Enhanced oral bioavailability of oligomeric proanthocyanidins by a self-double-emulsifying drug delivery system

被引:10
作者
Tian, Yuan [1 ]
Mao, Xinyu [1 ]
Sun, Rui [1 ]
Zhang, Ming [1 ]
Xia, Qiang [2 ]
机构
[1] Southeast Univ, Sch Biol Sci & Med Engn, Nanjing, Peoples R China
[2] Southeast Univ, Sch Biol Sci & Med Engn, State Key Lab Bioelect, Nanjing, Peoples R China
关键词
bioavailability; oligomeric proanthocyanidin; self-double-emulsifying drug delivery system; solid form; stability; IN-VITRO; CONTROLLED-RELEASE; EMULSIONS; CARRIER; FORMULATIONS; SOLUBILITY; ABSORPTION; PROTECTION; DIGESTION; VESICLES;
D O I
10.1002/fsn3.1673
中图分类号
TS2 [食品工业];
学科分类号
0832 ;
摘要
The present study aims at the formulation and evaluation of solid self-double-emulsifying drug delivery system (SDEDDS) to increase the bioavailability of oligomeric proanthocyanidin (OPC). The formulation is prepared through two-step method and is able to form water-in-oil-in-water (W/O/W) double emulsions after diluted with aqueous medium while keeping the drug in inner water phase. Solid-state characterization is performed by DSC and X-ray powder diffraction. Furthermore, antioxidant capacity shows that OPC is preserved by the solid SDEDDS. OPC-SDEDDS exhibit sustained release of OPC under the conditions mimicking gastrointestinal tract. The result shows that bioaccessibility of OPC is improved after incorporating into SDEDDS formulation compared to pure drug. The proposed SDEDDS is a promising carrier strategy for delivering the hydrophilic compounds with low-oral bioavailability.
引用
收藏
页码:3814 / 3825
页数:12
相关论文
共 42 条
[31]   Antiulcer activity of grape seed extract and procyanidins [J].
Saito, M ;
Hosoyama, H ;
Ariga, T ;
Kataoka, S ;
Yamaji, N .
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, 1998, 46 (04) :1460-1464
[32]   Influence of particle size on lipid digestion and β-carotene bioaccessibility in emulsions and nanoemulsions [J].
Salvia-Trujillo, L. ;
Qian, C. ;
Martin-Belloso, O. ;
McClements, D. J. .
FOOD CHEMISTRY, 2013, 141 (02) :1472-1480
[33]   Production of W/O/W (water-in-oil-in-water) multiple emulsions: droplet breakup and release of water [J].
Schuch, Anna ;
Deiters, Philipp ;
Henne, Julius ;
Koehler, Karsten ;
Schuchmann, Heike P. .
JOURNAL OF COLLOID AND INTERFACE SCIENCE, 2013, 402 :157-164
[34]   Regulation of inducible adhesion molecule expression in human endothelial cells by grape seed proanthocyanidin extract [J].
Sen, CK ;
Bagchi, D .
MOLECULAR AND CELLULAR BIOCHEMISTRY, 2001, 216 (1-2) :1-7
[35]   Long chain lipid based tamoxifen NLC. Part I: Preformulation studies, formulation development and physicochemical characterization [J].
Shete, Harshad ;
Patravale, Vandana .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2013, 454 (01) :573-583
[36]   Oral administration of insulin included in fine W/O/W emulsions to rats [J].
Shima, M ;
Tanaka, M ;
Fujii, T ;
Egawa, K ;
Kimura, Y ;
Adachi, S ;
Matsuno, R .
FOOD HYDROCOLLOIDS, 2006, 20 (04) :523-531
[37]   Design and evaluation of aspirin-loaded water-in-oil-in-water submicron multiple emulsions generated using two-stage ultrasonic cavitational emulsification technique [J].
Tang, Siah Ying ;
Sivakumar, Manickam .
ASIA-PACIFIC JOURNAL OF CHEMICAL ENGINEERING, 2012, 7 :S145-S156
[38]   Pluronic/gelatin composites for controlled release of actives [J].
Tatini, Duccio ;
Tempesti, Paolo ;
Ridi, Francesca ;
Fratini, Emiliano ;
Bonini, Massimo ;
Baglioni, Piero .
COLLOIDS AND SURFACES B-BIOINTERFACES, 2015, 135 :400-407
[39]   Estimation of intragastric solubility of drugs: In what medium? [J].
Vertzoni, Maria ;
Pastelli, Eleni ;
Psachoulias, Dimitris ;
Kalantzi, Lida ;
Reppas, Christos .
PHARMACEUTICAL RESEARCH, 2007, 24 (05) :909-917
[40]   THE EFFECT OF PROCYANIDOLIC OLIGOMERS ON THE COMPOSITION OF NORMAL AND HYPERCHOLESTEROLEMIC RABBIT AORTAS [J].
WEGROWSKI, J ;
ROBERT, AM ;
MOCZAR, M .
BIOCHEMICAL PHARMACOLOGY, 1984, 33 (21) :3491-3497