Liposomes attributes

As mentioned above, the ability to adsorb to the cornea and an optimal drug release rate have been defined as the two liposomal attributes most responsible for increasing bioavailability after topical ocular administration. A number of factors, including drug encapsulation efficiency, liposome size and charge, distribution of the drug within liposomes, stability of liposomes in the conjunctival sac and ocular tissues, their retention in the conjunctival sac, and most importantly their affinity toward the corneal surface and the rate of release of the encapsulated drug, have... 

Cationic quaternary ammonium compounds such as distearyldimethylammonium-chloride (DSDMAC) used as a softener and as an antistatic, form hydrated particles in a dispersed phase having a similar structure to that of the multilayered liposomes or vesicles of phospholipids 77,79). This liposome-like structure could be made visible by electron microscopy using the freeze-fracture replica technique as shown by Okumura et al. 79). The concentric circles observed should be bimolecular lamellar layers with the sandwiched parts being the entrapped water. In addition, the longest spacings of the small angle X-ray diffraction pattern can be attributed to the inter-lamellar distances. These liposome structures are formed by the hydrated detergent not only in the gel state but also at relatively low concentrations. 

Numerous experimental therapeutics have shown potency in vitro however, when they are tested in vivo, they often lack significant efficacy. This is often attributed to unfavorable pharmacokinetic properties and systemic toxicity, which limit the maximum tolerated dose. These limitations can be overcome by use of drug carriers. Two general types of carrier systems have been designed drug conjugation to macromolecular carriers, such as polymers and proteins and drug encapsulation in nanocarriers, such as liposomes, polymersomes and micelles. 

The important attributes of liposomes as a drug carrier are (a) they are biologically inert and completely biodegradable (b) they pose no concerns of toxicity, antigenicity, or pyrogenicity, because phospholipids are natural components of all cell membranes (c) they can be prepared in various sizes, compositions, surface charges, and so forth, depending on the requirements of... 

Jizomoto and Hirano [3.41 ] tried to increase the amount of drug inclusions in liposomes by inserting Ca2+ ions in dipalmitoylphosphatidylcholine (DPPC) liposomes. The included volume (mL) per g of liposomes is called Vcap, and this can be increased as a function of the Ca2+ concentration up to ten fold of the minimum Vcap The increase in Vcap is attributed to the electrostatic repulsion between the Ca ions, which reduces the number of lamella and increases the diameter of the liposomes to a certain extent, but increases substantially. A calculated simulation of this thesis is in reasonable agreement with the measurements... 

Zhang J, et al. Pharmaco attributes of dioleoylphosphatidylethanolamine/ cholesterylhemisuccinate liposomes containing different types of cleavable lipopolymers. Pharmacol Res 2004 49 185. 

Some investigators have used electrical current (electroporation) to improve DNA (or drug) entry into tumor cells with some preliminary success. Liposomes are attractive vehicles for gene delivery, since they can carry plasmid, antisense, or viral DNA. Compared with viral approaches, however, liposomes remain relatively inefficient at facilitating gene transfer, although their safety profile remains more desirable. Some of the attributes and limitations of the nonviral methods are listed in Table 58.1. 

Fluorescence probing has also been used by us to investigate the mechanism of vesicle to micelle transformation due to interaction of liposome with sodium dodecyl sulfate micelles. An increase in optical density and hydrodynamic diameter was observed at low SDS concentrations (Fig. 24). The increase was attributed to the incorporation of SDS monomers on liposome vesicles. The point where the hydrodynamic diameter and optical density reached a maximum was proposed to correspond to the saturation of bilayers of the first inflection point. Upon further increase in the SDS concentration... 

Domain Effect on Liposome Membrane Functional Attribute on Lipid BUayer... 

The higher generation dendrimeric derivative proved more effective in its interaction with liposomes. This behaviour was attributed to multivalent effects, exhibited at a greater extent by this dendrimeric derivative. Under an equal concentration of functional moieties the reactivity is favoured when the groups are located in a smaller number of particles. Thus the dendrimeric materials act as molecular glue causing adhesion of liposomal particles. 

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