AAPS PharmSciTech最新文献

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Retraction Note: Bi-polymeric Spongy Matrices Through Cross-linking Polymerization: Synthesized and Evaluated for Solubility Enhancement of Acyclovir 通过交联聚合的双聚海绵状基质:合成和评价阿昔洛韦的溶解度增强。
IF 5.1 4区 医学
AAPS PharmSciTech Pub Date : 2026-07-13 DOI: 10.1208/s12249-026-03497-1
Saima Asghar, Naveed Akhtar, Muhammad Usman Minhas, Kifayat Ullah Khan
{"title":"Retraction Note: Bi-polymeric Spongy Matrices Through Cross-linking Polymerization: Synthesized and Evaluated for Solubility Enhancement of Acyclovir","authors":"Saima Asghar, Naveed Akhtar, Muhammad Usman Minhas, Kifayat Ullah Khan","doi":"10.1208/s12249-026-03497-1","DOIUrl":"10.1208/s12249-026-03497-1","url":null,"abstract":"","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 5","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-07-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148434742","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
Correction: Scrutinizing the Feasibility of Nonionic Surfactants to Form Isotropic Bicelles of Curcumin: a Potential Antiviral Candidate Against COVID-19 更正:仔细研究非离子表面活性剂形成姜黄素各向同性小束的可行性:一种潜在的抗病毒候选药物,用于对抗COVID-19。
IF 5.1 4区 医学
AAPS PharmSciTech Pub Date : 2026-07-10 DOI: 10.1208/s12249-026-03470-y
Dina B. Mahmoud, Mohamed Mofreh Bakr, Ahmed A. Al-karmalawy, Yassmin Moatasim, Ahmed El Taweel, Ahmed Mostafa
{"title":"Correction: Scrutinizing the Feasibility of Nonionic Surfactants to Form Isotropic Bicelles of Curcumin: a Potential Antiviral Candidate Against COVID-19","authors":"Dina B. Mahmoud, Mohamed Mofreh Bakr, Ahmed A. Al-karmalawy, Yassmin Moatasim, Ahmed El Taweel, Ahmed Mostafa","doi":"10.1208/s12249-026-03470-y","DOIUrl":"10.1208/s12249-026-03470-y","url":null,"abstract":"","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 5","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1208/s12249-026-03470-y.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148417710","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
The Role of Contract Manufacturing in Antibody–Drug Conjugate (ADC) Drug Substance Development – Strategies for Successful Engagement 合同制造在抗体-药物偶联物(ADC)原料药开发中的作用——成功参与的策略。
IF 5.1 4区 医学
AAPS PharmSciTech Pub Date : 2026-07-09 DOI: 10.1208/s12249-026-03466-8
Conor S. Barry
{"title":"The Role of Contract Manufacturing in Antibody–Drug Conjugate (ADC) Drug Substance Development – Strategies for Successful Engagement","authors":"Conor S. Barry","doi":"10.1208/s12249-026-03466-8","DOIUrl":"10.1208/s12249-026-03466-8","url":null,"abstract":"<div><p>Antibody–Drug Conjugates (ADCs) represent a rapidly evolving, and increasingly important frontier in targeted therapeutics, demanding specialised approaches to development and manufacturing. With a highly complex supply chain, specialist Contract Development and Manufacturing Organisations (CDMOs) play a critical role in ADC development. Increasingly, positive CDMO partnerships with sponsor companies can build competitive advantage in an increasingly innovative and competitive clinical development environment for ADCs. Carefully considered CDMO engagement strategies can be employed to deliver successful outcomes for ADC development and manufacture across the full spectrum of the development life-cycle. This commentary considers early and late-stage ADC development, focusing on the systematic optimisation, technology transfer, and gap analysis essential for robust scale-up and manufacture. Facility design requirements and process modifications are discussed in the context of scalable, cGMP-compliant manufacturing, highlighting the engineering and environmental controls necessary for the safe and efficient handling of ADCs. The discussion will offers insights into the requirements for successful ADC development and manufacture with CDMO partners, while ensuring, regulatory compliance.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 5","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-07-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1208/s12249-026-03466-8.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148417797","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 Review on Nanocarrier-Based Strategies for Sunitinib Delivery: Advances in Pharmacokinetic Enhancement and Targeted Theranostics 基于纳米载体的舒尼替尼给药策略综述:药代动力学增强和靶向治疗的进展。
IF 5.1 4区 医学
AAPS PharmSciTech Pub Date : 2026-07-07 DOI: 10.1208/s12249-026-03493-5
Mahesha Keerikkadu, Akshay Shetty, Raagul Seenivasan, Praveen Halagali, Vamshi Krishna Tippavajhala, Mahalaxmi Rathnanand
