Transfer and exchange of phospholipid between small unilamellar liposomes and rat plasma high density lipoproteins Dependence on cholesterol content and phospholipid composition

Damen, J.J.M.; Regts, Joke; Scherphof, Gerrit L.

doi:10.1016/0005-2760(81)90268-x

Cited by 145 publications

(59 citation statements)

References 34 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…However, it was obvious that cationic-liposomes containing DOPE were not only transfer into the hair follicles but penetrate through the skin surface. It has been reported that Chol stabilizes liposomal membranes (Damen et al, 1981;Kirby et al, 1980), whereas DOPE, a fusogenic lipid, destabilizes the lipid bilayers by promoting transition from a lamellar to a hexagonal II phase (Guo and Szoka, 2001). As shown in Table I, although the physical characteristics (size, ζ-potential and polydispersity) of cationic liposomes consisted of DOTAP/EPC = 1:1 and DOTAP/EPC/DOPE = 2:1:1 were very similar, the distribution of lipid marker in the skin after iontophoresis was entirely different (Fig.…”

Section: Discussionmentioning

confidence: 99%

Noninvasive and persistent transfollicular drug delivery system using a combination of liposomes and iontophoresis

Kajimoto

Yamamoto

Watanabe

et al. 2011

International Journal of Pharmaceutics

View full text Add to dashboard Cite

Iontophoresis is a promising technique for enhancing transdermal administration of charged drugs. However, conventional iontophoresis is not sufficient for effective delivery of large, hydrophilic, or electrically neutral molecules. In this study, we utilized charged liposomes as carriers, focused on a transfollicular route for delivery of the liposomes, and optimized iontophoretic conditions and lipid composition for this method in both in vitro and in vivo conditions.As a result, we identified the optimum condition (lipid composition:DOTAP/EPC/Chol=2:2:1, current supply: 0.45 mA/cm 2 , duration: 1 hr) for effective iontophoretic delivery of aqueous solution, which can not be transferred into the skin without charged liposomes. We also examined the pharmacological effects of iontophoresis of liposomes encapsulating insulin (INS-lipo) using a rat model of type I diabetes. Interestingly, iontophoresis of INS-lipo onto a diabetes rat skin resulted in a gradual decrease in blood glucose levels, with levels reaching 20% of initial values at 18 hr after administration. These lower blood glucose levels were maintained for up to 24 hr. Significant amount of insulin were also detected in plasma 18 hr after iontophoresis of INS-lipo. We succeeded in developing a non-invasive and persistent transfollicular drug delivery system that used a combination of liposomes and iontophoresis.

show abstract

Section: Discussionmentioning

confidence: 99%

Noninvasive and persistent transfollicular drug delivery system using a combination of liposomes and iontophoresis

Kajimoto

Yamamoto

Watanabe

et al. 2011

International Journal of Pharmaceutics

View full text Add to dashboard Cite

show abstract

“…The decrease in the rate of cholesterol transfer at higher cholesterol contents might have been caused by decreased fluidity of the lipid interface, as was attributed to a decline in PC transfer with an increase in the cholesterol content of vesicles (29,30). Incorporation of cholesterol into egg PC vesicles is well known to transform the disordered bilayer into an ordered structure (34,35).…”

Section: Discussionmentioning

confidence: 99%

Phospholipid Transfer Protein Mediates Transfer of not Only Phosphatidylcholine but Also Cholesterol from Phosphatidylcholine-Cholesterol Vesicles to High Density Lipoproteins

