Formulation design and in vitro physicochemical characterization of surface modified self-nanoemulsifying formulations (SNEFs) of gentamicin

Abstract

Self-nanoemulsifying formulations (SNEFs) structured with PEG 4000 as PEGylated SNEFs, were formulated after solubility studies using rational blends of soybean oil, a combination of Kolliphor(®) EL and Kolliphor(®) P188 as surfactants, and Transcutol(®) HP as co-surfactant, and evaluated for oral delivery of gentamicin. Incorporation of gentamicin and PEG 4000 reduced the initial area of nanoemulsion of the ternary phase diagrams produced by water titration method using oil, surfactant mixture and co-surfactant. Emulsion droplets were in the nanometer scale ranging from 80-210 nm. FT-IR study revealed that gentamicin structure remained intact in all formulations, and SEM micrographs showed spherical globules. Zeta potentials of SNEFs were in the range of -25.4 to -42.5 mV, and showed a stable system with minor flips in electrostatic charges. There was high in vitro diffusion-dependent permeation of gentamicin from the SNEFs. Results obtained in this work showed that oral delivery of gentamicin was improved by formulation as surface modified SNEFs.

Keywords: Castor oil (PubChem CID: 14030006); Gentamicin; Gentamicin (PubChem CID: 3467); Kolliphor(®) EL (PubChem CID: 5849927); Kolliphor(®) P188 (PubChem CID: 24751); Maisine(®) 35-1 oil (PubChem CID: 6436630); PEG 4000; PEG 4000 (PubChem CID: 174); Polysorbate 80 (PubChem CID: 5284448); Propylene glycol (PubChem CID: 1030); Self-nanoemulsifying formulations; Surface modification; Ternary phase diagrams; Transcutol(®) HP (PubChem CID: 8146); Zeta potential; n-octanol (PubChem CID: 957).