Investigations of pectin nanostructures for enhanced percutaneous delivery of fusidic acid

Abstract

The study aims to formulate and characterize nanoformulations produced from amphipathically-modified pectin containing fusidic acid, making clear the importance of nanocarrier amphipathicity in boosting drug permeation through the skin. For this purpose, the amphipathically-modified pectin (GBE-PEC) fabrication was achieved following glycidol butyl ether modification via the nucleophilic substitution S N 2 reaction, which was then characterized using thermal analysis, spectroscopic, and chromatographic tools. The materials were subsequently converted into spherical nanostructures (NSs) (size 250-290 nm; zeta potential À25 to À34 mV) via a nanoprecipitation in situ cross-linking approach, demonstrating low viscosity and good colloidal stability under pH 4 conditions. The encapsulated fusidic acid (loading degree 14.9%) was released from GBE-PEC NSs in a more controlled fashion, with release profiles best characterized by the Higuchi model. Interactions with HaCaT cells in vitro demonstrated no apparent cytotoxicity at application relevant conditions, with efficient cellular absorption as evidenced by flow cytometry analysis. Using Franz diffusion cells, GBE-PEC NSs had a 2-fold greater penetration rate through the Strat-M ® membrane than the native pectin NSs. Overall, the study has introduced new insights into the design, fabrication, characterization, and tremendous potential of NSs formulated from GBE-PEC for percutaneous delivery of poorly penetrating actives, which merit further analysis.

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“…Initially, pectin in this study was isolated from head residues of sunflower to produce low-methoxyl pectin (AHP). Next, a study by Bostanudin et al proposed nanoformulations of amphipathica modified pectin-containing fusidic acid [41]. The amphipathic properties of a nanocarr are important to surmount cell membrane impenetrability to boost drug permeati through the skin and to allow the delivery of both hydrophilic and hydrophobic partic or macromolecules into cells [41,42].…”

“…Next, a study by Bostanudin et al proposed nanoformulations of amphipathically modified pectin-containing fusidic acid [41]. The amphipathic properties of a nanocarrier are important to surmount cell membrane impenetrability to boost drug permeation through the skin and to allow the delivery of both hydrophilic and hydrophobic particles or macromolecules into cells [41,42]. Amphipathically modified pectin (GBE-PEC) fabrication material is then converted into spherical nanostructures (NSs) [41].…”

“…The amphipathic properties of a nanocarrier are important to surmount cell membrane impenetrability to boost drug permeation through the skin and to allow the delivery of both hydrophilic and hydrophobic particles or macromolecules into cells [41,42]. Amphipathically modified pectin (GBE-PEC) fabrication material is then converted into spherical nanostructures (NSs) [41]. Encapsulated fusidic acid was released in a more controlled manner (loading degree 14.9%), and in vitro interaction with HaCaT cells showed a non-cytotoxicity profile and demonstrated a greater (two-fold) penetration rate through the Strat-M ® membrane compared to the native pectin NSs.…”

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“…There is a wide range of excipients used in the production of a matrix system. The selection of the matrix polymer depends on the desired release profile, method of preparation, and API characteristics, as well as on the various properties of the excipients [ 24 , 25 , 26 , 27 ].…”