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.
| 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 |