Preparation and Evaluation of Self-emulsifying Drug Delivery System (SEDDS) of Cepharanthine

被引:18
|
作者
Yang, Xinggang [2 ]
Gao, Pan [1 ]
Jiang, Zhujun [2 ]
Luo, Qiao [1 ]
Mu, Chengqiao [2 ]
Cui, Mengsuo [2 ]
机构
[1] Shenyang Pharmaceut Univ, Dept Tradit Chinese Med, 103 Wenhua Rd, Shenyang 110016, Peoples R China
[2] Shenyang Pharmaceut Univ, Dept Pharm, 103 Wenhua Rd, Shenyang 110016, Peoples R China
关键词
cepharanthine; self-emulsifying drug delivery system; central composite design; pseudo-ternary phase diagram; oral bioavailability; FORMULATION; OPTIMIZATION; INHIBITION; SOLUBILITY; WATER; OIL;
D O I
10.1208/s12249-021-02085-9
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The aim of this article was to design a self-emulsifying drug delivery system (SEDDS) of loaded cepharanthine (CEP) to improve the oral bioavailability in rats. Based on the solubility determination and pseudo-ternary phase diagram, isopropyl palmitate (IPP) was chosen as the oil phase. Meanwhile, Cremophor RH40 and Macrogol 200 (PEG 200) were chosen as the emulsifier and co-emulsifier, respectively. This prescription was further optimized by using central composite design of response surface methodology. The optimized condition was CEP:IPP:Cremophor RH40:PEG 200=3.6:30.0:55.3:11.1 in mass ratio with maximum drug loading (36.21 mg/mL) and the minimum particle size (36.70 nm). The constructed CEP-SEDDS was characterized by dynamic light scattering, transmission electron microscopy, in vitro release and stability studies. The dissolution level of CEP-SEDDS was nearly 100% after 30 min in phosphate-buffered saline (PBS, pH 6.8) which was higher than that of the pure CEP (approximately 20%). In addition, in vivo pharmacokinetic study in rats showed that CEP-SEDDS dramatically improved bioavailability compared with active pharmaceutical ingredient (API) (the relative bioavailability was 203.46%). In this study, CEP-SEDDS was successfully prepared to enhance the oral bioavailability which might facilitate to increase its better clinical application.
引用
收藏
页数:12
相关论文
共 50 条
  • [1] Preparation and Evaluation of Self-emulsifying Drug Delivery System (SEDDS) of Cepharanthine
    Pan Gao
    Zhujun Jiang
    Qiao Luo
    Chengqiao Mu
    Mengsuo Cui
    Xinggang Yang
    [J]. AAPS PharmSciTech, 22
  • [2] Correction to: Preparation and Evaluation of Self-emulsifying Drug Delivery System (SEDDS) of Cepharanthine
    Pan Gao
    Zhujun Jiang
    Qiao Luo
    Chengqiao Mu
    Mengsuo Cui
    Xinggang Yang
    [J]. AAPS PharmSciTech, 22
  • [3] Preparation and Evaluation of Self-emulsifying Drug Delivery System (SEDDS) of Cepharanthine (vol 22, 245, 2021)
    Gao, Pan
    Jiang, Zhujun
    Luo, Qiao
    Mu, Chengqiao
    Cui, Mengsuo
    Yang, Xinggang
    [J]. AAPS PHARMSCITECH, 2021, 22 (08)
  • [4] In vivo evaluation of an oral self-emulsifying drug delivery system (SEDDS) for exenatide
    Menzel, Claudia
    Holzeisen, Thomas
    Laffleur, Flavia
    Zaichik, Sergey
    Abdulkarim, Muthanna
    Gumbleton, Mark
    Bernkop-Schnuerch, Andreas
    [J]. JOURNAL OF CONTROLLED RELEASE, 2018, 277 : 165 - 172
  • [5] Development and Evaluation of a (SEDDS) Self-Emulsifying Drug Delivery System for Darifenacin Hydrobromide
    SreeHarsha, Nagaraja
    Shariff, Arshia
    Shendkar, Yogesh A.
    Al-Dhubiab, Bandar E.
    Meravanige, Girish
    [J]. INDIAN JOURNAL OF PHARMACEUTICAL EDUCATION AND RESEARCH, 2019, 53 (02) : S204 - S212
  • [6] Effect of formulation variables on preparation and evaluation of gelled self-emulsifying drug delivery system (SEDDS) of ketoprofen
    Patil P.
    Joshi P.
    Paradkar A.
    [J]. AAPS PharmSciTech, 5 (3)
  • [7] Effect of formulation variables on preparation and evaluation of gelled self-emulsifying drug delivery system (SEDDS) of ketoprofen
    Patil, P
    Joshi, P
    Paradkar, A
    [J]. AAPS PHARMSCITECH, 2004, 5 (03):
  • [8] Design and Evaluation of Self-Emulsifying Drug Delivery Systems (SEDDS) of Nimodipine
    Amit A. Kale
    Vandana B. Patravale
    [J]. AAPS PharmSciTech, 2008, 9 : 191 - 196
  • [9] Design and evaluation of self-emulsifying drug delivery systems (SEDDS) of nimodipine
    Kale, Amit A.
    Patravale, Vandana B.
    [J]. AAPS PHARMSCITECH, 2008, 9 (01) : 191 - 196
  • [10] In vitro evaluation of a self-emulsifying drug delivery system (SEDDS) for nasal administration of dimenhydrinate
    Leichner, Christina
    Baus, Randi Angela
    Jelkmann, Max
    Plautz, Melanie
    Barthelmes, Jan
    Duennhaupt, Sarah
    Bernkop-Schnuerch, Andreas
    [J]. DRUG DELIVERY AND TRANSLATIONAL RESEARCH, 2019, 9 (05) : 945 - 955