AI Article Synopsis
- - Recent advances in colloidal drug delivery systems have improved the bioavailability of poorly permeable drugs in topical ophthalmic formulations, like ribavirin, a class-III drug.
- - A bioadhesive multiple water-in-oil-in-water (W/O/W) microemulsion (ME) was developed for ribavirin, showing excellent stability and a small droplet size of 10 nm, which enhances its release and corneal permeability by three times.
- - The ME formulation indicated high cell viability in vitro and demonstrated no toxicity or irritation in vivo after single or repeated doses, suggesting its potential for delivering various drugs with low permeability.
Article Abstract
Corneal penetration is a key rate limiting step in the bioavailability of topical ophthalmic formulations that incorporate poorly permeable drugs. Recent advances have greatly aided the ocular delivery of such drugs using colloidal drug delivery systems. Ribavirin, a poorly permeable BCS class-III drug, was incorporated in bioadhesive multiple W/O/W microemulsion (ME) to improve its corneal permeability. The drug-loaded ME was evaluated regarding its physical stability, droplet size, PDI, zeta potential, ultrastructure, viscosity, bioadhesion, in vitro release, transcorneal permeability, cytotoxicity, safety and ocular tolerance. Our ME possessed excellent physical stability, as it successfully passed several cycles of centrifugation and freeze-thaw tests. The formulation has a transparent appearance due to its tiny droplet size (10 nm). TEM confirmed ME droplet size and revealed its multilayered structure. In spite of the high aqueous solubility and the low permeability of ribavirin, this unique formulation was capable of sustaining its release for up to 24 h and improving its corneal permeability by 3-fold. The in vitro safety of our ME was proved by its high percentage cell viability, while its in vivo safety was confirmed by the absence of any sign of toxicity or irritation after either a single dose or 14 days of daily dosing. Our ME could serve as a vehicle for enhanced ocular delivery of drugs with different physicochemical properties, including those with low permeability.
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|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7463957 | PMC |
| http://dx.doi.org/10.3390/pharmaceutics12080704 | DOI Listing |
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