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Successful preparation of a biopolymeric nanocarrier enables controlled release of antinociceptive monoterpene for local pain management after transdermal barrier permeation
Journal of Applied Polymer Science ( IF 3 ) Pub Date : 2024-04-12 , DOI: 10.1002/app.55568
Tatianny de Araujo Andrade 1, 2 , Jemmyson Romário de Jesus 2 , Marcos Vinícius de Sousa Pereira 2 , Paulo de Tarso Garcia 1 , Maria Alice Pimentel Falcão 3 , Cristiani Isabel Banderó Walker 3 , Luiza Abrahão Frank 4 , Mairim Russo Serafini 3
Affiliation  

Developing effective and targeted drug delivery systems is crucial in searching for improved pain management strategies. Here, it is shown the preparation of a nanocarrier using chitosan hydrogel, and polymeric nanocapsules loaded with linalool for enhancing transdermal permeation and targeted delivery of this antinociceptive monoterpene for the pain treatment. Extensive characterization was conducted to evaluate the properties of the nanocarrier, and several in vitro studies were performed to investigate the release kinetics of linalool from the nanocarrier and its permeation through the layers of the skin. As results, the prepared polymeric nanocarrier exhibited an average size of 160 ± 9 nm, with a polydispersion index of 0.12 ± 0.01. The kinetic study revealed that the nanocarrier effectively controlled and prolonged the release of linalool, following a pseudo‐second order model (R2 = 0.98). To evaluate the permeation of the nanocarrier through the transdermal barrier, swine ear skin was employed. The nanocarrier efficiently penetrated the transdermal barrier and successfully delivered linalool to the skin layers. Additionally, an in vivo toxicity study indicated no toxicity for the nanocarrier at the tested concentrations (<0.950 μg mL−1). The release kinetics showed a controlled and sustained release of the linalool, suggesting its potential for prolonged therapeutic effects.

中文翻译:

成功制备生物聚合物纳米载体,能够控制释放抗伤害单萜,用于透皮屏障渗透后的局部疼痛管理

开发有效且有针对性的药物输送系统对于寻求改进的疼痛管理策略至关重要。在这里,展示了使用壳聚糖水凝胶和负载芳樟醇的聚合物纳米胶囊制备纳米载体,以增强经皮渗透和靶向递送这种用于疼痛治疗的镇痛单萜。为了评估纳米载体的特性,进行了广泛的表征,并进行了几项体外研究来研究芳樟醇从纳米载体中的释放动力学及其通过皮肤层的渗透。结果,制备的聚合物纳米载体的平均尺寸为160±9nm,多分散指数为0.12±0.01。动力学研究表明,纳米载体遵循伪二级模型,有效控制和延长了芳樟醇的释放(2= 0.98)。为了评估纳米载体通过透皮屏障的渗透性,使用了猪耳皮肤。纳米载体有效地穿透透皮屏障,并成功地将芳樟醇递送至皮肤层。此外,体内毒性研究表明纳米载体在测试浓度(<0.950 μg mL−1)。释放动力学显示芳樟醇的受控和持续释放,表明其具有延长治疗效果的潜力。
更新日期:2024-04-12
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