Small Molecules Encapsulated into Liposomes

Drug encapsulated liposome

The following list contains examples of some of our products. There are thousands of molecules that can be encapsulated into the liposomal systems and therefore we can not list all our products. For more information email us at info@encapsula.com

Clodronate or Dichloromethylenediphosphonic acid (DMDP)

Clodronate or Dichloromethylenediphosphonic acid (DMDP) is a drug used in the treatment of hypercalcemia (abnormally high calcium levels in the blood) and cancer that has metastasized to the bone. It may decrease pain, the risk of fractures, and the development of new bone metastases.

Clodronate also depletes macrophages in animals. A liposome's inherent tendency to be endocytosed by macrophages makes it the ideal delivery system for Clodronate whenever the selective depletion of the macrophage population is required.

After injection, liposomes will be ingested and digested by macrophages followed by intracellular release and accumulation of Clodronate. At a certain intracellular concentration, Clodronate induces apoptosis of the macrophage. By injecting Clodronate liposomes to an animal and creating an animal with macrophage depleted tissues or organs, functional aspects of macrophages can be studied in vivo. Many promising results were obtained by application of Clodronate encapsulated liposomes for suppression of macrophage activity in various models of autoimmune diseases, transplantation, neurological disorders and gene therapy.

Clodronate is not a toxic molecule by itself and liposomes when they are prepared from phosphatidylcholine and cholesterol are not toxic either. Free Clodronate will not easily pass phospholipid bilayers of liposomes and cell membranes. Due to this the encapsulation efficiency of Clodronate is very low (about 1-2%). Liposomes are swallowed by macrophages. The implication is that Clodronate, once delivered into phagocytic cells using liposomes as vehicles, will not escape from the cell. After disruption of the phospholipid bilayers of the liposomes under the influence of the lysosomal phospholipases in the macrophage, Clodronate, which is dissolved in the aqueous compartments between the liposomal bilayers, is released into the cell. The Clodronate is accumulated intracellularly and after exceeding a threshold concentration, the cell is irreversibly damaged and dies by apoptosis (J. Immunol. Meth. 193: 93-99, 1996). Free clodronate, e.g. released from dead macrophages, has an extremely short half life in the circulation. It is removed from the circulation by the renal system. The short half life of the Cloronate is one of the main reasons that free Clodronate can not be used by itself for macrophage depletion and it should be encapsulated into the liposomes.

Naturally, the approach can only be successful when the liposomes are able to reach the macrophages which have to be eliminated. Vascular barriers (capillary walls) can not be crossed by liposomes. In short, macrophages can be depleted in the liver (Kupffer cells), spleen (different macrophage subpopulations), lung (alveolar but not interstitial macrophages), peritoneal cavity, lymph nodes, joints (phagocytic synovial lining cells) and testis if liposomes are adequately administered.

For more information about Clodronate liposomes see here:

http://www.encapsula.com/clodronate_liposomes2.html

Antibiotic Encapsulated Liposomes

Encapsulation of certain antibiotics into the liposomes can enhance their effect against microorganisms invading cells. In the treatment of the infectious diseases, liposomes are applied as carriers of antimicrobial agents to:

  1. Achieve localization at the infected site
  2. Serve as a microreservoir of the drug in circulation and
  3. Reduce the side effects of the antibiotics.

Encapsulation of the antibiotics into the liposomes enhances the antimicrobial activities of a number of antibiotics against infections both in vivo and cultured cells. The studies has shown that delivery of ampicillin, amphotericin and streptomycin in liposomes has enhanced the activities of these drugs against experimental infections induced by Listeria monocytogenes, Candida albicans and Salmonella enteritidis.

