Eudragit® L100/Polyvinyl Alcohol Nanoparticles Impregnated Mucoadhesive Films as Ocular Inserts for Controlled Delivery of Erythromycin: Development, Characterization and In Vivo Evaluation

Abstract

The fast elimination of drugs from the cornea is one of many challenges associated with the topical administration of conventional dosage forms. The present manuscript aimed to prepare modified-release inserts containing erythromycin (ERY) to enhance drug delivery and address the aforementioned limitation. Film formulations were developed using Eudragit® L100 (EUD) and Polyvinyl Alcohol (PVA) polymers. ERY-loaded EUD-based nanoparticles were developed by the colloidal dispersion method using PVA as the emulsifier. The film-casting method was applied to form the mucoadhesive films using sodium alginate, gelatin, cyclodextrin-α, and β as polymeric film matrices. Different physicochemical properties of the optimized formulations and in vitro release profiles were evaluated. The in vivo evaluation was performed by collecting tear samples of rabbits using a novel, non-invasive method following the administration of inserts in the cul-de-sac. The ERY amount was assayed using a microbiological assay. The developed films showed prolonged in vitro and in vivo release profiles over five to six days; they had suitable physicochemical properties and a tensile strength of 2–3 MPa. All formulations exhibited antibacterial efficacy against E. coli and S. aureus with more than 20 mm diameter of inhibited growth zones. None of the formulations caused irritation to the rabbit’s eye. The inserts showed promising pharmacokinetics with AUC0–120 of 30,000–36,000 µg.h/mL, a Cmax of more than 1800 µg/mL at 4 h, and maintained drug concentration over the threshold of 5 µg/mL during the following 120 h of study. Nanoparticle-containing, mucoadhesive films could be fabricated as ocular inserts and can prolong the topical ocular delivery of ERY.

Thermosensitive Polyhedral Oligomeric Silsesquioxane Hybrid Hydrogel Enhances the Antibacterial Efficiency of Erythromycin in Bacterial Keratitis

“…Building on previous research that validated the antibacterial efficacy of EM-loaded nanoparticles against S. aureus using the inhibition zone method, our study employed the same technique to assess the suppressive impact of hydrogels on this bacterium [ 62 ]. Figure 6 A and B reveals that F127-EM, 1BPEP-EM, 2BPEP-EM, and PBS-EM produced significant inhibition zones in the growth of S. aureus , but F127, 1BPEP, 2BPEP, and PBS did not show any inhibition zones.…”

Harnessing Nanotechnology for Optimized Herbal Cancer Treatment: A Comprehensive Review of Nanoscale Drug Delivery Systems

“…NDDS can improve patient compliance by enabling prolonged-release protocols, reducing the need for multiple-dose administrations, and enhancing the therapeutic value by reducing toxic side effects and increasing bioavailability. 26,27 Nanoparticles offer several advantages in delivering herbal compounds, including their ability to target specific tissues or organs. Targeting is beneficial because it increases the proportion of the drug that reaches the target tissue, thereby improving bioavailability, and potentially reducing off-target effects.…”

Release of delta-9-tetrahydrocannabinol from polyvinyl alcohol hydrogels and its safe interaction with human skin fibroblasts

“…Cannabis and cannabis delivery to the skin can also be achieved through polymeric hydrogels, and the hydrogels can be generated using polyvinyl alcohol (PVA). This polymer has been used for numerous biomedical and pharmaceutical applications (Phan et al, 2019;Gonçalves et al, 2022;Mirzaeei et al, 2022). PVA hydrogels offer a non-toxic, non-carcinogenic, and bioadhesive delivery system.…”

“…PVA hydrogels offer a non-toxic, non-carcinogenic, and bioadhesive delivery system. PVA gels have been used for contact lenses, drug delivery applications, and more (Phan et al, 2019;Gonçalves et al, 2022;Mirzaeei et al, 2022). The presence of glycerol can improve the mechanical properties of PVA hydrogels (Delavari et al, 2022;Fu et al, 2022).…”