Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, India.
Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, India.
Int J Pharm. 2024 Nov 15;665:124671. doi: 10.1016/j.ijpharm.2024.124671. Epub 2024 Sep 7.
The study aimed to improve the transdermal permeation of IBU utilizing menthosomes as a vesicular carrier. IBU-loaded menthosomes were formulated by thin film hydration & optimized using 2 factorial designs (Design Expert® version 13 software). In vitro & ex vivo skin permeation analysis of IBU-encapsulated menthosomes was studied across the rat skin sample. In vivo pharmacodynamic activity was studied in an arthritis rat model. The optimized IBU-loaded menthosomes exhibited an optimum vesicle size of 214.2 ± 2.96 nm, Zeta potential of -21.1 ± 2.72 mV, (PDI) Polydispersity Index of 0.267 ± 0.018 with Entrapment efficiency (EE%) of 78.7 ± 2.73 %. The in vitro & ex vivo skin penetration study displayed enhanced release of drug of 77.02 ± 1.0 % and 40.91 ± 0.81 % respectively, compared to conventional liposomes. In vivo pharmacodynamic study on carrageenan-induced paw edema in Wistar albino rats demonstrated superior anti-inflammatory activity of the optimized IBU-encapsulated menthosomes (**p < 0.01) and effective inhibition of paw edema (34.04 ± 0.155 %). The formalin test indicated a significant analgesic effect of optimized formulation during the chronic phase of analgesia (*p < 0.05) compared to the control group. Thus, the developed and optimized drug-loaded menthosomes could serve as a suitable vesicular delivery carrier in enhancing the transdermal delivery of other NSAID drugs.
本研究旨在利用薄荷醇脂质体作为囊泡载体来提高布洛芬的经皮渗透。通过薄膜水化法制备载有 IBU 的薄荷醇脂质体，并使用 2 因素设计（Design Expert® version 13 软件）进行优化。研究了载有 IBU 的薄荷醇脂质体在大鼠皮肤样本中的体外和体外皮肤渗透分析。在关节炎大鼠模型中研究了体内药效学活性。优化的载有 IBU 的薄荷醇脂质体表现出最佳的囊泡大小为 214.2±2.96nm，Zeta 电位为-21.1±2.72mV，（PDI）多分散指数为 0.267±0.018，包封效率（EE%）为 78.7±2.73%。体外和体外皮肤渗透研究显示，与普通脂质体相比，药物释放增加了 77.02±1.0%和 40.91±0.81%。在角叉菜胶诱导的 Wistar 白化大鼠爪肿胀的体内药效学研究中，优化的载有 IBU 的薄荷醇脂质体表现出优越的抗炎活性（**p<0.01）和有效抑制爪肿胀（34.04±0.155%）。福马林试验表明，与对照组相比，优化配方在镇痛的慢性期具有显著的镇痛作用（*p<0.05）。因此，开发和优化的载药薄荷醇脂质体可以作为一种合适的囊泡给药载体，用于增强其他 NSAID 药物的经皮递送。
