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

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.

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Materials: Glycerol monostearate 40–55 was purchased from Roig Farma S.A. (Barcelona, Spain). Soy lecithin was acquired from Acofarma® (Barcelona, Spain). Cholesterol from lanolin was provided by Sigma Aldrich Chemie GmbH (St Louis, USA). Compritol 888 ATO (a mixture of mono-, di- and triglycerides of behenic acid (C22)) and Capryol® 90 (propylene glycol monocaprylate) were generously presented by Gattefosse (Paris, France). Miglyol® 812 N (medium-chain triglycerides) was kindly donated by IOI Oleochemical GmbH (Witten, Germany). Poloxamer 407 (Kolliphor® P 407), Poloxamer 188 (Kolliphor® P 188) and D-α-Tocopherol Polyethylene Glycol 1000 Succinate were supplied by Sigma Aldrich Chemie GmbH (St Louis, USA). Lactoferrin was acquired from Sigma-Aldrich (St Louis, USA). All supplementary elements and reagents were of the uppermost available pureness score.

Article information: Rubén Varela-Fernández, Xurxo García-Otero, Victoria Díaz-Tomé, Uxía Regueiro, Maite López-López, Miguel González-Barcia, María Isabel Lema, Francisco Javier Otero-Espinar, Lactoferrin-loaded nanostructured lipid carriers (NLCs) as a new formulation for optimized ocular drug delivery, European Journal of Pharmaceutics and Biopharmaceutics, Volume 172, 2022. https://doi.org/10.1016/j.ejpb.2022.02.010.