This letter addresses challenges in the clinical translation of BIBR1532,a promising telomerase inhibitor,for the treatment of esophageal squamous cell carcinoma(ESCC).BIBR1532 exerts its anti-cancer effect by activat...This letter addresses challenges in the clinical translation of BIBR1532,a promising telomerase inhibitor,for the treatment of esophageal squamous cell carcinoma(ESCC).BIBR1532 exerts its anti-cancer effect by activating DNA damage response(ATR/CHK1 and ATM/CHK2)pathways and downregulating telomere-binding proteins.Although its therapeutic potential is limited by poor aqueous solubility,solid dispersion(SD)technology may overcome this obstacle.Systematic analysis using PubChem-derived simplified molecular input line entry system identifiers and artificial intelligence-driven FormulationDT platform evaluation(oral formulation feasibility index:0.38)revealed that the SD technology,with superior scalability(32 approved products by 2021)and lower production risks,outperforms lipid-based formulations as an optimal dissolution strategy.Material analysis revealed hydroxypropyl methylcellulose(HPMC)as the optimal carrier with lower hygroscopicity,higher temperature and no intestinal targeting,thus enabling ESCC therapy.HPMC-based SD enhances BIBR1532 solubility and bioavailability for effective ESCC treatment.Future studies should focus on pilot tests for SD fabrication.展开更多
Xiao et al reported on the natural product sinomenine(SIN),which is a traditional Chinese medicine for treating osteoporosis via its modulation of autophagy;however,SIN was dissolved in dimethyl sulfoxide prior to adm...Xiao et al reported on the natural product sinomenine(SIN),which is a traditional Chinese medicine for treating osteoporosis via its modulation of autophagy;however,SIN was dissolved in dimethyl sulfoxide prior to administration,which is not conducive to the development of clinical injectables.By comparing solubilization techniques,including amorphisation,emulsification,micellisation,nanocrystallisation and host-vip inclusion,we found that the solubilization of SIN by host-vip inclusion can enhance solubility and improve stability and has an increased release rate and enhanced bioavailability.Therefore,we conclude that host-vip inclusion holds promise for SIN solubilization.To solubilise SIN,we selectedβ-cyclodextrin as the host agent considering its excellent biocompatibility,efficient encapsulation ability,mature preparation process and adequate drug stability.If the prerequisites of SIN-β-cyclodextrin complexes in terms of safety,efficacy,stability and the relevant laws and regulations are met,its clinical application for the treatment of osteoporosis may be achieved.展开更多
Background:Chinese medicine is widely applied in Asian and Western countries for its outstanding therapeutic effect,but there are still unsolved problems such as unclear active ingredients and pharmacological effects....Background:Chinese medicine is widely applied in Asian and Western countries for its outstanding therapeutic effect,but there are still unsolved problems such as unclear active ingredients and pharmacological effects.The application of nano/microparticle technology in Chinese medicine may become a promising strategy to solve this problem in the near future(provided that more efforts are made to in-depth exploration).In this work,a comprehensive analysis of the field was carried out from a bibliometrics perspective,and further the publishing trends and research hotspots were figured out.Methods:The articles or reviews from 2000 to 2020 were retrieved in the database of Web of Science Core Collection.The documents were processed by Clarivate Analytic,Visualization of Similarities viewer,Statistical Analysis Toolkit for Informetrics and bibliometric online platform,and the data were visualized.Finally,a bibliometric summary,citation analysis results and research trends were described.Results:A bibliometric analysis of 773 articles of interest showed that research in this field had continued to grow in recent years,with a high degree of interdisciplinary integration.Secondly,this field attached great importance to the quantitative analysis of Chinese medicine combined with nano/micro particle technology.Chinese medicine,nanoparticles and liposomes were the most accessed keywords.China was the main contributing country,and the top-10 contributing organizations were all located in China.Co-authorship was a common phenomenon in this field.Conclusion:The published literature on the application of nano/micro particle technology in Chinese medicine was summarized.The results suggested that bibliometric analysis could predict possible directions for future research in this field.展开更多
基金Supported by“Continuation”Project of Excellent Doctors,Guangdong Basic and Applied Basic Research Foundation,No.2025A04J5082Guangdong Basic and Applied Basic Research Foundation,No.2024A1515011236.
