Lecithin-Based Novel Cationic Nanocarriers (Leciplex) II: Improving Therapeutic Efficacy of Quercetin on Oral Administration

被引：97

作者：

Date, Abhijit A. ^{[1
]}

Nagarsenker, Mangal S. ^{[1
]}

Patere, Shilpa ^{[1
]}

Dhawan, Vivek ^{[1
]}

Gude, R. P. ^{[2
]}

Hassan, P. A. ^{[3
]}

Aswal, V. ^{[3
]}

Steiniger, Frank ^{[4
]}

Thamm, Jana ^{[5
]}

Fahr, Alfred ^{[5
]}

机构：

[1] Bombay Coll Pharm, Dept Pharmaceut, Bombay 400098, Maharashtra, India

[2] ACTREC, Tata Mem Ctr, Navi Mumbai 410210, India

[3] Bhabha Atom Res Ctr, Mumbai 400085, Maharashtra, India

[4] Univ Jena, Fac Med, Ctr Electron Microscopy, D-07740 Jena, Germany

[5] Univ Jena, Dept Pharmaceut Technol, D-07743 Jena, Germany

来源：

MOLECULAR PHARMACEUTICS | 2011年 / 8卷 / 03期

关键词：

quercetin; poor solubility; phospholipids; lipid nanoparticles; lecithin; oral delivery; antitumorigenic activity; MELANOMA GROWTH; ANTIOXIDANT; ABSORPTION; FLAVONOIDS; VESICLES; EMULSIFIERS; SURFACTANTS; FORMULATION; TRANSPORT; CURCUMIN;

D O I：

10.1021/mp100305h

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

100103 [病原生物学]; 100218 [急诊医学];

摘要：

The objective of the present investigation was to evaluate ability of the novel self-assembled phospholipid- based cationic nanocarriers (LeciPlex) in improving the therapeutic efficacy of a poorly water-soluble natural polyphenolic agent, quercetin (QR), on oral administration. Quercetin loaded LeciPlex (QR-LeciPlex) were successfully fabricated using a biocompatible solvent Transcutol HP. The QR-LeciPlex were characterized for particle size, encapsulation efficiency, zeta potential, and particle morphology by cryo-TEM. UV and fluorescence spectral characterization was carried out to find out the association of QR with LeciPlex. Small angle neutron scattering studies (SANS) were carried out to understand the internal structure of Leciplex and to evaluate the influence of the incorporation of QR in the LeciPlex. Anti-inflammatory and antitumorigenic activity of QR-LeciPlex was determined in comparison to QR suspension to evaluate the potential of LeciPlex in improving oral delivery of QR. QR-LeciPlex exhibited a particle size of similar to 400 nm and had excellent colloidal stability. The QR-LeciPlex had a zeta potential greater than +30 mV and exhibited very high encapsulation efficiency of QR (>90%). UV and fluorescence spectral characterization indicated the interaction/association of QR with LeciPlex components. Cryo-TEM studies showed that LeciPlex and QR-LeciPlex have a unilamellar structure. SANS confirmed the unilamellar structure of LeciPlex and indicated that the incorporation of QR does not have any effect on the internal structure of the LeciPlex. QR-LeciPlex exhibited significantly higher anti-inflammatory and antitumorigenic activity (p < 0.01) as compared to that of QR suspension on oral administration.

引用

页码：716 / 726

页数：11

共 52 条

[1]

[Anonymous], 1975, CHEM NAT COMPD+, DOI [10.1007/BF00568459, DOI 10.1007/BF00568459]

[2]

Characterization of vesicles from ion-paired gemini surfactants by small angle neutron scattering [J].

Aswal, VK ;

Haldar, J ;

De, S ;

Goyal, PS ;

Bhattacharya, S .

PHYSICAL CHEMISTRY CHEMICAL PHYSICS, 2003, 5 (05) :907-910

[3]

Combination of lipids and emulsifiers enhances the absorption of orally administered quercetin in rats [J].

Azuma, K ;

Ippoushi, K ;

Ito, H ;

Higashio, H ;

Terao, J .

JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, 2002, 50 (06) :1706-1712

[4]

Sustained release nanoparticulate formulation containing antioxidant-ellagic acid as potential prophylaxis system for oral administration [J].

Bala, I ;

Bhardwaj, V ;

Hariharan, S ;

Kharade, SV ;

Roy, N ;

Kumar, MNVR .

JOURNAL OF DRUG TARGETING, 2006, 14 (01) :27-34

[5]

PLGA Nanoparticles Stabilized with Cationic Surfactant: Safety Studies and Application in Oral Delivery of Paclitaxel to Treat Chemical-Induced Breast Cancer in Rat [J].

Bhardwaj, V. ;

Ankola, D. D. ;

Gupta, S. C. ;

Schneider, M. ;

Lehr, C. -M. ;

Kumar, M. N. V. Ravi .

PHARMACEUTICAL RESEARCH, 2009, 26 (11) :2495-2503

[6]

Health effects of quercetin: From antioxidant to nutraceutical [J].

Boots, Agnes W. ;

Haenen, Guido R. M. M. ;

Bast, Aalt .

EUROPEAN JOURNAL OF PHARMACOLOGY, 2008, 585 (2-3) :325-337

[7]

Caltagirone S, 2000, INT J CANCER, V87, P595, DOI 10.1002/1097-0215(20000815)87:4<595::AID-IJC21>3.0.CO

[8]

2-5

[9]

CANTY DJ, 1994, NUTR REV, V52, P327, DOI 10.1111/j.1753-4887.1994.tb01357.x

[10]

Chabane MN, 2009, J PHARM PHARMACOL, V61, P1473, DOI [10.1211/jpp.61.11.0006, 10.1211/jpp/61.11.0006]

← 1 2 3 4 5 6 →