Pub Date : 2025-11-17DOI: 10.1016/j.ejpb.2025.114929
Andi Dian Permana , Alejandro J. Paredes , Fabiana Volpe-Zanutto , Qonita Kurnia Anjani , Emilia Utomo , Ryan F. Donnelly
{"title":"Corrigendum to “Dissolving microneedle-mediated dermal delivery of itraconazole nanocrystals for improved treatment of cutaneous candidiasis”. [Eur. J. Pharm. Biopharm. 154 (2020) 50–61]","authors":"Andi Dian Permana , Alejandro J. Paredes , Fabiana Volpe-Zanutto , Qonita Kurnia Anjani , Emilia Utomo , Ryan F. Donnelly","doi":"10.1016/j.ejpb.2025.114929","DOIUrl":"10.1016/j.ejpb.2025.114929","url":null,"abstract":"","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"218 ","pages":"Article 114929"},"PeriodicalIF":4.3,"publicationDate":"2025-11-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145548927","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-11-17DOI: 10.1016/j.ejpb.2025.114928
Qonita Kurnia Anjani , Natalia Moreno-Castellanos , Yaocun Li , Akmal Hidayat Bin Sabri , Ryan F. Donnelly
{"title":"Corrigendum to “Dissolvable microarray patches of levodopa and carbidopa for Parkinson’s disease management” [Eur. J. Pharm. Biopharm. 199 (2024) 114304]","authors":"Qonita Kurnia Anjani , Natalia Moreno-Castellanos , Yaocun Li , Akmal Hidayat Bin Sabri , Ryan F. Donnelly","doi":"10.1016/j.ejpb.2025.114928","DOIUrl":"10.1016/j.ejpb.2025.114928","url":null,"abstract":"","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"218 ","pages":"Article 114928"},"PeriodicalIF":4.3,"publicationDate":"2025-11-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145548929","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-11-16DOI: 10.1016/j.ejpb.2025.114926
Eva M. Vicente-Perez , Eneko Larrañeta , Maelíosa T.C. McCrudden , Adrien Kissenpfennig , Shauna Hegarty , Helen O. McCarthy , Ryan F. Donnelly
{"title":"Corrigendum to “Repeat application of microneedles does not alter skin appearance or barrier function and causes no measurable disturbance of serum biomarkers of infection, inflammation or immunity in mice in vivo” [Eur. J. Pharm. Biopharm. 117 (2017) 400–407]","authors":"Eva M. Vicente-Perez , Eneko Larrañeta , Maelíosa T.C. McCrudden , Adrien Kissenpfennig , Shauna Hegarty , Helen O. McCarthy , Ryan F. Donnelly","doi":"10.1016/j.ejpb.2025.114926","DOIUrl":"10.1016/j.ejpb.2025.114926","url":null,"abstract":"","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"218 ","pages":"Article 114926"},"PeriodicalIF":4.3,"publicationDate":"2025-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145539756","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Evidence and data supporting the co-administration of intravenous medication (IVM) and parenteral nutrition solutions (PNS) is scarce. However, co-administration is often unavoidable practice in paediatric patients and particularly neonates, where secured vascular access can be challenging. This is especially the case when multiple infusions must run simultaneously with limited intravenous access. Safe co-administration could offer a solution to challenges such as fluid restriction and provision of uninterrupted nutritional support. The American Society for Parenteral and Enteral Nutrition (A.S.P.E.N.) guidelines state that “the co-administration could be possible only if guided by supportive data on physicochemical compatibility and stability”, which is neither available nor agreed internationally. This systematic review was conducted to address the deficit in compatibility data on commonly used IVMs and PNS in paediatrics and neonates.
