Development and characterization of phytosterol nanoemulsions and self-microemulsifying drug delivery systems

Abstract

The aim of this study is to develop a self microemulsion drug delivery system for phytosterols to improve the solubility and bioavailability. The results showed that the formulation of phytosterol self-microemulsion is: lemon essential oil in oil phase, polyoxyethylene hydrogenated castor oil 40 and Tween 60 in emulsifier, polyethylene glycol 400 in co-emulsifier, Km = 7:3, Kp = 3:1, Ke = 50%. The drug loading of phytosterol self-microemulsion prepared by this method was 87.22 mg/g, encapsulation efficiency was 89.65%, particle size was 48.85nm, potential was -12.863mV. In vitro release experiment showed that the release of phytosterols in microemulsion was more than 90%, and the release curve was in accordance with the first-order kinetics equation. The pharmacokinetic analysis of PSSM synthesized by this method shows that PSSM can increase the bioavailability of PS more than three times, so it is necessary to do more in-depth research on the self-microemulsion delivery system of phytosterols.

Effects of food formulation on bioavailability of phytosterols: phytosterol structures, delivery carriers, and food matrices

“…14 Yuan et al (2019) reported that β-sitosterols in the microemulsion (emulsifier: polyoxyethylene hydrocastor oil 40 : tween 60 = 7 : 3, m/m, co-emulsifier : polyethylene glycol 400, emulsifier : co-emulsifier = 3 : 1, m/m, 33% lemon essential oil) increased the bioavailability more than 3 times that of commercial crystallized powder of β-sitosterols. 45 In another study, these researchers also reported that a β-sitosterol self-microemulsion has higher hypolipidemic efficiency than a sitosterol ester with linoleic acids, β-sitosterol healthy tablets and β-sitosterol powder, dissolved in tea seed oil. 46…”

Novel encapsulation approaches for phytosterols and their importance in food products: A review

“…Furthermore, an optimization of drug dosage can be conducted for other animals as well. Chuanxun et al (2019) prepared self-microemulsions for phytosterols using the lemon essential oil as oil phase, polyoxyethylene hydrogenated castor oil 40, and Tween 60 as emulsifiers, and polyethylene glycol 400 as co-emulsifier. Encapsulation efficiency of 89.65% was achieved and the drug loading of phytosterol self-microemulsion was 87.22 mg/g.…”

Innovative Delivery Systems Loaded with Plant Bioactive Ingredients: Formulation Approaches and Applications

“…Their incorporation into nanoemulsions can help overcome this issue. Chuanxun et al [ 360 ] proved the reduction of oxidation degradation of phytosterols caused during storage by using nanoemulsions while Acevedo-Estupiñan et al [ 361 ] prepared phosphatidylcholine and lysophosphatidylcholine nanoemulsions incorporating phytosterols and achieved the increase of their chemical stability as well as their water solubility. Borba et al [ 362 ] prepared β-carotene nanoemulsions by high-pressure homogenization, with an average size of 300 nm [ 362 ].…”