Melatonin-loaded lecithin/chitosan nanoparticles: Physicochemical characterisation and permeability through Caco-2 cell monolayers

Hafner, Anita; Lovrić, Jasmina; Voinovich, Dario; Filipović-Grčić, Jelena

doi:10.1016/j.ijpharm.2009.07.001

Cited by 100 publications

(62 citation statements)

References 36 publications

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“…There is a significant (P < 0.05), although slight, decrease in the zeta potential of CRG/AP nanoparticles at the beginning of the assay from +65 mV to +56 mV, but this did not induce any effect on nanoparticle size, as the zeta potential remains sufficiently high to induce repulsion of nanoparticles. Chitosan-based nanoparticles have been reported to exhibit physicochemical stability in similar time intervals (Hafner et al, 2009;Morris et al, 2011;Rodrigues et al, 2012b). No similar studies are reported for pullulan-based nanoparticles, thus not allowing a direct comparison.…”

Section: Nanoparticle Stability In Storage and Upon Freeze-dryingmentioning

confidence: 99%

Pullulan-based nanoparticles as carriers for transmucosal protein delivery

Dionísio

Cordeiro

Remuñán‐López

et al. 2013

European Journal of Pharmaceutical Sciences

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Polymeric nanoparticles have revealed very effective in transmucosal delivery of proteins. Polysaccharides are among the most used materials for the production of these carriers, owing to their structural flexibility and propensity to evidence biocompatibility and biodegradability. In parallel, there is a preference for the use of mild methods for their production, in order to prevent protein degradation, ensure lower costs and easier procedures that enable scaling up.In this work we propose the production of pullulan-based nanoparticles by a mild method of polyelectrolyte complexation. As pullulan is a neutral polysaccharide, sulfated and aminated derivatives of the polymer were synthesized to provide pullulan with a charge. These derivatives were then complexed with chitosan and carrageenan, respectively, to produce the nanocarriers. Positively charged nanoparticles of 180-270 nm were obtained, evidencing ability to associate bovine serum albumin, which was selected as model protein. In PBS pH 7.4, pullulan-based nanoparticles were found to have a burst release of 30% of the protein, which maintained up to 24h. Nanoparticle size and zeta potential were preserved upon freeze-drying in the presence of appropriate cryoprotectants. A factorial design was approached to assess the cytotoxicity of raw materials and nanoparticles by the metabolic test MTT. Nanoparticles demonstrated to not cause overt toxicity in a respiratory cell model (Calu-3). Pullulan has, thus, demonstrated to hold potential for the production of nanoparticles with an application in protein delivery.

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Section: Nanoparticle Stability In Storage and Upon Freeze-dryingmentioning

confidence: 99%

Pullulan-based nanoparticles as carriers for transmucosal protein delivery

Dionísio

Cordeiro

Remuñán‐López

et al. 2013

European Journal of Pharmaceutical Sciences

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“…15 Through self-association, negatively charged phospholipids and positively charged chitosan formed stiff and stable nanostructures, which demonstrated good biocompatibility and biodegradability, excellent mucosal adhesiveness, and minimal cytotoxicity. 16,17 This novel delivery system improved the bioavailability of model drugs and prolonged their retention times in the body. Several recent studies have investigated the efficiency of this novel nanocarrier in delivering various model drugs via different routes, including oral and transmucosal administration.…”

Section: Introductionmentioning

confidence: 99%

Self-assembled lecithin/chitosan nanoparticles for oral insulin delivery: preparation and functional evaluation

Liu¹,

Zhou²,

Xia³

et al. 2016

IJN

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Purpose Here, we investigated the formation and functional properties of self-assembled lecithin/chitosan nanoparticles (L/C NPs) loaded with insulin following insulin–phospholipid complex preparation, with the aim of developing a method for oral insulin delivery. Methods Using a modified solvent-injection method, insulin-loaded L/C NPs were obtained by combining insulin–phospholipid complexes with L/C NPs. The nanoparticle size distribution was determined by dynamic light scattering, and morphologies were analyzed by cryogenic transmission electron microscopy. Fourier transform infrared spectroscopy analysis was used to disclose the molecular mechanism of prepared insulin-loaded L/C NPs. Fast ultrafiltration and a reversed-phase high-performance liquid chromatography assay were used to separate free insulin from insulin entrapped in the L/C NPs, as well as to measure the insulin-entrapment and drug-loading efficiencies. The in vitro release profile was obtained, and in vivo hypoglycemic effects were evaluated in streptozotocin-induced diabetic rats. Results Our results indicated that insulin-containing L/C NPs had a mean size of 180 nm, an insulin-entrapment efficiency of 94%, and an insulin-loading efficiency of 4.5%. Cryogenic transmission electron microscopy observations of insulin-loaded L/C NPs revealed multilamellar structures with a hollow core, encircled by several bilayers. In vitro analysis revealed that insulin release from L/C NPs depended on the L/C ratio. Insulin-loaded L/C NPs orally administered to streptozotocin-induced diabetic rats exerted a significant hypoglycemic effect. The relative pharmacological bioavailability following oral administration of L/C NPs was 6.01%. Conclusion With the aid of phospholipid-complexation techniques, some hydrophilic peptides, such as insulin, can be successfully entrapped into L/C NPs, which could improve oral bioavailability, time-dependent release, and therapeutic activity.

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“…In the development of nanotherapeutics, nanotechnology tools are used to improve drug solubility (eg, micelles 7 and nanocrystals 8 ), to guide drugs to the desired location of action with increased precision (ie, drug targeting 9,10 ), to control the drug's release (eg, nanoparticles 11 and liposomes 12 ), and/or to enhance the transport across biological barriers (eg, micelles 13 and nanoparticles 14 ). The main goal is to improve drug bioavailability, pharmacokinetics, efficacy, and safety to promote the treatment of diseases which currently cannot be achieved with conventional dosage forms.…”

Section: Introductionmentioning

confidence: 99%

Nanotherapeutics in the EU: an overview on current state and future directions

Hafner¹,

Lovrić²,

Lakoš³

et al. 2014

IJN

Self Cite

108

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The application of nanotechnology in areas of drug delivery and therapy (ie, nanotherapeutics) is envisioned to have a great impact on public health. The ability of nanotherapeutics to provide targeted drug delivery, improve drug solubility, extend drug half-life, improve a drug’s therapeutic index, and reduce a drug’s immunogenicity has resulted in the potential to revolutionize the treatment of many diseases. In this paper, we review the liposome-, nanocrystal-, virosome-, polymer therapeutic-, nanoemulsion-, and nanoparticle-based approaches to nanotherapeutics, which represent the most successful and commercialized categories within the field of nanomedicine. We discuss the regulatory pathway and initiatives endeavoring to ensure the safe and timely clinical translation of emerging nanotherapeutics and realization of health care benefits. Emerging trends are expected to confirm that this nano-concept can exert a macro-impact on patient benefits, treatment options, and the EU economy.

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Melatonin-loaded lecithin/chitosan nanoparticles: Physicochemical characterisation and permeability through Caco-2 cell monolayers

Cited by 100 publications

References 36 publications

Pullulan-based nanoparticles as carriers for transmucosal protein delivery

Pullulan-based nanoparticles as carriers for transmucosal protein delivery

Self-assembled lecithin/chitosan nanoparticles for oral insulin delivery: preparation and functional evaluation

Nanotherapeutics in the EU: an overview on current state and future directions

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