{"title":"A Review on Nanocarrier-Based Strategies for Sunitinib Delivery: Advances in Pharmacokinetic Enhancement and Targeted Theranostics","authors":"Mahesha Keerikkadu,&nbsp;Akshay Shetty,&nbsp;Raagul Seenivasan,&nbsp;Praveen Halagali,&nbsp;Vamshi Krishna Tippavajhala,&nbsp;Mahalaxmi Rathnanand","doi":"10.1208/s12249-026-03493-5","DOIUrl":"10.1208/s12249-026-03493-5","url":null,"abstract":"<div><p>Sunitinib malate (SNB) is a multitargeted tyrosine kinase inhibitor that inhibits tumor angiogenesis and proliferation by blocking signaling through VEGFR, PDGFR, c-KIT, FLT3, and RET. SNB is currently used in the treatment of renal cell carcinoma, gastrointestinal stromal tumors, and pancreatic neuroendocrine tumors. The pharmacological efficacy of SNB is limited by its poor aqueous solubility, pH-dependent dissolution, poor oral bioavailability, extensive first pass metabolism, high interpatient pharmacokinetic variability, and dose-limiting toxicities such as cardiotoxicity, hypertension, and myelosuppression. Nanotechnology-based drug delivery systems have been explored as a promising strategy to overcome the limitations and improve the pharmacological efficacy of SNB. A wide variety of SNB-loaded nanocarriers, including polymeric nanoparticles, lipid-based nanocarriers, nanocapsules, polymeric micelles, dendrimers, and inorganic nanostructures, have been developed to improve solubilization, protect the drug from degradation, and provide controlled or stimulus-responsive release. These nanocarriers provide improved pharmacokinetic properties by prolonging systemic circulation, increasing tumor accumulation through enhanced permeability and retention effects, and reducing off-target exposure. Active targeting and intracellular delivery mechanisms further enhance cellular uptake and pharmacological efficacy while reducing systemic toxicity. In addition, multifunctional nanocarriers that incorporate imaging agents or microenvironment-responsive components also offer opportunities for theranostic and precision oncology applications. However, clinical adoption is currently hindered by challenges associated with large-scale nanomanufacturing, batch-to-batch reproducibility, long-term nanostability, regulatory acceptance, and limited human data. This review critically evaluates current nanocarrier platforms for SNB delivery, provides pharmacological advancements achieved through nanoformulation, and identifies key translational hurdles and future directions for clinical adoption.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 5","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-07-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1208/s12249-026-03493-5.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148403305","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 Review on Modular Peptide Anchoring Strategies for Functionalizing Liposomal Nanocarriers: Advancing Non-covalent Design Toward Targeted Cancer Therapy 功能化脂质体纳米载体的模块化肽锚定策略综述:推进非共价设计靶向癌症治疗。
IF 5.1 4区 医学
AAPS PharmSciTech Pub Date : 2026-07-07 DOI: 10.1208/s12249-026-03488-2
Adamu Safiyanu Maikifi, Veerakiet Boonkanokwong
{"title":"A Review on Modular Peptide Anchoring Strategies for Functionalizing Liposomal Nanocarriers: Advancing Non-covalent Design Toward Targeted Cancer Therapy","authors":"Adamu Safiyanu Maikifi,&nbsp;Veerakiet Boonkanokwong","doi":"10.1208/s12249-026-03488-2","DOIUrl":"10.1208/s12249-026-03488-2","url":null,"abstract":"<div><p>Targeted drug delivery systems play a crucial role in improving the effectiveness and precision of cancer treatments. Liposomes have been widely investigated as drug carriers due to their versatility. Traditional methods for functionalizing liposomes involve covalent bonding of targeting ligands, which, while effective, can be complex and may affect the activity of the ligands. In contrast, non-covalent peptide insertion offers a simpler, more adaptable approach for incorporating targeting peptides into liposomal membranes using mechanisms such as hydrophobic interactions and electrostatic forces. This review examines non-covalent peptide-liposome interactions as the primary focus. We analyze mechanisms, incorporation techniques, and therapeutic applications with emphasis on formulation-relevant criteria including stability, manufacturability, and clinical translation. Critical evaluation of comparative advantages and limitations of each strategy provides decision frameworks for formulation scientists. We also address manufacturing challenges, quality control strategies, and regulatory considerations that influence clinical translation.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 5","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-07-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148403299","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
