Enhancing solubility and bioavailability of octacosanol: Development of a green O/W nanoemulsion synthesis process

Mingxi Jia; Weidong Bai; Jing Deng; Wen Li; Qinlu Lin; Feifei Zhong; Feijun Luo

doi:10.1016/j.ijpharm.2023.123726

Enhancing solubility and bioavailability of octacosanol: Development of a green O/W nanoemulsion synthesis process

Int J Pharm. 2024 Feb 15:651:123726. doi: 10.1016/j.ijpharm.2023.123726. Epub 2023 Dec 21.

Authors

Mingxi Jia¹, Weidong Bai², Jing Deng³, Wen Li⁴, Qinlu Lin⁵, Feifei Zhong⁶, Feijun Luo³

Affiliations

¹ National Engineering Research Center of Rice and Byproduct Deep Processing, Hunan Province Key Laboratory of Edible forestry Resources Safety and Processing Utilization, College of Food Science and Engineering, Central South University of Forestry and Technology, Changsha 410004, Hunan, China; College of Light Industry and Food Sciences, Zhongkai University of Agriculture and Engineering, Guangzhou 510225, Guangdong, China; College of Food Science and Engineering, Nanjing University of Finance and Economics/Collaborative Innovation Center for Modern Grain Circulation and Safety, Nanjing 210023, JiangSu, China.
² College of Light Industry and Food Sciences, Zhongkai University of Agriculture and Engineering, Guangzhou 510225, Guangdong, China.
³ National Engineering Research Center of Rice and Byproduct Deep Processing, Hunan Province Key Laboratory of Edible forestry Resources Safety and Processing Utilization, College of Food Science and Engineering, Central South University of Forestry and Technology, Changsha 410004, Hunan, China.
⁴ National Engineering Research Center of Rice and Byproduct Deep Processing, Hunan Province Key Laboratory of Edible forestry Resources Safety and Processing Utilization, College of Food Science and Engineering, Central South University of Forestry and Technology, Changsha 410004, Hunan, China; College of Food Science and Engineering, Nanjing University of Finance and Economics/Collaborative Innovation Center for Modern Grain Circulation and Safety, Nanjing 210023, JiangSu, China; Hunan Provincial Engineering Technology Research Center of Seasonings Green Manufacturing, Changsha 410004, China. Electronic address: T20202532@csuft.edu.cn.
⁵ National Engineering Research Center of Rice and Byproduct Deep Processing, Hunan Province Key Laboratory of Edible forestry Resources Safety and Processing Utilization, College of Food Science and Engineering, Central South University of Forestry and Technology, Changsha 410004, Hunan, China; College of Food Science and Engineering, Nanjing University of Finance and Economics/Collaborative Innovation Center for Modern Grain Circulation and Safety, Nanjing 210023, JiangSu, China; Hunan Provincial Engineering Technology Research Center of Seasonings Green Manufacturing, Changsha 410004, China.
⁶ National Engineering Research Center of Rice and Byproduct Deep Processing, Hunan Province Key Laboratory of Edible forestry Resources Safety and Processing Utilization, College of Food Science and Engineering, Central South University of Forestry and Technology, Changsha 410004, Hunan, China; Changsha Institute for Food and Drug Control, Changsha 410016, Hunan, China.

PMID: 38135259
DOI: 10.1016/j.ijpharm.2023.123726

Abstract

Octacosanol, a naturally occurring higher fatty alcohol, possessed numerous biological effects. However, octacosanol limited solubility in water due to its lipophilic nature and large structure, resulting in poor absorption and low bioavailability. To overcome this challenge, we developed a simple, environmentally friendly, and energy-efficient O/W nanoemulsion synthesis process. The nanoemulsion achieved an average droplet size of approximately 30 nm, exhibited excellent dispersibility and stability at room temperature for 60 days, and showcased robust storage properties insensitive to ambient temperature, pH, NaCl, and sucrose. Remarkably, the preparation process of the nanoemulsion maintained the biological activity of octacosanol while demonstrating significantly enhancing antioxidant activity compared to octacosanol suspension. Additionally, the nanoemulsion displayed negligible cytotoxic effects on Caco-2 cells. Significantly, the octacosanol nanoemulsion exhibited a 5.4-fold enhancement in transmembrane transport efficiency when compared to the suspension in Caco-2 cell monolayers. Additionally, in an in vivo experiment, there was a notable 2.9-fold increase in rat intestinal absorption. These findings could provide valuable insights into the development of octacosanol nanoemulsion, supporting its future applications and paving the way for the design of stable nanoemulsion systems for other lipophilic and sparingly soluble substances.

Keywords: Bioavailability; Cytotoxicity; Octacosanol nanoemulsion; Solubility; Stability.

MeSH terms

Animals
Biological Availability
Caco-2 Cells
Emulsions / chemistry
Fatty Alcohols
Humans
Nanoparticles* / chemistry
Particle Size
Rats
Solubility

Substances

1-octacosanol
Emulsions
Fatty Alcohols