Integrity of liposomes in presence of cyclodextrins: effect of liposome type and lipid composition.
Liposome stability during incubation in presence of cyclodextrins (CDs) is studied. Dried-rehydrated vesicle (DRV), multilamellar vesicle (MLV) and small unilamellar vesicle (SUV) calcein-encapsulating liposomes, composed of different lipids are formulated, and retention of calcein is followed during vesicle incubation in hydroxypropyl-beta-CD (HP beta-CD), HP gamma-CD or methyl-beta-CD (Me beta-CD), for 24h. Results demonstrate that liposome integrity in cyclodextrins is affected by lipid composition and type. For the same lipid composition calcein release from vesicles is faster in the order: MLV > DRV > SUV. Me beta-CD influences liposome stability most, compared to the other CD's studied. Vesicles composed of saturated phospholipids were found more stable compared to phosphatidyl-choline (PC) liposomes, suggesting that phospholipid saturation and membrane rigidity influences the interaction between liposomal-lipids and CD molecules. Chol (cholesterol) addition in lipid membrane improves PC-liposome integrity, but has opposite or no effect on liposomes consisting of saturated lipids. Decrease of vesicle dispersion turbidity and size distribution in presence of CD, implies that Me beta-CD induces vesicle disruption and solubilization (to micelles). Turbidity measurements confirm that DRV liposomes are affected more than SUV.
Hatzi
Panayiota
P
Laboratory of Pharmaceutical Technology, Department of Pharmacy, School of Health Sciences, University of Patras, Rio 26500, Patras, Greece.
Mourtas
Spyridon
S
Klepetsanis
Pavlos G
PG
Antimisiaris
Sophia G
SG
D000073738:2-Hydroxypropyl-beta-cyclodextrin; D002626:Chemistry, Pharmaceutical; D002784:Cholesterol / Q000737:chemistry; D003505:Cyclodextrins / Q000737:chemistry*; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry*; D005452:Fluoresceins / Q000737:chemistry; D005456:Fluorescent Dyes / Q000737:chemistry; D008055:Lipids / Q000737:chemistry*; D008081:Liposomes; D008560:Membrane Fluidity; D036103:Nanotechnology; D009391:Nephelometry and Turbidimetry; D010316:Particle Size; D010713:Phosphatidylcholines / Q000737:chemistry; D012995:Solubility; D013678:Technology, Pharmaceutical; D013997:Time Factors; D047392:beta-Cyclodextrins / Q000737:chemistry; D047408:gamma-Cyclodextrins / Q000737:chemistry
D003505:Cyclodextrins; D005079:Excipients; D005452:Fluoresceins; D005456:Fluorescent Dyes; D008055:Lipids; D008081:Liposomes; D010713:Phosphatidylcholines; D047392:beta-Cyclodextrins; D047408:gamma-Cyclodextrins; C479659:hydroxypropyl-gamma-cyclodextrin; C108732:methyl-beta-cyclodextrin; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D002784:Cholesterol; C010942:1,2-distearoyllecithin; C007740:fluorexon