Preparation of β-CD-LA aggregate and its application as drug carriers

ABSTRACT

Linoleic acid (LA) and β-CD-NH₂ molecule are covalently conjugated to form a β-CD-LA molecule. The β-CD-LA molecule can self-assemble into spherical micelles with an average particle size of about 50.75±13.58 nm, which is beneficial for blood circulation.  The micelles has a high drug loading rate (84.78%±6.78), and in vitro release experiments show that the Dox release from the β-CD-LA-Dox nanomedicine has the characteristics of pH-responsive and slow-release.  Cell experiments show that the cytotoxicity of β-CD-LA micelles is relatively low, and β-CD-LA-Dox nanomedicine can enter the cytoplasm well and eventually enter the nucleus, which induce cancer cells apoptosis.  In vivo experiments show that β-CD-LA-Dox nanomedicine had a good inhibitory effect on tumor growth without affecting the body weight of mice, and tumor tissue sections proved that β-CD-LA-Dox nanomedicine could induce effectively cancer cell apoptosis which resulted in tumor tissue necrosis, and it showed has a good therapeutic effect on the tumor. 

KEYWORDS:

• Nanomedicine
• drug carrier
• linoleic acid
• cyclodextrin
• tumour
• cancer cell

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This study was financially supported by NSFC [Grant No. 21201020], the Shandong Provincial Independent Innovation and Achievements Transformation Foundation [Grant No. 2014CGZH1316], Projects of Shandong Province Higher Educational Science and Technology Program [Grant Nos. J15LC01 and J16LC19], Key Research and Development Plan of Yantai [Grant Nos. 2016ZH078 and 2018XSCC050], and the foundation of Key Laboratory of Colloid and Interface Chemistry (Shandong University), Ministry of Education, China [Grant No. 201703].