{"title":"Compatibility of parenteral nutrition solutions with intravenous medication in infants and children: A literature review","authors":"Mahmoud Farhan , Naomi McCallion , Joanne Bennett , Anne Cram , Fiona O’Brien","doi":"10.1016/j.ejpb.2025.114924","DOIUrl":"10.1016/j.ejpb.2025.114924","url":null,"abstract":"<div><div>Evidence and data supporting the co-administration of intravenous medication (IVM) and parenteral nutrition solutions (PNS) is scarce. However, co-administration is often unavoidable practice in paediatric patients and particularly neonates, where secured vascular access can be challenging. This is especially the case when multiple infusions must run simultaneously with limited intravenous access. Safe co-administration could offer a solution to challenges such as fluid restriction and provision of uninterrupted nutritional support<sup>.</sup> The American Society for Parenteral and Enteral Nutrition (A.S.P.E.N.) guidelines state that “the co-administration could be possible only if guided by supportive data on physicochemical compatibility and stability”, which is neither available nor agreed internationally. This systematic review was conducted to address the deficit in compatibility data on commonly used IVMs and PNS in paediatrics and neonates.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"219 ","pages":"Article 114924"},"PeriodicalIF":4.3,"publicationDate":"2025-11-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145530300","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-11-13DOI: 10.1016/j.ejpb.2025.114934
Chun Qiao , Jinru Hu , Yuxin Jin , Ruixiang Li , Fan Zhao , Yu Zhang , Xiaoyu Zhang , Ruofei Du
The aversive taste of pharmaceutical formulations, especially bitterness, has been identified as a significant barrier to patient compliance. Taste masking technologies have emerged as significant approaches to improve the acceptability of orally administered drugs. These technologies have evolved from empirical methods to more systematic, precise, and intelligent solutions. Artificial intelligence (AI) advances have given rise to novel opportunities in taste prediction, excipient selection, and formulation optimization. This review critically examines the historical progression of taste masking technologies, elucidates the molecular and physiological basis of taste perception alongside interindividual variability, and compares conventional sensory and analytical techniques with emerging digital and biosensing platforms. Particular emphasis is placed on integrating AI into drug taste assessment, the development of masking strategies, and the control of manufacturing processes. Furthermore, the potential of AI-driven intelligent taste systems to enable precision masking, controlled release, and patient-specific palatability is discussed. This work outlines a conceptual and technological framework for next-generation taste optimization strategies, providing insights into developing smart, efficient, and personalized drug delivery systems.
{"title":"From empirical exploration to data-driven innovation: The role of artificial intelligence in pharmaceutical taste masking","authors":"Chun Qiao , Jinru Hu , Yuxin Jin , Ruixiang Li , Fan Zhao , Yu Zhang , Xiaoyu Zhang , Ruofei Du","doi":"10.1016/j.ejpb.2025.114934","DOIUrl":"10.1016/j.ejpb.2025.114934","url":null,"abstract":"<div><div>The aversive taste of pharmaceutical formulations, especially bitterness, has been identified as a significant barrier to patient compliance. Taste masking technologies have emerged as significant approaches to improve the acceptability of orally administered drugs. These technologies have evolved from empirical methods to more systematic, precise, and intelligent solutions. Artificial intelligence (AI) advances have given rise to novel opportunities in taste prediction, excipient selection, and formulation optimization. This review critically examines the historical progression of taste masking technologies, elucidates the molecular and physiological basis of taste perception alongside interindividual variability, and compares conventional sensory and analytical techniques with emerging digital and biosensing platforms. Particular emphasis is placed on integrating AI into drug taste assessment, the development of masking strategies, and the control of manufacturing processes. Furthermore, the potential of AI-driven intelligent taste systems to enable precision masking, controlled release, and patient-specific palatability is discussed. This work outlines a conceptual and technological framework for next-generation taste optimization strategies, providing insights into developing smart, efficient, and personalized drug delivery systems.