Design and optimization of self-nanoemulsifying drug delivery systems for improved bioavailability of cyclovirobuxine D

Abstract

BackgroundThe main purpose of this research was to design a self-nanoemulsifying drug delivery system (SNEDDS) for improving the bioavailability of cyclovirobuxine D as a poorly water-soluble drug.Materials and methodsSolubility trials, emulsifying studies, and pseudo-ternary phase diagrams were used to screen the SNEDDS formulations. The optimized drug-loaded SNEDDS was prepared at a mass ratio of 3:24:38:38 for cyclovirobuxine D, oleic acid, Solutol SH15, and propylene glycol, respectively. The optimized formulation was characterized in terms of physicochemical and pharmacokinetic parameters compared with marketed cyclovirobuxine D tablets.ResultsThe optimized cyclovirobuxine-D-loaded SNEDDS was spontaneously dispersed to form a nanoemulsion with a globule size of 64.80±3.58 nm, which exhibited significant improvement of drug solubility, rapid absorption rate, and enhanced area under the curve, together with increased permeation and decreased efflux. Fortunately, there was a nonsignificant cytotoxic effect toward Caco-2 cells. The relative bioavailability of SNEDDS was 200.22% in comparison with market tablets, in rabbits.ConclusionSNEDDS could be a potential candidate for an oral dosage form of cyclovirobuxine D with improved bioavailability.

Preparation and antitumor evaluation of self-assembling oleanolic acid-loaded Pluronic P105/D-α-tocopheryl polyethylene glycol succinate mixed micelles for non-small-cell lung cancer treatment

“…Additionally, inhibiting P-glycoprotein (P-gp) efflux is a key property for solubilizers. [47][48][49] TPGS possesses a lipophilic nonpolar head and a hydrophilic tail and would be an ideal surface-active agent to provide a high drug emulsification effect. 50,51 It has been reported that a self-assembled mixture of micelles (TPGS-Icariside IIphospholipid complex) successfully improved the solubility of Icariside II and alleviated efflux in Caco-2 cells.…”

Bioactive Self-Nanoemulsifying Drug Delivery Systems (Bio-SNEDDS) for Combined Oral Delivery of Curcumin and Piperine

“…The anhydrous SNEDDS samples were visually evaluated for homogeneity and appearance. As a preliminary screening, drug-free SNEDDS formulations were mixed with deionized water at 1:100 w/w ratio to provide fast evaluation of formulation appearance, homogeneity and spontaneity upon aqueous dilution [62][63][64]. Furthermore, SNEDDS formulations were loaded with CUR and PP at ≈80% of their equilibrium solubility and were then subjected to 1:1000 w/w aqueous dilution prior to formulation evaluation.…”

Novel cuminaldehyde self-emulsified nanoemulsion for enhanced antihepatotoxicity in carbon tetrachloride-treated mice

“…The varying hydrocarbon chain lengths of fatty acids in oil, surface‐active agent and the degree of unsaturation play crucial roles in the spontaneous production of emulsions with smaller DS and stability . Other indices such as EE and DL which were also significant parameters of SEN may be used to evaluate the efficiency of drug loading into nanocarriers . The higher EE (91.51 ± 0.44%) and DL (9.77 ± 0.75%) values of cuminaldehyde entrapment in nanoemulsion indicated a better loading capability.…”

“…[76] Other indices such as EE and DL which were also significant parameters of SEN may be used to evaluate the efficiency of drug loading into nanocarriers. [77] The higher EE (91.51 AE 0.44%) and DL (9.77 AE 0.75%) values of cuminaldehyde entrapment in nanoemulsion indicated a better loading capability. These results might be due to the extreme lipophilicity of cuminaldehyde, which may result in the internalisation of cuminaldehyde in the aquaphobic core of the formulation.…”