Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS (Deemed to be University), Mumbai, India.
Expert Opin Drug Deliv. 2023 Jun;20(6):773-783. doi: 10.1080/17425247.2023.2206645. Epub 2023 Apr 24.
Tranexamic acid is used for the treatment of hyperpigmentation, and the topical route is the most favorable route for its administration. Tranexamic acid lowers plasmin and tyrosinase, which reduces melanin and skin hyperpigmentation. Low penetration through the outer layer of skin and low availability at target melanocyte cells limit tranexamic acid topical administration. Different novel delivery systems like liposomes, microneedles, topical beads, and microparticles can help in overcoming these limitations.
The mechanism of action of tranexamic acid and novel delivery systems for its topical delivery have been discussed. Further, patents related to the topical delivery of tranexamic acid and clinical trials undertaken to analyze their potential have been discussed.
Targeting tranexamic acid in the epidermal layer makes more amount of drug available for action on melanocytes, the target site for tranexamic acid. Novel drug delivery formulations like liposomes, solid lipid nanoparticles, nano-lipidic carriers, and topical beads have the potential of achieving epidermal targeting. Epidermal targeting of tranexamic acid can help in the superior delivery of the drug, making its topical treatment more efficient.
氨甲环酸用于治疗色素沉着，局部给药是其最有利的途径。氨甲环酸可降低纤溶酶和酪氨酸酶的活性，从而减少黑色素和皮肤色素沉着。氨甲环酸在外层皮肤的穿透性低，在目标黑素细胞中的可用性低，限制了其局部给药。不同的新型给药系统，如脂质体、微针、局部珠粒和微粒，可以帮助克服这些限制。
讨论了氨甲环酸的作用机制和其局部递药的新型给药系统。此外，还讨论了与氨甲环酸局部递药相关的专利和为分析其潜力而进行的临床试验。
将氨甲环酸靶向表皮层可使更多的药物可用于作用于黑素细胞，即氨甲环酸的靶位。脂质体、固体脂质纳米粒、纳米脂质载体和局部珠粒等新型药物递送制剂具有实现表皮靶向的潜力。氨甲环酸的表皮靶向有助于更有效地递药，使局部治疗更有效。