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"218 ","pages":"Article 114934"},"PeriodicalIF":4.3,"publicationDate":"2025-11-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145530324","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-11-12DOI: 10.1016/j.ejpb.2025.114914
Qien Zhao , Junhui Yang , Jialin Liu , Shengyu Zhang , Wei Zhao , Wenting Jiang , Yang Zhou , Lei Jiang , Jiantao Zhang
Poly(lactic-co-glycolic acid) (PLGA) is the most commonly used commercially available polymeric pharmaceutical excipient for developing injectable long-acting release products. Its degradation rate is influenced by factors, such as molecular weight, the lactic/glycolic ratio (L/G ratio), and the nature of terminal groups. These variables impose challenges in achieving a precisely controlled release of loaded active compounds from finished PLGA-based formulations. This study investigated the impact of varying PLGA terminal groups on drug loading, encapsulation efficiencies, and drug release profiles in PLGA microspheres. We synthesized PLGA with four distinct terminal groups: carboxyl, n-hexyl, dodecyl, and hexadecyl, while keeping molecular weights and L/G ratios consistent to isolate the effects of the terminal groups on PLGA properties. Also, we examined how terminal groups influence the degradation behavior of PLGA microspheres and found that longer carbon chain lengths in the terminal groups resulted in a slower degradation rate. We have developed a novel method for analyzing terminal groups, enabling us to verify our synthesized products and to compare them against commercially available products. This method enhances the accuracy of our analyses and ensures the integrity of our product verification process. Additionally, we explored the underlying mechanism by which terminal groups affect the PLGA degradation. We then prepared four PLGA microspheres loaded with cyproterone acetate (CYA) through emulsification. The resulting microspheres exhibited consistent morphology, and a volume mean diameter of 9 to 11 µm,a drug loading rate of about 10% and an encapsulation efficiency of approximately 97%. The results of in vitro release experiments showed that CYA release from all microspheres could be sustained for up to two months with a recovery rate reaching 100%. Meanwhile, we investigated the mechanism of loaded drug release from PLGA microspheres with different terminal groups and elucidated how the degradation of PLGA influences the release profile of loaded drugs. The insights gained from this study will enhance the understanding of PLGA degradation and the mechanisms underlying the release of loaded actives from PLGA microspheres. Furthermore, the modification of terminal groups has the potential to support the development of advanced pharmaceutical excipients.
{"title":"Impact of terminal groups on PLGA degradation rate and their role in sustained release of cyproterone acetate","authors":"Qien Zhao , Junhui Yang , Jialin Liu , Shengyu Zhang , Wei Zhao , Wenting Jiang , Yang Zhou , Lei Jiang , Jiantao Zhang","doi":"10.1016/j.ejpb.2025.114914","DOIUrl":"10.1016/j.ejpb.2025.114914","url":null,"abstract":"<div><div>Poly(lactic-co-glycolic acid) (PLGA) is the most commonly used commercially available polymeric pharmaceutical excipient for developing injectable long-acting release products. Its degradation rate is influenced by factors, such as molecular weight, the lactic/glycolic ratio (L/G ratio), and the nature of terminal groups. These variables impose challenges in achieving a precisely controlled release of loaded active compounds from finished PLGA-based formulations. This study investigated the impact