DESIGN AND IN VITRO CHARACTERIZATION OF MUCOADHESIVE BUCCAL PATCHES OF DULOXETINE HYDROCHLORIDE

Himabindu Peddapalli,Nagaraj Banala,Krishna Mohan Chinnala

doi:10.22159/ijpps.2017v9i2.13793

Abstract

Objective: Buccal mucosa is a potential site for the delivery of drugs to the systemic circulation, a drug administered through the buccal mucosa enters directly to the systemic circulation, thereby which bypass the drug from the ﬁrst-pass hepatic metabolism and adverse gastrointestinal effect. Duloxetine hydrochloride (DLX HCL) is a selective serotonin and noradrenaline reuptake inhibitor (SSNRI). It is used in the treatment of depression, diabetic peripheral neuropathic pain and in moderate to severe stress urinary incontinence in women.However, it undergoes extensive first-pass metabolism, and it is susceptible to undergo degradation in the acidic environment of the stomach, which results in the poor bioavailability. The objective of the present investigation is to design and evaluate the mucoadhesive buccal patches of DLX HCL with a goal of to increase the bioavailability and improve the patient compliance.Methods: Mucoadhesive buccal patches were prepared by solvent casting technique using mucoadhesive polymers. The patches were evaluated for weight variation, thickness, surface pH, folding endurance, moisture absorption, drug content uniformity, in vitro drug release, mechanical properties and ex vivo permeation studies.Results: The results of the optimised buccal patch F4 indicate that the mucoadhesive buccal patches of duloxetine hydrochloride may be a good choice for improving the bioavailability by bypassing the extensive first pass metabolism and acid degradation in the stomach.Conclusion: Duloxetine hydrochloride can be delivered through the buccal route of drug administration through the buccal patches.

Highlights

Over the decades, peroral delivery has been the popular route of administration for the majority of therapeutic agents targeting systemic delivery
Duloxetine hydrochloride can be delivered through the buccal route of drug administration through the buccal patches
Buccal mucosa is a potential site for the delivery of drugs to the systemic circulation, a drug administered through the buccal mucosa enters directly to the systemic circulation through the internal jugular vein, thereby which bypass the drug from the first -pass hepatic metabolism and adverse gastrointestinal effect [4, 5]

Summary

Introduction

Peroral delivery has been the popular route of administration for the majority of therapeutic agents targeting systemic delivery. Oral administration generally leads to ‘Transmucosal’ absorption in the gastrointestinal tract; this enteral route of delivery subjects compound to extensive presystemic elimination, which may include gastrointestinal degradation, metabolism, or first-pass clearance via the liver, which leads to lack of significant correlation between membrane permeability, absorption, and bioavailability [1]. This first pass hepatic metabolism has often resulted in low systemic bioavailability, short duration of therapeutic activity, the formation of inactive agents and, at times, toxic metabolites [2]. Adhesive mucosal dosage forms were prepared for oral delivery, in the form of adhesive tablets [7, 8], adhesive gels, buccal ointments [9, 10], and adhesive patches [11]

Methods

Results

Conclusion