4.1 Article

Improved pharmaceutical properties of surface modified bioactive plumbagin crystals

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INDERSCIENCE ENTERPRISES LTD
DOI: 10.1504/IJSURFSE.2013.053708

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plumbagin; PBN; crystallisation; crystal habit; cyclohexane; dissolution

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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.

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