Physicochemical and Pharmacological Characterization of Etodolac- Loaded Poloxamer Gel as a Rectal Delivery System

Nahla   S.   Barakat; Hoda   M.   El-Maradny

Abstract

Rectal anti-inflammatory poloxamer gel systems composed of Poloxamer and bioadhesive polymers were developed and evaluated. Hydroxypropylmethyl cellulose (HPMC), poly(vinyl) pyrrolidone (PVP), methyl cellulose (MC), hydroxyethylcellulose (HEC) and carbopol (CP) were examined as mucoadhesive polymers. The characteristics of the suppositories differed according to the properties of mucoadhesive polymers. The physicochemical properties such as gelation temperature, gel strength and bioadhesive force of various formulations were investigated. The gelation temperature was between 20.4 and 38.8 °C, the gel strength was between 20.4 and 88.3 sec, mucoadhesive force was between 30.5 and 110.3 x 102 dyne/cm2. The analysis of release mechanism showed that the release of etodolac was proportional to the square root of time, indicating that etodolac might be released from the suppositories by Fickian diffusion (n ranged from 0.220 - 0.498). The release rate constant was between 5.431 and 17.349 %/minn. The anti-inflammatory effect of etodolac poloxamer gel was also studied in rats. Moreover, liquid suppository of etodolac did not cause any morphological damage to the rectal tissues. These results suggested that in situ gelling liquid suppository with etodolac and mucoadhesive polymer was a physically safe, convenient, and effective rectal dosage form for etodolac.

Keywords: Etodolac, Poloxamer gel, Mucoadhesive polymers, Gel temperature, Gel strength, Anti-inflammatory effect

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