优化并表征载有利斯的明的纳米脂质载体透皮贴片，用于治疗痴呆。
Optimization and characterization of rivastigmine nanolipid carrier loaded transdermal patches for the treatment of dementia.
机构信息
NDDS Research Laboratory, Department of Pharmaceutics, Delhi Institute of Pharmaceutical Sciences and Research, New Delhi, 110017, India.
NDDS Research Laboratory, Department of Pharmaceutics, Delhi Institute of Pharmaceutical Sciences and Research, New Delhi, 110017, India.
出版信息
Chem Phys Lipids. 2019 Nov;224:104794. doi: 10.1016/j.chemphyslip.2019.104794. Epub 2019 Jul 27.
The present study aimed to develop nanolipid carrier (NLC) loaded transdermal system of rivastigmine for bioavailability enhancement. NLC was optimized using Box-Behnken Design (BBD). Optimized formulation comprises oil (4% w/w), tween 80 (3% w/w) and span 80 (1.8% w/w) and was characterized. It was found that the formulation exhibit 134.60 ± 15.10 nm, 0.286 ± 0.041, -11.80 ± 2.24 mV and 70.56 ± 1.20% of mean size, polydispersity index (PDI), zeta potential and entrapment efficiency, respectively. In vitro release studies showed there was more sustained release of drug from NLC loaded transdermal patches in comparison to Exelon® patch. Skin irritation studies proved the non-irritant nature of developed NLC based transdermal patch. From pharmacokinetic studies it was observed that there was increased C and AUC in plasma treated with NLC loaded transdermal patches as compared to conventional patch. These experimental results indicate that NLC based transdermal patch could be utilized as a potential carrier for enhancing bioavailability of rivastigmine for the better treatment and management of dementia.
本研究旨在开发用于提高生物利用度的利伐斯的明纳米脂质载体（NLC）经皮给药系统。采用 Box-Behnken 设计（BBD）对 NLC 进行了优化。优化的配方包含油（4%w/w）、吐温 80（3%w/w）和司盘 80（1.8%w/w），并对其进行了表征。结果发现，该配方的粒径为 134.60±15.10nm、PDI 为 0.286±0.041、zeta 电位为-11.80±2.24mV、包封率为 70.56±1.20%。体外释放研究表明，与 Exelon®贴剂相比，NLC 载药经皮贴片具有更持久的药物释放。皮肤刺激性研究证明了所开发的基于 NLC 的经皮贴片具有非刺激性。从药代动力学研究中可以观察到，与常规贴片相比，用 NLC 载药经皮贴片处理的血浆中的 C 和 AUC 增加。这些实验结果表明，基于 NLC 的经皮贴片可作为提高利伐斯的明生物利用度的潜在载体，用于痴呆症的更好治疗和管理。
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