Medium-chain fatty acid nanoliposomes for easy energy supply

Developing a nanoliposome delivery system for an easy energy supply of medium-chain fatty acids (MCFAs) to improve oral doses and bioavailability.

Bangham's method and high-pressure microfluidization were used to prepare MCFA liposomes. The easy energy-supply property of MCFA nanoliposomes was estimated by the anti-fatigue experiments of mice including a weight-loaded swimming test and its corresponding parameters (serum urea nitrogen, blood lactic acid, and hepatic glycogen). For comparison, nanoliposomes without MCFAs and MCFAs not entrapped in nanoliposomes were used throughout.

Compared with crude MCFA liposomes according to Bangham's method, the MCFA nanoliposomes made by high-pressure microfluidization exhibited great advantages in their characteristics, with a small average diameter (76.2 ± 34.7 nm), narrow size distribution (polydispersity index 0.207), high ζ-potential (-50.51 mV), great entrapment efficiency (70.5%) and drug loading (9.4%), and good stability. The high-dose group and the MCFA group (680 mg/kg) showed a longer weight-loaded swimming time (104 ± 29 min, P = 0.087, and 108 ± 11 min, P = 0.047, respectively) and significantly higher hepatic glycogen (16.40 ± 1.45 mg/g, P < 0.001 and 17.27 ± 2.13 mg/g, P < 0.001, respectively) than the control group (59 ± 11 min and 8.79 ± 2.76 mg/g, respectively). Moreover, serum urea nitrogen (891.5 ± 113.4 mg/L, P = 0.024, and 876.6 ± 70.8 mg/L, P = 0.015, respectively) and blood lactic acid (6.05 ± 1.40 mmol/L, P = 0.001, and 5.95 ± 1.27 mmol/L, P < 0.001, respectively) in the high-dose group and the group with an equivalent MCFA dose were significantly lower than those in the control group (1153.6 ± 102.5 mg/L and 12.53 ± 1.86 mmol/L, respectively).

Similar to MCFAs, MCFA nanoliposomes prepared by high-pressure microfluidization showed a strong easy energy-supply property, which suggested that MCFA nanoliposomes could be a potential drug candidate for an easy energy supply.