Antibiotics such as adriamycin, amikacin, amphotericin B, ampicillin, azithromycin, bacitracin, benzylpenicillin, bleomycin, capreomycin, carbenicillin, ceftazidime, ceftriaxone, cephalexin, chloramphenicol, ciprofloxacin, clarithromycin, clindamycin, clofazimine, cycloserine, daunorubicin, dibekacin, doxorubicin, doxycycline, enrofloxacin, erythromycin, ethambutol, ethionamide, gentamicin, isoniazid, kanamycin, meropenem, neomycin, netilmicin, oxacillin, paromomycin, penicillin G, piperacillin, polymyxin B, rifabutin, rifampicin, sisomicin, sparfloxacin, streptomycin, teicoplanin, tobramycin, vancomycin and viomycin can be encapsulated into the liposomes. There are hundreds of different antibiotics that can be encapsulated into the liposomal systems therefore we can not list all our products. For more information email us at: info@encapsula.com

Anti-Tumor Drugs Encapsulated Liposomes

Hundreds of different molecules with anti-tumor activities can be encapsulated into the liposomal systems. The encapsulation of various types of anti-tumor drugs has been extensively studied by many scientific research laboratories around the world.

Encapsula NanoSciences provides various formulations of anti-tumor encapsulated liposomes. For more information send us an email at info@encapsula.com

Antioxidant Liposomes

Antioxidant liposomes are used in the field of free radical biology and medicine. Antioxidant liposome refers to liposomes containing:

  1. Lipid-soluble chemical antioxidants such as ubiquinones (e.g CoQ10), retinoids, carotenoids, lipid soluble flavanoids (e.g. quercetin, hesperetin, naringenin), tamoxifen, vitamin E (tocopherols and tocotrienols), synthetic lipid-soluble anti-oxidants such as BHT, TBHQ and probucol.
  2. Water-soluble chemical antioxidants such as urate, glutathione, N-acetylcysteine (NAC), pro-cysteine, lipoic acid, dihydrolipoic acid, water-soluble flavonoids (e.g. pycnogenol) and ascorbate (vitamin C)
  3. Enzymatic antioxidants such as superoxide dismutase.

Encapsula NanoSciences provides various formulations of antioxidant liposomes. For more information send us an email at info@encapsula.com

NSAIDs encapsulated liposomes

Various types of liposome encapsulated NSAIDs such as indomethacin and naproxen have been studied. Based on these researches the negative side effects of NSAIDs decrease significantly upon encapsulation into the liposomal systems.

Encapsula NanoSciences provides various formulations of NSAID encapsulated liposomes. For more information send us an email at info@encapsula.com

ATP Encapsulated Liposomes

It is very well known that, under the conditions of ischemia, including myocardialischemia, the utilization of adenosine triphosphate (ATP) is reduced and contractile function is depressed. However, ATP consumption continues by various ATPases involved in a variety of metabolic reactions. ATP levels in the cardiomyocytes during cardiac ischemia drop to 20% of their initial value after approximately 15 min, which eventually leads to cell death.

The application/infusion of exogenous ATP seems to be an attractive possibility for restoration of the required level of ATP in ischemic cells. However, strongly charged anions such as ATP cannot penetrate the plasma membrane and enter cells. In addition, ATP rapidly degrades in vivo and, thus, has a very short life-time in the circulation. These limitations do not allow for the therapeutic use of free ATP as a bioenergetic substrate. Delivery of ATP to ischemic cells including cardiomyocytes requires alternative methods. Various formulations of ATP encapsulated liposomes are used for delivery of ATP to ischemic cells.

Encapsula NanoSciences provides various formulations of ATP encapsulated liposomes such as PEGylated ATP liposomes and non-PEGylated ATP liposomes. For more information send us an email at info@encapsula.com

Hemoglobin encapsulated Liposomes (artificial blood)

Liposome encapsulated hemoglobin (LEH) has numerous advantages as a red cell substitute. LEH has no blood type such (e.g. A, B, AB or O) and can be made virus-free and sterile in large quantities. Cofactors can be included in the liposome to modify the P50 and to prevent methemoglobin formation.

Encapsula NanoSciences provides various types of hemoglobin encapsulated liposomes such as PEGylated LEH and non-PEGylated LEH. Liposomal formulation of hemoglobin is only for research and development purposes. For more information send us an email at info@encapsula.com

Vitamin Encapsulated Liposomes

Various types of vitamin molecules such as Vitamins A, E and C can be encapsulated into the liposomes.

Encapsula NanoSciences provides various types of vitamin encapsulated liposomes. For more information send us an email at info@encapsula.com

Other types of Molecules Encapsulated into the Liposomes

There are so many molecules that can be encapsulated into liposomal systems. We can not make a list of all of them on this website. If you can not find your desired formulation on this website then simply contact us at info@encapsula.com

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