Solubility.

Mebendazole is a poorly soluble, highly permeable drug and the rate of its oral absorption is often controlled by the dissolution rate in the gastrointestinal. The poor dissolution rate of water-insoluble drugs is still a major problem confronting the pharmaceutical industry. There are several techniques to enhance the dissolution of poorly soluble drugs. Among them, the technique of Liquisolid compacts is a promising technique towards such a novel aim. In this study, the dissolution behaviour of mebendazole from liquisolid compacts was investigated in 0.1 N HCl. Liquisolid compacts were prepared by using PEG 400 as the liquid vehicle or non-volatile solvent. Avicel PH 102 as absorbing carrier and Aerosil 200 as adsorbing coating material. The ratio of carrier to coating powder material were kept different in formulations. The prepared liquisolid compacts were evaluated for their micromeritic properties and possible excipients interactions. The tableting properties were falling within acceptable limits. The in vitro dissolution study confirmed increase in drug release from liquisolid compacts compared to marketed preparation. This was due to an increase in wetting properties and surface of drug available for dissolution.

Development of amphiphilic drug-lipid complexes is a potential approach for improving delivery of the drugs by increasing solubility, release profile and oral bioavailability. Rutin, a polyphenolic flavonoid, shows several biological effects like capillary protectant, anti-oxidant, anti-inflammatory, anti-aging, cardio-protective, anti-thrombotic and neuroprotective, but its use is limited due to its low aqueous solubility. To overcome this limitation, phospholipid complex of Rutin was developed to improve its aqueous solubility for better absorption through the gastrointestinal tract and this might result in improved bioavailability. The Rutin phytosomes prepared by solvent evaporation method using different ratios of Rutin and Soybean phosphatidylcholine (1:1, 1:2 and 1:3) was evaluated for percentage yield, compatibility studies by infra-red spectroscopy, particle size, poly dispersity index, zeta potential, drug content and were found to be within the acceptable range. Surface morphology by scanning electron microscopy, solubility studies, in-vitro drug release and stability studies also were carried out. The phospholipid complex of Rutin was found to be fluffy and porous with rough surface. The water solubility of Rutin was improved from 0.058mg/ml to 0.475 mg/ml in the prepared Phytosomes. The in-vitro drug release studies showed that there is no drug release from pure drug and F1 formulation up to 120min in acidic buffer pH 1.2; while in phosphate buffer pH 7.4 showed releases about 49.3% and 92.85% respectively, which indicates the significant enhancement of dissolution of Rutin phytosomes compared to pure drug. Stability studies suggested that the formulations were stable. In this study, Phytosomes could be successfully tailored for Rutin with improved dissolution characteristics which is promising for lowering the influence of exogenous factors and increasing drug delivery.