Liposome preparations are simply artificial spherical vesicles consisting principally of cholesterol and phospholipid molecules. These molecules are organised to form bilayers. Vesicles are classified as either being multilamellar or unilamellar. The former is made up of several bilayers while the latter has only one. On average, most of the vesicles have a diameter of less than 400nm.
The phospholipids and the cholesterol are first put into a suspension. They are hydrated to make them swell and separate into various bilayers. They self-close to form large vesicles that have to be modified by some techniques. One of these techniques is known as sonication. Here, an instrument known as a sonicator is used to provide high energy that is used to break down the large vesicles into smaller ones. This is achieved within five to ten minutes.
Another popularly used technique is known as extrusion. In this technique, the suspension is subjected to a cyclical process of freezing and thawing that eventually results in the breakdown of the large vesicles. Homogenous of size is achieved after a few cycles. Another variant of the same is the passage of the vesicles through progressively decreasing pores until very fine particles are obtained.
Heterogeneity of particle size is not an uncommon finding. The degree of variation is dependent on a number of factors such as amount of energy used, duration of sonication, composition and proportion of the lipids in the suspension and the level of tuning of the sonicator. The vesicles have been found to closely resemble cell membranes in structure. Both have hydrophilic and hydrophobic ends. The physical characteristics are similar to those of surfactants.
Lipid vesicles have gained wide clinical usage in recent times. They now play a very important role in drug delivery systems and are rapidly replacing viral vectors. This is due to the various advantages that they have over the viral systems. One of these advantages is that they are rarely immunogenic and hence are unlikely to cause immunological reactions which are fairly common with viral vectors. Another major advantage is the fact that they can be synthesized more easily than the vectors.
The available drug formulations are used in the treatment of a wide variety of disease processes. The drugs include cytarabine (an anticancer agent), liposomal amphotericin B, a highly potent antifungal agent, liposomal IRIV vaccine, morphine and doxorubicin among others. Many other drug formulations are in different phases of clinical trials.
Apart from drug delivery, lipid vesicles also play a vital role in the administration of nutrients. They are especially useful in supplementing nutrients that are deficient in the diet or those that cannot be easily absorbed orally due to their low bioavailability. Liposome encapsulation is currently one of the most efficient ways of administering vitamin C. The same principle is employed in the delivery of pesticides to plants, delivery of enzymes to their sites of action in the body and in the fixing of dyes to textiles.
There are many other uses of liposome preparations. Most of these are still the subject of research that is aimed at increasing their efficiency. The most encouraging news is that, no serious side effects related to the use of these preparations have been reported. There are some concerns, however, that they have a potential to cause cellular toxicity especially when taken in large quantities. The presence of inhibitors in serum may be another downside since these may inhibit the potency of the vesicles.
The phospholipids and the cholesterol are first put into a suspension. They are hydrated to make them swell and separate into various bilayers. They self-close to form large vesicles that have to be modified by some techniques. One of these techniques is known as sonication. Here, an instrument known as a sonicator is used to provide high energy that is used to break down the large vesicles into smaller ones. This is achieved within five to ten minutes.
Another popularly used technique is known as extrusion. In this technique, the suspension is subjected to a cyclical process of freezing and thawing that eventually results in the breakdown of the large vesicles. Homogenous of size is achieved after a few cycles. Another variant of the same is the passage of the vesicles through progressively decreasing pores until very fine particles are obtained.
Heterogeneity of particle size is not an uncommon finding. The degree of variation is dependent on a number of factors such as amount of energy used, duration of sonication, composition and proportion of the lipids in the suspension and the level of tuning of the sonicator. The vesicles have been found to closely resemble cell membranes in structure. Both have hydrophilic and hydrophobic ends. The physical characteristics are similar to those of surfactants.
Lipid vesicles have gained wide clinical usage in recent times. They now play a very important role in drug delivery systems and are rapidly replacing viral vectors. This is due to the various advantages that they have over the viral systems. One of these advantages is that they are rarely immunogenic and hence are unlikely to cause immunological reactions which are fairly common with viral vectors. Another major advantage is the fact that they can be synthesized more easily than the vectors.
The available drug formulations are used in the treatment of a wide variety of disease processes. The drugs include cytarabine (an anticancer agent), liposomal amphotericin B, a highly potent antifungal agent, liposomal IRIV vaccine, morphine and doxorubicin among others. Many other drug formulations are in different phases of clinical trials.
Apart from drug delivery, lipid vesicles also play a vital role in the administration of nutrients. They are especially useful in supplementing nutrients that are deficient in the diet or those that cannot be easily absorbed orally due to their low bioavailability. Liposome encapsulation is currently one of the most efficient ways of administering vitamin C. The same principle is employed in the delivery of pesticides to plants, delivery of enzymes to their sites of action in the body and in the fixing of dyes to textiles.
There are many other uses of liposome preparations. Most of these are still the subject of research that is aimed at increasing their efficiency. The most encouraging news is that, no serious side effects related to the use of these preparations have been reported. There are some concerns, however, that they have a potential to cause cellular toxicity especially when taken in large quantities. The presence of inhibitors in serum may be another downside since these may inhibit the potency of the vesicles.
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