2. Academic Validation
  3. Chylomicron-mimicking supramolecular nano emulsion for oral luteolin delivery against hyperuricemia

Chylomicron-mimicking supramolecular nano emulsion for oral luteolin delivery against hyperuricemia

  • Pharm Dev Technol. 2025 Nov;30(10):1543-1556. doi: 10.1080/10837450.2025.2591746.
Miao Wang 1 2,  Linlin Zhao 3 4,  Yujiao Liu 3 4,  Deyong Tian 3 4,  Aijiao Jiang 3 4,  Qianqi Cai 3 4,  Yucheng Xiang 3 4,  Lie Zhang 5 6,  Yan Chen 2,  Jing Ye 3 4,  Aikebaier Reheman 1,  Quan Zhang 3 4 5 7 8
Affiliations

Affiliations

  • 1 Fujian Key Laboratory of Toxicant and Drug Toxicology, Medical College, Ningde Normal University, Ningde, China.
  • 2 Fujian Province University Engineering Research Center of Mindong She Nationality Medicine, Medical College, Ningde Normal University, Ningde, China.
  • 3 Key Laboratory of Structure-Specific Small Molecule Drugs at Chengdu Medical College of Sichuan Province, School of Pharmacy, Chengdu Medical College, Chengdu, China.
  • 4 Institute of Materia Medica, Chengdu Medical College, Chengdu, China.
  • 5 Department of Neurosurgery, The First Affiliated Hospital of Chengdu Medical College, Chengdu, China.
  • 6 School of Clinical Medicine, Chengdu Medical College, Chengdu, China.
  • 7 Aging Mechanisms and Interventions Key Laboratory of Sichuan Province, School of Basic Medical Sciences, Chengdu Medical College, Chengdu, China.
  • 8 R&D Department, Chengdu Nature's Grace Biological Technology Co., Ltd, Chengdu, China.
PMID: 41255224 DOI: 10.1080/10837450.2025.2591746
Abstract

Hyperuricemia, a prevalent metabolic disorder, severely impacts life quality. Luteolin (LUT), a natural flavonoid compound, demonstrates potential anti-hyperuricemic effects along with a high safety profile. However, its clinical application is greatly limited by poor oral bioavailability, mainly due to low permeability and inadequate gastrointestinal stability. To address this, we developed a chylomicron-mimicking supramolecular nanoemulsion (LUT-CMSN) composed of soybean oil and a supramolecular aggregate formed between LUT and Kolliphor® HS 15 (HS 15). LUT-CMSN exhibited a near-spherical morphology with an average particle size of approximately 14.2 nm. With CMSN encapsulation, LUT exhibited notably improved permeability and stability in the gastrointestinal tract. After oral administration, LUT-CMSN could be absorbed by lymphatic transport into blood circulation, consequently achieving 4.63-fold higher Cmax and 2.59-fold greater AUC(0-t) compared with free LUT. Additionally, LUT-CMSN showed markedly enhanced distribution in the liver and kidney relative to free LUT. In the acute and chronic hyperuricemia animal model, LUT-CMSN effectively reduced serum uric acid levels through inhibition of Xanthine Oxidase (XOD) activity and observably alleviated the renal injury induced by hyperuricemia. Taken together, LUT-CMSN represents a promising oral delivery platform for enhancing the bioavailability of LUT and a potential therapeutic strategy for the treatment of hyperuricemia.

Keywords

Supramolecular nanoemulsion; chylomicron; hyperuricemia; luteolin; lymphatic transport; oral bioavailability.

Figures
Products