Integrity of liposomes in presence of cyclodextrins: Effect of liposome type and lipid composition

Hatzi, Panayiota; Mourtas, Spyridon; Klepetsanis, Pavlos; Antimisiaris, Sophia G.

doi:10.1016/j.ijpharm.2006.09.059

Cited by 79 publications

(68 citation statements)

References 20 publications

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“…These results suggest that HPβCD is entrapped only in the intravesicular aqueous compartment and does not bind significantly to the liposome membrane. This is consistent with previous observations (16,19,20,22) that reported a lack of interaction between HPβCD and gel phase lipid bilayers.…”

Section: Validation Of Experimental Methodssupporting

confidence: 94%

“…Still lacking are quantitative relationships that would enable the formulator to predict the potential benefit of a complexing agent on the liposomal loading and retention of a hydrophobic drug. Additionally, unusual release kinetics characterized by an initial burst release followed by a second phase with slower or no drug release have been observed in several studies, particularly those employing liposomes comprised of liquid crystalline bilayers (8,11,14,16). It has been speculated that the initial burst phase is due to a membrane destabilizing effect of cyclodextrins (8,11,14).…”

Section: Introductionmentioning

confidence: 99%

“…While interactions of some cyclodextrins with certain liposome components such as cholesterol have been reported (17,18), the reason for the observed biphasic release kinetics remains unclear. Certain cyclodextrins such as HPβCD have been found to have a negligible effect on the gel to liquid crystalline phase transition enthalpy or temperature (19,20) and to induce no significant leakage of entrapped markers (16,21,22). Therefore, such non-interacting cyclodextrins may be more useful as excipients for prolonged release liposomal suspensions.…”

Section: Introductionmentioning

confidence: 99%

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Effect of Cyclodextrin Complexation on the Liposome Permeability of a Model Hydrophobic Weak Acid

Joguparthi

Anderson

2008

Pharm Res

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In liposomes, cyclodextrin complexation competes with liposomal membrane binding which may temper the potential benefit of complexation in prolonging hydrophobic drug retention. Cyclodextrin complexation combined with drug ionization may nevertheless significantly enhance the retention of ionizable hydrophobic drugs in liposomes as complexation may compete more favorably with membrane binding when the drug is ionized.

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Section: Validation Of Experimental Methodssupporting

confidence: 94%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Effect of Cyclodextrin Complexation on the Liposome Permeability of a Model Hydrophobic Weak Acid

Joguparthi

Anderson

2008

Pharm Res

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“…In some other cases, sample separation was not necessary and analysis was performed in situ [ 68 ] . For example, in the case of liposomes encapsulating a fl uoroscent dye, a very small fraction of the total sample volume was needed for analysis and the liposomes did not interfere with the analysis of the released fl uoroscent molecule; thus there was no need for sample separation.…”

Section: Sample and Separatementioning

confidence: 99%

In Vitro Drug Release Testing and In Vivo/In Vitro Correlation for Long Acting Implants and Injections

Kastellorizios

Burgess

2011

Long Acting Injections and Implants

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An advantage of long acting implants and injections is their ability to maintain a relatively constant drug concentration at the site of interest. In vitro drug release testing, particularly where an in vivo / in vitro relationship has been established, can help in ensuring in vivo performance. There are various in vitro release testing methods, which are chosen, based on availability, dosage form specifi cations and drug properties. These are categorized into three groups: sample and separate, fl ow-through and dialysis. Although there are currently no standard methods for in vitro release testing of controlled release parenterals, standard dissolution apparatus specifi ed by the United States Pharmacopeia have been adapted in some cases and the development of compendial monographs is anticipated. An in vivo / in vitro correlation can predict the bioavailability characteristics of a product based on release in vitro .

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“…The structural changes were also assessed using differential scanning calorimetry [48], freeze-fracture electron microscopy [47], binding isotherms [49] or photon-correlation spectroscopy [19,23,49,50]. Despite all these studies, rare are those involving specifically the interaction between b-CD and phospholipids [19,49,51]. And, to the best of our knowledge, only information on the global liposome size and dispersity could be inferred from the previously mentioned techniques which do not give access to the internal structure of the bilayer.…”

Section: Introductionmentioning

confidence: 99%

Investigation of the interaction between a β-cyclodextrin and DMPC liposomes: a small angle neutron scattering study

Joset

Grammenos

Hoebeke

et al. 2015

J Incl Phenom Macrocycl Chem

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The small angle neutron scattering technique has been applied to investigate the interaction between a cyclodextrin (CD) and liposomes. From the modelling of the experimental neutron scattering cross sections, the detailed structure of dimyristoylphosphatidylcholine (DMPC) liposomes is assessed upon addition of increasing amounts of randomly methylated b-CD (RAMEB). This study has been performed at two temperatures bracketing the phase transition of the DMPC bilayers. The fraction of DMPC molecules incorporated into the vesicles is inferred. The dose-dependent phospholipidic extraction by RAMEB is quantified as well as the concomitant evolution of the liposome radius and of the thickness of the hydrophobic and hydrophilic parts of the membrane. The possible formation of CD-DMPC inclusion complexes is also assessed. The data suggest the dose-dependent coverage by RAMEB of the outer liposome interface. Our analysis highlights the important role of temperature on the mechanism of action of RAMEB. These results are discussed in the framework of the area-difference-elasticity model.

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Integrity of liposomes in presence of cyclodextrins: Effect of liposome type and lipid composition

Cited by 79 publications

References 20 publications

Effect of Cyclodextrin Complexation on the Liposome Permeability of a Model Hydrophobic Weak Acid

Effect of Cyclodextrin Complexation on the Liposome Permeability of a Model Hydrophobic Weak Acid

In Vitro Drug Release Testing and In Vivo/In Vitro Correlation for Long Acting Implants and Injections

Investigation of the interaction between a β-cyclodextrin and DMPC liposomes: a small angle neutron scattering study

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