{"title":"新型s -氟比洛芬-二乙胺凝胶的研制与评价，具有优良的透皮给药和镇痛活性","authors":"Jian Zhang, Jinmeng Han, Anqi Zhu, Xiaoqian Zhu, Yuyu Zeng, Mingyue Yin, Yang Xiao, Chenchen Wang, Chaoyang Yin, Xingyin Wang, Guisen Zhang, Chao Hao","doi":"10.1002/jbm.a.37936","DOIUrl":null,"url":null,"abstract":"<div>\n \n <p>This study aimed to develop an innovative (S-flurbiprofen)-diethylamine (SFP-DEA) emulgel formulation via incorporating SFP as the active pharmaceutical ingredient within a carbomer 940 gel matrix. SFP-DEA emulgel was synthesized by dissolving SFP-DEA in the aqueous phase of an oil-in-water (O/W) emulsion, followed by dispersion into a carbomer 940 gel matrix. The physicochemical stability of SFP-DEA emulgel was evaluated via centrifuge, temperature swing test, high temperature, and long-term storage at ambient conditions. Ex vivo SFP transdermal delivery of SFP-DEA emulgel was evaluated using a Franz diffusion cell combined with excised rat skin. The in vivo analgesic activity and skin irritation test of SFP-DEA emulgel were evaluated using a mouse knee osteoarthritis model and healthy rats, respectively. Results demonstrated that SFP-DEA emulgel showed robust physicochemical stability and retain a final SFP content of 1.5% (w/w). Ex vivo transdermal study demonstrated that EMG5 (the emulgel optimized with laurocapram and menthol as penetration enhancers) achieved an 8-h cumulative SFP transdermal flux of 741.28 μg/cm<sup>2</sup> (44.23% of the administered dose), which is 27.94-fold higher than that of Loqoa (SFP tapes). In addition, SFP-DEA emulgel demonstrated rapid analgesic efficacy, with an 84.36% pain inhibition rate within 30 min in the osteoarthritis model, and elicited no signs of skin irritation in rats. In conclusion, the SFP-DEA emulgel developed herein exhibits high stability, enhanced transdermal delivery, preliminary analgesic activity, and favorable safety profiles, positioning it as a promising topical therapeutic candidate.</p>\n </div>","PeriodicalId":15142,"journal":{"name":"Journal of biomedical materials research. Part A","volume":"113 7","pages":""},"PeriodicalIF":3.9000,"publicationDate":"2025-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Development and Evaluation of an Innovative S-Flurbiprofen-Diethylamine Emulgel With Superior Transdermal Delivery and Analgesic Activity\",\"authors\":\"Jian Zhang, Jinmeng Han, Anqi Zhu, Xiaoqian Zhu, Yuyu Zeng, Mingyue Yin, Yang Xiao, Chenchen Wang, Chaoyang Yin, Xingyin Wang, Guisen Zhang, Chao Hao\",\"doi\":\"10.1002/jbm.a.37936\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div>\\n \\n <p>This study aimed to develop an innovative (S-flurbiprofen)-diethylamine (SFP-DEA) emulgel formulation via incorporating SFP as the active pharmaceutical ingredient within a carbomer 940 gel matrix. SFP-DEA emulgel was synthesized by dissolving SFP-DEA in the aqueous phase of an oil-in-water (O/W) emulsion, followed by dispersion into a carbomer 940 gel matrix. The physicochemical stability of SFP-DEA emulgel was evaluated via centrifuge, temperature swing test, high temperature, and long-term storage at ambient conditions. Ex vivo SFP transdermal delivery of SFP-DEA emulgel was evaluated using a Franz diffusion cell combined with excised rat skin. The in vivo analgesic activity and skin irritation test of SFP-DEA emulgel were evaluated using a mouse knee osteoarthritis model and healthy rats, respectively. Results demonstrated that SFP-DEA emulgel showed robust physicochemical stability and retain a final SFP content of 1.5% (w/w). Ex vivo transdermal study demonstrated that EMG5 (the emulgel optimized with laurocapram and menthol as penetration enhancers) achieved an 8-h cumulative SFP transdermal flux of 741.28 μg/cm<sup>2</sup> (44.23% of the administered dose), which is 27.94-fold higher than that of Loqoa (SFP tapes). In addition, SFP-DEA emulgel demonstrated rapid analgesic efficacy, with an 84.36% pain inhibition rate within 30 min in the osteoarthritis model, and elicited no signs of skin irritation in rats. In conclusion, the SFP-DEA emulgel developed herein exhibits high stability, enhanced transdermal delivery, preliminary analgesic activity, and favorable safety profiles, positioning it as a promising topical therapeutic candidate.