Pharmaceutical Science Advances最新文献

{"title":"Assay development and screening of inhibitors targeting the SARS-CoV-2 2′-O-methyltransferase NSP16","authors":"Mengtong Cao ,&nbsp;Carl W. Trieshmann ,&nbsp;Subodh Kumar Samrat ,&nbsp;Hongmin Li ,&nbsp;Yifei Wu ,&nbsp;Steven P. Maher ,&nbsp;Angela A. Bae ,&nbsp;Zhong-Ru Xie ,&nbsp;Robert J. Hogan ,&nbsp;Y. George Zheng","doi":"10.1016/j.pscia.2025.100076","DOIUrl":"10.1016/j.pscia.2025.100076","url":null,"abstract":"<div><div>The coronavirus disease-2019 (COVID-19) pandemic, etiologically caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has profoundly impacted the global health. While vaccines have been developed, they have shown limited efficacy in treating patients already under infection or preventing infection with emerging SARS-CoV-2 variants. The nonstructural protein 16 (NSP16), with the assistance of the nonstructural protein 10 (NSP10), is responsible for forming the Cap-1 structure, which is critical for viral replication and immune evasion through the 5′-capping of viral mRNA. As a result, NSP16/NSP10 has emerged as a promising target for antiviral treatment of coronaviruses. In this study, we aimed to discover small molecule inhibitors of NSP16/NSP10 by leveraging recent structural insights and combined tools of virtual and experimental screenings. We designed a simple scintillation proximity assay to enable biochemical testing for NSP16/NSP10 enzymatic activity and applied it to screen inhibitors from candidate hit compounds that are derived from molecular docking-based virtual screenings. We identified potential hits that inhibit the NSP16 activity with cellular efficacy. Together with structural analysis and chemotype categorization, this study lays the groundwork for novel antiviral therapeutics development against SARS-CoV-2 and related coronaviruses.</div></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"3 ","pages":"Article 100076"},"PeriodicalIF":0.0,"publicationDate":"2025-05-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144166610","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"D-pinitol modulates the anti-emetic effects of aprepitant, domperidone, and ondansetron in chicks","authors":"Md. Elit Rahman ,&nbsp;Md. Anisur Rahman ,&nbsp;Salehin Sheikh ,&nbsp;Md. Jannatul Islam Polash ,&nbsp;Sozoni Khatun ,&nbsp;Mst. Sonia Akter Bristi ,&nbsp;Md. Showkoth Akbor ,&nbsp;Mst. Farjanamul Haque ,&nbsp;Mehedi Hasan Bappi ,&nbsp;Tohidul Islam Tanim ,&nbsp;Siddique Akber Ansari ,&nbsp;Irfan Aamer Ansari ,&nbsp;Elaine Cristina Pereira Lucetti ,&nbsp;Carolina Bandeira Domiciano ,&nbsp;Henrique D.M. Coutinho ,&nbsp;Muhammad Torequl Islam","doi":"10.1016/j.pscia.2025.100073","DOIUrl":"10.1016/j.pscia.2025.100073","url":null,"abstract":"<div><div>Naturally occurring substance, D-pinitol (DPL) belongs to the significant inositol family has numerous pharmacological activity. In this study we evaluated the anti-emetic effect as well as modulation activities of DPL on the recent market drugs aprepitant (APR), domperidone (DOM), hyoscine butyl bromide (HYS), and ondansetron (ODN) on emesis in the chick model. To highlight the possible anti-emetic activity in copper sulfate induced emesis chick models, we use several reference drugs, such as APR (26 ​mg/kg), DOM (7 ​mg/kg), OND (5 ​mg/kg), and HYS (21 ​mg/kg), as positive controls, while the vehicles serve as negative controls. All reference drugs are given alone or in combined groups to evaluate their anti-emetic and modulation effects. The results suggest DPL (25 or 50 ​mg/kg) increases the mean number of latency in the chicks compared to vehicles, and the combination groups, DPL (25 ​mg/kg) showed better anti-emetic effects with DOM and ODN while DPL (50 ​mg/kg) reduces the number of retches compared to vehicles and combined drug therapy with reference drugs. Additionally, A variety of computational algorithms were used to visualise ligand–receptor interactions and quantify the binding affinities of DPL and other ligands towards the dopamine receptors (D2 and D3), muscarinic acetylcholine receptors (M1–M5), and serotonin receptor (5HT3). The molecular docking study indicated that DPL exhibits the highest binding affinity towards subtypes M2 (having a docking score of −5.7 ​kcal/mol) and D3 (having a docking score of −5.7 ​kcal/mol) in comparison to certain standards for these receptors, which have docking scores of DOM (−9.7 ​kcal/mol) and HYS (−7.1 ​kcal/mol) for M2 and D3, respectively. Our findings suggest that DPL has anti-emetic properties in chicks, possibly through interactions with the M2 and D3 receptor pathways.