Improved pharmaceutical properties of surface modified bioactive plumbagin crystals

被引:13
作者
Bothiraja, C. [1 ]
Pawar, Atmaram P. [2 ]
Mali, Ashwin J. [2 ]
Shaikh, Karimunnisa S. [3 ]
机构
[1] Sharadchandra Pawar Coll Pharm, Dept Pharmaceut, Pune 412409, Maharashtra, India
[2] Poona Coll Pharm, Dept Pharmaceut, Pune 411038, Maharashtra, India
[3] Modern Coll Pharm, Dept Pharmaceut, Pune 411044, Maharashtra, India
关键词
plumbagin; PBN; crystallisation; crystal habit; cyclohexane; dissolution; IN-VITRO; ZEYLANICA; EXTRACT; ROOTS;
D O I
10.1504/IJSURFSE.2013.053708
中图分类号
TH [机械、仪表工业];
学科分类号
0802 ;
摘要
Plumbagin recrystallised by cold crystallisation technique using a variety of polar and non-polar solvents was investigated for pharmaceutical properties. Different solvents gave varying sized and shaped plumbagin. Powder X-ray diffraction, differential scanning calorimetery and fourier transform infrared spectroscopy too confirmed differing crystal habit. Platy crystals, the most significant forms, obtained from cyclohexane possessed small size (62.93 +/- 3.74 mu m), higher bulk density (0.108 +/- 0.014 g/ml) and lower enthalpy of fusion (Delta H 62.62 +/- 3.67 J/g). These demonstrated approximately two-fold increase in saturation solubility (155.01 +/- 3.86 mu g/ml), higher Q(5min) (cumulative percentage dissolution in 5 min) and lower t(65%) (time required for 65% dissolution) owing to greater surface area. In-vivo anti-inflammatory study in Wistar rats demonstrated improvement in therapeutic efficacy of recrystallised plumbagin. In conclusion surface modification led to enhanced efficacy of plumbagin; an approach capable of improving the bioavailability and clinical efficacy of other poorly water soluble phytomedicine.
引用
收藏
页码:181 / 195
页数:15
相关论文
共 25 条
  • [21] Singh U.V., 1997, J PHYSIOL PHARMACOL, V41, P171
  • [22] Modification of crystal habit and its role in dosage form performance
    Tiwary, AK
    [J]. DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2001, 27 (07) : 699 - 709
  • [23] Plumbagin induces cell cycle arrest and apoptosis through reactive oxygen species/c-Jun N-terminal kinase pathways in human melanoma A375.S2 cells
    Wang, Clay C. C.
    Chiang, Yi-Ming
    Sung, Shu-Chiao
    Hsu, Ya-Ling
    Chang, Jiunn-Kae
    Kuo, Po-Lin
    [J]. CANCER LETTERS, 2008, 259 (01) : 82 - 98
  • [24] High-performance liquid chromatography for quantification of plumbagin, an anti-Helicobacter pylori compound of Plumbago zeylanica L.
    Wang, YC
    Huang, TL
    [J]. JOURNAL OF CHROMATOGRAPHY A, 2005, 1094 (1-2) : 99 - 104
  • [25] WATANABE A, 1982, CHEM PHARM BULL, V30, P2958