Stability, liposome interaction, and in vivo pharmacology of ghrelin in liposomal suspensions

Moeller, Eva Horn; Holst, Birgitte; Nielsen, Line Hagner; Pedersen, Pia Steen; Østergaard, Jesper

doi:10.1016/j.ijpharm.2009.05.067

Cited by 30 publications

(13 citation statements)

References 45 publications

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“…By contrast, PC and SM formulation exhibited much lower entrapment efficiency (PC, 45.07±0.78%; SM, 50.03±7.55%), which were significantly lower than those of the SP, MPPC and DPPC formulations. These results were consistent with a previous report, in which there were markedly different interactions among peptides and various types of charged liposome (27). Therefore, the SP formulation was chosen to further optimize the entrapment conditions for producing liposomal ACEI peptides because of its higher efficiency and lower cost.…”

Section: Resultssupporting

confidence: 90%

Preparation of liposome encapsulating angiotensin-I-converting enzyme inhibitory peptides from sunflower protein hydrolysates

Luo

2018

Mol Med Report

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Liposomal angiotensin-I-converting enzyme inhibitory (ACEI) peptides were prepared from sunflower protein hydrolysates by the thin‑film ultrasonic method. Response surface methodology (RSM), in combination with fractional factorial designs and central composite design methods were utilized to optimize entrapment efficiency and balance the drug release. We found that the ratio of phospholipids to cholesterol, ultrasound time and the ratio of phospholipids to ACEI peptides were significant factors affecting entrapment efficiency (P<0.001). Optimal preparation conditions of liposomal‑ACEI peptides were the ratio of soybean phospholipids to cholesterol (w/w) of 4.1:1, PEG‑2000 dosage (%) of 4, NaCl concentration in PBS (mM) of 50, hydration temperature of 45˚C, ultrasound time of 8.05 min and the ratio of soybean phospholipids to ACEI peptides of 15:1 (w/w). The experimental entrapment efficiency of liposomal‑ACEI peptides was (91.25±0.182%). Moreover, the balanced release rate of liposome encapsulated ACEI in phosphate buffer was 77.83% after 12 h.

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Section: Resultssupporting

confidence: 90%

Preparation of liposome encapsulating angiotensin-I-converting enzyme inhibitory peptides from sunflower protein hydrolysates

Luo

2018

Mol Med Report

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“…Indeed, the peptides described to be included in liposomes thus far are much longer (>20) compared to the ones (5–10 amino acids) used in the present study, e.g. appetite‐stimulating hormone ghrelin and peptidic antitumor agent Print 3G . In contrast, the incorporation of Ex527 using the ethanol injection method was highly efficient.…”

Section: Resultsmentioning

confidence: 80%

Novel Insights Into Appropriate Encapsulation Methods for Bioactive Compounds Into Polymers: A Study With Peptides and HDAC Inhibitors

et al. 2013

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The use of different nanoparticles (NPs) for successful encapsulation of bioactive substances is discussed. The inclusion efficiency into liposomes, acetalated dextran (Ac-Dex), and variants of poly[(lactic acid)-co-(glycolic acid)] (PLGA) NPs is analyzed after chemical degradation. Efficient inclusion of SIRT1 inhibitor Ex527 in liposomes, Ac-Dex- and PLGA-NPs is observed for all procedures used. Activity of Ex527 is demonstrated by monitoring the acetylation status of SIRT1-target p53. In contrast, small peptides are only incorporated into acid-terminated PLGA-NPs and marginally into Ac-Dex-NPs. The yield depends on peptide sequence and terminal modifications. Activity is exemplified for angiotensin II using the dynamic mass redistribution technology.

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“…To our knowledge, only a limited number of studies have focused on the development of formulations containing Ghrl, and these were intended for parenteral administration. 14 The intravenous route, which is rather cumbersome for chronic administration, 15 has been the most exploited for Ghrl administration, 16 while intranasal delivery has been considered very rarely. A recently published study was focused on the nasal administration of a vaccine containing Ghrl-antigen for the management of obesity, but this was not intended for nose-brain delivery.…”

Section: Introductionmentioning

confidence: 99%

Development of coated liposomes loaded with ghrelin for nose-to-brain delivery for the treatment of cachexia

Salade¹,

Wauthoz²,

Deleu³

et al. 2017

IJN

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The aim of the present study was to develop a ghrelin-containing formulation based on liposomes coated with chitosan intended for nose–brain delivery for the treatment of cachexia. Among the three types of liposomes developed, anionic liposomes provided the best results in terms of encapsulation efficiency (56%) and enzymatic protection against trypsin (20.6% vs 0% for ghrelin alone) and carboxylesterase (81.6% vs 17.2% for ghrelin alone). Ghrelin presented both electrostatic and hydrophobic interactions with the anionic lipid bilayer, as demonstrated by isothermal titration calorimetry. Then, anionic liposomes were coated with N -(2-hydroxy) propyl-3-trimethyl ammonium chitosan chloride. The coating involved a size increment from 146.9±2.7 to 194±6.1 nm, for uncoated and coated liposomes, respectively. The ζ-potential was similarly increased from -0.3±1.2 mV to 6±0.4 mV before and after coating, respectively. Chitosan provided mucoadhesion, with an increase in mucin adsorption of 22.9%. Enhancement of permeation through the Calu3 epithelial monolayer was also observed with 10.8% of ghrelin recovered in the basal compartment in comparison to 0% for ghrelin alone. Finally, aerosols generated from two nasal devices (VP3 and SP270) intended for aqueous dispersion were characterized with either coated or uncoated liposomes. Contrarily to the SP270 device, VP3 device showed minor changes between coated and uncoated liposome aerosols, as shown by their median volume diameters of 38.4±5.76 and 37.6±5.74 µm, respectively. Overall, the results obtained in this study show that the developed formulation delivered by the VP3 device can be considered as a potential candidate for nose–brain delivery of ghrelin.

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Stability, liposome interaction, and in vivo pharmacology of ghrelin in liposomal suspensions

Cited by 30 publications

References 45 publications

Preparation of liposome encapsulating angiotensin-I-converting enzyme inhibitory peptides from sunflower protein hydrolysates

Preparation of liposome encapsulating angiotensin-I-converting enzyme inhibitory peptides from sunflower protein hydrolysates

Novel Insights Into Appropriate Encapsulation Methods for Bioactive Compounds Into Polymers: A Study With Peptides and HDAC Inhibitors

Development of coated liposomes loaded with ghrelin for nose-to-brain delivery for the treatment of cachexia

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