</div></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"3 ","pages":"Article 100073"},"PeriodicalIF":0.0,"publicationDate":"2025-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144089481","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The crucial role of SPP1 in osteoporosis, osteoarthritis, and cancer","authors":"Yaru Qu ,&nbsp;Shuixian Li ,&nbsp;Huiyuan Luo ,&nbsp;Junnan Li ,&nbsp;Tong Wang ,&nbsp;Xiuzhen Han","doi":"10.1016/j.pscia.2025.100074","DOIUrl":"10.1016/j.pscia.2025.100074","url":null,"abstract":"<div><div>Osteopontin (OPN), also known as secreted phosphoprotein 1(SPP1), is a highly glycosylated and phosphorylated acidic protein, which is a multifunctional glycoprotein expressed in numerous cell types. SPP1 is involved in the attachment of osteoclasts to mineralized bone matrix, inflammatory reaction, cell recruitment, and tissue repair, and plays an important role in bone formation, fibrosis, immune diseases, and cancer. The role of SPP1 in osteoporosis, osteoarthritis and cancer is multi-faceted. While it holds potential therapeutic value, it also presents certain limitations. This review integrates the molecular structural characteristics of SPP1, including isoform variants and post-translational modifications, with its pathophysiological functions. It highlights the regulatory roles of SPP1 in these diseases: maintaining the dynamic balance between bone resorption and formation in osteoporosis, promoting cartilage degeneration and inflammation in osteoarthritis, and driving tumor progression in cancer through the activation of pathways such as PI3K/AKT/mTOR. Furthermore, SPP1 regulates tumor-associated macrophages and fibroblasts within the tumor microenvironment, thereby facilitating immune evasion and metastasis. The article also underscores the potential value of precisely modulating SPP1 activity in the treatment of osteoporosis and osteoarthritis and suggests a combined therapeutic strategy targeting SPP1, offering novel insights into overcoming the limitations of single-target cancer therapies.</div></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"3 ","pages":"Article 100074"},"PeriodicalIF":0.0,"publicationDate":"2025-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144070718","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"GLDC interacts with VPS34 to inhibit tumorigenesis and epithelial-mesenchymal transition in hepatocellular carcinoma","authors":"Zan Song ,&nbsp;Hao Dong ,&nbsp;Kailing Zhang ,&nbsp;Bingke Qiao ,&nbsp;Leilei Li ,&nbsp;Zhicheng Zhang ,&nbsp;Zhili Fan ,&nbsp;Jing Li ,&nbsp;Yu Li ,&nbsp;Mengfei Liu ,&nbsp;Ying Liu ,&nbsp;Xinyu Gu ,&nbsp;Tao Zhang","doi":"10.1016/j.pscia.2025.100072","DOIUrl":"10.1016/j.pscia.2025.100072","url":null,"abstract":"<div><div>Hepatocellular carcinoma (HCC) accounts for 90% of primary liver cancer with high mortality and limited therapeutic strategy. Glycine decarboxylase (GLDC) is the key limiting enzyme in glycine breakdown metabolism and acts as oncogene or tumor suppressor to impact tumor onset and progression in a context dependent manner. However, the underlying mechanism of GLDC on autophagy and progression is largely unexplored in HCC. Here, we showed that GLDC overexpression inhibited cell proliferation, cell migration and promoted cell senescence and autophagy in HCC. Intriguingly, induced GLDC remarkably attenuated epithelial-mesenchymal transition (EMT) progress and tumor growth <em>in vitro</em> and <em>in vivo</em>. Mechanically, we demonstrated that GLDC upregulated VPS34 protein and enhanced its interaction with VPS34, thus promoting the association of VPS34 with Beclin1/ATG14 complex and autophagy induction in HCC. Importantly, GLDC acetylation at K514 promoted interaction of GLDC-VPS34, whereas GLDC acetylation-dead mutant K514R abolished their binding. Furthermore, GLDC protein was decreased in HCC tissues compared with para-tumor tissues and reduced GLDC was significantly correlated with poor prognosis of patients. In conclusion, we unveil the key regulatory role of GLDC in autophagy and HCC progression through VPS34 and provide a potential strategy for HCC therapy.