Preparation and characterization of docetaxel self-nanoemulsifying powders (SNEPs): A strategy for improved oral delivery

被引:0
|
作者
Sharath Sunkavalli
Basanth Babu Eedara
Karthik Yadav Janga
Ashok Velpula
Raju Jukanti
Suresh Bandari
机构
[1] St. Peter’s Institute of Pharmaceutical Sciences,Department of Pharmaceutics
来源
Korean Journal of Chemical Engineering | 2016年 / 33卷
关键词
Docetaxel; Liquid Self-nanoemulsifying Drug Delivery Systems; Self-nanoemulsifying Powders; Oral Bioavailability; Cytotoxicity;
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学科分类号
摘要
Liquid self-nanoemulsifying drug delivery systems (L-SNEDDS) of docetaxel were prepared using varying ratios of Capmul PG 8 NF (oil), Cremophor EL (surfactant) and Transcutol-P (co-surfactant). The optimized L-SNEDDS (L11) was transformed into self-nanoemulsifying powder (SNEP) by physical adsorption on to Neusilin US2 and evaluated for dissolution behavior, in vitro cytotoxicity and in vivo oral bioavailability. Optimized L-SNEDDS (L11) composed of 50% of oil, 41.7% of surfactant and 8.3% co-surfactant produced stable emulsion with smaller globules (43±3 nm). In vitro dissolution studies showed the rapid drug release within 5min (95.42±1%) from SNEPN. In vitro cytotoxicity assessed by the MTT assay using MCF-7 human breast cancer cell lines revealed that L-SNEDDS significantly reduced the IC50 value and was 2.3 times lower than the pure docetaxel. Further, the oral bioavailability studies in male Wistar rats showed higher Cmax values following treatment with SNEPN (0.98±0.13 μg/mL) and L-SNEDDS (1.09±0.06 μg/mL) compared to pure docetaxel (0.37±0.04 μg/mL).
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页码:1115 / 1124
页数:9
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