Casanova Francisca, Pereira Carla F, Ribeiro Alessandra B, Costa Eduardo M, Freixo Ricardo, Castro Pedro M, Fernandes João C, Pintado Manuela, Ramos Óscar L
CBQF-Centro de Biotecnologia e Química Fina-Laboratório Associado, Escola Superior de Biotecnologia, Universidade Católica Portuguesa, Rua Diogo Botelho 1327, 4169-005 Porto, Portugal.
Pharmaceutics. 2023 Mar 18;15(3):981. doi: 10.3390/pharmaceutics15030981.
Poor aqueous solubility, stability and bioavailability of interesting bioactive compounds is a challenge in the development of bioactive formulations. Cellulose nanostructures are promising and sustainable carriers with unique features that may be used in enabling delivery strategies. In this work, cellulose nanocrystals (CNC) and cellulose nanofibers were investigated as carriers for the delivery of curcumin, a model liposoluble compound. Nanocellulose modification with the surfactant cetyltrimethylammonium bromide (CTAB), tannic acid and decylamine (TADA), and by TEMPO-mediated oxidation were also tested and compared. The carrier materials were characterized in terms of structural properties and surface charge, while the delivery systems were evaluated for their encapsulation and release properties. The release profile was assessed in conditions that mimic the gastric and intestinal fluids, and cytotoxicity studies were performed in intestinal cells to confirm safe application. Modification with CTAB and TADA resulted in high curcumin encapsulation efficiencies of 90 and 99%, respectively. While no curcumin was released from TADA-modified nanocellulose in simulated gastrointestinal conditions, CNC-CTAB allowed for a curcumin-sustained release of ca. 50% over 8 h. Furthermore, the CNC-CTAB delivery system showed no cytotoxic effects on Caco-2 intestinal cells up to 0.125 g/L, meaning that up to this concentration the system is safe to use. Overall, the use of the delivery systems allowed for the reduction in the cytotoxicity associated with higher curcumin concentrations, highlighting the potential of nanocellulose encapsulation systems.
具有生物活性的化合物水溶性差、稳定性低且生物利用度不佳,这是生物活性制剂开发过程中面临的一项挑战。纤维素纳米结构作为一种具有独特特性的、有前景的可持续载体,可用于实现递送策略。在本研究中,对纤维素纳米晶体(CNC)和纤维素纳米纤维作为递送姜黄素(一种典型的脂溶性化合物)的载体进行了研究。还测试并比较了用表面活性剂十六烷基三甲基溴化铵(CTAB)、单宁酸和癸胺(TADA)以及通过TEMPO介导的氧化对纳米纤维素进行的改性。对载体材料的结构特性和表面电荷进行了表征,同时对递送系统的包封和释放特性进行了评估。在模拟胃液和肠液的条件下评估释放曲线,并在肠细胞中进行细胞毒性研究以确认其安全应用。用CTAB和TADA改性分别导致姜黄素包封效率高达90%和99%。在模拟胃肠道条件下,TADA改性的纳米纤维素未释放出姜黄素,而CNC-CTAB可使姜黄素在8小时内持续释放约50%。此外,CNC-CTAB递送系统在浓度高达0.125 g/L时对Caco-2肠细胞未显示出细胞毒性作用,这意味着在该浓度以下该系统使用安全。总体而言,使用这些递送系统可降低与较高姜黄素浓度相关的细胞毒性,突出了纳米纤维素包封系统的潜力。