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首页> 外文会议>Annual meeting exposition of the Controlled Release Society >Tacrolimus Entrapped Lipid Nanoparticles for Improved Safety and Enhanced Targeting to Deeper Skin Layers for Treatment of Atopic Dermatitis
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Tacrolimus Entrapped Lipid Nanoparticles for Improved Safety and Enhanced Targeting to Deeper Skin Layers for Treatment of Atopic Dermatitis

机译：他克莫司截留的脂质纳米颗粒可改善安全性并增强靶向深层皮肤层的治疗特应性皮炎的能力

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Atopic dermatitis (AD) is a chronically relapsing eczematous disorder of the skin which has a significant impact on both the pediatric and adult population worldwide. Tacrolimus have been the drug of choice for treatment of AD which inhibits early T-cell activation in gene transcription such as interleukins resulting in suppression of inflammation. However, despite being quite effective, the most common adverse events associated with tacrolimus use are low and variable bioavailability, burning sensation and pruritus at the site of application. These findings prompt for development of novel carrier which could effectively target the tacrolimus molecule to the site of action without producing undesirable side effects.Tacrolimus loaded lipid nanoparticles (T-LN) have been prepared by high pressure homogenization technique, optimized and characterized for particle size and its distribution, entrapment efficiency, DSC and rheology. FT-IR revealed no incompatibility and drug remained encapsulated in lipid phase. T-LN enriched gels revealed much higher in vitro drug release, skin penetration and enhanced skin accumulation compared to reference ointment, Protopic. T-LN also displayed significantly higher drug levels penetrating into deeper skin layers which are the target sites for tacrolimus action. In vivo skin retention and visualization of cutaneous uptake using confocal laser scanning microscopy confirmed targeting potential and showed no irritation to rabbit skin with PII 0.00. T-LN was more effective with significant skin targeting potential and enhanced safety, supporting superior performance with better patient compliance.
机译：特应性皮炎（AD）是一种慢性复发性湿疹性皮肤疾病，对全世界的儿科和成人人群都有重大影响。他克莫司一直是治疗AD的首选药物，该药物可抑制基因转录（例如白介素）中早期的T细胞活化，从而抑制炎症。然而，尽管非常有效，但与他克莫司使用相关的最常见的不良事件是生物利用度低且变化，施用部位的灼热感和瘙痒。这些发现促进了新型载体的开发，该载体可以有效地将他克莫司分子靶向作用部位而不产生不良副作用。 通过高压均质技术制备了载有他克莫司的脂质纳米颗粒（T-LN），并对其粒径，分布，包封效率，DSC和流变性进行了优化和表征。 FT-IR显示没有不相容性，药物仍被包裹在脂质相中。与参考软膏Protopic相比，富含T-LN的凝胶显示出更高的体外药物释放，皮肤渗透和增强的皮肤积聚。 T-LN还显示出明显更高的药物水平，可渗透至更深的皮肤层，而这些皮肤层是他克莫司作用的目标部位。使用共聚焦激光扫描显微镜进行的体内皮肤保留和皮肤摄取的可视化证实了靶向潜力，并且显示PII 0.00对兔皮肤没有刺激性。 T-LN具有更强的皮肤靶向潜力和更高的安全性，因此更有效，可提供更好的性能和更好的患者依从性。

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