Table of Content

03 July 2025, Volume 34 Issue 6

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Review

Inhalable formulations in pharmacy: from basic research to clinical applications

Yuying Yan, Xuebin Yang, Zhaoshuai Ji

2025, 34(6):  503-518.  DOI: 10.5246/jcps.2025.06.038

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In recent years, the rising prevalence of respiratory diseases, coupled with advancements in biotechnology and pharmacology, has positioned inhalable formulations as a preferred method of drug administration. This approach enables direct and rapid delivery of medication to the lungs, maximizing therapeutic effects while minimizing dosage and potential side effects. In this review, we meticulously examined current literature and clinical trial databases to present a comprehensive overview of three key areas: (1) inhalation devices currently utilized in clinical settings; (2) the clinical applications of approved inhalable formulations; and (3) preclinical research on inhalable treatments targeting various lung conditions, including pulmonary infections, tuberculosis, lung cancer, pulmonary fibrosis, as well as systemic diseases like Parkinson’s disease. The objective was to delve into both foundational research and the clinical use of inhalable formulations within the pharmaceutical field, with the aim of fostering their broader adoption and guiding the development of inhalable therapies for a more comprehensive range of diseases.



Original articles

Innovative hydroxamic acid-derived HDAC inhibitors: design, synthesis, and anticancer evaluation with diverse Zn²⁺-binding groups

Zhengrong Wu, Jingsi Zhao, Peng Jing, Dian He

2025, 34(6):  519-529.  DOI: 10.5246/jcps.2025.06.039

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A series of potential HDACIs containing diverse Zn²⁺-chelating hydroxamate moieties were synthesized and evaluated for their anticancer activity in vitro on HeLa, A549, and HepG2 cell lines. The A549 cell line was the most sensitive, and the most active compound, e8, exhibited an IC₅₀ value of 1.68 μmol/L, surpassing the positive control, SAHA (IC₅₀ = 4.85 μmol/L). Additionally, compound e8 demonstrated lower toxicity to normal WI-38 cells compared to SAHA (IC₅₀ = 415.93 μmol/L vs. 9.09 μmol/L). Furthermore, e8 efficiently induced G0/G1 phase cell cycle arrest and apoptosis in A549 cells. Molecular docking studies showed that compound e8 coordinated the Zn²⁺ cation at the enzyme’s active site and formed hydrophobic and hydrogen bonds within the hydrophobic pocket of the enzyme, resulting in stable docking with the HDAC enzyme. These studies suggested that compound e8 has the potential to be developed as a promising lead for further optimization and development of HDACIs.



Identification and validation of key genes involved in cellular senescence in multiple sclerosis using bioinformatics

Xiaoqin Zhang, Qiuhong Qin, Xiaojie Li, Jiangang Yang, Jibin Ma, Jianping Ren

2025, 34(6):  530-542.  DOI: 10.5246/jcps.2025.06.040

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Multiple sclerosis (MS) is a neurodegenerative disease, with aging being a significant risk factor that increases neural susceptibility to damage and reduces resilience. Cellular senescence (CS), a critical biological process of aging, also plays a pivotal role in MS pathogenesis. This study investigated the role of CS in MS by bioinformatics analyses, identifying key genes and potential therapeutic drugs. In differential gene expression (DEG) analysis, we identified 565 DEGs, comprising 166 upregulated and 399 downregulated genes (P < 0.05, |LogFC| > 1.5). Gene Set Enrichment Analysis (GSEA) revealed that these DEGs were enriched in pathways related to ribosomes, CS, and MAPK signaling. Weighted gene co-expression network analysis (WGCNA) identified the turquoise module, consisting of 164 genes, as having the strongest correlation with MS (R² = 0.54, P = 1e^–14). KEGG pathway analysis indicated that this module was most enriched in autophagy, Salmonella infection, and apoptosis pathways. Intersecting the DEGs, WGCNA key module genes, and 1381 CS-associated genes, we identified 49 key genes involved in MS. Machine learning algorithms further pinpointed ATF7IP, ATR, BCL10, CTNNB1, PDCD1, PIK3CA, TNFSF13, MSH3, HTR2A, and ALPL as MS hub genes, which were validated using the GSE13732 testing set. Seven candidate gene-related drugs were identified from DrugBank and the Comparative Toxicogenomics Database (CTD). Molecular docking results indicated that the binding energies for ATF7IP, ATR, BCL10, HTR2A, and PDCD10 with these drugs ranged from –2.444 to –6.523 Kcal/mol.