文摘This letter addresses challenges in the clinical translation of BIBR1532,a promising telomerase inhibitor,for the treatment of esophageal squamous cell carcinoma(ESCC).BIBR1532 exerts its anti-cancer effect by activating DNA damage response(ATR/CHK1 and ATM/CHK2)pathways and downregulating telomere-binding proteins.Although its therapeutic potential is limited by poor aqueous solubility,solid dispersion(SD)technology may overcome this obstacle.Systematic analysis using PubChem-derived simplified molecular input line entry system identifiers and artificial intelligence-driven FormulationDT platform evaluation(oral formulation feasibility index:0.38)revealed that the SD technology,with superior scalability(32 approved products by 2021)and lower production risks,outperforms lipid-based formulations as an optimal dissolution strategy.Material analysis revealed hydroxypropyl methylcellulose(HPMC)as the optimal carrier with lower hygroscopicity,higher temperature and no intestinal targeting,thus enabling ESCC therapy.HPMC-based SD enhances BIBR1532 solubility and bioavailability for effective ESCC treatment.Future studies should focus on pilot tests for SD fabrication.
基金Supported by Guangdong Basic and Applied Basic Research Foundation,No.2024A1515011236General Program of Administration of Traditional Chinese Medicine of Guangdong Province,No.20241071.
文摘Xiao et al reported on the natural product sinomenine(SIN),which is a traditional Chinese medicine for treating osteoporosis via its modulation of autophagy;however,SIN was dissolved in dimethyl sulfoxide prior to administration,which is not conducive to the development of clinical injectables.By comparing solubilization techniques,including amorphisation,emulsification,micellisation,nanocrystallisation and host-vip inclusion,we found that the solubilization of SIN by host-vip inclusion can enhance solubility and improve stability and has an increased release rate and enhanced bioavailability.Therefore,we conclude that host-vip inclusion holds promise for SIN solubilization.To solubilise SIN,we selectedβ-cyclodextrin as the host agent considering its excellent biocompatibility,efficient encapsulation ability,mature preparation process and adequate drug stability.If the prerequisites of SIN-β-cyclodextrin complexes in terms of safety,efficacy,stability and the relevant laws and regulations are met,its clinical application for the treatment of osteoporosis may be achieved.
基金the financial supports from the Fundamental Research Funds for the Central Universities(No.21621012)the National Natural Science Foundation of China(No.82104070).
文摘Background:Chinese medicine is widely applied in Asian and Western countries for its outstanding therapeutic effect,but there are still unsolved problems such as unclear active ingredients and pharmacological effects.The application of nano/microparticle technology in Chinese medicine may become a promising strategy to solve this problem in the near future(provided that more efforts are made to in-depth exploration).In this work,a comprehensive analysis of the field was carried out from a bibliometrics perspective,and further the publishing trends and research hotspots were figured out.Methods:The articles or reviews from 2000 to 2020 were retrieved in the database of Web of Science Core Collection.The documents were processed by Clarivate Analytic,Visualization of Similarities viewer,Statistical Analysis Toolkit for Informetrics and bibliometric online platform,and the data were visualized.Finally,a bibliometric summary,citation analysis results and research trends were described.Results:A bibliometric analysis of 773 articles of interest showed that research in this field had continued to grow in recent years,with a high degree of interdisciplinary integration.Secondly,this field attached great importance to the quantitative analysis of Chinese medicine combined with nano/micro particle technology.Chinese medicine,nanoparticles and liposomes were the most accessed keywords.China was the main contributing country,and the top-10 contributing organizations were all located in China.Co-authorship was a common phenomenon in this field.Conclusion:The published literature on the application of nano/micro particle technology in Chinese medicine was summarized.The results suggested that bibliometric analysis could predict possible directions for future research in this field.