</div></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"3 ","pages":"Article 100072"},"PeriodicalIF":0.0,"publicationDate":"2025-04-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143927771","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Research progress of glutarimide-containing polyketides: Structures, bioactivities and their biosynthesis","authors":"Yanrong Shi ,&nbsp;Chunhua Lu ,&nbsp;Yuemao Shen","doi":"10.1016/j.pscia.2025.100071","DOIUrl":"10.1016/j.pscia.2025.100071","url":null,"abstract":"<div><div>Glutarimide-containing polyketides (GPs) are an important class of natural products with antifungal, antibacterial, antitumor and other biological activities. Generally, the structures have a six-membered ring of glutarimide (also known as 2,6-piperidinedione) and a polyketide side chain or a ring of varying lengths attached at C4 such as cycloheximide, 9-methylstreptimidone and migrastatin. Currently, at least 65 natural glutarimide antibiotics have been isolated and identified. The novel biosynthetic mechanism of the <em>trans</em>-AT PKS and multifaceted modes of action have promoted the progressive exploration of glutarimide-containing products. However, the related information on the aspects of new structure discovery, biological activity and biosynthesis of GPs is still not available. This review summarizes the current research from the aspects of new structure discovery, biological activity and biosynthesis, aiming to provide a reference for in-depth products mining and structure-activity relationship research. Special emphasis is placed on their potential as drug leads, particularly in cancer therapy, and the role of modern analytical techniques in their discovery and characterization.</div></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"3 ","pages":"Article 100071"},"PeriodicalIF":0.0,"publicationDate":"2025-04-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143912263","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Antimicrobial potentials and challenges of paracetamol: A comprehensive reassessment based on database reports","authors":"Muhammad Torequl Islam ,&nbsp;Raihan Chowdhury ,&nbsp;Md. Shimul Bhuia ,&nbsp;Md. Sakib Al Hasan ,&nbsp;Md. Showkot Akbor ,&nbsp;Fardin Farhad ,&nbsp;Carolina Bandeira Domiciano ,&nbsp;Davi Antas e Silva ,&nbsp;Henrique D.M. Coutinho","doi":"10.1016/j.pscia.2025.100070","DOIUrl":"10.1016/j.pscia.2025.100070","url":null,"abstract":"<div><div>Paracetamol (PMCL) is an analgesic-antipyretic drug. It is frequently used as an over-the-counter (OTC) drug in many countries around the world, especially for headaches, mild pain, and fever. Knowing its toxic effects on the nervous and hepatic systems, it has been combined with the psychoactive drug caffeine. However, PMCL's antipyretic action during fevers caused by various pathogens might be due to its antimicrobial power. Therefore, we have a question about whether PMCL can be used as an OTC medication or not. This review aimed to summarize the antimicrobial activity, facts behind it, possible action mechanisms, and causes of resistance growth, along with the antimicrobial and toxicological impacts of its metabolites, derived products, and combination products, on the basis of database reports. Numerous pieces of evidence suggest that both PMCL and caffeine have broad-spectrum antimicrobial effects. PMCL is evidently effective against gram-positive and gram-negative bacteria, fungi, viruses, and protozoa. Its major toxic metabolite, <em>N</em>-acetyl-p-benzoquinone imine (NAPQI), also has antimicrobial potential. Despite its antimicrobial effects, PMCL has contributed to antimicrobial resistance. In conclusion, according to the findings from database reports, PMCL is not only an analgesic-antipyretic drug, but it also has broad-spectrum antimicrobial potential against many pathogenic gram-positive and gram-negative bacteria and fungi as well as some viruses and protozoa. The use of PMCL as an OTC medication might bring a dangerous health issue in the future among the population, for example, growing microbial resistance and harmful toxicological impacts in different organs in humans.