Effects of NRDL price negotiations on the pricing, market penetration, and spending of targeted lung cancer medications in China

Cheng Wang, Hongbin Yi, Sheng Han, Luwen Shi

2025, 34(6):  543-555.  DOI: 10.5246/jcps.2025.06.041

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Between 2016 and 2024, the Chinese government incorporated several innovative drugs into the National Reimbursement Drug List (NRDL) through price negotiations. These negotiations led to significant price reductions, which in turn stimulated an increase in sales. This study aimed to assess the impact of this policy on the pricing, utilization, and overall expenditure of targeted lung cancer therapies included in the NRDL. Using an interrupted time series analysis of procurement data from 698 healthcare institutions, the study evaluated both immediate and long-term effects. In terms of immediate effects, price negotiations resulted in a significant decline in the defined daily dose cost (DDDc) for all targeted therapies (P < 0.05). Regarding long-term trends, a significant shift was observed only in the pricing trajectory of Gefitinib, Icotinib, and Ensartinib (P < 0.05). In terms of immediate effects on drug utilization, all targeted medicines experienced a substantial increase in volume (P < 0.05), except for Gefitinib and Icotinib. Over the long term, the usage of all targeted therapies exhibited a significant upward trend (P < 0.05). With respect to expenditure, the immediate impact of NRDL inclusion resulted in a significant increase in spending on Afatinib, Crizotinib, Osimertinib, Alectinib, and Ensartinib (P < 0.05). Over time, total spending on targeted medicines showed a significant increase (P < 0.05), except for Erlotinib. Overall, NRDL price negotiations successfully reduced the economic burden on lung cancer patients, improving both accessibility and affordability of targeted therapies in China.



Meta-analysis of the impact of sacubitril/valsartan and ARB drugs on renal function

Jianmei Zhang, Jungang Lv, Hao Fu, Anqi Zhu, Fengying Hu, Zhaoyuan Shen, Fang Wang

2025, 34(6):  556-565.  DOI: 10.5246/jcps.2025.06.042

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To evaluate the effects of sacubitril/valsartan and ARB on renal function in patients with and without heart failure, we conducted a comprehensive literature search using both Chinese and English databases. These included the Cochrane Library, Wanfang Database, PubMed, CNKI, Embase, and Clinical Trials. The search encompassed studies published from the inception of the databases to March 2024. Randomized controlled studies meeting the inclusion criteria were assessed for bias using the Cochrane risk of bias assessment tool. Data were analyzed using Review Manager 5.4, with relative risk (RR) as the effect indicator. Depending on the heterogeneity of the studies, either a fixed-effects model or a random-effects model was employed to combine effect sizes. Seven studies met the inclusion criteria. Compared with ARB drugs, sacubitril/valsartan showed a reduction in the deterioration of renal function (RR = 0.70, 95% CI: 0.44–1.12, P = 0.14) and acute renal function injury (RR = 0.77, 95% CI: 0.59–1.00, P = 0.05). The risk of end-stage renal disease was also lower (RR = 0.53, 95% CI: 0.30–0.96, P = 0.16). For serum creatinine levels greater than 2.5 mg/dL, the RR was 0.88 (95% CI: 0.68–1.15, P = 0.37). For a reduction in eGFR of more than 25%, the RR was 0.89 (95% CI: 0.57–1.41, P = 0.63). The incidence of serum potassium levels greater than 5.5 mmol/L was not significantly different between the groups (RR = 1.23, 95% CI: 0.86–1.75, P = 0.26), nor was the incidence of serum potassium levels greater than 6.0 mmol/L (RR = 1.06, 95% CI: 0.58–1.93, P = 0.86). However, the incidence of eGFR decreasing by more than 50% was significantly reduced (RR = 0.58, 95% CI: 0.34–0.99, P < 0.05). In conclusion, sacubitril/valsartan demonstrated a protective effect on the kidneys, effectively reducing the risk of renal deterioration and presenting a potential alternative to ARB drugs.



Unveiling the prescription patterns and mechanisms of Chinese herbal compound patents in the management of acute appendicitis: A data mining investigation

