Journal of Pharmacy and Pharmacology最新文献

{"title":"GC-MS- and LC-TOF-MS/MS-based ginger volatile oil serum analysis and the potential mechanism of the anticancer effect of serum component citral on MCF-7 breast cancer cells.","authors":"Wenkai Zhang, Zhiyong Liu, Liming Luo, Lei Xu, Qiuting Ma, Shuai Huang, Tao Hong","doi":"10.1093/jpp/rgae116","DOIUrl":"10.1093/jpp/rgae116","url":null,"abstract":"<p><strong>Background: </strong>To explore the blood components of ginger volatile oil (GVO) after gastric perfusion in rats and its different metabolites from blank serum and the network pharmacological analysis and preliminary verification of the main components against breast cancer.</p><p><strong>Methods: </strong>A total of 20 male rats were randomly allocated to 10 control groups and 10 experimental groups. The administration group was given diluted GVO and the blank group was given the same amount of soybean oil (weigh 12 g of GVO diluted to 100 ml with soybean oil), the serum of rats in the given and blank groups was analyzed by gas chromatography-time-of-flight mass spectrometry, and the differential metabolites were screened and enriched, and the blood components were analyzed by ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS).</p><p><strong>Results: </strong>A total of 34 different metabolites were screened, and 31 original components were identified. The content of citral in volatile oil and serum is high, and the pathway of action is also closely related to the results of network pharmacology. Cell experiments showed that both drug-containing serum and citral significantly inhibited the proliferation and lateral transfer ability of breast cancer MCF-7 cells in a concentration and time-dependent manner, flow cytometry was used to measure apoptosis, and the experimental results showed that the proportion of early and late apoptosis was significantly increased in each group compared with the control group, and the proportion of total apoptosis showed a certain concentration-dependent trend.</p><p><strong>Conclusions: </strong>A combination of serum metabolism, network pharmacology, and experiments was employed; this study offers a significant contribution to the clarification of the material basis and molecular mechanism of GVO- medicated serum against breast cancer.</p>","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":" ","pages":"532-549"},"PeriodicalIF":2.8,"publicationDate":"2025-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142716344","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}

{"title":"Inhaled exogenous thymosin beta 4 suppresses bleomycin-induced pulmonary fibrosis in mice via TGF-β1 signalling pathway.","authors":"Rui Yu, Shimeng Li, Li Chen, Enbo Hu, Dan Chai, Zhichao Liu, Qianyi Zhang, Yunyun Mao, Yanfang Zhai, Kai Li, Yanhong Liu, Xiaohe Li, Honggang Zhou, Cheng Yang, Junjie Xu","doi":"10.1093/jpp/rgae143","DOIUrl":"10.1093/jpp/rgae143","url":null,"abstract":"<p><strong>Objectives: </strong>Idiopathic pulmonary fibrosis (IPF) is a chronic, progressive, and fibrotic interstitial lung disease. The two drugs indicated for IPF have limited efficacy and there is an urgent need to develop new drugs. Thymosin β4 (Tβ4) is a natural endogenous repair factor whose antifibrotic effects have been reported. This study aimed to evaluate the effect of exogenous recombinant human thymosin beta 4 (rhTβ4) on pulmonary fibrosis.</p><p><strong>Methods: </strong>Pulmonary fibrosis was induced in mice with bleomycin, and rhTβ4 was administrated by nebulization following three strategies: early dosing, mid-term dosing, and late dosing. The rhTβ4 efficacy was assessed by hydroxyproline, lung function, and lung histopathology. In vitro, the effects of rhTβ4 on fibroblast and lung epithelial cell phenotypes, as well as the TGF-β1 pathway, were evaluated.</p><p><strong>Key findings: </strong>Aerosol administration of rhTβ4 could alleviate bleomycin-induced pulmonary fibrosis in mice at different stages of fibrosis. Studies conducted in vitro suggested that rhTβ4 could suppress lung fibroblasts from proliferating, migrating, and activation via regulating the TGF-β1 signalling pathway. In vitro, rhTβ4 also inhibited the epithelial-mesenchymal transition-like process of pulmonary epithelial cells.</p><p><strong>Conclusions: </strong>This study suggests that nebulized rhTβ4 is a potential treatment for IPF.</p>","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":" ","pages":"582-592"},"PeriodicalIF":2.8,"publicationDate":"2025-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142695621","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}

