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

Varela-Fernández, Rubén; García-Otero, Xurxo; Díaz-Tomé, Victoria; Regueiro, Uxía; López-López, Maite; González‐Barcia, Miguel; Lema, M; Otero-Espinar, Francisco J.

doi:10.1016/j.ejpb.2022.02.010

Cited by 52 publications

(22 citation statements)

References 86 publications

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“…SEM used to reveal the morphology of NPs as a fundamental property that indicates the surface features of the synthesized NPs and thus, it will influence the loading, release, pharmacokinetics and cellular/oocyst interaction [61]. The change of NPs shape occurs as it was reported Fig.…”

Section: Discussionmentioning

confidence: 99%

In Vitro Study to Evaluate the Efficacy of Ultrasonicated Ethanolic Extract of Rosmarinus officinalis and its Chitosan-Based Nanoparticles Against Eimeria tenella Oocysts of Chickens

et al. 2022

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In this study, chitosan nanoparticles (CsNPs) were used as nanocarrier for ultrasonicated ethanolic extract of Rosmarinus officinalis (UEERO) as a new nanoformulation against Eimeria tenella. Herein, CsNPs have been synthesized by ionic gelation method at pH 3 (CsNPs3) and pH 5 (CsNPs5), followed by characterization of morphology, size, polydispersity index (PDI), surface charge, and loading efficiency of UEERO. An in vitro sporulation inhibition assay (10, 5, 2.5, 1.25, 0.62, 0.31, 0.15, 0.07, 0.04, 0.02, and 0.01 mg/ml normal saline solution) against E. tenella was conducted. Results showed that free CsNPs and UEERO-CsNPs3/5 were cubic- and spherical-shaped with positive charge and average size of ~ 150.8 nm (314.4 nm) and 151.7 nm (321.1 nm), respectively. The total loading efficiency using UV–vis spectrophotometer, was 80.05 at pH 5 and 64.39% at pH 3. The in vitro sporulation inhibition assay revealed that UEERO, CsNPs3/5, and UEERO-CsNPs3/5 showed a potential inhibitory effect on sporulation (%), distortion in wall (%), and sporocyst abnormality (%) in a dose-dependent manner. Accordingly, the concentration (10 mg/ml) showed the best efficacy after 24 h in UEERO, free CsNPs, and UEERO-CsNPs. Moreover, UEERO-CsNPs3 and UEERO-CsNPs5 had stopped the sporulation (%) after 72 h. Taken all together, UEERO-CsNPs3 and UEERO-CsNPs5 are best effective against E. tenella in a dose-dependent manner in terms of sporulation (%), distortion in wall (%), and sporocysts abnormality. Graphical abstract

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Section: Discussionmentioning

confidence: 99%

In Vitro Study to Evaluate the Efficacy of Ultrasonicated Ethanolic Extract of Rosmarinus officinalis and its Chitosan-Based Nanoparticles Against Eimeria tenella Oocysts of Chickens

et al. 2022

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“…For example, a sustained release and new synthesis of cytokines in corneal tissues with long-term anti-inflammatory effects can be achieved from p-IL10 containing solid lipid nanoparticles [ 221 ]. Recently, a lactoferrin-based nanostructured lipid carrier was evaluated for its stability, cytotoxicity, entrapment efficiency, loading capacity, ocular surface retention, surface charge, and morphology [ 222 ]. The results showed nanostructured lipid carriers with an average size around 119.45 ± 11.44 nm, a PDI value of 0.151 ± 0.045, and a surface charge of 17.50 ± 2.53 mV [ 208 ].…”

Section: Formulation Approachesmentioning

confidence: 99%

“…The results showed nanostructured lipid carriers with an average size around 119.45 ± 11.44 nm, a PDI value of 0.151 ± 0.045, and a surface charge of 17.50 ± 2.53 mV [ 208 ]. Moreover, regulated release of lactoferrin, high entrapment efficiency, and lipid content (up to 75%) can be achieved [ 222 ]. Nonetheless, more research work is required for understanding the use of solid lipid nanoparticles and nanostructured lipid carriers for the ocular delivery of therapeutics.…”

