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.

journal_name

Int J Pharm

authors

Li W,Yi S,Wang Z,Chen S,Xin S,Xie J,Zhao C

doi

10.1016/j.ijpharm.2011.08.024

subject

Has Abstract

pub_date

2011-11-25 00:00:00

pages

161-71

issue

1

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(11)00786-1

journal_volume

420

pub_type

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