Title: Improved pharmaceutical properties of surface modified bioactive plumbagin crystals

Authors: C. Bothiraja; Atmaram P. Pawar; Ashwin J. Mali; Karimunnisa S. Shaikh

Addresses: Department of Pharmaceutics, Sharadchandra Pawar College of Pharmacy, Otur-412409, Pune, Maharashtra, India ' Department of Pharmaceutics, Poona College of Pharmacy, Erandwane, Pune-411038, Maharashtra, India ' Department of Pharmaceutics, Poona College of Pharmacy, Erandwane, Pune-411038, Maharashtra, India ' Department of Pharmaceutics, Modern College of Pharmacy, Nigdi, Pune-411044, Maharashtra, India

Abstract: 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 µm), higher bulk density (0.108 ± 0.014 g/ml) and lower enthalpy of fusion (ΔH 62.62 ± 3.67 J/g). These demonstrated approximately two-fold increase in saturation solubility (155.01 ± 3.86 µg/ml), higher Q5min (cumulative percentage dissolution in 5 min) and lower t65% (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.

Keywords: pharmaceutical properties; surface modification; bioactive plumbagin crystals; PBN oral formulation; crystallisation; crystal habit; cyclohexane; dissolution; solvents; therapeutic efficacy; recrystallised plumbagin; anti-inflammatory study; bioavailability.

DOI: 10.1504/IJSURFSE.2013.053708

International Journal of Surface Science and Engineering, 2013 Vol.7 No.2, pp.181 - 195

Received: 19 Apr 2012
Accepted: 28 Oct 2012

Published online: 05 May 2013 *

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