Pelletization of Lamotrigine Solid Dispersion for Improved Solubilization

Poorly solubility in water of many newly developed high-potential drugs is an obstacle in formulation development. The aim of this study was to increase the solubility of Lamotrigine which is a poorly soluble drug and comes under BCS class-II by using solid dispersion technique. Lamotrigine, PEG 4000 and PVPK-30 solid dispersion was prepared by solvent evaporation method and the formulation was characterized using stability studies, Fourier transform infrared spectroscopy (FTIR) and physical parameters. After checking the preformulation studies and getting satisfactory results pellets were formulated and evaluation was done. Drug entrapment efficiency was more than 98 % which indicates that the pellets formed are good possessing in vitro release of 94.89 & 92.30 % for X1 & X2 batches respectively. INTRODUCTION: Poorly water-soluble drugs are increasingly becoming a problem in terms of obtaining the satisfactory dissolution within the gastrointestinal tract that is necessary for good bioavailability. It is not only existing drugs that cause problems but it is the challenge of medicinal chemists to ensure that new drugs are not only active pharmacologically but have enough solubility to ensure fast enough dissolution at the site of administration, often gastrointestinal tract . It is estimated that 40% or more of new chemical entities (NCEs) being identified through combinatorial screening programs are poorly soluble in water, which is a critical determinant of oral bioavailability and solubility of many newly developed high-potential drugs is an obstacle in formulation development, in addition Biopharmaceutical Classification System (BCS) highlights dissolution as the rate-limiting step for oral absorption of class II and IV drugs . Solubilization techniques include addition of a cosolvent, salt formation, prodrug design, complexation, particle size reduction, and the use of surface active agents, use of solvate and hydrates, polymorphs, hydrotrophy ,use of absorbents ,pH adjustment, solubilizing vehicles, etc. are the some other physico-chemical approaches to enhancing oral absorption of poorly water soluble drugs . Solid dispersion technology is the science of dispersing one or more active ingredients in an inert matrix in the solid stage in order to achieve increased dissolution rate, sustained release of drugs, altered solid state properties, and enhanced release of drugs.Solid dispersions (SDs) traditionally have been used as an effective method to improve the dissolution properties and bioavailability of poorly water-soluble drugs . Lamotrigine is an antiepileptic drug which comes under BCS class II and causes lot of solubility problems. In order to increase the solubility of the drug solid dispersion was employed by using two polymers PEG 4000 and PVPK 30 and evaluation of solid dispersion mixture and pellets were formulated after getting satisfactory results. In the present work, pellets of Lamotrigine were prepared by orifice-ionic gelation technique using