of varying PLGA terminal groups on drug loading, encapsulation efficiencies, and drug release profiles in PLGA microspheres. We synthesized PLGA with four distinct terminal groups: carboxyl, n-hexyl, dodecyl, and hexadecyl, while keeping molecular weights and L/G ratios consistent to isolate the effects of the terminal groups on PLGA properties. Also, we examined how terminal groups influence the degradation behavior of PLGA microspheres and found that longer carbon chain lengths in the terminal groups resulted in a slower degradation rate. We have developed a novel method for analyzing terminal groups, enabling us to verify our synthesized products and to compare them against commercially available products. This method enhances the accuracy of our analyses and ensures the integrity of our product verification process. Additionally, we explored the underlying mechanism by which terminal groups affect the PLGA degradation. We then prepared four PLGA microspheres loaded with cyproterone acetate (CYA) through emulsification. The resulting microspheres exhibited consistent morphology, and a volume mean diameter of 9 to 11 µm,a drug loading rate of about 10% and an encapsulation efficiency of approximately 97%. The results of in vitro release experiments showed that CYA release from all microspheres could be sustained for up to two months with a recovery rate reaching 100%. Meanwhile, we investigated the mechanism of loaded drug release from PLGA microspheres with different terminal groups and elucidated how the degradation of PLGA influences the release profile of loaded drugs. The insights gained from this study will enhance the understanding of PLGA degradation and the mechanisms underlying the release of loaded actives from PLGA microspheres. Furthermore, the modification of terminal groups has the potential to support the development of advanced pharmaceutical excipients.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"218 ","pages":"Article 114914"},"PeriodicalIF":4.3,"publicationDate":"2025-11-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145522537","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-11-12DOI: 10.1016/j.ejpb.2025.114935
Soraia Santos , Joana Lopes , Daniela Lopes , Madineh Moradialvand , Huma Hameed , Patrícia C. Pires , Fouad Damiri , Amélia C.F. Vieira , Henrique Faneca , Francisco Veiga , Ana Cláudia Paiva-Santos
Nanovesicles (NVs) derived from biological membranes offer promising opportunities in the realm of ultra-precise cancer therapy, with proven therapeutic efficacy and safety profiles. These biomimetic NVs possess a versatile liposome-like structure capable of accommodating hydrophilic and hydrophobic agents. NVs derived from a plethora of biological sources, including eukaryotic cells [erythrocytes, platelets, immune cells, cancer cells and mesenchymal stem cells (MSCs)], extracellular vesicles (EVs), and bacteria, successfully proved to enable the tumor-targeted delivery of a wide panoply of therapeutic molecules. These include chemotherapeutics, imaging agents, nucleic acids and immunoadjuvants, highlighting their potential as natural lipid-based drug delivery systems (DDSs) in cancer-oriented therapies. Clinical translation, however, encounters challenging issues that require further research and refinement. Safety, immunogenicity, scalability, stability, production protocols, quality control, and understanding biological processes remain crucial aspects for clinical implementation. This review offers a critical and comparative analysis of different membrane sources, underlines several NV applications in tumor-targeted therapies, and outlines future research directions and current limitations. Addressing these challenges is pivotal to harnessing the full potential of NVs derived from biological membranes for safe and effective clinical use.
