Development and evaluation of emulsion-liposome blends for resveratrol delivery.
Nano- and submicron-sized vesicles are beneficial for the controlled delivery of drugs. Resveratrol, the main active polyphenol in red wine, was incorporated into various combinations of emulsions and liposomes to examine its physicochemical characteristics and cardiovascular protection. The blends of emulsion-liposome were composed of coconut oil, soybean lecithin, glycerol formal, and non-ionic surfactants. Multiple systems were assessed by evaluating the droplet size, surface charge, drug encapsulation, release rate, and stability. The vesicle diameter of the systems ranged from 114 to 195 nm. The liposomal vesicles in the systems had smaller diameters (of 43 approximately 56 nm) (F6 and F7). Drug encapsulation of approximately 70% were achieved by the vesicles. The inclusion of resveratrol in these systems retarded the drug release in both the presence and absence of plasma in vitro. The emulsion-liposome blends which incorporated Brij 98 (F5) exhibited the slowest release at zero-order for resveratrol delivery. Treatment using resveratrol in the blended formulations dramatically inhibited vascular intimal thickening, which was tested in an experimental model in which endothelial injury was produced in normal rat carotid arteries. Intraperitoneal injection of the multiple systems was associated with no or negligible liver and kidney toxicity. We concluded that encapsulation by the emulsion-liposome blends is a potent way to enhance the preventative and therapeutic benefits of resveratrol.
Hung
Chi-Feng
CF
School of Medicine, Fu Jen Catholic University, Taipei, Taiwan.
Chen
Jan-Kan
JK
Liao
Mei-Hui
MH
Lo
Huey-Ming
HM
Fang
Jia-You
JY
D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003327:Coronary Disease / Q000188:drug therapy* / Q000473:pathology; D004058:Diffusion; D004337:Drug Carriers / Q000737:chemistry*; D004655:Emulsions / Q000737:chemistry; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D007668:Kidney / Q000187:drug effects / Q000473:pathology; D008081:Liposomes / Q000737:chemistry*; D008099:Liver / Q000187:drug effects / Q000473:pathology; D008297:Male; D049329:Nanostructures / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D000077185:Resveratrol; D012995:Solubility; D013267:Stilbenes / Q000008:administration & dosage* / Q000737:chemistry*; D016896:Treatment Outcome
D000975:Antioxidants; D004337:Drug Carriers; D004655:Emulsions; D008081:Liposomes; D013267:Stilbenes; D000077185:Resveratrol