UCLA

Inflammation is one of the most common conditions that impact the health of the eye. Due to the static and dynamic barriers caused by the tear film and blinking, effective and sustained delivery of anti-inflammatory pharmaceutics remains a challenge of ocular treatment. Surface functionalization with mucoadhesion moieties has the ability to boost the bioavailability of pharmaceutics by increasing the retention time on corneal mucin. Herein, we developed a polymeric micelle (MC) as a nano-drug carrier and functionalized it with ocular-targeted moieties, including phenylboronic acid (PBA), gallic acid (GA), and tannic acid (TA). The MC composed with poly(ethylene glycol)-b-poly(N-(2-hydroxypropyl) methacrylamide-oligolactate) (PEG-b-(HPMA-Lacm+1)) copolymers. The HPMA-Lacm+1 was modified to increase encapsulation efficiency (EE%) of anti-inflammatory drugs. The EE% of loteprednol etabonate (LE) was increased by more than 20% compared to the result prior to the modification. In addition, the resulting MC exhibited a sustained release profile for 12 days. PBA funtionalization achieved 91.5% conjugation efficiency on PEG and the resulting PBA-MC exhibited excellent adhesion to mucin. However, the incorporation density of GA and TA were suboptimal. Therefore, PBA-MC was concluded as the best candidate for delivering anti-inflammatory drug, LE, to the ocular target.