Hot-Melt Extrusion of Bupropion with Three Ethylcellulose Grades for Pellet Feedstock Preparation and Screw-Based 3D Printing of Sustained-Release Tablets 三种乙基纤维素级安非他酮颗粒原料的热熔挤出及缓释片的螺旋3D打印。
IF 5.1 4区 医学
AAPS PharmSciTech Pub Date : 2026-07-06 DOI: 10.1208/s12249-026-03494-4
Chrystalla Protopapa, Laura Andrade Junqueira, Siva Satyanarayana Kolipaka, Sophia Economidou, Dimitris Pappas, Dennis Douroumis, Marilena Vlachou
{"title":"Hot-Melt Extrusion of Bupropion with Three Ethylcellulose Grades for Pellet Feedstock Preparation and Screw-Based 3D Printing of Sustained-Release Tablets","authors":"Chrystalla Protopapa,&nbsp;Laura Andrade Junqueira,&nbsp;Siva Satyanarayana Kolipaka,&nbsp;Sophia Economidou,&nbsp;Dimitris Pappas,&nbsp;Dennis Douroumis,&nbsp;Marilena Vlachou","doi":"10.1208/s12249-026-03494-4","DOIUrl":"10.1208/s12249-026-03494-4","url":null,"abstract":"<div><p>3D printing has emerged as a novel technology for producing personalized dosage forms tailored to patients’ therapeutic needs. Hot-melt extrusion (HME) is commonly used to produce filaments for most extrusion-based 3D printers. This study aimed to investigate the effect of three different ethylcellulose (EC) grades (7N, 10N, and 20N) on the physicochemical properties, matrix restructuring, and sustained-release behavior of bupropion hydrochloride (BUP·HCl)-loaded tablets. The extrudates were fabricated using HME, pelletized, and used as feedstock for screw-based 3D printing, thereby overcoming the limitations of filament-based systems. The formulations were evaluated for drug release, hardness, swelling, and porosity before and after dissolution using micro-computed tomography (microCT). The influence of tablet geometry on drug release was also investigated. Morphology, crystallinity, and thermal properties were characterized using scanning electron microscopy (SEM), X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and thermogravimetric analysis (TGA). All formulations exhibited sustained BUP·HCl release, with drug release decreasing as EC viscosity grade increased. Tablets prepared with higher-viscosity EC showed greater hardness, reduced swelling, and lower post-dissolution porosity. MicroCT analysis revealed raster-related internal pores in all tablets before dissolution. However, initial porosity did not correlate with release behavior; tablets containing EC 20N exhibited the highest initial porosity but the lowest post-dissolution porosity and slowest drug release, whereas EC 7N tablets showed the opposite trend. Larger, thinner tablets released drug faster due to higher surface-area-to-volume ratio. The findings demonstrate that EC molecular weight plays a critical role in governing hydration-driven matrix restructuring and controlling sustained-release behavior of the 3D-printed tablets.</p><h3>Graphical abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 5","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-07-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1208/s12249-026-03494-4.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148395254","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
Vegetable Butter-Based Nanocarriers: Do Nanoparticulation and Quercetin Loading Modulate In vitro Cellular Effects Involved in Wound Healing? 基于蔬菜黄油的纳米载体:纳米关节和槲皮素负载是否调节涉及伤口愈合的体外细胞效应?
IF 5.1 4区 医学
AAPS PharmSciTech Pub Date : 2026-07-06 DOI: 10.1208/s12249-026-03490-8
Ana Beatriz Chieco Costa, Regina Gomes Daré, Luciana B. Lopes
{"title":"Vegetable Butter-Based Nanocarriers: Do Nanoparticulation and Quercetin Loading Modulate In vitro Cellular Effects Involved in Wound Healing?","authors":"Ana Beatriz Chieco Costa,&nbsp;Regina Gomes Daré,&nbsp;Luciana B. Lopes","doi":"10.1208/s12249-026-03490-8","DOIUrl":"10.1208/s12249-026-03490-8","url":null,"abstract":"<div><p>The need for advanced yet cost-effective topical strategies for chronic skin wounds motivated this study to evaluate nanostructured lipid carriers (NLCs) based on shea or cocoa butter. Our first goal was to compare NLCs with conventional emulsions to evaluate whether butter nanoparticulation confers biological advantages for wound-related applications. NLCs were produced by hot homogenization-sonication and characterized in terms of particle size, polydispersity, morphology, and stability. Both butter-based NLCs formed stable, monodisperse nanometric systems (size 197–240 nm, PDI &lt; 0.2). In HaCaT keratinocytes, shea and cocoa butter-based NLCs significantly enhanced proliferation (up to 137% for shea and 127% for cocoa butter) and wound repopulation (up to 96% and 65%, respectively) compared with the respective emulsions. Our second goal was to assess the effect