Glycerosomes: Use of hydrogenated soy phosphatidylcholine mixture and its effect on vesicle features and diclofenac skin penetration

Manca, Maria Letizia; Cencetti, Claudia; Matricardi, Pietro; Castangia, Inés; Zaru, Marco; Sales, Octavio Diez; Nácher, Amparo; Valenti, Donatella; Maccioni, Anna Maria; Fadda, Anna Maria; Manconi, Maria

doi:10.1016/j.ijpharm.2016.07.009

Cited by 67 publications

(56 citation statements)

References 23 publications

(35 reference statements)

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“…224 However, non-traditional routes of EV administration, such as orally administered EVs have shown uptake via the intestinal mucosal surface and subsequent accumulation in the liver and spleen. 225 Irrespective of administration route, a key outcome measure is biodistribution, to trace where exogenously applied EVs go after they have been introduced into an animal.…”

Section: In Vivo Studies Of Ev-functionmentioning

confidence: 99%

Technical challenges of working with extracellular vesicles

et al. 2018

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Extracellular Vesicles (EVs) are gaining interest as central players in liquid biopsies, with potential applications in diagnosis, prognosis and therapeutic guidance in most pathological conditions. These nanosized particles transmit signals determined by their protein, lipid, nucleic acid and sugar content, and the unique molecular pattern of EVs dictates the type of signal to be transmitted to recipient cells. However, their small sizes and the limited quantities that can usually be obtained from patient-derived samples pose a number of challenges to their isolation, study and characterization. These challenges and some possible options to overcome them are discussed in this review.

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Section: In Vivo Studies Of Ev-functionmentioning

confidence: 99%

Technical challenges of working with extracellular vesicles

et al. 2018

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“…18,19 Glycerol is a harmless and fully acceptable short-chain alcohol that can improve the fluidity and deformability of the liposomal bilayer, thus improving the ability of preparations to penetrate through the skin. Furthermore, transdermal drug delivery efficiency can be improved by using penetration enhancers that can reversibly decrease barrier resistance.…”

Section: Introductionmentioning

confidence: 99%

Essential oil-mediated glycerosomes increase transdermal paeoniflorin delivery: optimization, characterization, and evaluation in vitro and in vivo

Zhang

et al. 2017

IJN

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In this study, a novel glycerosome carrier containing essential oils was prepared for topical administration of paeoniflorin (PF) to enhance its transdermal drug delivery and improve drug absorption in the synovium. The formulation of glycerosomes was optimized by a uniform design, and the final vehicle was composed of 5% (w/v) phospholipid, 0.6% (w/v) cholesterol, and 10% (v/v) glycerol, with 2% (v/v) Speranskia tuberculata essential oil (STO) as the transdermal enhancer. The in vitro transdermal flux of PF loaded in the STO-glycerosomes was 1.4-fold, 1.6-fold, and 1.7-fold higher than those of glycerosomes, liposomes, and tinctures, respectively. In vivo studies showed that the use of STO-glycerosomes was associated with a 3.1-fold greater accumulation of PF in the synovium than that of common glycerosomes. This finding was confirmed by in vivo imaging studies, which found that the fluorescence intensity of Cy5.5-loaded STO-glycerosomes in mice knee joints was 1.8-fold higher than that of the common glycerosomes 5 h after administration. The glycerosomes mediated by STO exhibited considerable skin permeability as well as improved drug absorption in the synovium, indicating that STO-glycerosomes may be a potential PF transdermal delivery vehicle for the treatment of rheumatoid arthritis caused by synovium lesions.

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“…Liposome combined with highly concentrated glycerol, known as glycerosome, was used as the drug delivery system. The glycerosome membrane has high fluidity and stability ( Manca et al, 2016 ). High fluidity and stability might stabilize GPCR function, as glycerol induced a dose-dependent increase in size stability of the HRH1 proteoglycerosomes ( Table 1 ).…”

Section: Discussionmentioning

confidence: 99%

“…Therefore, it is important to confirm whether the method of using a wheat germ cell-free protein synthesis system combined with liposomes can provide other functional GPCRs. To achieve increased efficiency in GPCR synthesis, liposome conditions have been shown to be optimized, when compared with previous methods, by using glycerosomes ( Manca et al, 2013 , 2016 ; Taladrid et al, 2017 ). Glycerosomes contain a high concentration of glycerol in liposome membranes, providing a new drug delivery system, and they have a high stability and a high fluidity ( Manca et al, 2013 , 2016 ; Taladrid et al, 2017 ).…”

Section: Introductionmentioning

confidence: 99%

Functional G-Protein-Coupled Receptor (GPCR) Synthesis: The Pharmacological Analysis of Human Histamine H1 Receptor (HRH1) Synthesized by a Wheat Germ Cell-Free Protein Synthesis System Combined with Asolectin Glycerosomes

et al. 2018

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G-protein-coupled receptors (GPCRs) are membrane proteins distributed on the cell surface, and they may be potential drug targets. However, synthesizing GPCRs in vitro can be challenging. Recently, some cell-free protein synthesis systems have been shown to produce a large amount of membrane protein combined with chemical chaperones that include liposomes and glycerol. Liposomes containing high concentrations of glycerol are known as glycerosomes, which are used in new drug delivery systems. Glycerosomes have greater morphological stability than liposomes. Proteoglycerosomes are defined as glycerosomes that contain membrane proteins. Human histamine H1 receptor (HRH1) is one of the most studied GPCRs. In this study, we synthesized wild-type HRH1 (WT-HRH1) proteoglycerosomes and D107A-HRH1, (in which Asp107 was replaced by Ala) in a wheat germ cell-free protein synthesis system combined with asolectin glycerosomes. The mutant HRH1 has been reported to have low affinity for the H1 antagonist. In this study, the amount of synthesized WT-HRH1 in one synthesis reaction was 434 ± 66.6 μg (7.75 ± 1.19 × 103pmol). The specific binding of [3H]pyrilamine to the WT-HRH1 proteoglycerosomes became saturated as the concentration of the radioligand increased. The dissociation constant (Kd) and maximum density (Bmax) of the synthesized WT-HRH1 were 9.76 ± 1.25 nM and 21.4 ± 0.936 pmol/mg protein, respectively. However, specific binding to D107A-HRH1 was reduced compared with WT-HRH1 and the binding did not become saturated. The findings of this study highlight that HRH1 synthesized using a wheat germ cell-free protein synthesis system combined with glycerosomes has the ability to bind to H1 antagonists.

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Glycerosomes: Use of hydrogenated soy phosphatidylcholine mixture and its effect on vesicle features and diclofenac skin penetration

Cited by 67 publications

References 23 publications

Technical challenges of working with extracellular vesicles

Technical challenges of working with extracellular vesicles

Essential oil-mediated glycerosomes increase transdermal paeoniflorin delivery: optimization, characterization, and evaluation in vitro and in vivo

Functional G-Protein-Coupled Receptor (GPCR) Synthesis: The Pharmacological Analysis of Human Histamine H1 Receptor (HRH1) Synthesized by a Wheat Germ Cell-Free Protein Synthesis System Combined with Asolectin Glycerosomes

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