Postgraduate Program in Pharmaceutical Sciences, Federal University of Pampa, Campus Uruguaiana, BR 472, Km 7, Uruguaiana, RS, 97500-970, Brazil.
Postgraduate Program in Pharmaceutical Sciences, Federal University of Santa Maria, Av. Roraima no. 1000, Santa Maria, RS, 97105-900, Brazil.
Pharmacol Rep. 2022 Feb;74(1):135-147. doi: 10.1007/s43440-021-00331-2. Epub 2021 Nov 5.
Surface functionalization enhances the properties and characteristics of polymeric nanocapsules (NCs) mainly due to the surface charge, surfactants, and polymer coating type. Curcumin (CUR) is a bioactive compound with several proven pharmacological properties and low bioavailability. This study aimed to develop anionic (poly-ɛ-caprolactone; PCL) and cationic (Eudragit RS100 (EUD)) NCs prepared with sorbitan monostearate (Span 60) or sorbitan monooleate (Span 80), coated with d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) and optimized using 2 factorial analysis. Subsequently, the biological activity was evaluated.
A two-level, three-factor design (polymer, Span type, and TPGS concentration) was used. The biological effects of CUR-loaded TPGS-coated cationic and anionic NCs were assessed in apomorphine-induced stereotyped behavior in rats.
The type of polymer (anionic or cationic) and Span had a factorial influence on the physical and chemical characteristics of NCs according to the changes in TPGS concentrations. Both cationic and anionic CUR-NCs could block apomorphine-induced behavioral changes.
The CUR-loaded TPGS-coated NCs proved to be a promising brain delivery system.
表面功能化主要由于表面电荷、表面活性剂和聚合物涂层类型增强了聚合物纳米胶囊（NCs）的性质和特性。姜黄素（CUR）是一种具有多种已证实的药理学性质和低生物利用度的生物活性化合物。本研究旨在开发带负电荷的（聚己内酯；PCL）和带正电荷的（Eudragit RS100（EUD））NCs，它们由山梨醇单硬脂酸酯（Span 60）或山梨醇油酸酯（Span 80）制备，用 d-α-生育酚聚乙二醇 1000 琥珀酸酯（TPGS）包被，并使用 2 因子分析进行优化。随后，评估了生物活性。
使用两水平、三因素设计（聚合物、Span 类型和 TPGS 浓度）。在阿扑吗啡诱导的大鼠刻板行为中评估载 CUR 的 TPGS 包被的阳离子和阴离子 NCs 的生物学效应。
根据 TPGS 浓度的变化，聚合物（阳离子或阴离子）和 Span 的类型对 NCs 的物理化学特性具有因子影响。阳离子和阴离子 CUR-NCs 均可阻断阿扑吗啡诱导的行为变化。
载 CUR 的 TPGS 包被的 NCs 被证明是一种有前途的脑递药系统。
