Research Article: Optimization of Chitosan and Cellulose Acetate Phthalate Controlled Delivery of Methylprednisolone for Treatment of Inflammatory Bowel Disease

Date Published: June 30, 2017

Publisher: Tabriz University of Medical Sciences

Author(s): Swati Jagdale, Apoorva Chandekar.


Purpose: Inflammatory bowel disease (IBD) is a chronic, relapsing and often life-long disorder. The best way to tackle IBD is to develop a site targeted drug delivery. Methylprednisolone is a potent anti-inflammatory steroid. The relative potency of methylprednisolone to hydrocortisone is at least four is to one. The aim of the present research was to develop a colon targeted drug delivery for treatment of IBD.

Partial Text

Oral drug delivery is always the preferred form of delivery. The main problem with oral drug delivery is first pass metabolism. This becomes a major problem when drug needs to reach to the lower part of the gastrointestinal tract (GIT). To overcome this problem, targeted drug delivery systems are being developed. These formulations are designed to reach to the specific site to deliver drug.1 Controlled delivery technology is divided in two subtypes as programmed and triggered release technology. Programmed release depends largely on the build-in program to release the drug rather than depending on interaction with the environment in a certain gastrointestinal segment (site specific target) or with a disease specific target. Examples of release profiles in this category are prolonged or delayed release. Triggered release technologies are the one where release is initiated upon interaction of the delivery system with a site specific target as pH, pressure or microbial flora. Since there is no influence of disease specific factors, this profile is often called site specific release.2 In last few years the development of colon targeted drug delivery has received an increasing interest not only for a better treatment of specific local pathologies but also for the systemic therapy of both conventional and labile molecules. Colon targeted drug delivery system can be used to treat a number of diseases like colitis, Crohn’s disease and colorectal cancer.3 Especially those drugs that degrade in the hostile environment of the stomach and intestine can be protected from degradation and delivered directly to the colon. A large number of anti-asthmatics are delivered through this route.

Methylprednisolone, chitosan, cellulose acetate phthalate (CAP), avicel, croscarmellose sodium (CCS), dicalcium phosphate (DCP), crospovidone, talc and magnesium stearate were purchased from Analab Fine chemicals, Mumbai.

An attempt had been made to optimize a colon targeted drug delivery containing polymer chitosan and cellulose acetate phthalate. The main objective was to avoid first pass metabolism of the drug and to give a therapy for colon diseases. Direct compression technique was used for compression coated delivery. Design of experiment was applied for optimization of coating layer. F8 was the optimized batch. ANOVA results indicated that swelling index was the most significant factor in controlling the lag time and hence release of drug. CAP played most important role in swelling. In-vitro as well as in –vivo study indicated presence of delivery in third media indicating protection of the drug from being released in the upper region of GI system, i.e. stomach and small intestine. Thus F8 formulation can act as potential for treatment of colon diseases that can achieve maximum therapeutic efficacy.

The authors are thankful to Savitribai Phule Pune University, Maharashtra, India for providing financial assistance under Board of College and University Development (BCUD) Project Grant for the present research work. The authors are thankful to SKN General Hospital and Medical College, Narhe, Pune, for providing facility to carry In-vivo x-ray imaging (placebo) study. Authors are also thankful to Dr. B. S. Kuchekar, Principal and management of MAEER’s Maharashtra Institute of Pharmacy, Pune for providing all the facilities to carry out the research work.

The study was carried out as per World Medical Association guidelines and Helsinki ethical principle.

The authors declare no conflict of interests.




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