Phytoconstituents have been utilized as medicines for thousands of years, yet their application is limited owing to major hurdles like deficit lipid solubility, large molecular size and degradation in the gastric environment of gut. Recently, phospholipid-complex technique has unveiled in addressing these stumbling blocks either by enhancing the solubilizing capacity or its potentiating ability to pass through the biological membranes and it also protects the active herbal components from degradation. Hence, this phospholipid-complex-technique can enable researchers to deliver the phytoconstituents into systemic circulation by using certain conventional dosage forms like tablets and capsules. This review highlights the unique property of phospholipids in drug delivery, their role as adjuvant in health benefits, and their application in the herbal medicine systems to improve the bioavailability of active herbal components. Also we summarize the prerequisites for phytosomes preparation like the selection of type of phytoconstituents, solvents used, various methods employed in phytosomal preparation and its characterization. Further we discuss the key findings of recent research work conducted on phospholipid-based delivery systems which can enable new directions and advancements to the development of herbal dosage forms.
The aim of present study was to investigate the effects of apigenin and rutin on the pharmacokinetics of paclitaxel after oral administration of paclitaxel with apigenin and rutin to rats. Paclitaxel (40 mg/kg) was administered orally alone and in combination with apigenin and rutin (10, 20, and 40 mg/kg) for 15 consecutive days. In the single-dose pharmacokinetic study (SDS), blood samples were collected on 1st day whereas on 15th day in the multiple-dose pharmacokinetic study (MDS). The plasma concentrations of paclitaxel were increased dose-dependently in the combination of apigenin and rutin compared to that of paclitaxel control in SDS and MDS (p < 0.01). The areas under the plasma concentration-time curve (AUC) and the plasma peak concentrations (C max) of paclitaxel with apigenin and rutin were significantly higher (p < 0.01) than that of the control. The AUCs and C max of paclitaxel were increased with apigenin and rutin in the dose-dependent manner. The half-life (t 1/2) was significantly longer than that of the control. Non-everted sacs were filled with paclitaxel 100 μM in the presence and absence of verapamil (50 μM), apigenin, and rutin (50, 100 μM) and incubated at 37 ºC for 60 min. The absorption of paclitaxel was increased in the presence of apigenin, rutin, and verapamil, a typical P-glycoprotein and Cyp3A4 inhibitor. If these results are confirmed in humans in a clinical setting, the paclitaxel dose should be adjusted when it is given concomitantly with apigenin and rutin.
From these results it can be understood that plant extract showing its pharmacological action on diabetes between the time intervals of 1-2 hr after its administration. This is exactly what the action that is being observed from the standard Glibenclamide group which also shown its action at its 1-2 hr of administration to the animals. Here the statistically significant action of the higher dose of plant extract can be compared with that of the standard Glibenclamide group. From these results it can be understood that the plant extract is capable of inhibiting the elevation of blood glucose level to the extent of the action that has been shown by the standard Glibenclamide group. Particularly at the time interval of 2-4 hr both the Glibenclamide and plant extract at its high dose group that is 400 mg/kg has been significantly inhibited the elevation of the blood glucose levels in the animals.DOI: http://dx.doi.org/10.3329/icpj.v2i3.13581 International Current Pharmaceutical Journal, February 2013, 2(3): 53-56
Aim: The aim of this study was to simultaneously enhance the solubility and stability of bacogenins by a ternary system comprised of hydrogenated soy lecithin and a third auxiliary substance, fulvic acid. Method: Both ternary and binary complexes were prepared using the solvent evaporation method and prepared binary and ternary systems were characterized by Fourier transform infrared technique, differential scanning calorimeter and scanning electron microscope. The entrapment efficacy in both binary and ternary system was calculated and the effect on the solubility, dissolution and stability of bacogenins (hydrolyzed bacoside rich extract) in 40% ethanol was found out. Furthermore, the prepared formulations were subjected to behavioural pharmacological studies. Results : FTIR, DSC, and SEM studies in totality confirmed the formation of binary and ternary complexes. Enhancement in solubility was observed, and the order of releasecharacteristics was found to be BHFS> BHSL>BHF> BH when the dissolution studies were carried out in 40% aqueous solution of ethanol. A significant improvement in the memory and antioxidant capacity was noticed in both binary, ternary complexes and fulvic acid treatment groups. Conclusion: The results revealed that the ternary complex could be a promising drug delivery system to improve the oral bioavailability of the bacogenins.
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