{"title":"Tiaogan Jiejiu Tongluo formula alleviates hepatic steatosis in NAFLD mice by regulating AMPK signaling pathway.","authors":"Yuting Lei, Lianping Wang, Linze Song, Jiajun Han, He Ma, Haoming Luo, Yan Ma, Dong Han","doi":"10.1093/jpp/rgaf005","DOIUrl":"10.1093/jpp/rgaf005","url":null,"abstract":"<p><strong>Objectives: </strong>Tiaogan Jiejiu Tongluo formula (TJTF) is a traditional Chinese medicine formula for liver disease. The purpose of this study was to explore the protective effects and mechanisms of TJTF on nonalcoholic fatty liver disease (NAFLD) mice.</p><p><strong>Methods: </strong>A NAFLD model of mice was established by a combination of a high-fat diet and CCL4 and then treated with TJTF. The damage to liver tissue was observed through histopathology, and the levels of AST, ALT, TG, TC, LDL-C, and HDL-C in the serum, as well as SOD, GSH, and MDA in the liver tissue were determined using biochemistry or ELISA kit. The expression of proteins related to the AMPK pathway was detected by western blotting.</p><p><strong>Results: </strong>Biochemical indicators and pathological examination showed that TJTF could enhance the antioxidant capacity of liver tissue and significantly reduce liver lipid deposition. In addition, TJTF significantly increased levels of LKB1 and p-AMPK, and decreased the levels of HMGCR, SREBP-1c, FAS, and ACC.</p><p><strong>Conclusion: </strong>TJTF can alleviate hepatic steatosis and effectively improve NAFLD by regulating AMPK signaling pathway in NAFLD mice.</p>","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":" ","pages":"492-500"},"PeriodicalIF":2.8,"publicationDate":"2025-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143414475","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}

{"title":"Activation of HSPA5 contributes to pazopanib-induced hepatotoxicity through l-ornithine metabolism pathway and endoplasmic reticulum stress.","authors":"Jian Chen, Tieming Zhu, Yaping Deng, Jinliang Chen, Guojun Jiang, Qiaojun He","doi":"10.1093/jpp/rgae130","DOIUrl":"10.1093/jpp/rgae130","url":null,"abstract":"<p><strong>Objectives: </strong>The clinical application of Pazopanib (Paz) is often accompanied by hepatotoxicity. However, the mechanisms of hepatic toxicity induced by pazopanib are not entirely clarified.</p><p><strong>Methods: </strong>Male C57BL/6J mice were treated with pazopanib every day for 2, 4, or 8 weeks. Transcriptomics and metabolomics analyses of liver tissues were performed. In vitro experiments were carried out to estimate cell viability, apoptosis, and autophagy in L02 cells after Paz treatment. We also examined apoptosis and autophagy-related genes under 4-PBA, l-ornithine, nor-NOHA treatments, and HSPA5 knockdown.</p><p><strong>Key findings: </strong>Repeated Paz treatment for 8 weeks resulted in more severe hypofunction of the liver in mice. Moreover, Paz treatment inhibited L02 cells cell viability in a dose-dependent manner. We also discovered activation of endoplasmic reticulum stress, apoptosis, and autophagy in Paz-treated L02 cells, as evidenced by the boosted expression of HSPA5, p-IRE1α, ATF4, ATF6, p-eIF2α, LC3, Beclin-1, and a decrease of phosphorylated PI3K, AKT, and mTOR levels. Moreover, 4-PBA, l-ornithine, and HSPA5 knockdown inhibited apoptosis and autophagy, while nor-NOHA weakened the effects of HSPA5 knockdown on apoptosis in Paz-treated L02 cells.</p><p><strong>Conclusions: </strong>In summary, our study revealed that Paz-induced liver toxicity is related to HSPA5 expression and l-ornithine metabolism pathway in mice.</p>","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":" ","pages":"564-581"},"PeriodicalIF":2.8,"publicationDate":"2025-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142824285","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}

