Preparation and evaluation of a self-nanoemulsifying drug delivery system loaded with Akebia saponin D–phospholipid complex

• DOI: 10.2147/ijn.s108765
• Publication Date: 2016-09-27T01:22:41Z
• Authors: Fei Li; Jinyang Shen; Jianping Bi; Hongli Tian; Ye Jin; Yuan Wang; Xiaolin Yang; Zhonglin Yang; Junping Kou
• Keywords: Zeta potential

Akebia saponin D (ASD) exerts various pharmacological activities but with poor oral bioavailability. In this study, a self-nanoemulsifying drug delivery system (SNEDDS) based on the drug-phospholipid complex technique was developed to improve absorption of ASD.ASD-phospholipid (APC) prepared using solvent-evaporation method and characterized by infrared spectroscopy, differential scanning calorimetry, morphology observation, solubility test. Oil cosurfactant were selected according their ability dissolve APC, while surfactant chosen its emulsification efficiency in SNEDDS. Pseudoternary phase diagrams constructed determine optimized APC-SNEDDS formulation, which droplet size determination, zeta potential observation. Robustness dilution thermodynamic stability formulation also evaluated. Subsequently, pharmacokinetic parameters bioavailability ASD, investigated rats.The liposolubility significantly increased 11.4-fold after formation verified test n-octanol. Peceol (Glyceryl monooleate [type 40]), Cremophor® EL (Polyoxyl 35 castor oil), Transcutol HP (Diethylene glycol monoethyl ether) as oil, surfactant, cosurfactant, respectively. The optimal composed Glyceryl (type 40), Polyoxyl Diethylene ether, APC (1:4.5:4.5:1.74, w/w/w/w), showed particle 148.0±2.7 nm -13.7±0.92 mV distilled water at ratio 1:100 (w/w) good colloidal stability. Pharmacokinetic studies that exhibited greater Cmax1 (733.4±203.8 ng/mL) than ASD (437.2±174.2 ng/mL), Cmax2 (985.8±366.6 (180.5±75.1 (549.7±113.5 ng/mL). Compared Tmax1 Tmax2 both remarkably shortened APC-SNEDDS. rats enhanced 183.8% 431.8% APC-SNEDDS, respectively.These results indicated promising enhance ASD.