Boonpetcharat Natkhanang Mookkie, Thu Kyaw May Thu, Boonkanokwong Veerakiet, Luckanagul Jittima Amie
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Phyathai Road, Bangkok 10330, Thailand.
Center of Excellence in Plant-Produced Pharmaceuticals, Chulalongkorn University, Phyathai Road, Bangkok 10330, Thailand.
Gels. 2025 Jul 29;11(8):585. doi: 10.3390/gels11080585.
Curcumin is widely recognized for its various pharmacological properties, including antioxidant, anti-inflammatory, and anti-tumor activities. Nevertheless, the development of curcumin as a therapeutic agent is impeded by its limited oral bioavailability, which stems from its chemical instability, poor aqueous solubility, and rapid degradation. This study aimed to develop granule formulations incorporating poly(N-isopropylacrylamide)-grafted hyaluronic acid or HA-g-pNIPAM to enhance dissolution and protect curcumin from degradation. Three formulations were developed: F10 (HA-g-pNIPAM physically mixed with curcumin), F10 Encap (curcumin encapsulated within HA-g-pNIPAM), and F11 (curcumin granules without HA-g-pNIPAM). The stability results showed that F10 Encap effectively maintained curcumin content throughout the study period, retaining approximately 94% of its initial concentration by day 30, compared to 70% from F11 ( < 0.05) at 30 °C and 75% relative humidity. All dried curcumin granules exhibited excellent flowability, as determined by the angle of repose measurements. All three formulations exhibited a consistent particle size distribution across replicates, with a peak in the 150-180 μm size range. The sustained release observed for F10 Encap and F10 after the initial burst suggested that the HA-g-pNIPAM provided a controlled release mechanism, ensuring continuous curcumin dissolution over 240 min in gastric and intestinal conditions. These findings suggested that HA-g-pNIPAM improved dissolution and stability of curcumin.
姜黄素因其多种药理特性而被广泛认可,包括抗氧化、抗炎和抗肿瘤活性。然而,姜黄素作为一种治疗剂的开发受到其口服生物利用度有限的阻碍,这源于其化学不稳定性、水溶性差和快速降解。本研究旨在开发包含聚(N-异丙基丙烯酰胺)接枝透明质酸或HA-g-pNIPAM的颗粒制剂,以提高姜黄素的溶解度并保护其不被降解。开发了三种制剂:F10(HA-g-pNIPAM与姜黄素物理混合)、F10 Encap(姜黄素包封在HA-g-pNIPAM内)和F11(不含HA-g-pNIPAM的姜黄素颗粒)。稳定性结果表明,在整个研究期间,F10 Encap有效地维持了姜黄素含量,在30℃和75%相对湿度下,到第30天保留了约94%的初始浓度,相比之下,F11在第30天仅保留了70%(<0.05)。通过休止角测量确定,所有干燥的姜黄素颗粒均表现出优异的流动性。所有三种制剂在重复样品中均呈现一致的粒度分布,峰值在150-180μm尺寸范围内。F10 Encap和F10在初始突释后观察到的缓释表明,HA-g-pNIPAM提供了一种控释机制,确保姜黄素在胃和肠道条件下240分钟内持续溶解。这些发现表明,HA-g-pNIPAM改善了姜黄素的溶解度和稳定性。