Targeted Drug Delivery of Anti Cancer Drug by Applying Gastro Retentive Systems and Its Pharmacological Evaluation

Abstract

Targeted drug delivery systems are designed to release the medicament continuously in a predetermined pattern for a fixed period of time either systemically or to a specified organ to ensure safety and to improve its efficacy as well as patient compliance. Drug released from these drug delivery systems should be at a desired, predictable and reproducible rate. Gastroretentive system (GRS) is a topic of current interest in the design of controlled release drug delivery systems to target the drug to the site of absorption. It prolongs the residence time of the dosage form at the site of application or absorption and facilitates an intimate contact of the dosage form with the underlying absorption surface and thus contributes to improved and/or better therapeutic performance of the drugs. In the present investigation design of floating tablets (GRS) of fluorouracil for oral controlled release is aimed. Fluorouracil is used in the treatment of cancer. It is sparingly soluble in water and its absorption is dissolution rate limited. Fluorouracil has a short biological half life and erratic absorption. To avoid the dose related toxicity and to prolong its duration of action controlled release products are necessary. The first chapter deals with introduction about the clear advantage of controlled release dosage forms and the advantages derived with gastro retentive system. It may be concluded that the formulation of floating effervescent tablets and floating microspheres of 5 fluoro uracil is feasible and may be manufactured with reproducible characteristics even from batch to batch. Therefore, a stomach specific Gastro retentive tablet and microsphere of 5 fluorouracil were formulated and characterized. It was found to reduce the unwanted dose dependent side effects, at other sites, by targeted drug delivery to gastric tumors. This may serve as an alternative to painful intravenous therapy.