{"title":"Biomembrane-Derived vesicles for targeted cancer Therapies: Novel treatment avenues from Cells, Bacteria, and extracellular sources","authors":"Soraia Santos , Joana Lopes , Daniela Lopes , Madineh Moradialvand , Huma Hameed , Patrícia C. Pires , Fouad Damiri , Amélia C.F. Vieira , Henrique Faneca , Francisco Veiga , Ana Cláudia Paiva-Santos","doi":"10.1016/j.ejpb.2025.114935","DOIUrl":"10.1016/j.ejpb.2025.114935","url":null,"abstract":"<div><div>Nanovesicles (NVs) derived from biological membranes offer promising opportunities in the realm of ultra-precise cancer therapy, with proven therapeutic efficacy and safety profiles. These biomimetic NVs possess a versatile liposome-<em>like</em> structure capable of accommodating hydrophilic and hydrophobic agents. NVs derived from a plethora of biological sources, including eukaryotic cells [erythrocytes, platelets, immune cells, cancer cells and mesenchymal stem cells (MSCs)], extracellular vesicles (EVs), and bacteria, successfully proved to enable the tumor-targeted delivery of a wide panoply of therapeutic molecules. These include chemotherapeutics, imaging agents, nucleic acids and immunoadjuvants, highlighting their potential as natural lipid-based drug delivery systems (DDSs) in cancer-oriented therapies. Clinical translation, however, encounters challenging issues that require further research and refinement. Safety, immunogenicity, scalability, stability, production protocols, quality control, and understanding biological processes remain crucial aspects for clinical implementation. This review offers a critical and comparative analysis of different membrane sources, underlines several NV applications in tumor-targeted therapies, and outlines future research directions and current limitations. Addressing these challenges is pivotal to harnessing the full potential of NVs derived from biological membranes for safe and effective clinical use.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"218 ","pages":"Article 114935"},"PeriodicalIF":4.3,"publicationDate":"2025-11-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145523274","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-11-12DOI: 10.1016/j.ejpb.2025.114912
Kholod A. Elhasany , Sherine N. Khattab , Adnan A. Bekhit , Doaa M. Ragab , Mohammad A. Abdulkader , Amira Zaky , Maged W. Helmy , Hayam M.A. Ashour , Mohamed Teleb , Nesreen S. Haiba , Ahmed O. Elzoghby
{"title":"Corrigendum to “Combination of magnetic targeting with synergistic inhibition of NF-κB and glutathione via micellar drug nanomedicine enhances its anti-tumor efficacy.” [Eur. J. Pharm. Biopharm. 155 (2020) 162–176]","authors":"Kholod A. Elhasany , Sherine N. Khattab , Adnan A. Bekhit , Doaa M. Ragab , Mohammad A. Abdulkader , Amira Zaky , Maged W. Helmy , Hayam M.A. Ashour , Mohamed Teleb , Nesreen S. Haiba , Ahmed O. Elzoghby","doi":"10.1016/j.ejpb.2025.114912","DOIUrl":"10.1016/j.ejpb.2025.114912","url":null,"abstract":"","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"218 ","pages":"Article 114912"},"PeriodicalIF":4.3,"publicationDate":"2025-11-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145502845","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-11-12DOI: 10.1016/j.ejpb.2025.114925
Xinyi Xu , Jianhua Han , Xuefang Lou , Xiaoling Xu , Yongzhong Du
Melanoma is highly aggressive and remains difficult to treat. Traditional treatment options often result in damage to normal tissues and a high rate of recurrence. Conventional photodynamic therapy (PDT) is limited by poor light penetration, oxygen depletion, and extracellular matrix (ECM) barriers. In this study, we developed an acid-responsive liposome system that co-loads indocyanine green (ICG, a photosensitizer) and 1-bromoperfluorooctane (PFOB) modified with collagenase (Col-LIP-(ICG + PFOB)) to facilitate the degradation of the tumor extracellular matrix and enable near-infrared (NIR)-triggered PDT. Our findings demonstrated that Col-LIP-(ICG + PFOB) effectively degrades the tumor extracellular matrix via collagenase, resulting in increased accumulation of the formulation within the tumor. Upon NIR irradiation, ICG produced reactive oxygen species and heat, while PFOB provided supplemental oxygen and collagenase degraded the extracellular matrix, together contributing to enhanced antitumor efficacy. In melanoma models, this system significantly inhibited tumor growth and reduced HIF-1α levels. In conclusion, this study offers a novel strategy to increase the efficacy of PDT in the treatment of melanoma.
