Dissolution enhancement of flavonoids by solid dispersion in PVP and PEG matrixes: A comparative study

被引:109
作者
Kanaze, F. I.
Kokkalou, E.
Niopas, I.
Georgarakis, M. [1 ]
Stergiou, A.
Bikiaris, D.
机构
[1] Aristotle Univ Thessaloniki, Sch Hlth Sci, Dept Pharm, Thessaloniki 54124, Greece
[2] Aristotle Univ Thessaloniki, Dept Phys, Appl Phys Lab, Thessaloniki 54124, Greece
[3] Aristotle Univ Thessaloniki, Dept Chem, Lab Organ Chem Technol, Thessaloniki 54124, Greece
关键词
flavonoids; naringin; hesperidin; hesperetin; naringenin; PVP; PEG; solid dispersions; enhanced dissolution; LIQUID-CHROMATOGRAPHIC METHOD; WATER-SOLUBLE DRUGS; IN-VITRO; THERMAL-ANALYSIS; INHIBITION; BIOAVAILABILITY; NARINGENIN; HESPERETIN; HESPERIDIN; MECHANISM;
D O I
10.1002/app.24200
中图分类号
O63 [高分子化学(高聚物)];
学科分类号
070305 [高分子化学与物理];
摘要
Polyvinylpyrroliclone (PVP) and poly(ethylene glycol) (PEG) solid dispersion systems with flavanone glycosides, naringin and hesperidin, and their aglycones, naringenin and hesperetin, were prepared, using solvent evaporation method, to enhance their dissolution rates that may affect their bioavailability. Drug release of both flavanone glycosides and their aglycones was directly affected by the physical state of solid dispersions. Powder-XRD technique in combination with scanning and transmission electron microscopy revealed that PVP polymer formed amorphous nanodispersion systems with flavanone aglycones, while such systems could not be formed with their glycosides, which are bulkier molecules. Fourier transform infrared spectra suggest the presence of hydrogen bonds between PVP carbonyl groups and hydroxyl groups of both flavanone aglycones. These interactions prevent the crystallization of naringenin and hesperetin aglycones in PVP matrix. On the other hand, the ability of PEG carrier to form hydrogen bonds with flavanone glycosides or aglycones was limited, and as a result both flavanone glycosides and their aglycones remain in the crystalline form. For this reason, the solubility enhancement of PEG solid dispersions was lower than when PVP was used as drug carrier. At pH 6.8, the % release of naringenin and hesperetin from PVP/naringenin-hesperetin (80/20 w/w) solid dispersion was 100% while in PEG solid dispersions, it was not higher than 60-70%. (c) 2006 Wiley Periodicals, Inc.
引用
收藏
页码:460 / 471
页数:12
相关论文
共 33 条
[1]
TEMPLATE POLYMERIZATION OF METHACRYLIC-ACID IN THE PRESENCE OF POLY(ETHYLENE GLYCOL) AND POLY(N-VINYLPYRROLIDONE) IN BENZENE [J].
BARANOVSKY, VY ;
KOTLYARSKY, IV ;
ETLIS, VS ;
KABANOV, VA .
EUROPEAN POLYMER JOURNAL, 1992, 28 (11) :1427-1432
[2]
The effect of polyethylene glycol 400 on gastrointestinal transit: Implications for the formulation of poorly-water soluble drugs [J].
Basit, AW ;
Newton, JM ;
Short, MD ;
Waddington, WA ;
Ell, PJ ;
Lacey, LF .
PHARMACEUTICAL RESEARCH, 2001, 18 (08) :1146-1150
[3]
Accuracy of calculated pH-dependent aqueous drug solubility [J].
Bergström, CAS ;
Luthman, K ;
Artursson, P .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2004, 22 (05) :387-398
[4]
Physicochemical studies on solid dispersions of poorly water-soluble drugs - Evaluation of capabilities and limitations of thermal analysis techniques [J].
Bikiaris, D ;
Papageorgiou, GZ ;
Stergiou, A ;
Pavlidou, E ;
Karavas, E ;
Kanaze, F ;
Georgarakis, M .
THERMOCHIMICA ACTA, 2005, 439 (1-2) :58-67
[5]
Regulation of HepG2 cell apolipoprotein B metabolism by the citrus flavanones hesperetin and naringenin [J].
Borradaile, NM ;
Carroll, KK ;
Kurowska, EM .
LIPIDS, 1999, 34 (06) :591-598
[6]
Spectral methods for the characterization of polymorphs and solvates [J].
Brittain, HG .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1997, 86 (04) :405-412
[7]
Chaumeil JC, 1998, METHOD FIND EXP CLIN, V20, P211
[8]
Mucoadhesive drug carrier based on interpolymer complex of poly(vinyl pyrrolidone) and poly(acrylic acid) prepared by template polymerization [J].
Chun, MK ;
Cho, CS ;
Choi, HK .
JOURNAL OF CONTROLLED RELEASE, 2002, 81 (03) :327-334
[9]
The mechanisms of drug release from solid dispersions in water-soluble polymers [J].
Craig, DQM .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2002, 231 (02) :131-144
[10]
Anti-inflammatory activity of diosmin and hesperidin in rat colitis induced by TNBS [J].
Crespo, ME ;
Gálvez, J ;
Cruz, T ;
Ocete, MA ;
Zarzuelo, A .
PLANTA MEDICA, 1999, 65 (07) :651-653