%0 Journal Article
%T Solubility Enhancement of Budesonide and Statistical Optimization of Coating Variables for Targeted Drug Delivery
%A Himanshu Bhatt
%A Bhargavi Naik
%A Abhay Dharamsi
%J Journal of Pharmaceutics
%D 2014
%I Hindawi Publishing Corporation
%R 10.1155/2014/262194
%X The purpose of the research was to present Budesonide (BUD) as a novel formulation showing improved aqueous solubility, which may decrease variability in and found in inflammatory bowel disease (IBD) patients, and drug targeting to colon. To improve aqueous solubility, solid dispersion (SD) of the BUD with poloxamer 188 was prepared by melting method. Physical characterization of solid dispersion was performed. The SD was used to prepare tablet equivalent to 9£¿mg of BUD. The tablet was coated with enteric polymers Eudragit S100 and Eudragit L100 to target colon. The ratio of polymers and percentage coating was optimized using statistical design. Variables studied in design were ratio of enteric polymers and the effect of percentage coating on in vitro drug release. Dissolution at different pH showed that drug release in colon could be modified by optimizing the ratio of polymers and percentage coating. The dissolution data showed that the percentage coating and ratio of polymers are very important to get lag time and optimum formulation. The optimized batch from statistical design was kept under accelerated condition for three months. After accelerated stability study, there was no significant change in the drug release. 1. Introduction Inflammatory bowel disease (IBD) involves the inflammation of mucosa in the small and large intestine. In IBD, two conditions persist, for example, Ulcerative colitis (UC) and Crohn¡¯s disease (CD). In UC, inflammation occurs into proximal regions of the colon over time. In CD, inflammation occurs to the distal ileum. Thus, there is need of development of drug delivery to both conditions at a time. The formulation design to treat CD will also be beneficial to treat UC. A drug, only in its dissolved form, can be absorbed into stomach and intestine. Drug dissolution occurrs in the distal portions of GIT. In this region, the viscosity of the colonic contents is very high which impede dissolution of poorly water soluble drug [1¨C3]. Budesonide (BUD) is a potent corticosteroid that is used in the IBD. The absorption variability in the is very high (30¨C600£¿min.) in the patient. Budesonide, BCS Class II, with a of 3.2, is practically insoluble in water (28£¿¦Ìg/mL) [4] at physiological pH in the intestinal region, which may be the rate limiting for the dissolution and therapeutic potential of budesonide. The objective is to improve the solubility of Budesonide to decrease variability found in . Moreover, bioavailability is only about 20% due to first pass effect. We can minimize variability in and by improving the solubility so
%U http://www.hindawi.com/journals/jphar/2014/262194/