Abstract
The complex nanoliposomes encapsulating both a hydrophilic drug vitamin C (vit C) and hydrophobic drug medium-chain fatty acids (MCFAs) was prepared by combining double emulsion method with dynamic high pressure microfluidization. The complex nanoliposomes was further freeze-dried under −86 °C for 48 h with sucrose at the sucrose/lipids ratio of 2:1(w/w) in order to enhance its stability. The freeze-dried complex nanoliposomes under the suitable conditions exhibited high entrapment efficiency of MCFAs (44.26 ± 3.34)%, relatively high entrapment efficiency of vit C (62.25 ± 3.43)%, low average size diameter (110.4 ± 7.28) nm and good storage stability at 4 °C for 60 days with slight changes in mean particle diameter and drug entrapment efficiencies. The results of transmission electron microscopy of freeze-dried complex nanoliposomes also showed that the freeze-dried samples with sucrose were stable without great increase in their particle sizes and without destroying their spherical shape. The results indicated that sucrose presented well protection effects in MCFAs-vit C complex nanoliposomes, suggesting the possibility of further usage in commercial liposomes.
Highlights
Hydrophobic drug medium-chain fatty acids (MCFAs) composed of octanoic acid and decanoic acid has unique characteristics different from long-chain fatty acids [1]
The results showed that the qualities of MCFAs-vitamin C (vit C) complex nanoliposomes improved after the addition of sucrose, which made freeze-dried liposomes with relative small size increase and high drug entrapment efficiencies compared with liposomes suspension before lyophilization
The stability was assessed by comparing different changes in mean diameters and drug encapsulation efficiencies of freshly prepared and freeze-dried MCFAs-vit C complex nanoliposomes prepared by DE-Dynamic high pressure microfluidization (DHPM) at fixed time intervals (1, 4, 7, 10, 13, 16, 30, 45, 60 days) respectively
Summary
Hydrophobic drug medium-chain fatty acids (MCFAs) composed of octanoic acid and decanoic acid has unique characteristics different from long-chain fatty acids [1]. MCFAs are more rapidly hydrolyzed into triglycerides by pancreatic lipase than long chain fatty acids, and transported via portal vein to the liver where they are preferentially β-oxidized by carnitine-independent pathway [2] They can save the amount of protein [1], inhibit the formation of body fat and suppress diseases caused by pathogenic bacteria [3,4]. Preparation of complex nanoliposomes is very challenging by traditional methods, due to the difficulties in the implementation of small particle size and high entrapment efficiency. Many methods were used for preparing liposomes, most of which exhibit favorable characteristics when entrapping one hydrophobic or hydrophilic drug [17,18]. Combined methods consisting of two or more different methods are investigated for preparation of liposomes that entrap both hydrophobic and hydrophilic drugs. Traditional methods and DHPM were combined for preparing MCFAs-vit C complex nanoliposomes suspension. In order to enhance the stability of liposomes, strengthen its functional effect, the lyophilized liposomes were prepared in this study with an expectation on its application in feedstuff or as injection and aerosol after rehydration
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