ABSTRACT
Among the various routes of drug delivery oral route is the most widely accepted route by the
patients for delivery of therapeutically active drugs. So buccal route was widely used and
convenient method for drug administration. Aim of the present study was to prepare and
characterize mucoadhesive buccal tablets of Candesartan by direct compression method using
different mucoadhesive polymers such like carbopol, hydroxypropyl methylcellulose and
sodium alginate. Nine formulations were prepared while (F1) to (F3) were prepared by taking
individual concentrations whereas all the remaining formulations prepared by taking
combinations of polymers. Formulations (F4) to (F6) were composed of carbopol,
hydroxypropyl methylcellulose and sodium alginate in ratio of 1: 2. Formulations (F7) to (F9)
were composed by taking polymers like carbopol, hydroxypropyl methylcellulose and
sodium alginate in 1.5: 1.5 ratios. Candesartan is an angiotensin II receptor antagonist which
is widely used for the treatment of hypertension to reduce cardiovascular mortality in patients
with left ventricular dysfunction following myocardial infraction and heart failure. The
prepared buccal tablets were characterized for thickness, hardness, weight variation, drug
content, friability and in vitro drug release. Among all the formulations the (F3) formulation
with sodium alginate showed 93% drug release, while (F7) with equal ratios 1.5:1.5 ratios of
hydroxypropyl methylcellulose and sodium alginate showed 98% drug release within 8 hrs.
All the formulations were following zero order release kinetics. Key words: Buccal tablet, Candesartan, Carbopol, Hydroxypropyl methylcellulose, Sodium
alginate.
INTRODUCTION
Historically the oral route of drug administration has been the one used most for both
conventional as well as novel drug delivery.1 The concept of mucosal adhesion or
mucoadhesive was introduced into controlled drug delivery area in the early 1980’s, which is
become a major part of novel drug delivery system in the recent era. Some of the potential
sites for attachment of any mucoadhesive system are included in buccal cavity, nasal cavity,
eyes, vagina, rectal, sublingual route and gastrointestinal area.2 The term bioadhesion is
typically used to describe the adhesion between polymer either synthetic of natural to soft
tissue. In instances when bond is formed between mucus membrane and polymer the term
“mucoadhesion” is used. Mucus membrane is one in which the goblet cells are present for the
secretion of mucus which is composed of glycoprotein mucin.3 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 systemic circulation, thereby minimizing the first pass
hepatic metabolism and adverse gastrointestinal effect. Buccal region of the oral cavity is an
attractive target for administration of the drug of choice. Buccal drug absorption can be
promptly terminated in case of toxicity by removing the dosage form fro