{"title":"Brazilian red propolis synergistically with imipenem modulates immunological parameters and the bactericidal activity of human monocytes against methicillin-resistant Staphylococcus aureus (MRSA).","authors":"Nicolas Ripari, Mariana da Silva Honorio, Arthur Alves Sartori, Larissa Ragozo Cardoso de Oliveira, Jairo Kenupp Bastos, José Maurício Sforcin","doi":"10.1093/jpp/rgae135","DOIUrl":"10.1093/jpp/rgae135","url":null,"abstract":"<p><strong>Objectives: </strong>Propolis is a bee product found all over the globe and has a well-known antibacterial activity. Previous findings of our group revealed that the combination of Brazilian red propolis (BRP) with a lower concentration of imipenem (IPM) exerted a bactericidal action against methicillin-resistant Staphylococcus aureus (MRSA) in vitro. Here, we aimed at investigating the effects of BRP in combination or not with IPM on human monocytes to assess a possible immunomodulatory action.</p><p><strong>Methods: </strong>Monocyte metabolic activity was analysed by MTT assay, cytokine production (TNF-α, IL-1β, IL-6, IL-8, and IL-10) by ELISA, and the expression of cell markers (TLR-2, TLR-4, HLA-DR, and CD80) by flow cytometry. The bactericidal activity of monocytes over MRSA was determined by colony-forming units' count.</p><p><strong>Key findings: </strong>BRP alone or in combination with IPM exerted no cytotoxic effects on monocytes. BRP downregulated TLR-2 expression and inhibited TNF-α, IL-1β, and IL-6 production, while BRP + IPM stimulated these parameters. BPR alone or in combination increased the bactericidal activity similarly to LPS-activated monocytes.</p><p><strong>Conclusions: </strong>Data indicated the potential of BRP as an anti-inflammatory agent increasing the bactericidal activity of monocytes against MRSA. The combination of BRP + IPM exhibited a stimulatory profile that may be potentially useful in treating patients with MRSA infection.</p>","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":" ","pages":"524-531"},"PeriodicalIF":2.8,"publicationDate":"2025-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142502626","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}

{"title":"Capsaicin: pharmacological applications and prospects for drug designing.","authors":"Anshita Gupta, Renjil Joshi, Lokkanya Dewangan, Kamal Shah, Deependra Soni, Umesh K Patil, Nagendra Singh Chauhan","doi":"10.1093/jpp/rgae150","DOIUrl":"10.1093/jpp/rgae150","url":null,"abstract":"<p><strong>Objectives: </strong>A primary objective of this review is to summarize the evidence-based pharmacological applications of capsaicin, particularly its use to manage pain and treat various health conditions. A second goal of the review is to research how recent technological advances are improving the bioavailability and therapeutic index of capsaicin, as well as the development of novel capsaicin-mimetics that are able to enhance therapeutic responses in various human diseases.</p><p><strong>Methods: </strong>In the review, numerous human clinical trials and preclinical studies are examined to determine how effective, safe, and optimal dosages of capsaicin can be used in pain management and therapeutic applications. Furthermore, it discusses capsaicin's mechanisms of action, specifically its interactions with the transient receptor potential vanilloid 1 (TRPV1) channel. As a result of this review, the potential of nanotechnology systems for bypassing the limits of capsaicin's pungency is discussed. The review takes into account individual factors such as pain tolerance and skin sensitivity.</p><p><strong>Key findings: </strong>For topical applications, capsaicin is typically used in concentrations ranging from 0.025% to 0.1%, with higher concentrations being used under medical supervision for neuropathic pain. The formulation can come in the form of creams, gels, or patches, which provide sustained release over the course of time. A condition such as arthritis or neuropathy can be relieved with capsaicin as it depletes substance P from nerves. Neuropathy and osteoarthritis as well as musculoskeletal disorders have been treated successfully with this herbal medicine. A major mechanism through which capsaicin relieves pain is through activating TRPV1 channels, which induce calcium influx and neurotransmitter release. Additionally, it affects the transcription of genes related to pain modulation and inflammation, particularly when disease conditions or stress are present. There have been recent developments in technology to reduce capsaicin's pungency and improve its bioavailability, including nanotechnology.</p><p><strong>Conclusions: </strong>It is proven that capsaicin is effective in pain management as well as a variety of therapeutic conditions because of its ability to deplete substance P and desensitize nerve endings. Although capsaicin is highly pungent and associated with discomfort, advancements in delivery technologies and the development of capsaicin-mimetics promise improved therapeutic outcomes. There is a great deal of complexity in the pharmacological action of capsaicin due to its interaction with TRPV1 channels and its ability to affect gene transcription. There is a need for further research and development in order to optimize capsaicin's clinical applications and to enhance its therapeutic index in a variety of human diseases.</p>","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":" ","pages":"459-474"},"PeriodicalIF":2.8,"publicationDate":"2025-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142807440","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}

