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全反式视黄酸载脂纳米粒作为一种经皮给药载体。

All-trans retinoic acid-loaded lipid nanoparticles as a transdermal drug delivery carrier.

机构信息

Pharmaceutical Development of Green Innovations Group, Faculty of Pharmacy, Silpakorn University , Nakhon Pathom , Thailand.

出版信息

Pharm Dev Technol. 2014 Mar;19(2):164-72. doi: 10.3109/10837450.2013.763261. Epub 2013 Jan 28.

Abstract

The objective of this study was to investigate the effects of drug amounts (0.1%, 0.2% and 0.3% w/w), amounts of the oil (10%, 15% and 20% w/w of lipid matrix) and types of the oil (soybean oil (S), medium chain triglycerides (M), oleic acids (O) and linoleic acids (L)) in lipid matrix of all-trans retinoic acid (ATRA)-loaded nanostructured lipid carriers (NLCs) for transdermal drug delivery. The ATRA-loaded solid lipid nanoparticles (SLNs) were formulated with 30% w/w cetyl palmitate. All lipid nanoparticles had average sizes between 130 and 241 nm and had negative zeta potentials. The drug loading of all formulations was higher than 95%. The release of drug from all lipid nanoparticles followed zero-order kinetics. The amount of drug released from all the NLCs and SLNs was significantly greater than the drug released from the ATRA suspension. The ATRA flux of the SLNs was higher than the NLCs. The flux of the NLCs containing oleic acid was significantly higher than the other types of oils. The chemical stability at 4 °C, the percentage of ATRA remaining in all the lipid nanoparticles tested was higher than 80%. It can be concluded that both the SLNs and NLCs are promising dermal drug delivery systems for ATRA.

摘要

本研究旨在考察药物剂量(0.1%、0.2%和 0.3%w/w)、油剂量(脂质基质的 10%、15%和 20%w/w)和油类型(大豆油(S)、中链甘油三酯(M)、油酸(O)和亚油酸(L))对全反式维甲酸(ATRA)负载的纳米结构脂质载体(NLC)经皮给药的影响。载有 ATRA 的固体脂质纳米粒(SLN)由 30%w/w 十六烷醇棕榈酸酯制成。所有脂质纳米粒的平均粒径在 130 至 241nm 之间,且具有负的 Zeta 电位。所有制剂的药物载药量均高于 95%。所有脂质纳米粒的药物释放均遵循零级动力学。所有 NLC 和 SLN 释放的药物均明显多于 ATRA 混悬剂释放的药物。SLN 的 ATRA 通量高于 NLC。含油酸的 NLC 的通量明显高于其他类型的油。在 4°C 下的化学稳定性测试中,所有脂质纳米粒中 ATRA 的剩余百分比均高于 80%。可以得出结论,SLN 和 NLC 均是 ATRA 有前途的经皮给药系统。

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