收藏切换
Preparation, pharmacokinetic and pharmacodynamic studies of ketorolac tromethamine oral mucosal microneedles
收藏切换
Gui-yu HUANG1, 2, Jing-zhe WANG1, Li-na DU1, 2, *
Acta Pharmaceutica Sinica | 2026, 61(9) : 3466 - 3474
Less
收藏切换
Acta Pharmaceutica Sinica | 2026, 61(9): 3466-3474
• Original Articles •
Preparation, pharmacokinetic and pharmacodynamic studies of ketorolac tromethamine oral mucosal microneedles
Full
Gui-yu HUANG1, 2, Jing-zhe WANG1, Li-na DU1, 2, *
Affiliations
  • 1Academy of Military Medical Sciences, Academy of Military Sciences, Beijing 100850, China
  • 2School of Pharmacy, Henan University, Kaifeng 450001, China
Published: 2026-09-12 doi: 10.16438/j.0513-4870.2026-0030
Outline
收藏切换

Ketorolac tromethamine (KT) is characterized by a short half-life and rapid systemic clearance, necessitating frequent dosing when administered via traditional oral or injectable routes, and is associated with pronounced first-pass metabolism and gastrointestinal adverse effects. To mitigate these limitations, this study developed ketorolac tromethamine microneedles (KTMN) for buccal mucosal delivery and evaluated their analgesic efficacy. The microneedle tips were fabricated using a photosensitive hyaluronic acid methacrylate solution as the matrix, which was cast into polydimethylsiloxane molds, followed by drying and UV crosslinking to yield well-formed KTMNs. Each microneedle exhibited a mechanical strength of 0.70 N and achieved a penetration depth of 120 μm in rat buccal mucosa. In artificial saliva, KTMNs demonstrated sustained and stable drug release, with an in vitro release rate of 55.33% at 2 h and 76.77% at 12 h. Pharmacokinetic analysis revealed a peak plasma concentration of 5.91 μg·mL-1 at 2 h post-administration, with an average residence time extending up to 15.52 h. In vivo, KTMN administration significantly attenuated pain responses in both the formalin-induced pain model and the carrageenan-induced inflammatory pain model in rats. Overall, buccal mucosal delivery of KTMNs represents a safe, rapid, and efficient formulation, offering a promising new strategy for fast-acting, long-lasting, and convenient analgesia.

analgesia  /  microneedle  /  oral mucosa  /  mucosal drug delivery  /  pharmacokinetics
黄桂玉, 王京哲, 杜丽娜. 酮咯酸氨丁三醇口腔黏膜微针的制备及药动学、药效学研究. 药学学报, 2026 , 61 (9) : 3466 -3474 . DOI: 10.16438/j.0513-4870.2026-0030
Gui-yu HUANG, Jing-zhe WANG, Li-na DU. Preparation, pharmacokinetic and pharmacodynamic studies of ketorolac tromethamine oral mucosal microneedles[J]. Acta Pharmaceutica Sinica, 2026 , 61 (9) : 3466 -3474 . DOI: 10.16438/j.0513-4870.2026-0030
Year 2026 volume 61 Issue 9
104
46
Cite this Article
BibTeX
Article Info
doi: 10.16438/j.0513-4870.2026-0030
  • Receive Date:2026-01-08
  • Online Date:2026-10-22
  • Published:2026-09-12
Article Data
Affiliations
History
  • Received:2026-01-08
  • Revised:2026-03-10
Affiliations
    1Academy of Military Medical Sciences, Academy of Military Sciences, Beijing 100850, China
    2School of Pharmacy, Henan University, Kaifeng 450001, China
References
Share
https://castjournals.cast.org.cn/joweb/yxxb/EN/10.16438/j.0513-4870.2026-0030
Share to
QR

Scan QR to access full text

Cite this article
BibTeX
Citations
表12种不同金属材料的力学参数
科
Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)
属
Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
关闭全屏
  • BibTeX
  • EndNote
  • RefWorks
  • TxT