Nanoemulsions as novel oral carriers of stiripentol: insights into the protective effect and absorption enhancement.
Oral administration remains a significant challenge in regards to drugs with serious solubility and stability issues. This article aimed to investigate the suitability of nanoemulsions as oral carriers of stiripentol (STP), an acid-labile drug, for enhancement of stability and bioavailability. STP-loaded nanoemulsions (STP-NEs) were prepared by using a solvent-diffusion/ultrasonication technique. STP-NEs were characterized in a variety of ways such as by particle size, entrapment efficiency, in vitro drug release, and transmission electron microscopy. A bioavailability study was performed in rats after oral administration of either STP-NEs, or commercial formulation (Diacomit). The resultant nanoemulsions were 146.6 nm in particle size with an entrapment efficiency of 99.47%. It was demonstrated that nanoemulsions significantly improved the biochemical stability and bioavailability of STP. The bioavailability of STP-NEs was up to 206.2% relative to Diacomit. Nanoemulsions fabricated from poly(ethylene glycol) monooleate/medium-chain triglycerides exhibited excellent performance in drug stabilization and absorption enhancement. The results suggest that STP-NEs are a promising means to solve the problems associated with stability and solubility of STP.
School of Ocean, Shandong University, Weihai, People's Republic of China.
Rong
R
Lu
School of Ocean, Shandong University, Weihai, People's Republic of China.
Shan
S
Liu
School of Ocean, Shandong University, Weihai, People's Republic of China.
Qilin
Q
Wang
School of Ocean, Shandong University, Weihai, People's Republic of China ; School of Pharmaceutical Sciences, Shandong University, Jinan, People's Republic of China.
Xia
X
Li
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004148:Dioxolanes / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics; D004355:Drug Stability; D004655:Emulsions / Q000737:chemistry / Q000493:pharmacokinetics; D053758:Nanoparticles / Q000737:chemistry*; D051381:Rats
D004148:Dioxolanes; D004337:Drug Carriers; D004655:Emulsions; C021092:stiripentol
bioavailability; intestinal permeability; nanoemulsions; stability; stiripentol