Lactoferrin-loaded nanostructured lipid carriers (NLCs) as a new formulation for optimized ocular drug delivery

Eur J Pharm Biopharm. 2022 Mar:172:144-156. doi: 10.1016/j.ejpb.2022.02.010. Epub 2022 Feb 17.

Abstract

Nanostructured lipid carriers (NLC) are novel lipidic nanosystems that provide significant improvements in terms of high drug loading capacity and controlled drug release. The purpose of the present work was based on the design, development, and physicochemical characterization of lactoferrin-loaded NLCs as a new therapeutic alternative for the keratoconus treatment. Lactoferrin-loaded NLCs were successfully prepared by a double emulsion/solvent evaporation method. The resultant NLC were assessed in terms of particle size, size distribution, surface charge, morphology, encapsulation efficiency (EE), loading capacity (LC), stability, cytotoxicity, in vitro release, and ocular surface retention. Resulting data showed a size of 119.45 ± 11.44 nm, a 0.151 ± 0.045 PDI value and a surface charge of -17.50 ± 2.53 mV. Besides, high EE and LC values were obtained (up to 75%). The in vitro release study demonstrated a lactoferrin controlled release pattern. NLCs were also stable, non-toxic and show mucoadhesive properties. Thus, a consistent preclinical base was obtained, where NLC may be considered as a potential controlled release novel drug delivery system of lactoferrin for the keratoconus treatment.

Keywords: Double emulsification-solvent evaporation method; Keratoconus; Lactoferrin; Nanostructured lipid carriers (NLC); Ocular drug delivery; Topical ophthalmic administration.

MeSH terms

  • Drug Carriers* / chemistry
  • Drug Delivery Systems / methods
  • Drug Liberation
  • Lactoferrin
  • Lipids / chemistry
  • Nanostructures* / chemistry
  • Particle Size

Substances

  • Drug Carriers
  • Lipids
  • Lactoferrin