of quercetin (QT) incorporation in the NLCs, since oxidative stress has been related to healing difficulties. QT incorporation did not further increase proliferation or repopulation but significantly improved antioxidant protection, reducing H₂O₂-induced intracellular reactive oxygen species by up to 53–62% at 12 µg/mL QT. Shea butter-based NLCs exhibited superior biological performance, including a modest intrinsic antioxidant effect (~ 15% DPPH inhibition), probably due to endogenous lipid bioactives. QT-loaded shea butter NLCs promoted enhanced QT retention within the stratum corneum (~ 14 vs. ~ 9 µg/cm<sup>2</sup>) and dermis (~ 9 vs. ~ 3 µg/cm<sup>2</sup>) of injured porcine skin while limiting permeation. These results demonstrate that vegetable butter-based NLCs, particularly from shea butter, represent a promising wound management platform that combines intrinsic lipid bioactivity, nanoscale-mediated drug availability, and skin barrier support.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 5","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-07-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1208/s12249-026-03490-8.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148395240","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
Enhanced Stability and Transdermal Delivery of Semaglutide Using an L-Arginine Based Dissolving Microneedle System 利用l -精氨酸溶解微针系统增强西马鲁肽的稳定性和透皮递送。
IF 5.1 4区 医学
AAPS PharmSciTech Pub Date : 2026-07-02 DOI: 10.1208/s12249-026-03455-x
Priyanka Panchal, Snehal Daware, Yi Guo, Ganming Mao, Blase Billack, Pulkit Khatri, Ketan Patel
{"title":"Enhanced Stability and Transdermal Delivery of Semaglutide Using an L-Arginine Based Dissolving Microneedle System","authors":"Priyanka Panchal,&nbsp;Snehal Daware,&nbsp;Yi Guo,&nbsp;Ganming Mao,&nbsp;Blase Billack,&nbsp;Pulkit Khatri,&nbsp;Ketan Patel","doi":"10.1208/s12249-026-03455-x","DOIUrl":"10.1208/s12249-026-03455-x","url":null,"abstract":"<div><p>Glucagon-like peptide-1 agonists, especially Semaglutide (SMG), have revolutionized the management of diabetes and obesity, yet its clinical application is hindered by challenges in oral bioavailability and patient adherence to injectable formulations. Transdermal delivery offers a promising alternative, and this study explores dissolving microneedle (DMN) technology for SMG administration. PETOX is a water-soluble polymer utilized for the fabrication of dissolving microneedles and unique stabilization of SMG by incorporating L-arginine. Our study presents the first comprehensive investigation of L-arginine as an excipient in dissolving microneedles to enhance peptide integrity and stability. This study focuses on the development and characterization of DMN arrays formulated with a polymeric blend of hyaluronic acid, PETOX, and L-arginine, designed for the transdermal delivery of SMG. The SMG loaded microneedles (SMG-DMNs) exhibit robust mechanical strength (3.47 N/needle; fracture force), excellent Parafilm M® insertion (&gt; 50% at 450 μm depth), and drug release over 12 h. Extensive SMG-DMNs characterization include <i>ex-vivo</i> porcine skin insertion, scanning electron microscopy, confocal microscopy, and unique agarose-based dissolution model showed effective optimization of polymeric matrix for SMG, ensuring better insertion capabilities. The florescence imaging verified efficient transdermal deposition and penetration of dye suggesting potential transdermal delivery of SMG upon insertion. While the DMN approach addresses key barriers such as low oral bioavailability, injection-related discomfort and patient compliance; challenges persist regarding loss of therapeutic activity and stability of peptide. Nevertheless, DMN technology presents a promising, patient-friendly alternative for peptide therapeutics, with the potential to significantly improve outcomes in T2DM and obesity management.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 5","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148374188","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 Preparation and Physicochemical Characterization of a Triple Synergistic Nanoplatform Designed for Targeted Subcutaneous Delivery of Sitagliptin with Potential for β-Cell Preservation 具有β细胞保存潜力的西格列汀靶向皮下递送三协同纳米平台的制备和物理化学表征。
IF 5.1 4区 医学
AAPS PharmSciTech Pub Date : 2026-07-02 DOI: 10.1208/s12249-026-03489-1
Mo’tasem M. Alsmadi, Rana Obaidat
