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.

Proniosomes derived niosomes: recent advancements in drug delivery and targeting

“…Proniosomes have been extensively investigated as potential oral drug delivery system. Several studies have been reported which prove the utility of oral proniosomal powders in providing the enhanced solubility and bioavailability for poorly soluble drugs (Nasr, 2010). Song et al (2015) showed that proniosomes are promising carrier in industrial production by formulating free-flowing and stable proniosomes of poorly water-soluble drug vinpocetine to augment its oral bioavailability and gastrointestinal absorption.…”

Formulation and optimisation of famotidine proniosomes: anin vitroandex vivostudy

“…FAM2 and FAM5 were found to sustain drug release due to high cholesterol content, this may be due to the fact that cholesterol is known to provide rigidity to the membrane, and also abolishes the gel to liquid-phase transition of niosomes and thus prevent the leakage of drug from vesicle. [15] The values of correlation coefficients of in vitro drug-release profile that fit best into the Higuchi model revealed that the batches follow super class II transport mechanism of drug release from proniosomes-derived niosome is by diffusion. [15] The ex vivo data of the release of famotidine (Table 2, Figure 9) from proniosomal formulations have shown significantly increased per cent release and flux with comparison to the same dose of marketed preparation of famotidine.…”

“…[15] The values of correlation coefficients of in vitro drug-release profile that fit best into the Higuchi model revealed that the batches follow super class II transport mechanism of drug release from proniosomes-derived niosome is by diffusion. [15] The ex vivo data of the release of famotidine (Table 2, Figure 9) from proniosomal formulations have shown significantly increased per cent release and flux with comparison to the same dose of marketed preparation of famotidine. Proniosomes should be hydrated to form niosomal vesicles before the drug is released and permeates across the stomach.…”

Comparative in vitro-in vivo correlation analysis with pioglitazone tablets

“…In common with other TZDs, PTZ ameliorates insulin resistance associated with T2DM without stimulating insulin release from pancreatic β cell, thus lowering the risk of hypoglycemia [12] . A single dose of 30 mg of PTZ has no hypoglycemic or hypolipidemic effect or liver toxicity within 24 h of treatment among healthy Bengali males [13] .…”