Self-nanoemulsifying drug delivery system of fisetin: Formulation, optimization, characterization and cytotoxicity assessment

被引:48
|
作者
Kumar, Rajan [1 ]
Khursheed, Rubiya [1 ]
Kumar, Rakesh [1 ]
Awasthi, Ankit [1 ]
Sharma, Neha [1 ]
Khurana, Shelly [2 ]
Kapoor, Bhupinder [1 ]
Khurana, Navneet [1 ]
Singh, Sachin Kumar [1 ]
Gowthamarajan, Kuppusamy [3 ]
Wadhwani, Ashish [4 ]
机构
[1] Lovely Profess Univ, Sch Pharmaceut Sci, Phagwara 144411, Punjab, India
[2] Govt Polytech Coll, Dept Pharm, Amritsar, Punjab, India
[3] JSS Acad Higher Educ & Res, JSS Coll Pharm, Dept Pharmaceut, Ootacamund, Tamil Nadu, India
[4] JSS Acad Higher Educ & Res, JSS Coll Pharm, Dept Pharmaceut Biotechnol, Ootacamund, Tamil Nadu, India
关键词
Fisetin; SNEDDS; Permeation; Dissolution; Box-Behnken design; PRE/POST-COMPRESSION PROPERTIES; IN-VITRO; FLAVONOID FISETIN; ORAL BIOAVAILABILITY; SOLID CARRIERS; SNEDDS; DISSOLUTION; IMPACT; SOLUBILITY; PREVENTION;
D O I
10.1016/j.jddst.2019.101252
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Fisetin is a plant derived flavonoid that possesses anti-cancer, anti-oxidant and anti-Parkinson's activities. However, due to its lipophilicity it suffers from dissolution rate limited oral bioavailability that reduces its therapeutic efficacy. In order to overcome this issue self-nanoemulsifying drug delivery system (SNEDDS) of fisetin were formulated and characterized for droplet size, shape, zeta potential, cell viability, dissolution and permeability studies. Prepared SNEDDS (1.2 mL) were composed of castor oil (0.1 mL), Lauroglycol FCC (0.1 mL), tween 80 (0.4 mL), Transcutol P (0.6 mL) and fisetin (5 mg). The formulation was optimized using Box Behnken Design. Droplet size and zeta potential of optimized SNEDDS were found to be 154 nm and - 37 mV. Dissolution rate of fisetin got significantly (p < 0.05) enhanced through SNEDDS formulation in all the media as compared to unprocessed fisetin. Toxicity studies revealed more cell viability (89.05%) for fisetin loaded in SNEDDS as compared to its unprocessed form (10.8%) at a fixed concentration (62.5 mu g/mL). The in-vitro cell line study revealed about 3.79 folds increase in permeation rate for fisetin loaded in SNEDDS. The developed formulation was found to be stable with change in temperature, dilution and pH. The study entailed successful formulation of SNEDDS loaded with fisetin.
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页数:14
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