SOLUBILITY ENHANCEMENT OF BCS CLASS II ANTIHYPERTENSIVE DRUG USING SOLID SELF EMULSIFICATION TECHNIQUE
Shwetha Krishnamurthy*, Srinivasan Bharath, Varadharajan Madhavan
ABSTRACT
Self emulsifying drug delivery systems (SEDDS) are isotropic
mixtures of oil, surfactant and co-surfactant which are generally
present in the form of liquid or semi-solid. Solid- SEDDS (S-SEDDS)
are solid forms of liquid SEDDS converted into solid by suitable
means. Candesartan cilexetil a Biopharmaceutical classification system
(BCS) Class II drug is a nonpeptide angiotensin II type 1(AT1)
receptor antagonist used in the treatment of hypertension. It has an
oral bioavailability of 15% because to its low solubility across the
physiological pH. The main objective of the study was to formulate SSEDDS
of candesartan cilexetil by adsorption process using a solid
inert carrier. Various formulations were prepared at concentrations of
oleic acid 20%, 40%, Poly ethylene glycol (PEG) 400 and Tween 80 at
1:2 and 1:4 ratios, and liquid SEDDS to Microcrystalline cellulose (MCC) at 1:1 and 1:2
ratios. The results of micromeritic properties showed that S- SEDDS had good powder flow
properties. A visual test was carried out to asses self emulsification of S-SEDDS which
showed spontaneous emulsification and there was no sign of phase separation. A fine milky
emulsion was formed within 2 min. The formulations containing 1:4 surfactant to cosurfactant
ratio showed faster drug release when compared to 1:2 ratio. The effect of
adsorbent in drug release characteristics of Liquid SEDDS was assessed and its
concentration in the formulation was optimized. Thus S-SEDDS of candesartan showed
better solubility enhancement and dissolution rate in contrast to pure drug formulation
which would further prove to enhance the oral bioavailability.
Keywords: Candesartan cilexetil, Solid self emulsifying drug delivery system, solid carriers, solubility enhancement.
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