

Zhongjin Huang, Guoxin Du, Minghu Chen, Zuliang Yao, Bo Liang, Fei Ren

{"title":"Development and preclinical evaluation of a copper-based acidic hydrogel for atopic dermatitis.","authors":"Zhongjin Huang, Guoxin Du, Minghu Chen, Zuliang Yao, Bo Liang, Fei Ren","doi":"10.1080/10837450.2026.2708938","DOIUrl":"10.1080/10837450.2026.2708938","url":null,"abstract":"Atopic dermatitis (AD) features impaired skin barrier, elevated cutaneous pH, and Staphylococcus aureus overcolonization. Restoring acidic skin pH while suppressing microbial overgrowth represents a promising non-steroidal strategy. To develop a copper-based acidic hydrogel and evaluate its properties, antimicrobial activity, efficacy, and safety. A hydrogel with 0.115% copper ions was prepared from basic copper carbonate, acetic acid (6% w/w), and xanthan gum, formulated at a final pH of ∼3.2, and characterized by rheology and stability testing. Antimicrobial activity was evaluated by a quantitative carrier test against S. aureus, E. coli, and C. albicans. Efficacy was assessed in DNFB-induced AD-like BALB/c mice. Dermal safety was examined in a 14-day study in rabbits. The hydrogel showed gel-like behavior (G' > G″) with 94.6% structural recovery and remained stable over 23 months. It achieved >98% killing of all pathogens within 5 min and >99.6% within 10 min. In mice, treatment dose-dependently reduced ear swelling and dermatitis scores, attenuated epidermal hyperplasia, and decreased mast cell infiltration. In rabbits, only mild, reversible local irritation occurred, without systemic toxicity. This copper-based acidic hydrogel exhibits potent broad-spectrum antimicrobial activity, ameliorates AD-like lesions, and shows a favorable short-term dermal safety profile, supporting further development as a non-steroidal topical option for AD.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1126-1136"},"PeriodicalIF":2.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148685508","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}

引用次数: 0

Solid modification strategies for active pharmaceutical ingredients (APIs): a systematic review on approaches, improvements, and limitations. 活性药物成分（api）固体改性策略：方法、改进和局限性的系统综述。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-09-01 Epub Date: 2026-09-20 DOI: 10.1080/10837450.2026.2725578

George Patrick Devon, Dzava Prawinsyah Fairus Ismail, Jenio Lagut, Iyan Sopyan

{"title":"Solid modification strategies for active pharmaceutical ingredients (APIs): a systematic review on approaches, improvements, and limitations.","authors":"George Patrick Devon, Dzava Prawinsyah Fairus Ismail, Jenio Lagut, Iyan Sopyan","doi":"10.1080/10837450.2026.2725578","DOIUrl":"10.1080/10837450.2026.2725578","url":null,"abstract":"Poor aqueous solubility remains a major barrier in drug development, affecting approximately 40% of marketed drugs, up to 75% of drugs under development, and nearly 90% of new chemical entities. To overcome this limitation, solid modification of active pharmaceutical ingredients (APIs) emerged as a strategy to enhance drug physicochemical properties, particularly for Biopharmaceutics Classification System (BCS) II and IV drugs. This review systematically analyzes recent advancements in solid modification techniques, including salt formation, cocrystallization, polymorphs, solvate and hydrate forms, amorphous and co-amorphous systems, inclusion complexes, and nanocrystallization. A systematic literature search spanning 2020-2025 was conducted using PubMed and ScienceDirect databases, focusing on studies that improve the physicochemical properties of the APIs. By categorizing APIs, matrices, and methods of each study, this review shows the most frequently used techniques and their matrices, advantages, and limitations of each modification, providing insights for optimizing drug performance and future research in pharmaceutical development. Among the various approaches reviewed, cocrystals, amorphous systems, nanocrystals, and inclusion complexes emerged as the most frequently used techniques. Amorphous systems and inclusion complexes offer the highest median solubility enhancements by maximizing kinetic supersaturation or equilibrium solubility, respectively, while nanocrystals efficiently improve equilibrium solubility via particle size reduction, and cocrystals provide reliable, moderate gains with superior long-term thermodynamic stability.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1172-1196"},"PeriodicalIF":2.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149002222","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}

引用次数: 0

Innovative hybrid microneedle patch for co-delivery of varenicline and melatonin: development, characterization, and potential for smoking cessation. 联合给药伐尼克兰和褪黑素的创新混合微针贴片：开发、表征和戒烟潜力。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-09-01 Epub Date: 2026-09-08 DOI: 10.1080/10837450.2026.2726936

Mohammad Hassan Shahriari, Hossein Salmani, Mohammad Adel Ghiass, Nader Kamali, Atefeh Malek-Khatabi, Hussein Abdelamir Mohammad, Saba Saei, Mohammad Akrami

