Optimization of Sodium Deoxycholate-Based Transfersomes for Percutaneous Delivery of Peptides and Proteins

Abstract

Objective: This study aims to formulate and characterize the transfersomes for percutaneous delivery of peptides and proteins. In particular, this study was a preliminary study for the transfersomes formulation of recombinant human epidermal growth factor (rhEGF) for topical delivery.
 Methods: The transfersomes was prepared by thin film hydration method using phosphatidylcholine and sodium deoxycholate as vesicle former. In this study, transfersomes formulas were optimized, namely TF1, TF2, TF3, and TF4 with several ratios of phospholipid and surfactant which were 90:10, 85:15, 80:20, and 75:25, respectively. Afterward, the transfersomes were characterized in terms of particle size distribution, polydispersity index, zeta potential, morphology of vesicles, and deformability index.
 Results: The results showed that the best formulation was TF3 with the ratio of 80:20 with a particle size of 118.6±1.33 nm, polydispersity index of 0.102±0.011, zeta potential of-30.9±0,46 mV, and deformability index of 1.182±0.08. TEM analysis also showed spherical and unilamellar vesicles of transfersomes.
 Conclusion: This work demonstrated that the sodium deoxycholate-based transfersomes could be potential to be further formulated with peptide and protein for percutaneous delivery.

Formulation and In Vitro Penetration Study of Recombinant Human Epidermal Growth Factor-Loaded Transfersomal Emulgel

“…The data illustrated that the deformability indices of the three rhEGF transfersome formulations were similar to that of the transfersomes formula lacking rhEGF (data not shown). 18 Changes in particle size after extrusion did not occur in this test, proving that the vesicles maintained their integrity even after passing through smaller pores.…”

“…The selected concentrations of phospholipid and edge activator in the transfersome vesicle preparation were based on our earlier findings. 18 We determined that the formulation with a phosphatidylcholine:sodium deoxycholate ratio of 80:20 was superior given its characteristics such as spherical and unilamellar vesicles, a particle size of less than 200 nm, a polydispersity index close to 0, a zeta potential smaller than −30 mV, and good elasticity and deformability. In this present study, we encapsulated rhEGF at several concentrations into the selected optimized formulation.…”

“…The resulting transfersome suspension was extruded 11 times through polycarbonate membranes (200 nm). 18 …”

“…The resulting transfersome suspension was extruded 11 times through polycarbonate membranes (200 nm). 18 Characterization of rhEGF-loaded transfersomes Particle size and zeta potential analysis The particle size distribution and zeta potential of the formulations were determined using Zetasizer ZS90 (Malvern, UK) in triplicate. The size distribution was expressed as the mean hydrodynamic diameter (Z average ) and polydispersity index.…”

<p>Formulation of Nanospanlastics as a Promising Approach for ‎Improving the Topical Delivery of a Natural Leukotriene Inhibitor (3-‎Acetyl-11-Keto-β-Boswellic Acid): Statistical Optimization, in vitro ‎Characterization, and ex vivo Permeation Study</p>

“…This difference between SNVs and the conventional niosomes is attributable to the addition of EA that destabilizes the lipid bilayer improving its elasticity and deformability and enhance the ability of nanovesicles to squeeze through different biological membranes without losing their integrity. 51 Besides, the preliminary screening study was used to choose the EA that could achieve the highest elasticity for AKBA-loaded SNVs. It was detected that the elasticity of Tween 80 nanospanlastic vesicles was higher than other EAs (Tween 40 and Tween 20).…”