| Popis: |
Ocular drug delivery by topical application is the most popular for the treatment of ocular diseases. However, a number of inherent anatomical and physiological ocular barriers limit the bioavailability of the drug administered by topical application. To overcome this limitation, dissolving polymeric microneedles (dMNs) have been used to create transport pathways and enhance the permeability of ocular drugs with minimal invasion. The aim of this study was to design and evaluate Optimized dMNs for ocular delivery of a hydrophilic drug using a computational design strategy. Polyvinyl alcohol/hyaluronic acid mixture was used as the dMN-forming polymers. A micromolding technique was used to fabricate the dMNs. The dMNs were evaluated for physical appearance using a digital microscope, mechanical strength using a texture analyzer. Moreover, the dissolution time, penetration depth, and permeation study on the porcine corneal tissues were investigated. The results showed that the optimal dMNs formulation was 20%PVA and 5%HA in a 1:5 weight ratio. The physical appearance showed conical microneedles with an average 601.23 ± 1.01 μm in height and 300.02 ± 0.23 μm in the base width. The optimal dMNs showed a maximum tolerance force of about 33.70 ± 0.30 N and created micro-channels on corneal tissues surface with the depth about 134.71±16.51 μm. The optimal dMNs can be completely dissolved in the corneal tissue within 3 min with high % permeation and flux of fluorescein sodium about 10.10 ± 0.55% and 14.21 ± 1.45 μg/cm2/h, respectively. In conclusion, the optimal dMNs showed high efficiency to enhance ocular delivery of the hydrophilic drug with safe and minimal invasion for ocular tissue. |
