Solubility is the phenomenon of dissolution of solid in liquid phase to give a homogenous system. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for optimum pharmacological response. Poorly water-soluble drugs often require high doses in order to reach therapeutic plasma concentrations after oral administration. Poor aqueous solubility is a major problem encountered with formulation development of new chemical entities. There are over 40% of new chemical entities that exhibit poor solubility and low bioavailability. As per BCS classification system, these drugs comes under BCS class II that show poor solubility and high permeability. The bioavailability of these drugs can be dramatically improved by increasing the solubility of these drugs. This review article highlights a number of techniques for enhanc
The oral route is one of the most important routes for local and systemic drug delivery, as it has a large surface, high permeability, and rich blood supply. Mouth dissolving films, are now becoming more popular than fast-dissolving tablets. The films are designed to disintegrate quickly when they come into touch with a surface that contains water, such the tongue. This allows the consumer to consume the product without the use of water. It can boost patient compliance and provide you a marketing advantage. The polymer used in mouth dissolving films is crucial to their quick dissolution and disintegration. The polymer must be non-toxic, non-irritating, flavorless, and simple to use. Natural and synthetic polymers are the two types of polymers that are employed. Natural polymers used in formulation of film include chitosan, gaur gum, xanthan gum, soy polysaccharide, gellan gum, locust bean gum, maltodextrin, and rosin. Hydroxypropyl cellulose, polyvinyl pyrrolidone, Hydroxypropyl Methylcellulose, Polyethylene Oxide, and Polyvinyl Alcohol are synthetic polymers that are frequently used to make films. The current overview gives a description of the numerous polymers that are utilized to make films that dissolve in the mouth.
The present work was aimed at formulating a SMEDDS self-micro emulsifying drug delivery system) of Ezetimibe and evaluating its in vitro and in vivo activity. Ezetimibe belongs to a new class of lipid-lowering agents that selectivity inhibits the intestinal absorption of cholesterol and related plant sterols. Due to very low solubility in the aqueous media ezetimibe shows low bioavailability. The aim of the present study investigation was to develop a Lipid Based Formulation (LBF) to enhance the dissolution as well as the oral bioavailability of practically water insoluble Ezetimibe. Type I & Type IV LBF formulation was prepared and evaluated. Solubility of the drug in different oils, Surfactant & co-surfactant was determined. On the basis of the solubility of the ezetimibe in different oil, surfactant & co-surfactant. Type I & Type IV formulation was prepared in Capriyol 90 (83 mg/ml), Capmul MCM C8 (73.7783 mg/ml) & Cremophor RH 40 (260 mg/ml), Cremophor EL (148 mg/ml), Acysol K 140 (327 mg/ml), Acrysol EL 135 (138 mg/ml), combination of various surfactants with PEG 400. Lipid based formulation then further evaluated for its percentage transmittance, robustness to dilution, stability and drug content. The optimized formulation of Ezetimibe loaded in Lipid based formulation shows complete in vitro drug release in 20min while drug shows only 25.5% drug release in 90 min. In Vitro study proved that the potential use of Lipid based formulation improves the dissolution rate of poorly water-soluble drug-Ezetimibe. Comparative pharmacodynamic evaluation was investigated in terms of lipid-lowering efficacy, using a Triton WR 1339-induced hypercholesterolemia model in rats. The SMEDDS formulation significantly reduced serum lipid levels in phases I and II of the Triton WR 1339 test, as compared with plain Ezetimibe. The optimized formulation was then subjected to stability studies as per International Conference on Harmonization (ICH) guidelines and was found to be stable over 12 months. Thus, the study confirmed that the SMEDDS formulation can be used as a possible alternative to traditional oral formulations of Ezetimibe to improve its bioavailability.
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