{"title":"Oxygenated collagenase nanoliposomes for deep photodynamic therapy via remodelling the tumor extracellular matrix","authors":"Xinyi Xu , Jianhua Han , Xuefang Lou , Xiaoling Xu , Yongzhong Du","doi":"10.1016/j.ejpb.2025.114925","DOIUrl":"10.1016/j.ejpb.2025.114925","url":null,"abstract":"<div><div>Melanoma is highly aggressive and remains difficult to treat. Traditional treatment options often result in damage to normal tissues and a high rate of recurrence. Conventional photodynamic therapy (PDT) is limited by poor light penetration, oxygen depletion, and extracellular matrix (ECM) barriers. In this study, we developed an acid-responsive liposome system that co-loads indocyanine green (ICG, a photosensitizer) and 1-bromoperfluorooctane (PFOB) modified with collagenase (Col-LIP-(ICG + PFOB)) to facilitate the degradation of the tumor extracellular matrix and enable near-infrared (NIR)-triggered PDT. Our findings demonstrated that Col-LIP-(ICG + PFOB) effectively degrades the tumor extracellular matrix via collagenase, resulting in increased accumulation of the formulation within the tumor. Upon NIR irradiation, ICG produced reactive oxygen species and heat, while PFOB provided supplemental oxygen and collagenase degraded the extracellular matrix, together contributing to enhanced antitumor efficacy. In melanoma models, this system significantly inhibited tumor growth and reduced HIF-1α levels. In conclusion, this study offers a novel strategy to increase the efficacy of PDT in the treatment of melanoma.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"218 ","pages":"Article 114925"},"PeriodicalIF":4.3,"publicationDate":"2025-11-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145511950","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-11-11DOI: 10.1016/j.ejpb.2025.114933
Parag Roy, Oisín N. Kavanagh
Every month thousands of patients are treated with ocular ciprofloxacin, yet crystalline deposits form on the surface of the cornea in one in ten patients. This occurs due to a pH shift when the formulation is instilled onto the eye, since ciprofloxacin formulations are buffered to pH 4.5 to keep the drug in solution, whereas the tear pH is around 7. We deconstruct the formulation and the chemical pathophysiology of this condition to enable the selection of inhibitors that can derisk corneal toxicity. Through in vitro and ex vivo models we show that some structurally similar fluoroquinolones (levofloxacin and ofloxacin) can successfully inhibit the nucleation of ciprofloxacin. In contrast, other fluoroquinolones like norfloxacin can promote the formation of a less soluble ciprofloxacin–norfloxacin complex, increasing the risk of corneal deposition. We further identify that mannitol, a common excipient in marketed ophthalmic formulations, accelerates nucleation and could promote the risk of crystallisation. These findings identify both beneficial and counterproductive formulation components and define a practical anticrystal engineering strategy to prevent ciprofloxacin-induced ocular precipitation. We anticipate that this study may inspire further work designing nucleation inhibitors for transient, high supersaturation conditions such as those seen regularly during drug delivery.
{"title":"A strategy to prevent ciprofloxacin induced corneal toxicity","authors":"Parag Roy, Oisín N. Kavanagh","doi":"10.1016/j.ejpb.2025.114933","DOIUrl":"10.1016/j.ejpb.2025.114933","url":null,"abstract":"<div><div>Every month thousands of patients are treated with ocular ciprofloxacin, yet crystalline deposits form on the surface of the cornea in one in ten patients. This occurs due to a pH shift when the formulation is instilled onto the eye, since ciprofloxacin formulations are buffered to pH 4.5 to keep the drug in solution, whereas the tear pH is around 7. We deconstruct the formulation and the chemical pathophysiology of this condition to enable the selection of inhibitors that can derisk corneal toxicity. Through <em>in vitro</em> and <em>ex vivo</em> models we show that some structurally similar fluoroquinolones (levofloxacin and ofloxacin) can successfully inhibit the nucleation of ciprofloxacin. In contrast, other fluoroquinolones like norfloxacin can promote the formation of a less soluble ciprofloxacin–norfloxacin complex, increasing the risk of corneal deposition. We further identify that mannitol, a common excipient in marketed ophthalmic formulations, accelerates nucleation and could promote the risk of crystallisation. These findings identify both beneficial and counterproductive formulation components and define a practical anticrystal engineering strategy to prevent ciprofloxacin-induced ocular precipitation. We anticipate that this study may inspire further work designing nucleation inhibitors for transient, high supersaturation conditions such as those seen regularly during drug delivery.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"218 ","pages":"Article 114933"},"PeriodicalIF":4.3,"publicationDate":"2025-11-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145511862","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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