</p>\\n </div>\",\"PeriodicalId\":15142,\"journal\":{\"name\":\"Journal of biomedical materials research. Part A\",\"volume\":\"113 7\",\"pages\":\"\"},\"PeriodicalIF\":3.9000,\"publicationDate\":\"2025-07-04\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of biomedical materials research. Part A\",\"FirstCategoryId\":\"5\",\"ListUrlMain\":\"https://onlinelibrary.wiley.com/doi/10.1002/jbm.a.37936\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"ENGINEERING, BIOMEDICAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of biomedical materials research. Part A","FirstCategoryId":"5","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/jbm.a.37936","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"ENGINEERING, BIOMEDICAL","Score":null,"Total":0}
Development and Evaluation of an Innovative S-Flurbiprofen-Diethylamine Emulgel With Superior Transdermal Delivery and Analgesic Activity
This study aimed to develop an innovative (S-flurbiprofen)-diethylamine (SFP-DEA) emulgel formulation via incorporating SFP as the active pharmaceutical ingredient within a carbomer 940 gel matrix. SFP-DEA emulgel was synthesized by dissolving SFP-DEA in the aqueous phase of an oil-in-water (O/W) emulsion, followed by dispersion into a carbomer 940 gel matrix. The physicochemical stability of SFP-DEA emulgel was evaluated via centrifuge, temperature swing test, high temperature, and long-term storage at ambient conditions. Ex vivo SFP transdermal delivery of SFP-DEA emulgel was evaluated using a Franz diffusion cell combined with excised rat skin. The in vivo analgesic activity and skin irritation test of SFP-DEA emulgel were evaluated using a mouse knee osteoarthritis model and healthy rats, respectively. Results demonstrated that SFP-DEA emulgel showed robust physicochemical stability and retain a final SFP content of 1.5% (w/w). Ex vivo transdermal study demonstrated that EMG5 (the emulgel optimized with laurocapram and menthol as penetration enhancers) achieved an 8-h cumulative SFP transdermal flux of 741.28 μg/cm2 (44.23% of the administered dose), which is 27.94-fold higher than that of Loqoa (SFP tapes). In addition, SFP-DEA emulgel demonstrated rapid analgesic efficacy, with an 84.36% pain inhibition rate within 30 min in the osteoarthritis model, and elicited no signs of skin irritation in rats. In conclusion, the SFP-DEA emulgel developed herein exhibits high stability, enhanced transdermal delivery, preliminary analgesic activity, and favorable safety profiles, positioning it as a promising topical therapeutic candidate.
期刊介绍：
The Journal of Biomedical Materials Research Part A is an international, interdisciplinary, English-language publication of original contributions concerning studies of the preparation, performance, and evaluation of biomaterials; the chemical, physical, toxicological, and mechanical behavior of materials in physiological environments; and the response of blood and tissues to biomaterials. The Journal publishes peer-reviewed articles on all relevant biomaterial topics including the science and technology of alloys,polymers, ceramics, and reprocessed animal and human tissues in surgery,dentistry, artificial organs, and other medical devices. The Journal also publishes articles in interdisciplinary areas such as tissue engineering and controlled release technology where biomaterials play a significant role in the performance of the medical device.
The Journal of Biomedical Materials Research is the official journal of the Society for Biomaterials (USA), the Japanese Society for Biomaterials, the Australasian Society for Biomaterials, and the Korean Society for Biomaterials.
Articles are welcomed from all scientists. Membership in the Society for Biomaterials is not a prerequisite for submission.
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