Lipoic acid nanoparticles: effect of polymeric stabilizer on appetite suppression.
Alpha-lipoic acid (ALA), which is common in the human body, is efficacious in appetite suppression. However, its typical formulations of salt or micronized crystals cannot satisfy the desired bioavailability requirements for appetite suppression due to low absorption and a short plasma half-life. Herein, we describe a new ALA nanoparticulate formulation produced by nano-comminution using polymeric stabilizers, such as hydroxypropyl cellulose, Pluronic F127, and polyvinylpyrrolidone. Nanoparticles of similar sizes did not show any remarkable differences in the in vitro release profiles. However, the in vivo results from food intake studies in mice demonstrated that the hydroxypropyl cellulose case had the largest improved efficacy among the three polymeric stabilizer cases. Compared to the nanosuspension formulations, the powder formulations of nanoparticles had improved efficacy in reducing food intake for six hours, possibly because of the delayed release kinetics. Therefore, the ALA powder formulation of nanoparticles is a candidate to replace the current formulations to achieve proper appetite suppression.
Park
Chul Ho
CH
Department of Chemical Engineering and Materials Science, Chung-Ang University, 221, Heukseok-dong, Dongjak-gu, Seoul 156 756, South Korea.
Lee
Ki-Up
KU
Park
Joong-Yeol
JY
Koh
Eun-Hee
EH
Kim
Hyoun-Sik
HS
Lee
Jonghwi
J
D000818:Animals; D001067:Appetite Depressants / Q000008:administration & dosage; D001682:Biological Availability; D002482:Cellulose / Q000031:analogs & derivatives; D002626:Chemistry, Pharmaceutical; D004435:Eating / Q000187:drug effects; D005079:Excipients; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D053758:Nanoparticles; D010316:Particle Size; D020442:Poloxamer; D011108:Polymers; D011205:Povidone; D011208:Powders; D012995:Solubility; D008063:Thioctic Acid / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*
D001067:Appetite Depressants; D005079:Excipients; D011108:Polymers; D011208:Powders; D020442:Poloxamer; D008063:Thioctic Acid; D002482:Cellulose; C008079:hydroxypropylcellulose; D011205:Povidone