Self-nanoemulsifying drug delivery system of cefpodoxime proxetil containing tocopherol polyethylene glycol succinate

Abstract

SNEDDS formulations led to improved oral bioavailability due to enhanced solubilization of selected drug.

Improving the oral bioavailability of buprenorphine: an in-vivo proof of concept

“…Adding water to PEG400 resulted in the gradual dissolution of BUP and NX.HCl, but this was unstable overnight. Non‐aqueous solvent combinations such as PEG400, a surfactant such as polysorbate 80 (Tween 80) and a cosurfactant such as TPGS have been used to form self‐emulsifying drug delivery systems . Such a system was used to solubilize the compounds used in the present study.…”

“…When diluted and mixed with water, the formulation was found to form a stable solution or dispersion which did not precipitate or separate at room temperature for at least overnight. Thus, for oral dosing with vehicle or adjuvants, the liquid formulation was an aqueous spontaneous micro‐/nanoemulsion formulation containing ~33% w/v PEG400, 3% w/v Tween 80 and 6% TPGS, with the balance (~58%) being water.…”

“…The adjuvant combinations comprised a near‐eutectic mixture of eugenol 20 mg/kg, isoeugenol 16 mg/kg, ethyl vanillin 20 mg/kg, vanillin 20 mg/kg, curcumin 5 mg/kg, silybin 5 mg/kg, α‐mangostin 5 mg/kg, resveratrol 20 mg/kg, propyl gallate 12 mg/kg and naringin hydrate 60 mg/kg dosed by oral gavage with BUP 10 mg/kg and NX.HCl 2.5 mg/kg with or without an adjuvant combination. The nature of the formulation (solution vs emulsion; micro‐ vs nanoemulsion) has not yet been experimentally established, but a stable nanoemulsion may be expected . The IV dosing formulation was a commercial preparation of BUP 0.5 mg/ml to which NX.HCl was added to reach a concentration of 0.125 mg/ml.…”

Understanding peroral absorption: regulatory aspects and contemporary approaches to tackling solubility and permeability hurdles

“…The poly(methacrylic acid and methacrylate) copolymer allows release of load at a specific pH within the gastrointestinal tract. Table 6, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147 reveals a few examples of nanoparticulate systems which improve bioavailability.…”

“…Food effect on cinnarazine could be significantly reduced by dosing either as SNEDDS capsule or tablet.122SNEDDSPre-concentrate preparation methodAmiodarone and talinololIISNEDDS resulted in higher and less variable AUC and T max . SNEDDS increases the solubilization, reduces intraenterocyte metabolism, reduced P-gp efflux and does not cause intestinal tissue damage.123SNEDDSVortexingCefpodoxime proxetilIVSNEDDS containing campul MCM (oil), Tween 80 as surfactant, TPGS as co surfactant which was further pelletised has shown to improve solubilization which improves the permeability by 10-fold and bioavailability by 4-fold.124SNEDDSVortexingValsartanIISolid-SNEDDS system was prepared containing campul MCM (oil), labrasol (surfactant) and Tween 20 (co-surfactant) SNEDDS adsorbed on the solid carrier (Sylysia 350) and compressed into tablet. The system has shown 3.5-fold increase in dissolution rate of drug due to enhanced solubility.125SNEDDSVortexingZiprasidoneIISNEDDS prepared using campul MCM (oil phase), labrasol (surfactant) and PEG 400 (co surfactant) which was further used to prepare sustained release pellets showed prolonged action with enhanced bioavailability.126SMEDDSVortexingPioglitazoneIISMEDDS prepared using cottonseed oil, Tween 80 as surfactant and PEG as co-surfactant has been used to improve rate of dissolution of pioglitazone 2- to 3-fold when compared with commercial tablet.127SMEDDSVortexingFuresemideIVSMEDDS was developed using oleic acid based heterolipid as oil phase, solutol HS 15 as surfactant and ethanol as co surfactant.…”