title: Self-nanoemulsifying drug delivery system of persimmon leaf extract: Optimization and bioavailability studies.
abstract: In current study, a self-nanoemulsifying drug delivery system (SNEDDS) of persimmon (Diospyros kaki) leaf extract (PLE) was developed and characterized to compare its in vitro dissolution and relative bioavailability with commercially available tablets (Naoxinqing tablets). Pseudo-ternary phase diagrams were constructed by phase diagram by micro plate dilution (PDMPD) method, of which the evaluation method was improved to use Multiskan Ascent for identifying turbidity. The formulation of PLE-loaded SNEDDS was optimized by an extreme vertices experimental design. The optimized nanoemulsion formulation, loading with 44.48 mg/g PLE total flavonoids, consisted of Cremophor EL, Transcutol P, Labrafil M 1944 CS (56:34:10, w/w), and it remained stable after storing at 40°C, 25°C, 4°C for at least 6 months. When diluted with water, the SNEDDS droplet size was 34.85 nm and the zeta potential was -6.18 mV. Compared with the commercial tablets, the AUC of both quercetin and kaempferol, which are representative active flavonoids of PLE, was increased by 1.5-fold and 1.6-fold respectively following oral administration of PLE-loaded SNEDDS in fasting beagle dogs. These results indicate that SNEDDS is a promising drug delivery system for increasing the oral bioavailability of PLE.
authors: School of Pharmaceutical Sciences, Sun Yat-sen University, 132 Waihuan East Road, Guangzhou Higher Education Mega Center, GuangZhou 510006, PR China.
authors: Wanwen
authors: W
authors: Li
authors: Shaoling
authors: S
authors: Yi
authors: Zhouhua
authors: Z
authors: Wang
authors: Si
authors: S
authors: Chen
authors: Shuang
authors: S
authors: Xin
authors: Jingwen
authors: J
authors: Xie
authors: Chunshun
authors: C
authors: Zhao
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D029788:Diospyros; D004285:Dogs; D004337:Drug Carriers; D004339:Drug Compounding; D004355:Drug Stability; D004356:Drug Storage; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D004655:Emulsions; D006868:Hydrolysis; D044949:Kaempferols / Q000493:pharmacokinetics; D053758:Nanoparticles; D036103:Nanotechnology; D010316:Particle Size; D018515:Plant Leaves; D011794:Quercetin / Q000493:pharmacokinetics; D012995:Solubility; D013607:Tablets; D013678:Technology, Pharmaceutical / Q000379:methods; D013696:Temperature
chemical_list: D004337:Drug Carriers; D004365:Drugs, Chinese Herbal; D004655:Emulsions; D044949:Kaempferols; D013607:Tablets; C006552:kaempferol; D011794:Quercetin