</div></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"3 ","pages":"Article 100070"},"PeriodicalIF":0.0,"publicationDate":"2025-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143882264","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Microdynamic flowability for early API characterisation: A case study on Palbociclib","authors":"David Blanco ,&nbsp;Nicolas Pätzmann ,&nbsp;Pablo García-Triñanes","doi":"10.1016/j.pscia.2025.100069","DOIUrl":"10.1016/j.pscia.2025.100069","url":null,"abstract":"<div><div>This study explores microdynamic flowability as an innovative approach for early active pharmaceutical ingredient (API) characterisation, when compounds are often scarce and/or expensive. By incorporating small-scale flow measurements during the pre-formulation stage, we aim to support strategic decision-making in formulation development and process design. Laboratory-scale micronisation of the poorly water-soluble drug Palbociclib, while enhancing dissolution, was found to adversely affect flowability. Agglomeration driven by cohesive forces was quantitatively described for the first time via image analysis using sample quantities of less than 200 mg. Our findings demonstrate that microdynamic flow studies provide critical insights into the processability of APIs under low-stress conditions, such as those relevant to research and development (R&amp;D) tablet presses. These results highlight the value of advanced flowability analysis in early-stage development, enabling improved understanding and control of powder processing in pharmaceutical manufacturing and particle engineering.</div></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"3 ","pages":"Article 100069"},"PeriodicalIF":0.0,"publicationDate":"2025-03-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143714447","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Nasal powder formulation employing microenvironmental pH-modifier for rapid absorption of mirtazapine","authors":"Kohei Yamada ,&nbsp;Tsubasa Kihara ,&nbsp;Kaori Shinsato ,&nbsp;Hirofumi Yasui ,&nbsp;Michihiro Shino ,&nbsp;Hideyuki Sato ,&nbsp;Satomi Onoue","doi":"10.1016/j.pscia.2025.100068","DOIUrl":"10.1016/j.pscia.2025.100068","url":null,"abstract":"<div><div>Antidepressant mirtazapine (MRZ) has been drawing attention in the management of delirium. However, oral use of MRZ could have drawbacks in onset of actions and ease of administration by caregivers. This study was the first attempt to develop nasal powder formulation (NP), an easily-administered formulation, of MRZ containing a microenvironmental pH-modifier for rapid dissolution and absorption. Ten mixtures of MRZ and counterions were tested in terms of the supersaturation level and stability to select a favorable pH-modifier. NP of MRZ (NP/MRZ) with the selected counterion was prepared by jet milling and characterized regarding physicochemical properties and pharmacokinetic (PK) behaviors after intranasal administration to rabbits. In phosphate buffer solution (PBS, pH5.6), glutamic acid (Glu) showed 10.7-fold supersaturation of MRZ, with the value being the highest among the ten counterions tested. The addition of Glu led to no significant change in the photostability or chemical stability of MRZ compared with crystalline MRZ. NP/MRZ with Glu (NP/MRZ-E) consisted of microcrystals of MRZ and Glu attached to lactose carriers, and over 93% of MRZ was emitted from a capsule in Jetlizer™. Both NP/MRZ-E and NP/MRZ exhibited enhanced dissolution in PBS compared with crystalline MRZ, and more rapid dissolution was observed for NP/MRZ-E. In rabbits, a crushed MRZ tablet (3 ​mg-MRZ/kg, <em>p.o.</em>) exhibited a time to maximum plasma concentration (<em>T</em>_max) and bioavailability (BA) of 72 ​min and 10%, respectively. NP/MRZ-E (0.3 ​mg-MRZ/kg, <em>i.n.</em>) showed <em>T</em>_max of &lt;5 ​min with BA of 93%, and this result might be due to rapid dissolution/permeation in nasal mucosa and avoidance of the hepatic first-pass effect. In conclusion, NP employing a microenvironmental pH-modifier would be a promising dosage form of MRZ to offer rapid nasal absorption.