Amphiphilic Alkylated Pectin Hydrogels for Enhanced Topical Delivery of Fusidic Acid: Formulation and In Vitro Investigation

Abstract

Hydrogels constructed of amphiphilically modified polysaccharides have attracted a lot of interest because of their potential to augment drug diffusion over the skin. This research describes the synthesis of amphiphilic alkylated pectin via glycidyl tert-butyl ether modification (alkylation degree 15.7%), which was characterized using spectroscopic and thermal analysis techniques and then formulated into hydrogels for the study of their potential in regulating fusidic acid diffusion topically. The hydrogels were formulated by the ionic interaction of negatively charged pectin and positively charged crosslinker CaCl2, with a reported fusidic acid loading degree of 93–95%. Hydrogels made of alkylated pectin showed a lower swelling percentage than that of native pectin, resulting in a slower fusidic acid release. The influence of pH on the swelling percentage and drug release was also investigated, with results revealing that greater pH enhanced swelling percentage and drug release. The in vitro interactions with HaCaT cells revealed negligible cytotoxicity under application-relevant settings. Utilizing Franz diffusion cells, the alkylated pectin hydrogels caused fusidic acid to penetrate the Strat-M® membrane at a 1.5-fold higher rate than the native pectin hydrogels. Overall, the in vitro results showed that alkylated pectin hydrogels have a lot of promise for topical distribution, which needs further investigation.

Amphiphilic Chitosan Porous Membranes as Potential Therapeutic Systems with Analgesic Effect for Burn Care

“…In addition, the use of the epoxy compounds, such as DS, allows the attaching of alkyl fragments to the hydrophilic chitosan derivative, providing an amphiphilic character to the final material. This fact might be essential for the stabilization and release of insoluble drugs with hydrophobic sequences in their structure (such as lidocaine) [ 46 ]. Moreover, the DS crosslinking agent can increase the hydrodynamic and mechanical stability of the membranes formulations and can also regulate the tissue adhesion by varying the hydrophobic/hydrophilic ratio.…”

Fusidic acid-loaded Chitosan Nanoparticle Cream for Improved Antimicrobial Activity and Percutaneous Delivery

“…The ineffectiveness of percutaneous antibiotic treatment, which is characterized by insufficient skin penetration and local discomfort, has been linked to antibiotic resistance [1]. Amphiphilically-modified polysaccharide-based drug delivery systems have drawn a lot of interest because of their capacity to increase skin penetration [2]. Here we describe the formation of nanoparticles from amphiphilically-modified chitosan loaded with fusidic acid prior to their inclusion into cream dosage form for the evaluation of their potential in boosting fusidic acid percutaneous penetration.…”

Pectin Based Hydrogels for Drug Delivery Applications: A Mini Review

“…The effect of pH on the swelling rate and drug release was also studied, with outcomes showing that higher pH increased the swelling percentage and drug release. Interestingly, in vitro co-related with HaCaT cells displayed significantly less cytotoxicity, however, further extensive investigation is required [ 68 ].…”