Nanostructured mucoadhesive microparticles for enhanced preocular retention

Area of Science:

• Ophthalmology
• Materials Science
• Pharmaceutics

Background:

• Topical ocular drug delivery faces challenges with poor drug retention due to rapid clearance from the preocular surface.
• Conventional microparticle formulations often exhibit limited residence time, necessitating frequent administration.
• Developing advanced drug delivery systems is crucial for improving therapeutic efficacy in the eye.

Purpose of the Study:

• To design and evaluate nanostructured microparticles (NMs) with enhanced mucoadhesive properties for improved preocular drug retention.
• To investigate the role of nanostructured morphology in optimizing the mucoadhesive effect of polyethylene glycol (PEG).
• To assess the in vivo preocular retention of these NMs compared to conventional microparticles.

Main Methods:

• Fabrication of nanostructured microparticles (NMs) using poly(lactic-co-glycolic acid) (PLGA) and polyethylene glycol (PEG).
• Characterization of NM morphology, focusing on entangled nanofibers and increased surface area.
• In vivo evaluation of preocular retention of NMs formulated as dry tablets in an animal model.

Main Results:

• The nanostructured morphology of NMs, composed of entangled nanofibers, significantly increased specific surface area.
• Mucoadhesive properties were enhanced by the nanostructured design, synergistically improving PEG's effect.
• In vivo studies demonstrated a greater than 10-fold increase in preocular retention for NMs compared to conventional spherical microparticles.

Conclusions:

• Mucoadhesive nanostructured microparticles (NMs) offer significantly prolonged residence time on the preocular surface.
• These NMs represent a promising platform for advanced topical drug delivery to the eye.
• The findings support the potential of NMs for enhancing the efficacy of ocular therapies.