Relevant Physicochemical Methods to Functionalize, Purify, and Characterize Surface-Decorated Lipid-Based Nanocarriers

Guyon, Léna; Groo, Anne-Claire; Malzert‐Fréon, Aurélie

doi:10.1021/acs.molpharmaceut.0c00857

Cited by 13 publications

(12 citation statements)

References 121 publications

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“…It is an intriguing approach to target the specific receptors with specific ligands so that the uptake of drugs in the respective targeted cells can be improved. Nowadays, targeting ligands come in a variety of forms, including proteins, aptamers, peptides, and small molecules …”

Section: Surface Modifiers Utilized For Surface Modification Of Lipid...mentioning

confidence: 99%

Surface Modification of Lipid-Based Nanocarriers: A Potential Approach to Enhance Targeted Drug Delivery

2022

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Nanocarriers have the utmost significance for advancements in drug delivery and nanomedicine technology. They are classified as polymer-based nanocarriers, lipid-based nanocarriers, viral nanoparticles, or inorganic nanoparticles, depending on their constituent parts. Lipid-based nanocarrier systems have gained tremendous attention over the years because of their noteworthy properties like high drug-loading capacity, lower toxicity, better bioavailability and biocompatibility, stability in the gastrointestinal tract, controlled release, simpler scale-up, and validation process. Nanocarriers still have some disadvantages like poor drug penetration, limited drug encapsulation, and poor targeting. These disadvantages can be overcome by their surface modification. Surface-modified nanocarriers result in controlled release, enhanced penetration efficiency, and targeted medication delivery. In this review, the authors summarize the numerous lipidbased nanocarriers and their functionalization through various surface modifiers such as polymers, ligands, surfactants, and fatty acids. Recent examples of newly developing surface-modified lipid-based nanocarrier systems from the available literature, along with their applications, have been compiled in this work.

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Section: Surface Modifiers Utilized For Surface Modification Of Lipid...mentioning

confidence: 99%

Surface Modification of Lipid-Based Nanocarriers: A Potential Approach to Enhance Targeted Drug Delivery

2022

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“…In their review of relevant strategies to functionalize lipid-based nanocarriers, Guyon et al mentioned four methods: (i) the direct ligand conjugation on preformed nanocarriers, (ii) the post-insertion of PEG-ligand on preformed nanocarriers, (iii) the incorporation of PEG-ligand during the formulation process and (iv) the noncovalent adsorption of the ligand at the surface of nanocarriers [23]. This last method has already demonstrated its advantages with good adsorption efficiency and preservation of peptide activity [73].…”

Section: Peptide-22 Adsorption On Tg-nesmentioning

confidence: 99%

“…Isothermal titration calorimetry (ITC) assays have been carried out to objectify and further characterize the peptide-22/Tg-NEs interactions. Indeed, this label-free and sensitive technique, which is based on heat measurement absorbed or generated during binding event in a titrating manner, appears as a method of choice to provide a complete thermodynamic profile of such biomolecule-nanocarrier interactions [23,74,75]. To ensure small background heats of dilution that would affect binding measurements, the native Tg-NEs formulation was placed into the sample cell, and titration by peptide-22 up to a final concentration of 6 mg/mL was performed.…”

Section: Peptide-22 Adsorption On Tg-nesmentioning

confidence: 99%

“…Moreover, to ensure the best delivery to the new target, e.g., a limited peripheral distribution when a central drug accumulation is required in central nervous system (CNS)-pathologies treatment, functionalized drug-loaded nanocarriers can be developed. Indeed, thanks to their functionalization with targeting ligands, the nanocarriers become able to overcome some physiological barriers and to increase drug delivery into target tissues to treat without causing damage to healthy tissues [23].…”

