Improvement of digoxin oral absorption in rabbits by incorporation into solid lipid nanoparticles

被引:14
作者
Hu, LianDong [1 ]
Jia, Huiqing [1 ]
Luo, ZhaoLiang [1 ]
Liu, Ci [1 ]
Xing, QianBin [1 ]
机构
[1] Hebei Univ, Coll Pharm, Sch Pharm, Baoding 071002, Hebei, Peoples R China
来源
PHARMAZIE | 2010年 / 65卷 / 02期
关键词
P-GLYCOPROTEIN; BIOAVAILABILITY; ENHANCEMENT; SLN;
D O I
10.1691/ph.2010.9241
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In this study, digoxin (DG)-loaded solid lipid nanoparticles (DG-SLNs) were successfully prepared by an ultrasonic and high pressure homogenization method. The particle size and distribution, drug loading capacity, drug entrapment efficiency (EE %), zeta potential, and long-term physical stability of the SLNs were characterized in detail. A pharmacokinetic study was conducted in rabbits after oral administration of 0.25 mg DG in different SLNs and it was found that the relative bioavailability of DG in the SLNs was significantly increased compared with that of a DG solution. The addition of CMC-Na in SLNs also markedly increased the oral absorption of DG. These results indicate that DG absorption is enhanced significantly by employing SLN formulations and SLNs are a potential as an oral delivery carrier for poorly water soluble drugs.
引用
收藏
页码:110 / 113
页数:4
相关论文
共 17 条
  • [1] Enhanced oral bioavailability of Coenzyme Q10 by self-emulsifying drug delivery systems
    Balakrishnan, Prabagar
    Lee, Beom-Jin
    Oh, Dong Hoon
    Kim, Jong Oh
    Lee, Young-Im
    Kim, Dae-Duk
    Jee, Jun-Pil
    Lee, Yong-Bok
    Woo, Jong Soo
    Yong, Chul Soon
    Choi, Han-Gon
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2009, 374 (1-2) : 66 - 72
  • [2] Enhanced oral absorption of halofantrine enantiomers after encapsulation in a proliposomal formulation
    Brocks, DR
    Betageri, GV
    [J]. JOURNAL OF PHARMACY AND PHARMACOLOGY, 2002, 54 (08) : 1049 - 1053
  • [3] CHEN Y, 2009, INT J PHARMACEUT, V376, P53
  • [4] Solid lipid namoparticles (SLNs) to improve oral bioavailability of poorly soluble drugs
    Hu, LD
    Tang, X
    Cui, FD
    [J]. JOURNAL OF PHARMACY AND PHARMACOLOGY, 2004, 56 (12) : 1527 - 1535
  • [5] Improvement of physicochemical properties of N-4472 Part II: characterization of N-4472 microemulsion and the enhanced oral absorption
    Itoh, K
    Matsui, S
    Tozuka, Y
    Oguchi, T
    Yamamoto, K
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2002, 246 (1-2) : 75 - 83
  • [6] Enhanced Bioavailability of a Poorly Soluble VR1 Antagonist Using an Amorphous Solid Dispersion Approach: A Case Study
    Kennedy, Michael
    Hu, Jack
    Gao, Ping
    Li, Lan
    Ali-Reynolds, Alana
    Chal, Ben
    Gupta, Vicki
    Ma, Chandra
    Mahajan, Nidhi
    Akrami, Anna
    Surapaneni, Sekhar
    [J]. MOLECULAR PHARMACEUTICS, 2008, 5 (06) : 981 - 993
  • [7] Enhancement of gastrointestinal absorption of quercetin by solid lipid nanoparticles
    Li, HouLi
    Zhao, XiaoBin
    Ma, YuKun
    Zhai, GuangXi
    Li, LingBing
    Lou, HongXiang
    [J]. JOURNAL OF CONTROLLED RELEASE, 2009, 133 (03) : 238 - 244
  • [8] Lucks S., 1996, EP Patent, Patent No. [0605497B1, 0605497]
  • [9] Solid lipid nanoparticles -: Production, characterization and applications
    Mehnert, W
    Mäder, K
    [J]. ADVANCED DRUG DELIVERY REVIEWS, 2001, 47 (2-3) : 165 - 196
  • [10] Solid lipid nanoparticles (SLN) for controlled drug delivery II. drug incorporation and physicochemical characterization
    Schwarz, C
    Mehnert, W
    [J]. JOURNAL OF MICROENCAPSULATION, 1999, 16 (02) : 205 - 213