Modern lipid‐, carbohydrate‐, and peptide‐based delivery systems for peptide, vaccine, and gene products

Simerská, Pavla; Moyle, Peter M.; Tóth, István

doi:10.1002/med.20191

Cited by 52 publications

(42 citation statements)

References 172 publications

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“…In the delivery of bioactive compounds, a balance between lipophilic and hydrophilic characters must be considered, and liposaccharide-based delivery systems can be used to address this problem (13). Glycosylation of peptides may also confer many other advantages, including enhanced physicochemical properties, stability, permeability and targeting (18). The use of both lipids and carbohydrates in one delivery system affords the benefits of both approaches by enhancing the bioavailability of peptides (13).…”

Section: Introductionmentioning

confidence: 98%

Stability, Permeability and Growth-Inhibitory Properties of Gonadotropin-Releasing Hormone Liposaccharides

et al. 2014

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Section: Introductionmentioning

confidence: 98%

Stability, Permeability and Growth-Inhibitory Properties of Gonadotropin-Releasing Hormone Liposaccharides

et al. 2014

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“…Modification of therapeutic peptides by substitution of D-isoform of amino acids is known to be the effective strategy to improve their pharmacological properties and metabolic stability (Seitz, 2000;Werle and Bernkop-Schnürch, 2006). Glycosylation is another useful approach to improve the metabolic stability of peptides in physiological environments and increase their biological activity (Simerska et al, 2009;Ueda et al, 2009). …”

Section: Discussionmentioning

confidence: 99%

In vivo pharmacological evaluation of a lactose-conjugated luteinizing hormone releasing hormone analogue

Moradi

Varamini

Steyn

et al. 2015

International Journal of Pharmaceutics

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Abstract:In the current study, the efficacy and pharmacokinetic profile of lactose-conjugated luteinizing hormone releasing hormone (LHRH) was examined following oral administration in male rats. A rapid and sensitive liquid chromatography/mass spectrometry technique was developed and applied for measuring the concentration of lactose[Q 1 ][w 6 ]LHRH (compound 1) in rat plasma in order to allow measurement of pharmacokinetic parameters. LH release was evaluated using a sandwich ELISA. Maximum serum concentration (Cmax= 0.11 µg/ml) was reached at 2 h (Tmax) following oral administration of the compound at 10 mg/kg. The half-life was determined to be 2.6 h. The absolute bioavailability of the orally administered compound was found to be 14%, which was a remarkable improvement compared to zero-tolow oral bioavailability of the native peptide. Compound 1 was effective in stimulating LH release at 20 mg/kg after oral administration. The method was validated at a linear range of 0.01-20.0 µg/ml and a correlation coefficient of r 2 ≥0.999. The accuracy and precision values showed the reliability and reproducibility of the method for evaluation of the pharmacokinetic parameters. These findings showed that the lactose derivative of LHRH has a therapeutic potential to be further developed as an orally active therapeutics for the treatment of hormone-dependent diseases.

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“…Purified, fully characterized synthetic peptides can be produced using modern solid phase peptide synthesis (SPPS). However, peptides alone are poorly immunogenic and need a strong adjuvant (immunostimulant) to elicit the desired immune response [2][3][4]. Many adjuvants are poorly characterized complex mixtures derived from bacteria.…”

Section: Introductionmentioning

confidence: 99%

pH-triggered peptide self-assembly into fibrils: a potential peptide-based subunit vaccine delivery platform

Skwarczynski¹,

Kowapradit²,

Ziora³

et al. 2013

Bio Chem Comp

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Background: Peptide-based subunit vaccines require strong adjuvants (immunostimulant) for therapeutic potency. There is strong demand for the discovery of new safe adjuvants and vaccine delivery systems that can be produced in a highly controlled manner. The pH dependent self-assembly of isopeptide derivatives into fibrils has been reported. Appropriately designed fibrils may have adjuvanting potency. Methods: Isopeptides conjugated to B-cell peptide epitopes (antigens) were synthesized. Properties of the resultant conjugates and their ability to undergo O-N intramolecular acyl migration reaction were analysed by HPLC, circular dichroism, and transmission electron microscopy. Results: The conjugates were converted to "parent" peptides via the pH-triggered O-N acyl migration reaction. The parent peptides aggregated into fibrils. The differences in conjugates composition resulted in different fibril morphology. Aggregation of produced peptides induced desired secondary conformation of antigens (peptide epitopes). Conclusions:The isopeptide approach presented herein may serve as a new self-adjuvanting delivery system for peptide-based vaccines. Such vaccines could be stable when stored in a non-aggregative form, and then converted on demand to the active form in pH-controlled manner. The use of a vaccine that is solely composed of endogenous components may reduce vaccine-associated side effects.

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Modern lipid‐, carbohydrate‐, and peptide‐based delivery systems for peptide, vaccine, and gene products

Cited by 52 publications

References 172 publications

Stability, Permeability and Growth-Inhibitory Properties of Gonadotropin-Releasing Hormone Liposaccharides

Stability, Permeability and Growth-Inhibitory Properties of Gonadotropin-Releasing Hormone Liposaccharides

In vivo pharmacological evaluation of a lactose-conjugated luteinizing hormone releasing hormone analogue

pH-triggered peptide self-assembly into fibrils: a potential peptide-based subunit vaccine delivery platform

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