AAPS PharmSciTech最新文献

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Advancement in Sodium Alginate-Based Drug Delivery Systems: Applications and Future Prospects 海藻酸钠基给药系统的研究进展:应用与展望
IF 4 4区 医学
AAPS PharmSciTech Pub Date : 2026-05-05 DOI: 10.1208/s12249-025-03284-4
Anjali Kumari, Bonthu Varunteja, Satyajit Mohanty, Anjali Mishra, Nayan Gupta, Tuhin Mukherjee, Bhawna Sharma, Nikita Nayak, Anwesha Sahu, Ashok Pattnaik, Pranav Kumar Prabhakar, Uttam Kumar Mishra
{"title":"Advancement in Sodium Alginate-Based Drug Delivery Systems: Applications and Future Prospects","authors":"Anjali Kumari,&nbsp;Bonthu Varunteja,&nbsp;Satyajit Mohanty,&nbsp;Anjali Mishra,&nbsp;Nayan Gupta,&nbsp;Tuhin Mukherjee,&nbsp;Bhawna Sharma,&nbsp;Nikita Nayak,&nbsp;Anwesha Sahu,&nbsp;Ashok Pattnaik,&nbsp;Pranav Kumar Prabhakar,&nbsp;Uttam Kumar Mishra","doi":"10.1208/s12249-025-03284-4","DOIUrl":"10.1208/s12249-025-03284-4","url":null,"abstract":"<div><p>For over five decades, sodium alginate (SA) has been widely employed in pharmaceutical formulations due to its environmentally friendly, biodegradable, and biocompatible nature. Primarily sourced from brown seaweed, this natural polymer plays a crucial role in enhancing drug delivery control. It serves as a versatile excipient in numerous dosage forms such as capsules, tablets, liposomes, and microspheres. SA ionotropic gelation with calcium ions allows drug and enzyme encapsulation for controlled release. Structurally, SA consists of α-L-guluronic acid and β-D-mannuronic acid monomers linked via glycosidic bonds, enabling the formation of strong, porous hydrogels capable of carrying bioactive substances. These hydrogels have been extensively utilized in ocular and oral drug delivery systems for prolonged therapeutic effect. This review highlights the structural and physicochemical characteristics of SA, its pharmaceutical and biomedical applications, food industry relevance, and recent innovations, while also discussing its potential as a multifunctional material for future drug delivery systems.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture><span>The alternative text for this image may have been generated using AI.</span></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 4","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-05-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147829163","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
Cyclodextrins: Synthesis, Pharmaceutical Applications, Drug Delivery Systems and Safety Perspectives 环糊精:合成,药物应用,给药系统和安全性展望
IF 4 4区 医学
AAPS PharmSciTech Pub Date : 2026-05-04 DOI: 10.1208/s12249-026-03400-y
Aman Kumar, Ravi Raj Pal, Preeti Patel, Atul Jain, Nitin Sharma, Umesh Kumar Patil, Balak Das Kurmi
{"title":"Cyclodextrins: Synthesis, Pharmaceutical Applications, Drug Delivery Systems and Safety Perspectives","authors":"Aman Kumar,&nbsp;Ravi Raj Pal,&nbsp;Preeti Patel,&nbsp;Atul Jain,&nbsp;Nitin Sharma,&nbsp;Umesh Kumar Patil,&nbsp;Balak Das Kurmi","doi":"10.1208/s12249-026-03400-y","DOIUrl":"10.1208/s12249-026-03400-y","url":null,"abstract":"<div><p>Cyclodextrins (CDs) are cyclic oligosaccharides composed of α-(1,4)-linked glucopyranose units that have emerged as multifunctional and versatile pharmaceutical excipients. One of the major challenges in modern drug development is that nearly half of newly discovered drug molecules exhibit poor aqueous solubility, which adversely affects formulation development, bioavailability, and therapeutic efficacy. CDs address this limitation by forming non-covalent inclusion and non-inclusion complexes, thereby enhancing drug solubility, stability, dissolution rate, and overall biopharmaceutical performance. This review provides a comprehensive overview of CDs, including their historical background, structural characteristics, and production through starch conversion by the enzyme cyclodextrin glucanotransferase (CGTase). Special emphasis is placed on the transglycosylation reactions catalyzed by CGTase, including cyclization, coupling, and disproportionation, which play a critical role in CD synthesis. Recent advances in structural elucidation techniques, such as X-ray crystallography, nuclear magnetic resonance spectroscopy, molecular dynamics simulations, and ion mobility mass