三氯醋酸载纳米脂质载体（NLCs）的研制及其在口腔给药中的应用。

Development of Triamcinolone Acetonide-Loaded Nanostructured Lipid Carriers (NLCs) for Buccal Drug Delivery Using the Box-Behnken Design.

机构信息

Division of Pharmaceutical Sciences, Faculty of Pharmacy, Thammasat University, Pathumthani 12120, Thailand.

出版信息

Molecules. 2018 Apr 23;23(4):982. doi: 10.3390/molecules23040982.

DOI:10.3390/molecules23040982

PMID:29690622

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6017338/

Abstract

The aim of this present work was to prepare triamcinolone acetonide (TA)-loaded nanostructured lipid carriers (TA-loaded NLCs) for buccal drug delivery systems using the Box-Behnken design. A hot homogenization method was used to prepare the TA-loaded NLCs. Spermaceti (X₁), soybean oil (X₂), and Tween 80 (X₃) were used as solid lipid, liquid lipid, and stabilizer, respectively. The particle size of TA-loaded NLCs was lower than 200 nm and the zeta potential displayed the negative charge in all formulations. The percentage encapsulation efficiency (%EE) of the TA-loaded NLCs showed that it was higher than 80% for all formulations. Field emission scanning electron microscope (FESEM) confirmed that the size of TA-loaded NLCs was approximately 100 nm and energy-dispersive X-ray spectroscopy (EDS) confirmed that the TA could be incorporated in the NLC system. The Higuchi model gave the highest value of the R², indicating that this model was a fit for the TA release profiles of TA-loaded NLCs. Confocal laser scanning microscopy (CLSM) was used to observe the drug penetration within the porcine buccal mucosa and Nile red-loaded NLCs showed significantly higher penetration depth at 8 h than at 2 h. Therefore, TA-loaded NLCs could be an efficient carrier for drug delivery through the buccal mucosa.

摘要

本研究旨在采用 Box-Behnken 设计制备曲安奈德（TA）负载的纳米结构脂质载体（TA-loaded NLCs）用于口腔给药系统。采用热熔匀化法制备 TA-loaded NLCs。鲸蜡（X₁）、大豆油（X₂）和吐温 80（X₃）分别用作固体脂质、液体脂质和稳定剂。TA-loaded NLCs 的粒径均小于 200nm，所有配方的 Zeta 电位均呈负电荷。TA-loaded NLCs 的包封率（%EE）均高于 80%。场发射扫描电子显微镜（FESEM）证实 TA-loaded NLCs 的粒径约为 100nm，能量色散 X 射线能谱（EDS）证实 TA 可被包裹于 NLC 系统中。Higuchi 模型给出了最高的 R²值，表明该模型适合 TA-loaded NLCs 的 TA 释放曲线。共聚焦激光扫描显微镜（CLSM）用于观察药物在猪口腔黏膜内的渗透情况，尼罗红负载的 NLCs 在 8h 时的渗透深度明显高于 2h。因此，TA-loaded NLCs 可作为口腔黏膜给药的有效载体。