Nishida

1997

Journal of Biological Chemistry

View full text Add to dashboard Cite

Phospholipid transfer protein (PLTP) purified from human plasma was found to enhance the transfer of cholesterol from single bilayer vesicles containing phosphatidylcholine and cholesterol to high density lipoprotein-3. The rate of cholesterol transfer was greatly influenced by the cholesterol content of the donor vesicles. The maximal rate was observed with the vesicles containing 20 -25 mol % cholesterol. This was in contrast to a progressive decline in the rate of phosphatidylcholine transfer with an increase in the cholesterol content. To determine the binding of cholesterol and phosphatidylcholine to PLTP, the mixtures of PLTP and the vesicles containing 3 H-labeled phosphatidylcholine and 14 C-labeled cholesterol were incubated and subjected to sucrose density gradient centrifugation. Determination of the label profiles showed that cholesterol as well as phosphatidylcholine were transferred from the vesicles to PLTP. The reversible nature of the binding was shown by the transfer of labeled cholesterol and phosphatidylcholine bound to PLTP to the acceptor vesicles or low density lipoprotein. Isothermal equilibrium binding of PLTP for cholesterol and phosphatidylcholine showed that PLTP possessed a considerably higher affinity and binding capacity for phosphatidylcholine than for cholesterol. The phosphatidylcholine binding affinity and capacity were greater when PLTP was incubated with phosphatidylcholine vesicles without cholesterol. A possible importance of PLTP-mediated cholesterol transfer in the circulation was described.

show abstract

“…Unsaturated phospholipids, like DOPE, fluidize the liposome membrane thereby increasing the membrane permeability at physiological temperature due to their low gel-to-liquid-crystalline phase transition temperature (T c ) (Demel et al, 1976). Previous studies have shown that addition of cholesterol to liposomes rigidifies the bilayer and reduces leakage of entrapped material at temperatures above the T c of the membrane (Gregoriadis, 1988;Damen et al, 1981;Ishida et al, 2006).…”

Section: Effect Of Lipid Composition On Dxr Blood Pharmacokinetics Ofmentioning

confidence: 99%

Sonosensitive dioleoylphosphatidylethanolamine-containing liposomes with prolonged blood circulation time of doxorubicin

Evjen¹,

Hagtvet

Nilssen³

et al. 2011

European Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

Ultrasound sensitive (sonosensitive liposomes) are drug delivery systems designed for releasing their drug load upon exposure to ultrasound (US). Inclusion of dioleoylphosphatidylethanolamine (DOPE) in liposome membranes was previously shown to induce sonosensitivity. For efficient US mediated drug delivery to solid tumours, a long blood circulation time of the liposomal drug providing high tumour uptake is required. In this study, blood pharmacokinetics of DOPE-based liposomal doxorubicin (DXR) were evaluated in mice. A markedly faster blood clearance of DXR was observed for DOPE-rich liposomes compared to Caelyx! (standard liposomal DXR). Subsequently, liposome membrane composition was altered to improve drug retention in the bloodstream, while maintaining sonosensitivity. Formulations with reduced blood clearance of DXR were obtained by reducing the content of DOPE from 62 to 32 or 25 mol%. These formulations showed long blood circulation time, as approximately 20% of the administered DXR dose was present in the bloodstream 24 h after intravenous injection. The reduction in liposomal DOPE content did not significantly reduce US mediated DXR release in vitro, indicating that DOPE is a potent modulator to sonosensitivity. The novel liposome formulations, containing moderate amounts of DOPE, displayed similar blood pharmacokinetic profiles as standard liposomal DXR, but a markedly improved sonosensitivity.

show abstract

Transfer and exchange of phospholipid between small unilamellar liposomes and rat plasma high density lipoproteins Dependence on cholesterol content and phospholipid composition

Cited by 145 publications

References 34 publications

Noninvasive and persistent transfollicular drug delivery system using a combination of liposomes and iontophoresis

Noninvasive and persistent transfollicular drug delivery system using a combination of liposomes and iontophoresis

Phospholipid Transfer Protein Mediates Transfer of not Only Phosphatidylcholine but Also Cholesterol from Phosphatidylcholine-Cholesterol Vesicles to High Density Lipoproteins

Sonosensitive dioleoylphosphatidylethanolamine-containing liposomes with prolonged blood circulation time of doxorubicin

Contact Info

Product

Resources

About