In vitro and in vivo evaluation of proniosomes containing celecoxib for oral administration

Abstract

The objectives of this research were to prepare celecoxib proniosomes and evaluate the influence of proniosomal formulation on the oral bioavailability of the drug in human volunteers. A new proniosomal delivery system for a poorly water-soluble drug such as celecoxib was developed and subjected to in vitro and in vivo studies. Proniosomes were prepared by sequential spraying method, which consisted of cholesterol, span 60, and dicetyl phosphate in a molar ratio of 1:1: 0.1, respectively. The average entrapment percent of celecoxib proniosome-derived niosomes was about 95%. The prepared proniosomes showed marked enhancement in the dissolution of celecoxib as compared to pure drug powder. The bioavailability of 200 mg single dose of both celecoxib proniosomal formulation and a conventional marketed celecoxib capsule was studied in human volunteers. The obtained results show that the proniosomal formulation significantly improved the extent of celecoxib absorption than conventional capsule. The mean relative bioavailability of the proniosomal formulation to the conventional capsule was 172.06 +/- 0.14%. The mean T (max) for celecoxib was prolonged when given as proniosomal capsule. There was no significant difference between the values of K (el) and t (1/2) for both celecoxib preparations. In conclusion, the proniosomal oral delivery system of celecoxib with improved bioavailability was established.

Fig. 1

Transmission electron microphotograph of celecoxib proniosome-derived niosomes stained with 2% potassium phosphotungstate

Fig. 2

Dissolution profiles of celecoxib proniosomes and pure celecoxib in 900 ml phosphate buffer (pH 6.8) containing 1% sodium lauryl sulfate (mean ± SD; n = 3)

Fig. 3

Mean plasma concentration–time curves of celecoxib (±SD) in human volunteers (n = 6) after oral administration of 200 mg as single oral dose of proniosomal formulation and Celebrex® capsules