|
KMID : 0369820170470040325
|
|
Jorunal of Korean Pharmaceutical Sciences
2017 Volume.47 No. 4 p.325 ~ p.333
|
|
|
Development and pharmacokinetic evaluation of spray-dried self-nanoemulsifying drug delivery system of sertraline
|
|
Rahman Akhlaquer
Mujahid
Hussain Arshad
Iqbal Zeenat
|
|
|
Abstract
|
|
|
|
The objective of the present study was to develop solid self-nanoemulsifying drug delivery system (SNEDDS) of poorly absorbed drug sertraline (SRT) and evaluation of its pharmacokinetic parameters in rats. The composition of optimized liquid SNEDDS was (25.42 % v/v) Labrafil M 2125 CS and Maisine 35-1 (1:1), (49.72 % v/v) Tween 80 and (24.86 % v/v) Lauroglycol 90 containing 25 mg SRT. Solid SNEDDS was prepared by spray-drying the liquid SNEDDS using dextran 40 as solid carrier. There was no significant difference (p > 0.05) in the droplet size of reconstituted nanoemulsion between both liquid and solid SNEDDS. The surface characterization of spray-dried powder showed a satisfactory regular spherical shape of particles. The internal physical state of SRT was verified by X-ray diffraction analysis indicated the transformation of crystalline structure of SRT to amorphous and molecularly dispersed state. In vitro release of SRT from solid SNEDDS was highly significant (p < 0.01) as compared to unformulated SRT. After oral administration of solid SNEDDS to adult Sprague?Dawley (SD) rats, the area under the curve (AUC) were 2.8- and 6.8-folds and the maximum plasma concentration (Cmax) were 3.5 -and 13-folds higher, respectively compared to those of conventional capsule and unformulated drug suspension. These results reveal that solid SNEDDS results in a significantly increased absorption of SRT compared with that from the marketed conventional capsule and aqueous suspension of SRT. Thus, this solid SNEDDS may provide a useful solid dosage form for oral delivery of poorly-water soluble lipophilic compounds.
|
|
|
KEYWORD
|
|
|
SNEDDS, Dextran 40, Spray-drying, Oral delivery, Absorption, Bioavailability
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
|