Yuewen Li, Qinsheng Zhang, Suqin Hu

2025, 34(6):  566-580.  DOI: 10.5246/jcps.2025.06.043

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In the present study, data mining and network pharmacology were utilized to explore the principles and mechanisms of traditional Chinese medicine (TCM) in treating acute appendicitis. The goal was to provide a scientific basis for clinical treatment and further research on this disease. First, we searched the National Patent Database for Chinese herbal compound prescriptions used to treat acute appendicitis. We then applied frequency analysis, character and taste meridian analysis, association rule analysis, and hierarchical cluster analysis to identify the patterns of TCM treatment for acute appendicitis, selecting key combinations of Chinese medicines. Next, we screened the main active components of these key TCM based on quality markers. Using databases such as SwissTargetPrediction, SymMap, ETCM, and STRING, we analyzed the pharmacological mechanisms of these key TCM in treating acute appendicitis. Key active components and targets were further verified through molecular docking. We identified a total of 129 patents involving 316 Chinese medicines, with 24 being frequently used. The results indicated that most Chinese herbs used for acute appendicitis were heat-clearing drugs, blood-activating and stasis-removing drugs, and purging drugs. The primary active ingredients of the Rhubarb-cortex moutan-flos lonicerae combination for treating acute appendicitis included Emodin, Paeonol, Physcion, Chlorogenic acid, Chrysophanol, Rhein acid, and Aloe-emodin. These ingredients targeted key proteins such as ALB, TP53, BCL2, STAT3, IL-6, and TNF, and were involved in cellular responses to lipopolysaccharides, cell composition, and various cytokine-mediated biological processes. They also interacted with signaling pathways like AGE-RAGE, TNF, IL-17, and FoxO. Based on patent data, this study analyzed medication patterns in the treatment of acute appendicitis, discussed the possible mechanisms of key TCM combinations, and provided a scientific basis and new perspectives for the diagnosis and treatment of the disease.



Retrospective analysis of tigecycline-associated hypofibrinogenemia in patients with hypoproteinemia

Xiuzhen Liu, Jianjun Liu, Weiju Xue, Haiyan Xing, Yingli Zhao, Xing Fang

2025, 34(6):  581-591.  DOI: 10.5246/jcps.2025.06.044

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This study aimed to investigate the prevalence and risk factors associated with tigecycline-induced hypofibrinogenemia, providing critical insights for safer clinical drug use. A retrospective analysis was conducted on the medical records of patients with hypoproteinemia who received tigecycline treatment during hospitalization between January 1, 2020, and December 31, 2023. Key patient information was collected, including age, gender, weight, history of hematological diseases, medication dosage, treatment duration, concomitant medications, serum albumin and fibrinogen (FIB) levels before and after tigecycline administration, hepatic and renal function parameters, and other clinical characteristics. Patients were categorized into adverse drug reaction (ADR) and non-ADR groups, and comparisons were made to identify baseline characteristics and drug-related factors influencing tigecycline-induced FIB level reductions. Among 222 eligible patients, 71 (31.98%) developed hypofibrinogenemia. Univariate analysis identified significant associations between hypofibrinogenemia and treatment duration (P = 0.000), baseline FIB levels (P = 0.006), concomitant use of cefoperazone-sulbactam (P = 0.034), and concurrent administration of fat emulsion and heparin sodium injections (P < 0.044). Further multivariate logistic regression analysis revealed that a baseline FIB level below 5.1 g/L and concomitant use with cefoperazone-sulbactam were independent risk factors for tigecycline-induced FIB reduction. Conversely, a treatment duration of fewer than 9 d and higher albumin levels (light/medium/weight) were protective factors that reduced the risk of hypofibrinogenemia. This study highlighted that tigecycline-induced hypofibrinogenemia was a frequently encountered adverse effect in clinical practice. Patients with hypoproteinemia should undergo thorough evaluation prior to tigecycline administration, with particular attention to baseline FIB and albumin levels. Long-term use should be avoided, and combinations with medications that impair coagulation function should be minimized to mitigate the risk of hypofibrinogenemia associated with tigecycline.



News

The research team of Prof. Xinshan Ye has made significant progress in the comprehensive synthesis of a diverse fucoidan library and the evaluation of anticoagulant 

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center

2025, 34(6):  592-593. 

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The research team of Prof. Xinshan Ye has made significant progress in the comprehensive synthesis of a diverse fucoidan library and the evaluation of anticoagulant.



The research team of Prof. Min Ye and their collaborators have made progress in the research of a chalcone di-C-methyltransferase RdCMT from Rhododendron Dauricum

School of Pharmaceutical Sciences, Peking University Health Science Center

2025, 34(6):  594-595. 

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The research team of Prof. Min Ye and their collaborators have made progress in the research of a chalcone di-C-methyltransferase RdCMT from Rhododendron Dauricum.



The research team of Prof. Ming Ma analyzed the novel THDP-dependent enzyme structure and prepared carbon-carbon bond-linkage compounds by enzymatic method

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center

2025, 34(6):  596-601. 

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The research team of Prof. Ming Ma analyzed the novel THDP-dependent enzyme structure and prepared carbon-carbon bond-linkage compounds by enzymatic method.



The research team of Prof. Yimin Cui explored a new method for evaluating the  intestinal permeability of BCS drug regulated by gut microbiota

Department of Pharmacy Administration and Clinical Pharmacy, School of Pharmaceutical Sciences, Peking University Health Science Center

2025, 34(6):  602-604. 

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The research team of Prof. Yimin Cui explored a new method for evaluating the  intestinal permeability of BCS drug regulated by gut microbiota.