spectrometry, are also discussed. The pharmaceutical applications of CDs are critically evaluated, with particular emphasis on their roles as solubility enhancers, taste-masking agents, and stabilizers in nanocarrier-based and targeted drug delivery systems. Their applications in cosmetics and dermopharmaceuticals are also explored, particularly in improving formulation stability and enabling controlled drug delivery. Furthermore, the pharmacokinetics, toxicological safety, and regulatory acceptability of various CDs are discussed. Overall, this review highlights the growing importance of CDs as pharmaceutical excipients that bridge supramolecular chemistry and advanced drug delivery systems.</p><h3>Graphical Abstract</h3><p>Illustration of (a) production of CDs from starch via transglycosylation reactions catalyzed by CGTase through four reaction mechanisms, i.e., disproportion, coupling, cyclization, and hydrolysis, (b) their pharmaceutical, targeted delivery, and dermopharmaceutical applications are also illustrated here.</p><div><figure><div><div><picture><source><img></source></picture><span>The alternative text for this image may have been generated using AI.</span></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 4","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147829356","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 of a New Aerosol Delivery System for Administering Aerosol Surfactant Therapy to Preterm Infants Through a Laryngeal Mask Airway 一种新的气溶胶输送系统的发展,用于通过喉罩气道给早产儿施用气溶胶表面活性剂治疗
IF 4 4区 医学
AAPS PharmSciTech Pub Date : 2026-04-24 DOI: 10.1208/s12249-026-03421-7
Sarah C. Strickler, Caleb J. Dalton, Felicia G. Hall, Dale R. Farkas, Mohammad A. M. Momin, Robert M. DiBlasi, Michael Hindle, P. Worth Longest
{"title":"Development of a New Aerosol Delivery System for Administering Aerosol Surfactant Therapy to Preterm Infants Through a Laryngeal Mask Airway","authors":"Sarah C. Strickler,&nbsp;Caleb J. Dalton,&nbsp;Felicia G. Hall,&nbsp;Dale R. Farkas,&nbsp;Mohammad A. M. Momin,&nbsp;Robert M. DiBlasi,&nbsp;Michael Hindle,&nbsp;P. Worth Longest","doi":"10.1208/s12249-026-03421-7","DOIUrl":"10.1208/s12249-026-03421-7","url":null,"abstract":"<div><p>In this study, aerosol surfactant therapy administered through a laryngeal mask airway (LMA) was investigated as an alternative to the more invasive approach of surfactant liquid bolus instillation, which carries significant risks to infants with respiratory distress syndrome. Combining a recently developed synthetic lung surfactant excipient enhanced growth (SLS-EEG) dry powder formulation with a novel LMA aerosol delivery system (LMA-ADS) was intended to avoid the side effects associated with current liquid bolus therapies. A new patient connection system (PCS) was developed for introducing the aerosol from an infant air-jet DPI into the LMA. Using <i>in vitro</i> benchtop studies with a 1.5 kg preterm infant extrathoracic model, the effectiveness of a co-flow (CF) strategy was investigated for improving lung delivery efficiencies of the aerosol. Next, different tubing sizes and aerosolization parameters were explored using laser diffraction to quantify their effects on aerosol size distribution metrics, and insights gained were implemented to develop four PCS designs. The best-performing PCS was tested with a realistic pulmonary mechanics (PM) model. Large-diameter tubing (&gt; 1 mm diameter) was shown to produce large aerosol size increases that could be minimized with smaller-diameter tubing. Following integration of 0.8 mm inner diameter tubing, all PCS designs were capable of at least ~ 24% lung delivery efficiency (based on loaded dose) with the best-performing PCS reaching ~ 29%, which represented a &gt; 1.7-fold improvement from baseline. PM simulations confirmed safe delivery pressures with only minor reductions in aerosol transmission. Therefore, the LMA-ADS could be a promising alternative for effective aerosol surfactant therapies.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture><span>The alternative text for this image may have been generated using AI.</span></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 4","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1208/s12249-026-03421-7.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147738555","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}
