This project investigated the targeted buccal mucosal delivery of (i) hydrophilic small molecules and an antibody by using iontophoresis (ii) poorly water soluble drugs using polymeric nanocarriers. A short duration topical delivery of therapeutics to the buccal mucosa for locally occuring diseases would increase the bioavailability of drugs in the target area, which in turn would improve the therapeutic response and patient compliance. Chapter 1 presents a detailed analysis on the biodistribution of buflomedil hydrochloride (BUF) in the mucosa upon the application of iontophoresis, which was analysed using UPLC-MS/MS. Building on these findings; Chapter 2 investigates the co-iontophoresis of two oppositely charged drugs in the same mucosal area, BUF and dexamethasone disodium phosphate. Chapter 3 describes the topical iontophoretic delivery of rituximab to the mucosa, which was quantified using ELISA technique. Chapter 4 focuses on the development and delivery of polymeric micellar nano sized formulations of poorly water soluble corticosteroids triamcinolone acetonide and fluocinonide to the mucosa.