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

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 AUC_0–120 of 30,000–36,000 µg·h/mL, a C_max 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.

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Materials

Sodium alginate (ALG), cyclodextrin-α and β (CD-α and β), gelatin (GEL), PVA (M_w = 72,000) were purchased from Sigma Aldrich (St. Louis, MO, USA). EUD L100 was procured from Ropharma (Milan, Italy). Methanol, sodium hydroxide, and hydrophosphoric acid were procured from Merck (Darmstadt, Germany). ERY was supplied from Dr. Reddy’s Pharmaceutical Company, Bengaluru, India. Trypticase soy agar (TSA), thioglycollate broth, soybean casein digest agar, and sabouraud dextrose agar were purchased from Merck (Seoul, South Korea). The bacterial strains Micrococcus luteus (ATCC 4698), Staphylococcus aureus (ATCC 25923), and Escherichia coli (PTCC 1399) were procured from the American Type Culture Collection. All of the other compounds were of analytical grade and were used without further purification.

Mirzaeei, S.; Taghe, S.; Alany, R.G.; Nokhodchi, A. Eudragit^® L100/Polyvinyl Alcohol Nanoparticles Impregnated Mucoadhesive Films as Ocular Inserts for Controlled Delivery of Erythromycin: Development, Characterization and In Vivo Evaluation. Biomedicines 2022, 10, 1917.
https://doi.org/10.3390/biomedicines10081917