School of Chemistry Chemical Engineering and Biotechnology, Nanyang Technological University, Singapore 637459, Singapore.
School of Chemical and Biomolecular Engineering, Seoul University of Science and Technology, Seoul 01811, Korea.
Int J Mol Sci. 2022 Oct 3;23(19):11731. doi: 10.3390/ijms231911731.
An amorphous curcumin (CUR) and bovine serum albumin (BSA) nanoparticle complex (nanoplex) was previously developed as a promising anticancer nanotherapy. The CUR-BSA nanoplex had been characterized in its aqueous suspension form. The present work developed a dry-powder form of the CUR-BSA nanoplex by lyophilization using sucrose as a cryoprotectant. The cryoprotective activity of sucrose was examined at sucrose mass fractions of 33.33, 50.00, and 66.66% by evaluating the lyophilized nanoplex's (1) aqueous reconstitution and (2) CUR dissolution and kinetic solubility. The physicochemical stabilizing effects of sucrose upon the nanoplex's 30-day exposures to 40 °C and 75% relative humidity were examined from (i) aqueous reconstitution, (ii) CUR dissolution, (iii) CUR and BSA payloads, (iv) amorphous form stability, and (v) BSA's structural integrity. The good cryoprotective activity of sucrose was evidenced by the preserved BSA's integrity and good aqueous reconstitution, resulting in a fast CUR dissolution rate and a high kinetic solubility (≈5-9× thermodynamic solubility), similar to the nanoplex suspension. While the aqueous reconstitution, CUR dissolution, and amorphous form were minimally affected by the elevated heat and humidity exposures, the treated nanoplex exhibited a lower BSA payload (≈7-26% loss) and increased protein aggregation postexposure. The adverse effects on the BSA payload and aggregation were minimized at higher sucrose mass fractions.
先前已开发出一种无定形姜黄素（CUR）和牛血清白蛋白（BSA）纳米颗粒复合物（纳米复合物）作为有前途的抗癌纳米疗法。已经对其水悬浮液形式的 CUR-BSA 纳米复合物进行了表征。本工作通过使用蔗糖作为冷冻保护剂的冻干法开发了 CUR-BSA 纳米复合物的干粉形式。通过评估冻干纳米复合物的（1）水重构和（2）CUR 溶解和动力学溶解度，检查了蔗糖质量分数为 33.33、50.00 和 66.66%的蔗糖的冷冻保护活性。通过（i）水重构，（ii）CUR 溶解，（iii）CUR 和 BSA 载药量，（iv）无定形形式稳定性和（v）BSA 的结构完整性，检查了蔗糖对纳米复合物在 40°C 和 75%相对湿度下暴露 30 天的物理化学稳定作用。蔗糖的良好冷冻保护活性表现为 BSA 完整性的良好保持和良好的水重构，从而导致 CUR 快速溶解率和高动力学溶解度（≈5-9×热力学溶解度），类似于纳米复合物悬浮液。虽然水重构、CUR 溶解和无定形形式受高温和高湿度暴露的影响最小，但处理后的纳米复合物表现出较低的 BSA 载药量（≈7-26%的损失）和暴露后蛋白质聚集增加。在较高的蔗糖质量分数下，BSA 载药量和聚集的不利影响最小化。
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