Section: Formulation Approachesmentioning

confidence: 99%

Ocular Delivery of Therapeutic Proteins: A Review

2023

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Therapeutic proteins, including monoclonal antibodies, single chain variable fragment (ScFv), crystallizable fragment (Fc), and fragment antigen binding (Fab), have accounted for one-third of all drugs on the world market. In particular, these medicines have been widely used in ocular therapies in the treatment of various diseases, such as age-related macular degeneration, corneal neovascularization, diabetic retinopathy, and retinal vein occlusion. However, the formulation of these biomacromolecules is challenging due to their high molecular weight, complex structure, instability, short half-life, enzymatic degradation, and immunogenicity, which leads to the failure of therapies. Various efforts have been made to overcome the ocular barriers, providing effective delivery of therapeutic proteins, such as altering the protein structure or including it in new delivery systems. These strategies are not only cost-effective and beneficial to patients but have also been shown to allow for fewer drug side effects. In this review, we discuss several factors that affect the design of formulations and the delivery of therapeutic proteins to ocular tissues, such as the use of injectable micro/nanocarriers, hydrogels, implants, iontophoresis, cell-based therapy, and combination techniques. In addition, other approaches are briefly discussed, related to the structural modification of these proteins, improving their bioavailability in the posterior segments of the eye without affecting their stability. Future research should be conducted toward the development of more effective, stable, noninvasive, and cost-effective formulations for the ocular delivery of therapeutic proteins. In addition, more insights into preclinical to clinical translation are needed.

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“…The main methods for fabricating NLCs are hot homogenization, cold homogenization and solvent emulsification-evaporation (Roohinejad et al 2018 ). Solvent emulsification-evaporation is typically employed to encapsulate hydrophilic drugs like the protein LF (Varela-Fernández et al 2022 ).…”

Section: Nanostructured Lipid Carriers (Nlcs)mentioning

confidence: 99%

“…Only one study investigated LF-loaded NLCs (Varela-Fernández et al 2022 ). The context of the research was ocular drug delivery for keratoconus treatment.…”

Section: Nanostructured Lipid Carriers (Nlcs)mentioning

confidence: 99%

Nanoparticular and other carriers to deliver lactoferrin for antimicrobial, antibiofilm and bone-regenerating effects: a review

2022

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Bone and joint infections are a rare but serious problem worldwide. Lactoferrin’s antimicrobial and antibiofilm activity coupled with its bone-regenerating effects may make it suitable for improving bone and joint infection treatment. However, free lactoferrin (LF) has highly variable oral bioavailability in humans due to potential for degradation in the stomach and small intestine. It also has a short half-life in blood plasma. Therefore, encapsulating LF in nanocarriers may slow degradation in the gastrointestinal tract and enhance LF absorption, stability, permeability and oral bioavailability. This review will summarize the literature on the encapsulation of LF into liposomes, solid lipid nanoparticles, nanostructured lipid carriers, polymeric micro and nanoparticles and hydroxyapatite nanocrystals. The fabrication, characterization, advantages, disadvantages and applications of each system will be discussed and compared.

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

Cited by 52 publications

References 86 publications

In Vitro Study to Evaluate the Efficacy of Ultrasonicated Ethanolic Extract of Rosmarinus officinalis and its Chitosan-Based Nanoparticles Against Eimeria tenella Oocysts of Chickens

In Vitro Study to Evaluate the Efficacy of Ultrasonicated Ethanolic Extract of Rosmarinus officinalis and its Chitosan-Based Nanoparticles Against Eimeria tenella Oocysts of Chickens

Ocular Delivery of Therapeutic Proteins: A Review

Nanoparticular and other carriers to deliver lactoferrin for antimicrobial, antibiofilm and bone-regenerating effects: a review

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