Characterisation of 2-HP-β-cyclodextrin-PLGA nanoparticle complexes for potential use as ocular drug delivery vehicles

Abstract

Aim

2-HP-β-cyclodextrin-PLGA nanoparticle complexes were prepared to enhance the aqueous humour delivery of Triamcinolone acetonide.

Materials & methods

Drug-loaded 2-HP-β-CD/PLGA nanoparticle complexes prepared by adapting a quasi-emulsion solvent evaporation technique. In vitro drug release, in vitro transcorneal permeation study, histopathological study and in vivo transcorneal penetration of PLGA nanoparticles and 2-HP-β-CD/PLGA nanoparticle complexes were evaluated.

Results

Particle size distributions of 2-HP-β-CD/PLGA nanoparticle complexes were 149.4 ± 3.7 nm and presented stable system. Corneal penetration studies revealed steady sustained drug release (First-order); 2-HP-β-CD/PLGA nanoparticle complexes increased ocular bioavailability by increasing dispersion in the tear film and improving drug release.

Conclusion

2-HP-β-CD/PLGA nanoparticle complex formulation is a promising alternative to conventional eye drops.

Graphical Abstract

Keywords:

• Hydrophilicity
• ocular drug delivery
• PLGA nanoparticles
• triamcinolone acetonide
• 2-hydroxypropyl-beta-cyclodextrin

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was supported by the R&D Team for Formulation Innovation [under Grant No. 2015CXQX150]; Innovation and Strong School Project of Guangdong Pharmaceutical University [under Grant No. 2015KQNCX077]; and Guangdong “Climbing” Programme for Undergraduates [under Grant No. PDJH2018B0263].