期刊
DRUG DELIVERY AND TRANSLATIONAL RESEARCH
卷 8, 期 3, 页码 670-692出版社
SPRINGER HEIDELBERG
DOI: 10.1007/s13346-018-0514-8
关键词
Solubility; Bioavailability; Quality by design; Nanoemulsion; Experimental designs; Cytotoxicity
资金
- M/s Zydus Cadila (Ahmedabad, India)
- M/s Gattefosse (Saint Priest, France)
- M/s BASF (Mumbai, India)
- M/s Colorcon Asia Pvt. Ltd. (Verna, India)
- M/s ACG Capsules (Mumbai, India)
- M/s Stat-Ease (Minneapolis, USA)
The work describes systematic development of nanomicellar cationic supersaturable self-nanoemulsifying drug delivery systems (CS-SNEDDS) for augmenting oral biopharmaceutical performance of raloxifene hydrochloride. Plain SNEDDS formulation containing Capryol 90, Cremophor RH 40, and Transcutol HP was optimized using D-optimal mixture design. SNEDDS were characterized for emulsification time, globule size, in vitro drug release, and ex vivo permeation. The CS-SNEDDS formulation was prepared firm the optimized SNEDDS by adding oleylamine as the cationic charge inducer and HPMC as the polymeric precipitation inhibitor. Evaluation of CS-SNEDDS was carried out through in vitro cell line studies on Caco-2 and MCF-7 cells, in situ perfusion, and in vivo pharmacokinetic studies, which indicated significant improvement in biopharmaceutical attributes of the drug from CS-SNEDDS over plain drug.
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