Formulation and Development of Self-Nanoemulsifying Granules of Olmesartan Medoxomil for Bioavailability Enhancement

Abstract

The present investigation was aimed to formulate self-nanoemulsifying granules (SNEGs) of poorly water soluble drug, Olmesartan Medoxomil (OLM) to improve its solubility and oral bioavailability. Acconon sorb 20, Tween 80, and Carbitol were selected as oil, surfactant and cosurfactant, respectively for the development of liquid self-nanoemulsifying system (L-SNEDDS), which subsequently adsorbed on a carrier (Aerosil 200) to develop SNEGs. The results of in vitro and in vivo study of OLM-SNEGs revealed remarkable improvement compared to pure OLM. The present study proposed SNEGs as one of the suitable approach for developing nanosized solid oral dosage forms of OLM.

Keywords:

• Bioavailability
• Box-Behnken design
• Olmesartan medoxomil
• oral drug delivery
• self-nanoemulsifying granules

Notes

^a X₁: Amount of oil (Acconon sorb 20).

^b X₂: Amount of surfactant (Tween 80).

^c X₃: Amount of cosurfactant (Carbitol).

The results are of mean ±SD (n = 3).

The results are of mean ±SD (n = 3).

^a FM: Full model.

^b RM: Reduced model.

^c Nonsignificant (P > 0.05) coefficients for Y₁.

^d Nonsignificant (P > 0.05) coefficients for Y₂.

^e Nonsignificant (P > 0.05) coefficients for Y₃.

^a FM: Full model.

^b RM: Reduced model.

^c DF: Degree of freedom.

^d SSR: Sum of square residuals.

^e MS: Mean of squares.

^a The results are of mean ±SD (n = 3).

^a %DE: Percent dissolution efficiency at particular time.

^b MDT: Mean dissolution time (h).

^c f₁: Difference factor.

^d f₂: Similarity factor.

The results are mean ±SD (n = 3).

The results are mean ±SD (n = 3).

^a %DE: Percent dissolution efficiency at particular time.

^b MDT: Mean dissolution time (h).

^c f₁: Difference factor.

^d f₂: Similarity factor.

The results are mean ±SD (n = 6).

^a Test formulation: OLM-loaded SNETs by oral route.

^b Reference formulation: Marketed tablets by oral route.