{"title":"Innovative hybrid microneedle patch for co-delivery of varenicline and melatonin: development, characterization, and potential for smoking cessation.","authors":"Mohammad Hassan Shahriari, Hossein Salmani, Mohammad Adel Ghiass, Nader Kamali, Atefeh Malek-Khatabi, Hussein Abdelamir Mohammad, Saba Saei, Mohammad Akrami","doi":"10.1080/10837450.2026.2726936","DOIUrl":"10.1080/10837450.2026.2726936","url":null,"abstract":"Smoking cessation remains a therapeutic challenge, and limitations associated with conventional oral varenicline therapy may affect patient adherence. This study aimed to develop and characterize a dissolving microneedle patch co-loaded with varenicline and melatonin for transdermal delivery. Microneedle arrays were fabricated using polyvinyl alcohol (PVA) and polyvinylpyrrolidone (PVP), with Tween-80 incorporated to enhance the solubility of varenicline. The fabricated microneedles were evaluated for their mechanical and surface properties using nanoindentation, scratch testing, and atomic force microscopy. In vitro drug release and transdermal permeation studies were performed, while fluorescence imaging and histological analysis were used to assess microneedle insertion and skin integrity. The microneedles exhibited adequate hardness and flexibility, together with a uniform surface morphology, supporting effective penetration into the skin. Following 48 h of application, cumulative transdermal permeation of varenicline and melatonin reached 34.3% and 41.6%, respectively. The co-loaded microneedle formulation provided sustained release of both drugs over the study period. Histological evaluation confirmed the formation of discrete microchannels following microneedle insertion without significant disruption of the surrounding tissue. Overall, the findings demonstrate the feasibility of a varenicline-melatonin-loaded microneedle patch as a transdermal drug-delivery system for smoking cessation. Further investigation, including comparison with established commercial therapies and ex vivo dissolution and permeation studies, is warranted to establish its translational potential.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1255-1279"},"PeriodicalIF":2.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148840586","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}

引用次数: 0

Soft gelatin capsules and die roll engineering: a comprehensive review of die roll designs, global manufacturing technologies, sealing mechanisms, encapsulation machine advances, advantages, and limitations. 软明胶胶囊和模卷工程：模卷设计、全球制造技术、密封机制、包封机的进步、优点和局限性的综合综述。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-09-01 Epub Date: 2026-09-12 DOI: 10.1080/10837450.2026.2726933

Senthilraja Kaliyamoorthy

{"title":"Soft gelatin capsules and die roll engineering: a comprehensive review of die roll designs, global manufacturing technologies, sealing mechanisms, encapsulation machine advances, advantages, and limitations.","authors":"Senthilraja Kaliyamoorthy","doi":"10.1080/10837450.2026.2726933","DOIUrl":"10.1080/10837450.2026.2726933","url":null,"abstract":"Soft gelatin capsules (softgels) are among the most commercially significant oral dosage forms, offering hermetic liquid and semi-solid encapsulation with superior bioavailability. Central to their manufacture is the rotary die encapsulation process, in which precision die rolls simultaneously form, fill, and seal capsules from two gelatin ribbons. Despite its critical role in determining seam integrity, leakage resistance, and efficiency, a comprehensive peer-reviewed analysis of die roll design classifications has not been published previously. This review analyses seven principal designs: single-step (uni-lip), double-step (bi-lip), D-Step Outer (DS-O), D-Step Inner (DS-I), triple-step (tri-lip), Max Offset Seal (MOS), and blasted surface. For each design, the mechanistic basis, application domain, advantages, limitations, and quality implications are examined. Special attention is given to the MOS architecture for trailing-edge seam asymmetry in suspension fills, the DS-I configuration for moisture-sensitive active pharmaceutical ingredients, and the glass bead-blasted surface for universal pinhole leakage mitigation. A global survey of encapsulation machine and die roll manufacturers-including Changsung, Technophar, Schaefer Technologies, United Pharmatek, Joysun, SEC Softgel, Hedagel, SKY Softgel, CapPlus Technologies, and AIPAK/SaintyCo-is presented (Table 2). Five comparative tables and six annotated figure placeholders cover die roll specifications, process parameters, service life, troubleshooting, and advantages versus limitations. Regulatory considerations under ICH Q8/Q9/Q10, FDA 21 CFR 314.70, and GCC/SFDA frameworks are discussed. Future directions include digital twin simulation, AI-assisted die design, and additive manufacturing tooling. This review serves as an authoritative reference for die roll selection, optimisation, troubleshooting, and regulatory lifecycle management.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1217-1231"},"PeriodicalIF":2.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148866402","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}

引用次数: 0

Sustained oral drug delivery using PEGylated liposomes incorporated into polysaccharide hydrogel formulations. 持续口服药物递送使用聚乙二醇化脂质体纳入多糖水凝胶制剂。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-09-01 Epub Date: 2026-09-11 DOI: 10.1080/10837450.2026.2729443

Sora Nishida, Eriko Yamazoe, Takaaki Ito, Kohei Tahara

{"title":"Sustained oral drug delivery using PEGylated liposomes incorporated into polysaccharide hydrogel formulations.","authors":"Sora Nishida, Eriko Yamazoe, Takaaki Ito, Kohei Tahara","doi":"10.1080/10837450.2026.2729443","DOIUrl":"10.1080/10837450.2026.2729443","url":null,"abstract":"In this study, PEGylated liposomes (PEG-Lip) were combined with polysaccharides to sustain their oral absorption-enhancing effect. PEG-Lip was prepared by the thin-film hydration method and mixed with carrageenan (CGN), xanthan gum (XG), or locust bean gum (LBG). The prepared PEG-Lip had a particle size of ∼100 nm and a zeta potential of approximately -50 mV. The polysaccharide concentrations that did not inhibit PEG-Lip behavior were 0.5% for CGN and 0.25% for XG and XG-LBG mixtures. At 25 °C, the release of PEG-Lip from each polysaccharide was generally consistent with its diffusion within the polysaccharide. In the rheological evaluation, only XG3-LBG7, a 3:7 mixture of XG and LBG, exhibited gel-like behavior, whereas the other formulations functioned as viscosity modifiers. Oral administration in rats showed improved gastrointestinal retention compared with PEG-Lip alone. Furthermore, XG3-LBG7 provided the greatest improvement in the oral absorption of FITC-dextran (FD4). These findings suggest that optimizing both PEG-Lip release and the rheological properties of polysaccharides is important for improving oral absorption.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1311-1324"},"PeriodicalIF":2.9,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148892376","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}

引用次数: 0