Development and Characterization of a Novel Peptide-Loaded Antimicrobial Ocular Insert

Area of Science:

• Ophthalmology
• Materials Science
• Microbiology

Background:

• Infectious ocular keratitis is a primary cause of global blindness.
• Increasing bacterial resistance necessitates novel therapeutic strategies, such as antimicrobial peptides (AMPs).
• hLF 1-11, a synthetic AMP, shows antimicrobial efficacy but suffers from poor stability.

Purpose of the Study:

• To develop and characterize novel freeze-dried matrices for enhanced ocular delivery of the antimicrobial peptide hLF 1-11.
• To evaluate the stability, mucoadhesion, and drug release properties of the developed matrices.
• To assess the preserved antimicrobial activity of hLF 1-11 within the matrix formulation.

Main Methods:

• Preparation and characterization of freeze-dried solid matrices incorporating mucoadhesive polymers.
• Evaluation of rheology, hydration time, bioadhesion, drug content, and in vitro release kinetics.
• Long-term stability studies (up to 15 months) assessing chemical integrity and peptide bioactivity.

Main Results:

• A specific formulation (HPMC/T2/HA/hLF 1-11fd) demonstrated good drug recovery and no chemical degradation for at least 6 months.
• The matrix facilitated controlled drug release in simulated physiological conditions with optimal hydration.
• Antimicrobial activity of hLF 1-11 was maintained for up to 15 months in the freeze-dried formulation.

Conclusions:

• The developed freeze-dried matrix offers a promising platform for stable ocular delivery of antimicrobial peptides.
• This formulation can potentially improve the treatment of infectious ocular surface diseases.
• The study addresses the challenge of proteinaceous drug instability for topical ophthalmic applications.