{"title":"In vitro antidiabetic activity of Treculia africana leaf extracts: identification of chlorogenic acid and α-mangostin.","authors":"Victorine Lorette Yimgang, Elisa Pangrazzi, Francine Medjiofack Djeujo, Yanick Kevin Dongmo Melogmo, Franklin Loïc Tchinda Taghu, Rufin Marie Toghueo Kouipou, Fabrice Fekam Boyom, Guglielmina Froldi","doi":"10.1093/jpp/rgaf003","DOIUrl":"10.1093/jpp/rgaf003","url":null,"abstract":"<p><strong>Objective: </strong>This research studied two extracts from Treculia africana leaves for their potential against hyperglycaemia-related disorders.</p><p><strong>Methods: </strong>The influence of the extracts on α-glucosidase activity and albumin glycation was investigated, and cell viability was estimated in HT-29 human colorectal cells. Phenolic and flavonoid contents and antiradical activity were also detected. The extracts were examined using HPLC-DAD analysis.</p><p><strong>Key findings: </strong>The methanol and dichloromethane leaf extracts showed a significant concentration-dependent inhibition of α-glucosidase activity (IC50= 3.73 and 21.28 µg/ml, respectively). Both extracts also inhibited ribose-induced glycation of bovine serum albumin from 250 µg/ml. Phytochemical analysis revealed the presence of chlorogenic acid and α-mangostin in the extracts. The extracts did not change HT-29 cell viability up to 250 µg/ml, thus showing very low cytotoxicity.</p><p><strong>Conclusions: </strong>The methanol leaf extract of T. africana inhibited α-glucosidase activity in a concentration-dependent manner, supporting the use of the leaves in traditional medicine to control hyperglycaemia. Chlorogenic acid and α-mangostin, the latter identified for the first time in this species, were found in the T. africana leaves. Further, in vivo studies and pilot clinical trials should be conducted using standardized T. africana leaf extracts to evaluate their potential effectiveness in diabetes mellitus.</p>","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":" ","pages":"501-510"},"PeriodicalIF":2.8,"publicationDate":"2025-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143414466","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}

{"title":"Mechanism of Guishao Yigong decoction in treating colorectal cancer based on network pharmacology and experimental validation.","authors":"Yuwen Fan, Quyi Wang, Yun Zhang, Yu Wang, Wenwen Li, Shu Jiang, Ji-Nao Duan","doi":"10.1093/jpp/rgae045","DOIUrl":"10.1093/jpp/rgae045","url":null,"abstract":"<p><strong>Objectives: </strong>To explore the effective components of Guishao Yigong decoction (GYD) in the treatment of colorectal cancer and reveal its potential mechanism of action.</p><p><strong>Methods: </strong>Through network pharmacology, the main target and signaling pathway of GYD therapy for colorectal cancer (CRC) were found. Subsequently, the effect of GYD was verified by in vitro cell viability measurements, colony formation, and scratch healing tests. The effects of GYD on metabolic pathways in vivo were found through plasma metabolomics. Finally, flow cytometry and qPCR experiments were used to verify the cycle-blocking effect of GYD on CRC cells.</p><p><strong>Key findings: </strong>Based on the network pharmacological analysis and molecular docking technology, it was found that GYD could restrain the growth of CRC cells by affecting lipid metabolic pathways and mitogen-activated protein kinase (MAPK) signaling pathways. A series of cell experiments showed that GYD could inhibit the proliferation, migration and clonogenic ability of CRC cells. Furthermore, the plasma metabolomics results showed that GYD could affect the production of unsaturated fatty acids in mice. Flow cytometry and qPCR experiments further proved that GYD blocked the CRC cells in the G1 phase and modulated the expression of cell cycle-related targets, such as AKT, TP53, CDKN1A, and CDK2.</p><p><strong>Conclusions: </strong>All the results indicated that GYD could regulate the related metabolism of unsaturated fatty acids. Thus, the cell cycle was blocked and the expressions of the key proteins such as AKT and TP53 were regulated, which achieved the purpose of intervention in colorectal cancer.</p>","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":" ","pages":"430-445"},"PeriodicalIF":2.8,"publicationDate":"2025-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142348962","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}