{"title":"The Preparation and Physicochemical Characterization of a Triple Synergistic Nanoplatform Designed for Targeted Subcutaneous Delivery of Sitagliptin with Potential for β-Cell Preservation","authors":"Mo’tasem M. Alsmadi,&nbsp;Rana Obaidat","doi":"10.1208/s12249-026-03489-1","DOIUrl":"10.1208/s12249-026-03489-1","url":null,"abstract":"<div><p>Effective diabetes management necessitates innovative strategies that simultaneously stimulate β-cell growth and prevent apoptosis. While sitagliptin is an established therapeutic, its clinical utility is often hampered by suboptimal oral bioavailability and a lack of site-specific delivery. This research details the development and <i>in vitro</i> assessment of Sita-Ex-Cs-SeNPs, a subcutaneous nanocarrier composed of sitagliptin-loaded chitosan-selenium nanoparticles conjugated with exenatide. The platform is engineered to leverage GLP-1 receptor affinity for pancreatic targeting and utilize selenium’s intrinsic antioxidant properties to achieve therapeutic synergy. We employed the ionotropic gelation technique to encapsulate sitagliptin and integrate exenatide and selenium into a unified, stable delivery system. The resulting nanoparticles exhibited a spherical architecture with an average diameter of 314.1 nm and a zeta potential of + 18.7 mV. We achieved a high encapsulation efficiency of 98%. Analytical techniques (DSC and PXRD) confirmed that sitagliptin transitioned to an amorphous state, while FTIR validated successful peptide conjugation. Release kinetics followed the Weibull model, demonstrating a controlled biphasic profile (57% over 24 h) that significantly extends the therapeutic window compared to the free drug. <i>Sita-Ex-Cs-SeNPs</i> offer a promising, biocompatible approach for targeted diabetes intervention. Although <i>in vitro</i> results confirm stable sustained release, subsequent <i>in vivo</i> trials are essential to validate their efficacy in β-cell preservation.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 5","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148374324","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
Repurposing Non-oncologic Drugs via Targeted Nanocarriers for Cancer Therapy: Mechanisms, Synergistic Combinations, and Clinical Translation 通过靶向纳米载体重新利用非肿瘤药物进行癌症治疗:机制、协同组合和临床转化
IF 5.1 4区 医学
AAPS PharmSciTech Pub Date : 2026-06-26 DOI: 10.1208/s12249-026-03491-7
Nur Aininie Yusoh, Afiq Azil, Ahlam Zaid Alkilani, Mohd Basyaruddin Abdul Rahman, Azren Aida Asmawi, Rosniza Razali, Fatmawati Adam, Nurul Akmarina Mohd Abdul Kamal
{"title":"Repurposing Non-oncologic Drugs via Targeted Nanocarriers for Cancer Therapy: Mechanisms, Synergistic Combinations, and Clinical Translation","authors":"Nur Aininie Yusoh,&nbsp;Afiq Azil,&nbsp;Ahlam Zaid Alkilani,&nbsp;Mohd Basyaruddin Abdul Rahman,&nbsp;Azren Aida Asmawi,&nbsp;Rosniza Razali,&nbsp;Fatmawati Adam,&nbsp;Nurul Akmarina Mohd Abdul Kamal","doi":"10.1208/s12249-026-03491-7","DOIUrl":"10.1208/s12249-026-03491-7","url":null,"abstract":"<div><p>The urgent need for innovative cancer therapies has driven increasing interest in repurposing drugs originally developed for non-oncological diseases. Several FDA-approved and clinically investigated agents, including mesalamine, celecoxib, gliclazide, metformin, itraconazole, and doxycycline, have shown anticancer potential through diverse mechanisms. However, despite their therapeutic potential, many of these drugs suffer from limited tumor selectivity, suboptimal bioavailability, and off-target toxicity when used in oncology. Nanocarrier-based delivery systems offer a promising strategy to address these limitations by improving drug solubility, enhancing tumor accumulation, and enabling more selective delivery to cancer cells and the tumor microenvironment. In this context, nanocarriers not only serve as delivery vehicles but also provide opportunities for controlled release, combination therapy, and stimulus-responsive treatment strategies. This review summarizes recent progress in repurposing non-oncologic drugs for cancer therapy with a particular focus on nanocarrier-enabled delivery approaches. We discuss the molecular mechanisms underlying the anticancer activity of repurposed drugs, as well as their targeting of tumor cells, the tumor microenvironment, and cancer stem cells. In addition, we highlight advances in integrating these agents into nanocarrier platforms for combination therapy, photodynamic therapy, dual-drug delivery, and stimuli-responsive systems. Finally, we address translational challenges, including regulatory and intellectual property considerations, and discuss future perspectives involving artificial intelligence and personalized medicine to accelerate clinical implementation.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 5","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148323724","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
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