Oral Ionic Liquid for Transdermal Delivery and Obesity Treatment

ACS Biomater Sci Eng. 2023 Jun 12;9(6):3356-3367. doi: 10.1021/acsbiomaterials.3c00118. Epub 2023 Apr 28.

Abstract

Obesity is currently a prerequisite for more than 70% of adults, including chronic obesity and long-term obesity. With the increase of diabetes patients in the world, it is urgent to develop effective oral drugs to replace insulin. However, the gastrointestinal tract is a main obstacle to oral drug preparations. Here, a highly effective oral drug was developed, mainly formulated as an ionic liquid (IL) prepared by l-(-)-carnitine and geranic acid. Density functional theory (DFT) calculations showed that l-(-)-carnitine and geranic acid can exist stably through hydrogen bonding. IL can significantly enhance the transdermal transport of drugs. In vitro study of intestinal permeability showed that particles formed by IL can prevent the absorption of intestinal fat. Compared with the control group, oral administration of IL (10 mL kg-1) significantly reduced blood glucose, white adipose tissue in the liver and epididymis, and the expression of SREBP-1c and ACC in IL. Therefore, these results and high-throughput sequencing analysis showed that IL can effectively reduce the intestinal absorption of adipose tissue to reduce blood glucose. IL has good biocompatibility and stability. Therefore, IL has a certain application value in the field of oral drug-delivery carriers, which provides an effective means for the treatment of diabetes and is a potential tool to solve the epidemic of obesity.

Keywords: geranic acid; ionic liquid; l-(−)-carnitine; obesity; transdermal delivery.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Cutaneous
  • Blood Glucose
  • Drug Carriers
  • Humans
  • Ionic Liquids*
  • Male
  • Obesity / drug therapy

Substances

  • decaprenoic acid
  • Ionic Liquids
  • Blood Glucose
  • Drug Carriers