引用次数: 0
Emerging and Prospective Engineering Technologies Enabling Microneedle Based Vaccine Therapeutics 实现基于微针的疫苗治疗的新兴和前瞻性工程技术
IF 4 4区 医学
AAPS PharmSciTech Pub Date : 2026-04-23 DOI: 10.1208/s12249-026-03409-3
N. Ahmad, N. A. Jalil, R. Benziane, H. Iqbal, S. J. Rana, T. AbuAin, A. Al-Asiri, A. T. Kola-Mustapha, M.S. Arshad, Z. Ahmad
{"title":"Emerging and Prospective Engineering Technologies Enabling Microneedle Based Vaccine Therapeutics","authors":"N. Ahmad,&nbsp;N. A. Jalil,&nbsp;R. Benziane,&nbsp;H. Iqbal,&nbsp;S. J. Rana,&nbsp;T. AbuAin,&nbsp;A. Al-Asiri,&nbsp;A. T. Kola-Mustapha,&nbsp;M.S. Arshad,&nbsp;Z. Ahmad","doi":"10.1208/s12249-026-03409-3","DOIUrl":"10.1208/s12249-026-03409-3","url":null,"abstract":"<div><p>Microneedles (MNs) have progressed to a potentially viable method of transdermal vaccination and have accrued immense attention in recent years. By overcoming first-pass metabolism, this emerging technology elicits efficacious therapeutic effects and improved patient compliance. Various technologies and material compositions have been explored to enable drug delivery including solid, coated, dissolving, hollow and hydrogel-forming MNs. In progressive science, there are several emerging engineering techniques that have been used to fabricate MNs for use in drug delivery and aligning therapies, including (not limited to) micromoulding, 3D printing, aerosol jet printing and various electrohydrodynamic strategies. These explorations have yielded promising outcomes in terms of facile MN manufacturing, processing, enhanced mechanical features, applicability (self-administered), portability and therapeutic efficiency. More recently, emerging engineering aspects (e.g. 3D printing, various laser-based techniques and electrospray technology) have been adapted to develop MN vaccine platforms or demonstrate potential in this remit, adding to more established MN vaccine engineering platforms (e.g. micrmoulding). Such developments are viewed as crucial; firstly, to eliminate/reduce the spread of infection as the emergence and occurrence of outbreaks increase, and secondly, to limit the strain on national healthcare systems which rely heavily upon assisted vaccine administration. This review focuses on selected, up-to-date developments and progression of engineering MN technologies/devices into MN vaccine therapeutic platforms. It also embraces specific examples, highlighting applicability and adaptability of existing technologies, with current advances shown and future scope highlighted.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture><span>The alternative text for this image may have been generated using AI.</span></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 4","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-04-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1208/s12249-026-03409-3.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147737859","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}
引用次数: 0
A Quality-by-Design Approach Based Formulation, Optimization, In Vitro and Ex Vivo Evaluation of Delafloxacin-Loaded Ethosomal Gel 基于质量设计法的德拉沙星运载体凝胶的处方、优化及体外、离体评价
IF 4 4区 医学
AAPS PharmSciTech Pub Date : 2026-04-23 DOI: 10.1208/s12249-026-03433-3
Deesha Jain, Devaraj Yallappa, Modhusmita Gogoi, Kunal Gonage, Sapan Borah, Aakanchha Jain
{"title":"A Quality-by-Design Approach Based Formulation, Optimization, In Vitro and Ex Vivo Evaluation of Delafloxacin-Loaded Ethosomal Gel","authors":"Deesha Jain,&nbsp;Devaraj Yallappa,&nbsp;Modhusmita Gogoi,&nbsp;Kunal Gonage,&nbsp;Sapan Borah,&nbsp;Aakanchha Jain","doi":"10.1208/s12249-026-03433-3","DOIUrl":"10.1208/s12249-026-03433-3","url":null,"abstract":"<div><p>The current work aims to fabricate and examine a delafloxacin (DFX)-loaded ethosomal (ETHs) gel for improved topical delivery and improved antibacterial efficiency against skin infections. ETHs were prepared using the cold method followed by two-stage homogenization, involving vesicle fabrication and subsequent gel conversion. A Quality by Design framework was employed, with initial screening using a fractional factorial design and optimization through a Box–Behnken design. Entrapment efficiency (EnE), Vesicle size, and PDI were chosen as critical quality attributes. The optimized nanoformulation was evaluated for size, morphology, drug release, cytotoxicity, irritation potential, <i>ex vivo</i> studies antimicrobial activity, and skin safety. The optimized DFX-ETHs exhibited a vesicle size of 263.6 ± 3 nm, zeta potential of − 5.99 ± 1.466 mV, PDI of 0.173 ± 0.019, and EnE of 90.17 ± 0.14%. FE-SEM confirmed globular vesicles with a smooth surface. The formulation showed sustained drug release following Weibull kinetics. Cytotoxicity studies on NIH/3T3 cells and irritation studies using HET-CAM and rat skin models confirmed the cytocompatible and non-irritant nature of the formulation. Enhanced antimicrobial activity against <i>Staphylococcus aureus</i> and <i>Cutibacterium acnes</i> was observed compared to DFX dispersion. The <i>ex vivo</i> studies results showed that the ETHs formulation significantly improved drug permeation relative to the free DFX. The results demonstrate that ethosomal gel systems are a potential and safe carrier for the topical application of DFX, offering improved antibacterial efficacy against bacterial skin infections.</p><h3>Graphical Abstract</h3><p>Illustrates the development of delafloxacin-loaded ethosomes followed by comprehensive characterization, including particle size and zeta potential analysis, SEM imaging, and <i>in vitro</i> drug release studies. Further, the formulated ethosomal gel was evaluated for rheological behavior, antibacterial efficacy, and skin irritation, demonstrating its potential as an effective topical delivery system</p>\u0000<div><figure><div><div><picture><source><img></source></picture><span>The alternative text for this image may have been generated using AI.</span></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 4","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-04-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147738538","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
Liposome-Based Drug Delivery Systems: Mechanisms, Preparation Strategies, Clinical Status, and Therapeutic Applications 基于脂质体的药物传递系统:机制、制备策略、临床状况和治疗应用
IF 4 4区 医学
AAPS PharmSciTech Pub Date : 2026-04-23 DOI: 10.1208/s12249-026-03425-3
Abdul Shadab, Md. Faheem Haider, Mohammad Abohassan
{"title":"Liposome-Based Drug Delivery Systems: Mechanisms, Preparation Strategies, Clinical Status, and Therapeutic Applications","authors":"Abdul Shadab,&nbsp;Md. Faheem Haider,&nbsp;Mohammad Abohassan","doi":"10.1208/s12249-026-03425-3","DOIUrl":"10.1208/s12249-026-03425-3","url":null,"abstract":"<div><p>Nanotechnology-based drug delivery systems have significantly advanced modern pharmaceutics by addressing limitations associated with conventional therapies, including poor solubility, rapid systemic clearance, and nonspecific drug distribution. Among various nanocarriers, liposomes remain one of the most clinically validated platforms due to their biocompatibility, structural similarity to biological membranes, and capacity to encapsulate both hydrophilic and lipophilic drugs. Despite extensive research, important translational challenges persist, including formulation stability, variability in tumor targeting via the EPR effect, manufacturing scalability, and immunogenicity associated with repeated dosing. This review provides an integrated and critical overview of liposome-based drug delivery systems, combining mechanistic insights, formulation design principles, preparation technologies, and clinical translation perspectives within a single framework. Particular emphasis is placed on recent advances in liposomal engineering <b>strategies,</b> including surface modification, stimuli-responsive systems, and scalable manufacturing approaches such as microfluidics. Clinically established formulations such as Doxil® and AmBisome® are highlighted as representative examples demonstrating improved therapeutic efficacy and reduced toxicity compared with conventional formulations. In addition, the review discusses emerging trends in next-generation liposomal systems, including targeted liposomes, RNA-delivery platforms, and hybrid lipid–polymer vesicles. By integrating formulation science with translational considerations and recent developments (2022–2025), this review provides an updated perspective on the evolving role of liposomes in nanomedicine and highlights key directions for future research and clinical development.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture><span>The alternative text for this image may have been generated using AI.</span></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 4","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-04-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147737860","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