</div></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"3 ","pages":"Article 100068"},"PeriodicalIF":0.0,"publicationDate":"2025-03-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143714445","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Nanodispersion of lutein with use of metastable polymorph for improved dissolution and oral absorption","authors":"Kodai Ueno,&nbsp;Monami Sugihara,&nbsp;Tetsuya Matsushita,&nbsp;Kohei Yamada,&nbsp;Hideyuki Sato,&nbsp;Satomi Onoue","doi":"10.1016/j.pscia.2025.100067","DOIUrl":"10.1016/j.pscia.2025.100067","url":null,"abstract":"<div><div>Lutein (LT) is an attractive nutrient for eye health, although it has low water solubility and poor oral absorption. The present study aimed to develop a novel nanodispersion (ND) of LT using a metastable polymorph, offering improved oral absorption of LT. A metastable crystalline form of LT (LT-II) and hydroxypropyl cellulose were subjected to wet-milling followed by freeze-drying to obtain the ND of LT-II (ND/LT-II), and its physicochemical, photochemical, and pharmacokinetic properties of LT samples were evaluated. The mean particle size of LT-II in ND/LT-II was 354 ​nm, and there was no significant change in the crystalline form of LT-II, even after wet milling and freeze-drying. LT generated significant amounts of superoxide anions upon exposure to pseudo-sunlight (250 ​W/m²), indicating high photoreactivity. After irradiation with pseudo-sunlight (250 ​W/m², 30 ​min), the percentages of LT remaining in the LT solution, amorphous LT, and ND/LT-II were 75, 79, and 92%, respectively. LT-II dissolved slightly faster than the stable crystalline form of LT (LT-I) in the dissolution media. ND/LT-II further improved the dissolution property of LT-II, and the dissolved amount of LT was 137- and 7.2-fold higher than that of LT-I and LT-II, respectively, at 2 ​h after dispersion in water. After administration of LT samples (100 ​mg-LT/kg), systemic exposure to LT in the LT-I and LT-II was negligible, whereas a marked improvement in oral absorption was observed in the ND/LT-II groups. Thus, applying ND technology to LT-II may improve oral absorption, and thus the nutrient function of LT.</div></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"3 ","pages":"Article 100067"},"PeriodicalIF":0.0,"publicationDate":"2025-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143619296","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Preparation and characterization of tadalafil-loaded hydrogel: An in-vivo evaluation of wound healing activity","authors":"Anita Sadat Haji Seyed Javadi Pajouhi ,&nbsp;Amir Larki-Harcheghani ,&nbsp;Mojdeh Mohammadi ,&nbsp;Sajjad Makhdoomi ,&nbsp;Alireza Nourian ,&nbsp;Katayoun Derakhshandeh","doi":"10.1016/j.pscia.2025.100066","DOIUrl":"10.1016/j.pscia.2025.100066","url":null,"abstract":"<div><div>Tadalafil (TD) is a phosphodiesterase type 5 (PDE-5) inhibitor that has gained attention for its wound healing properties. In this study, a TD-loaded hydrogel was prepared and characterized, and its wound-healing efficacy was evaluated. After preparing the TD hydrogel, its physicochemical properties such as viscosity, pH, drug-loading capacity (DL%), <em>in vitro</em> release behavior, and stability were characterized. Moreover, <em>in vivo</em> studies were performed to evaluate hydroxyproline (HP) and the wound healing efficacy of 1, 1.5, 3% (w/w) TD hydrogels in New Zealand rabbits. Histopathological analysis was also performed using hematoxylin and eosin (H&amp;E) staining. We successfully prepared a TD hydrogel with high stability. The results of the <em>in vivo</em> experiments on full-thickness wounds showed that the 1.5% TD hydrogel with a pH of 5.81 ​± ​0.421, viscosity of 12,435 ​± ​63, drug-loading capacity of 91.73 ​± ​1.482%, and drug release rate of 88% was superior to other formulations when HP level was increased, which decreased the time required for wound healing; this was corroborated by the histological analysis. Thus, the TD hydrogel formulation prepared in this study is a promising topical therapeutic agent for wound healing.</div></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"3 ","pages":"Article 100066"},"PeriodicalIF":0.0,"publicationDate":"2025-02-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143714446","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}