Section: Introductionmentioning

confidence: 99%

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Active Targeted Nanoemulsions for Repurposing of Tegaserod in Alzheimer’s Disease Treatment

et al. 2021

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Background and Purpose: The activation of 5-HT4 receptors with agonists has emerged as a valuable therapeutic strategy to treat Alzheimer’s disease (AD) by enhancing the nonamyloidogenic pathway. Here, the potential therapeutic effects of tegaserod, an effective agent for irritable bowel syndrome, were assessed for AD treatment. To envisage its efficient repurposing, tegaserod-loaded nanoemulsions were developed and functionalized by a blood–brain barrier shuttle peptide. Results: The butyrylcholinesterase inhibitory activity of tegaserod and its neuroprotective cellular effects were highlighted, confirming the interest of this pleiotropic drug for AD treatment. In regard to its drugability profile, and in order to limit its peripheral distribution after IV administration, its encapsulation into monodisperse lipid nanoemulsions (Tg-NEs) of about 50 nm, and with neutral zeta potential characteristics, was performed. The stability of the formulation in stock conditions at 4 °C and in blood biomimetic medium was established. The adsorption on Tg-NEs of peptide-22 was realized. The functionalized NEs were characterized by chromatographic methods (SEC and C18/HPLC) and isothermal titration calorimetry, attesting the efficiency of the adsorption. From in vitro assays, these nanocarriers appeared suitable for enabling tegaserod controlled release without hemolytic properties. Conclusion: The developed peptide-22 functionalized Tg-NEs appear as a valuable tool to allow exploration of the repurposed tegaserod in AD treatment in further preclinical studies.

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“…Liposomes are small bilayer vesicles of typically 100–400 nm in size that are formed from phospholipids. − Liposomes are commonly used to encapsulate small molecules within their hydrophilic interior core for biomedical applications such as the transport of small molecule drugs in vivo. , Liposomes have biodistribution profiles that are distinct from those of small molecules and thus may improve the pharmacokinetic profile of the drug . For example, liposomes, as examples of nanoparticles, accumulate in tumors by the enhanced permeability retention effect .…”

Section: Introductionmentioning

confidence: 99%

Liposomal Fe(III) Macrocyclic Complexes with Hydroxypropyl Pendants as MRI Probes

Abozeid

Chowdhury

Asik

et al. 2021

ACS Appl. Bio Mater.

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Paramagnetic liposomes containing Fe(III) complexes were prepared by incorporation of mononuclear (Fe(L1) or Fe(L3)) or dinuclear (Fe2(L2)) coordination complexes of 1,4,7-triazacyclononane macrocycles containing 2-hydroxypropyl pendant groups. Two different types of paramagnetic liposomes were prepared. The first type, LipoA, has the mononuclear Fe(L1) complex loaded into the internal aqueous core. The second type, LipoB, has the amphiphilic Fe(L3) complex inserted into the liposomal bilayer and the internal aqueous core loaded with either Fe(L1) (LipoB1) or Fe2(L2) (LipoB2). LipoA enhances both T1 and T2 water proton relaxation rates. Treatment of LipoA with osmotic gradients to produce a nonspherical liposome produces a liposome with a chemical exchange saturation transfer effect as shown by an asymmetry analysis but only at high osmolarity. LipoB1, which contains an amphiphilic complex in the liposomal bilayer, produced a broadened Z-spectrum upon treatment of the liposome with osmotic gradients. The r 1 relaxivity of LipoB1 and LipoB2 were higher than the r 1 relaxivity of LipoA on a per Fe basis, suggesting an important contribution from the amphiphilic Fe(III) center. The r 1 relaxivities of paramagnetic liposomes are relatively constant over a range of magnetic field strengths (1.4–9.4 T), with the ratio of r 2/r 1 substantially increasing at high field strengths. MRI studies of LipoB1 in mice showed prolonged contrast enhancement in blood compared to the clinically employed Gd(DOTA), which was injected at a 2-fold higher dose per metal than the Fe(III)-loaded liposomes.

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Relevant Physicochemical Methods to Functionalize, Purify, and Characterize Surface-Decorated Lipid-Based Nanocarriers

Cited by 13 publications

References 121 publications

Surface Modification of Lipid-Based Nanocarriers: A Potential Approach to Enhance Targeted Drug Delivery

Surface Modification of Lipid-Based Nanocarriers: A Potential Approach to Enhance Targeted Drug Delivery

Active Targeted Nanoemulsions for Repurposing of Tegaserod in Alzheimer’s Disease Treatment

Liposomal Fe(III) Macrocyclic Complexes with Hydroxypropyl Pendants as MRI Probes

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