Hybrid Photometric–Geometric 3D Reconstruction Framework for Manufacturing-Oriented Assessment of Tablet Surface CQAs under PAT/RTRT PAT/RTRT下面向制造的片剂表面cqa评价的混合光度-几何三维重建框架
IF 4 4区 医学
AAPS PharmSciTech Pub Date : 2026-04-23 DOI: 10.1208/s12249-026-03435-1
Phakdee Sukpornsawan, Jakkarin Suksawatchon, Watcharaphong Chaemsawang, Somchart Chokchaitam, Ureerat Suksawatchon
{"title":"Hybrid Photometric–Geometric 3D Reconstruction Framework for Manufacturing-Oriented Assessment of Tablet Surface CQAs under PAT/RTRT","authors":"Phakdee Sukpornsawan,&nbsp;Jakkarin Suksawatchon,&nbsp;Watcharaphong Chaemsawang,&nbsp;Somchart Chokchaitam,&nbsp;Ureerat Suksawatchon","doi":"10.1208/s12249-026-03435-1","DOIUrl":"10.1208/s12249-026-03435-1","url":null,"abstract":"<p>Surface-related critical quality attributes (CQAs) of solid oral dosage forms influence mechanical integrity, coating uniformity, imprint readability, and downstream product performance. Conventional two-dimensional visual inspection and geometry-focused three-dimensional (3D) systems primarily assess gross deviations but often lack mechanistic surface descriptors relevant to CQA interpretation. This study tested the hypothesis that integrating complementary photometric and geometric imaging modalities can enhance sensitivity to surface-related CQAs beyond single-modality inspection. A hybrid photometric–geometric reconstruction framework was developed for manufacturing-oriented surface integrity assessment. A hybrid photometric–geometric 3D reconstruction pipeline integrating photometric stereo and structured-light acquisition captured complementary local reflectance and global geometric information. Depth maps derived from both modalities were spatially aligned and fused to generate a unified surface representation. Surface descriptors, including curvature entropy and roughness metrics, were evaluated to assess surface complexity and stability. Micro-defect detectability was examined to compare reconstruction modalities under controlled experimental conditions. The hybrid reconstruction approach demonstrated improved balance between local imprint fidelity and global surface continuity compared with single-modality methods, while maintaining reproducible surface metrics across repeated sessions. Surface descriptors provided structured measures of surface variation beyond visual inspection alone. The proposed framework is positioned as a CQA-linked surface anomaly assessment tool within a Process Analytical Technology (PAT) context, rather than as a direct surrogate for traditional release testing. By enhancing mechanistic interpretation of surface variability, the approach may support risk-based PAT strategies in manufacturing. This proof-of-concept study used a small dataset (n = 4), requiring further validation with larger, diverse samples.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 4","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-04-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147738556","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
Integrative Perspectives on Pirfenidone: Mechanistic Insights, Pharmacodynamics, and Emerging Therapeutic Strategies for Fibrotic Disorders 吡非尼酮的综合观点:纤维化疾病的机制、药效学和新兴治疗策略
IF 4 4区 医学
AAPS PharmSciTech Pub Date : 2026-04-22 DOI: 10.1208/s12249-026-03429-z
Abhidnya Kudterkar, Sarika Wairkar
