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Eudragit<sup>®</sup> L100/Polyvinyl Alcohol Nanoparticles Impregnated Mucoadhesive Films as Ocular Inserts for Controlled Delivery of Erythromycin: Development, Characterization and In Vivo Evaluation
oleh: Shahla Mirzaeei, Shiva Taghe, Raid G. Alany, Ali Nokhodchi
Format: | Article |
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Diterbitkan: | MDPI AG 2022-08-01 |
Deskripsi
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<sup>®</sup> 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 <i>E. coli</i> and <i>S. aureus</i> 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<sub>0–120</sub> of 30,000–36,000 µg·h/mL, a C<sub>max</sub> 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.