{"title":"Ginsenoside Rb1 ameliorates hippocampal neuroinflammation in rats after intracerebral hemorrhage by inactivating the TLR4/NF-kB pathway.","authors":"Xi Liu, Yuying Wang, Ling Han, Xing Li, Yan Zhong, Jilin Zhou, Xiyun Fei, Min Peng, Jixin Duan, Zhijun Zhong","doi":"10.1093/jpp/rgae145","DOIUrl":"10.1093/jpp/rgae145","url":null,"abstract":"<p><strong>Purpose: </strong>This work elucidated the therapeutic effect and mechanism of ginsenoside Rb1 on intracerebral hemorrhage (ICH).</p><p><strong>Methods: </strong>ICH rat models were treated by ginsenoside Rb1. Modified neurological deficit score, and Y-maze and Morris water-maze tests were performed on rats. Hippocampal neuronal damage was observed by Nissl staining. Rat primary astrocytes were exposed to ginsenoside Rb1, Hemin, and lipopolysaccharide (LPS). TNF-α, IL-1β, and IL-6 levels were assessed via enzyme-linked immunosorbent assay. TLR4/NF-kB pathway activity was appraised by Western blot. Immunofluorescence staining was for hippocampal glial fibrillary acidic protein (GFAP) expression and P65 protein location in hippocampus and astrocytes.</p><p><strong>Results: </strong>In rats after ICH, ginsenoside Rb1 ameliorated neurological impairment and hippocampal neuronal damage; improved learning and memory ability; reduced brain water content; decreasedhippocampal TNF-α, IL-1β, and IL-6; inactivated TLR4/NF-kB pathway; and declined hippocampal GFAP expression. In rat primary astrocytes exposed to Hemin, ginsenoside Rb1 declined TNF-α, IL-1β, and IL-6; inactivated TLR4/NF-kB pathway; and hindered P65 protein entry into nucleus. However, these functions of ginsenoside Rb1 on the Hemin-induced astrocytes were abolished by LPS.</p><p><strong>Conclusion: </strong>Ginsenoside Rb1 has promising future for clinical ICH treatment, which exerts therapeutic effect on ICH by ameliorating hippocampal neuroinflammation via inactivating the TLR4/NF-kB pathway.</p>","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":" ","pages":"386-395"},"PeriodicalIF":2.8,"publicationDate":"2025-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142729722","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}

{"title":"Impact of nanostructured formulations for schistosomiasis treatment: a systematic review of in vivo preclinical evidence.","authors":"Laís de Castro Carvalho Silva, Luís Felipe Cunha Dos Reis, Luiz Cosme Cotta Malaquias, Flávia Chiva Carvalho, Rômulo Dias Novaes, Marcos José Marques","doi":"10.1093/jpp/rgae155","DOIUrl":"10.1093/jpp/rgae155","url":null,"abstract":"<p><strong>Background: </strong>Schistosomiasis is a neglected tropical disease caused by Schistosoma sp., and praziquantel (PZQ) is the first-line treatment. However, traditional PZQ formulations have low solubility and fast metabolism, limiting its effectiveness. Thus, nanoparticles have been proposed to improve the bioavailability and efficacy of poorly soluble antischistosomal drugs.</p><p><strong>Aims: </strong>This systematic review used in vivo preclinical studies to map the available evidence and compare the efficacy of free PZQ and PZQ-based nanostructured formulations (N-PZQ) for schistosomiasis treatment.</p><p><strong>Methods: </strong>PubMed, Embase, Scopus, and Web of Science were searched, and 1186 experimental studies published between 1974 and 2024 were screened. Parasitological, histopathological, pharmacokinetic, and toxicological outcomes were evaluated.</p><p><strong>Results: </strong>Twelve relevant studies were identified exploring N-PZQ formulations based on liposomes, nanoliposomes, and nanocrystals. N-PZQ demonstrated better therapeutic efficacy than free PZQ, reducing parasite load, modifying oogram profiles, and down-regulating liver granuloma development (number and size). N-PZQ also exhibited improved pharmacokinetic profile, with enhanced bioavailability and longer half-life, as well as reduced toxicity (cytotoxicity, genotoxicity, and hepatotoxicity) compared to free PZQ.</p><p><strong>Conclusion: </strong>PZQ-based nanostructured formulations represent a promising strategy to enhance schistosomiasis treatment by improving chemotherapy efficacy, optimizing antiparasitic responses, pharmacokinetics, and reducing drug toxicity.</p>","PeriodicalId":16960,"journal":{"name":"Journal of Pharmacy and Pharmacology","volume":" ","pages":"341-351"},"PeriodicalIF":2.8,"publicationDate":"2025-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143007252","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}