{"title":"Integrative Perspectives on Pirfenidone: Mechanistic Insights, Pharmacodynamics, and Emerging Therapeutic Strategies for Fibrotic Disorders","authors":"Abhidnya Kudterkar,&nbsp;Sarika Wairkar","doi":"10.1208/s12249-026-03429-z","DOIUrl":"10.1208/s12249-026-03429-z","url":null,"abstract":"<div><p>Pirfenidone is a synthetic pyridone derivative that is primarily beneficial in treating idiopathic pulmonary fibrosis (IPF). Initially synthesized as an anti-inflammatory agent, it was later identified as the first oral antifibrotic therapy to improve progression-free survival in IPF, with an acceptable safety profile. Mechanistically, pirfenidone inhibits fibroblast proliferation, extracellular matrix deposition, and pro-inflammatory cytokine release by modulating the transforming growth factor-β (TGF-β) and its downstream pathways. Beyond IPF, emerging evidence suggests therapeutic potential across various fibrotic disorders related to aging, including systemic sclerosis-associated interstitial lung disease, cardiac fibrosis, uterine fibrosis, corneal fibrosis, liver fibrosis, intestinal fibrosis, wound healing, and lung cancer. However, high dose requirements and adverse events such as gastrointestinal intolerance and photosensitivity remain limiting factors of pirfenidone. To address these limitations, novel delivery systems, including lipid carriers, polymeric formulations, and other advanced systems, have been developed to enhance bioavailability, enable site-specific targeting, and sustain drug release over time. These developments underscore the evolving role of pirfenidone as a versatile antifibrotic therapy in the aging population with significant translational applications.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture><span>The alternative text for this image may have been generated using AI.</span></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 4","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147738617","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
Formulation-Based Repurposing of Mifepristone Using a Drug-Eluting Intrauterine Insert for Localized Uterine Fibroid Therapy: A Preclinical Study 基于配方的米非司酮再利用药物洗脱宫内插入物治疗局部子宫肌瘤:一项临床前研究
IF 4 4区 医学
AAPS PharmSciTech Pub Date : 2026-04-21 DOI: 10.1208/s12249-026-03404-8
Riya Patel, Alkesh Patel, Gayatri Patel
{"title":"Formulation-Based Repurposing of Mifepristone Using a Drug-Eluting Intrauterine Insert for Localized Uterine Fibroid Therapy: A Preclinical Study","authors":"Riya Patel,&nbsp;Alkesh Patel,&nbsp;Gayatri Patel","doi":"10.1208/s12249-026-03404-8","DOIUrl":"10.1208/s12249-026-03404-8","url":null,"abstract":"<div><p>The majority of currently available treatments for uterine fibroids (UFs) are invasive and are delivered via either oral or parenteral means. Mifepristone (MFP), a particular drug that alters the activity of progesterone receptors, is selected as the preferred treatment. Presently, it is used for the purpose of inducing abortion. Recent clinical trials have demonstrated that MFP effectively reduces the size of UFs. This study proposes the use of MFP for repurposing UF. The objective of this study was to develop a drug-eluting intrauterine insert (DE-IUI) containing MFP and investigate its effectiveness in targeting the uterus via the intrauterine route. A biodegradable insert with a capsule-like shape was developed using the melting process. The drug exhibited a release rate of 45–50% within a 15-day period, achieving the desired level of degradation. The preclinical <i>in vivo</i> findings demonstrated that the biodegradation of DE-IUI resulted in a substantial decrease in the size of the UF. The MFP-insert was effectively developed and assessed for repurposing to treat UF by targeting the uterus through the vaginal route. Targeted drug delivery to the site of action allows for a decrease in dose, maintaining the desired therapeutic effect and mitigating the side effects associated with current treatments.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture><span>The alternative text for this image may have been generated using AI.</span></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 4","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-04-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147738078","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
Smart In Situ-Forming Ocular Therapeutics for Dry Eye Disease: Bridging Biomaterials, Nanotechnology, and Clinical Translation 干眼病的智能眼疗法:桥接生物材料、纳米技术和临床转化。
IF 4 4区 医学
AAPS PharmSciTech Pub Date : 2026-04-20 DOI: 10.1208/s12249-026-03420-8
Adiba Rahman, Poonam Kushwaha, Bipasha Ray, Sapna Yadav
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