Acta Chimica Sinica ›› 2023, Vol. 81 ›› Issue (2): 116-123.DOI: 10.6023/A22110464 Previous Articles     Next Articles



殷雪旸, 顾恺, 邵正中*()   

  1. 聚合物分子工程国家重点实验室 复旦大学高分子科学系 先进材料实验室 上海 200433
  • 投稿日期:2022-11-16 发布日期:2022-12-13
  • 通讯作者: 邵正中
  • 基金资助:

Preparation of the Protein/Polyphenylboronic Acid Nanospheres for Drug Loading and Unloading

Xueyang Yin, Kai Gu, Zhengzhong Shao()   

  1. State Key Laboratory of Molecular Engineering of Polymers, Department of Macromolecular Science, Laboratory of Advanced Materials, Fudan University, Shanghai 200433
  • Received:2022-11-16 Published:2022-12-13
  • Contact: Zhengzhong Shao
  • Supported by:
    National Natural Science Foundation of China(21935002)

Protein nanoparticles (NPs), biocompatible and biodegradable, can be easily surface modified. In particular, amphiphilic proteins act as “surfactants” that help form microparticles while undergoing molecular chain rearrangement. These NPs have been successfully used as drug delivery systems, improving bioavailability and reducing the toxic effects of drug molecules. The use of regenerated silk protein (RSF) with m-acrylamidophenylboronic acid (APBA) composites as drug carriers for loading anti-inflammatory herbal extracts was reported. Firstly, a simple and rapid method was used to prepare silk protein/polyphenylboronic acid nanospheres, in brief, RSF solution and a certain amount of initiator were added to APBA solution, and the pH was adjusted by NaOH, and the polymerization was initiated by heating at 90 ℃ under nitrogen protection with stirring at 500 r/min. After 2 h of reaction, a milky solution was obtained, which formed silk protein/benzeneboronic acid nanospheres with hydrophobic interior and hydrophilic surface. The drug-loaded silk protein/polyphenylboronic acid nanospheres with an average size of 550 to 600 nm were prepared by mixing with the drug solution after dialysis and stirring at room temperature for 12 h to load the drug by adsorption. By the same method, drug-loaded albumin/polyphenylboronic acid microspheres and collagen/polyphenylboronic acid microspheres with sizes around 260 nm and 100 nm, respectively, could be prepared. The results observed by scanning and projection electron microscopy and dynamic light scattering showed that the drug-loaded silk protein/polyphenylboronic acid nanomicrospheres displayed regular spherical shape indicating smoothness and good dispersion with no obvious aggregation. The highest drug loading rate was about 13.4%, and the encapsulation rate was over 90%. Also, such drug-loaded nanospheres could achieve controlled release for about seven days and their slow release behavior was pH-responsive, with faster drug release in buffer solution at pH=5.5 than in buffer solution at pH=7.4. In addition, the synergistic interaction of the silk protein/polyphenylboronic acid nanomicrospheres with the subject drug improved its free radical scavenging rate and scavenging efficiency, which was superior to that of the direct drug delivery group. Thus, three protein/polyphenylboronic acid nanomicrospheres with different sizes, electrical properties and drug release rates may be adaptable to a wide range of intravenous and subcutaneous or intraperitoneal drug delivery needs and have great potential for clinical applications.

Key words: proteins, phenylboronic acid, anti-inflammatory drugs, nanocarriers, controlled release