Ulcer-protective property of bryophyllum pinnatum leaf extract and their phytosomal formulations

Abstract

Active phytoconstituents usually exhibit robust in vitro pharmacological properties that do not correspond proportionately to the in vivo clinical benefits owing to their low gastrointestinal absorption. To improve on the bioavailability of the plant natural products, a strategy to enhance their in vivo absorption is developed via novel formulation of phytosome – a phospholipid-phytoconstituent complex. This study formulated Bryophyllum pinnatum extract into phytosome, evaluated and compared the ulcer-protective properties of the phytosome and the Bryophyllum pinnatum free extract in indomethacin-induced ulcerative animal ulcer model. Phytosomal formulations of Bryophyllum pinnatum leaves were prepared by combination of ethanol extract of Bryophyllum pinnatum and phosphatidylcholine (phospholipon® 90H) in different ratios of 1:1, 1:3, and 1:5, respectively. The phyto-phospholipid complexes were evaluated for some physical and chemical properties, which include entrapment efficiency, Fourier transform infrared (FTIR) spectroscopy and in vitro drug release. Standard laboratory methods were employed in the phytosome formulation, evaluation and ulcer-protective studies. Ulcer protective studies were carried out using 400 mg/kg of phytosome and crude extract. All the phytosomal formulations showed increased drug release profile in phosphate buffer (pH 6.8) when compared to the free extract. At 400 mg/kg, the complexes significantly (p < 0.05) improved ulcer-protective property and oxidative stress parameters when compared to the free extract, and hence, could be a better form for ulcer management.