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One of the most recent advancements in the domain of solubility enhancement lead to the development of pharmacosomes, a novel lipid based drug delivery system. Pharmacosomes are the colloidal dispersions of drugs covalently bound to the phospholipids. Pharmacosomes may exist as ultrafine vesicular, micellar or hexagonal aggregates depending upon the chemical structure of the drug lipid complex. Their very small size and unique properties such as amphiphilicity, active loading of drugs, high and predetermined entrapment efficiency, stability make them an appropriate carrier for delivering drugs with precision and selectivity. They help in achieving increased bioavailability, reduce the cost of therapy and provide controlled as well as targeted release of drug. There is reduction in the drug leakage and toxicity while the therapeutic efficacy increases. It is advancing as a method used for delivery of various drugs like non-steroidal, anti-inflammatory drugs, cardiovascular drugs, antineoplastic drugs and proteins. This approach as a drug delivery system certainly promises a reliable, safe, selective and precise method of drug delivery.
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Pharmacosomes is not only having high entrapment efficiency but it can be predetermined because drug itself in conjugation with lipids forms vesicles. Unlike liposomes, there is no need of following the tedious, time consuming step for removing the free, unentrapped drug from the formulation. Since the drug is covalently linked, loss due to leakage of drug, does not take place. However, loss may occur by hydrolysis. There is no problem of drug incorporation. Encaptured volume and drug bilayer interactions do not influence entrapment efficiency, in case of pharmacosome. These factors on the other hand have great influence on entrapment efficiency in case of liposomes. The lipid composition in liposomes decides its membrane fluidity, which in turn influences the rate of drug release, and physical stability of the system. However, in pharmacosomes, membrane fluidity depends upon the phase transition temperature of the drug lipid complex, but it does not affect release rate since the drug is covalently bound. The drug is released from pharmacosome by hydrolysis (including enzymatic). Phospholipid transfer/exchange is reduced, and solubilization by HDL is low.
The physicochemical stability of the pharmacosome depends upon the physicochemical properties of the drug lipid complex. Due to their amphiphilic behavior, such systems allow, after medication, a multiple transfer through the lipophilic membrane system or tissue, through cellular walls piggyback endocytosis and exocytosis. Following absorption, their degradation velocity into active drug molecule depends to a great extension the size and functional groups of drug molecule, the chain length of the lipids, and the spacer. These can be varied relatively precisely for optimized in vivo pharmacokinetics. They can be given orally, topically, extra or intravascularly. They help in achieving increased bioavailability, reduce the cost of therapy and provide controlled as well as targeted release of drugs.
According to IMS Health Consulting, an international research company, in 2012 the size of the global pharmaceutical market reached $940 billion. In monetary terms it grew by 6%. In the future the sector is expected to grow at no less than 3% to 4% a year and if this happens the global pharmaceutical market is expected to reach $1.1 trillion by 2015 and will reach $1.2 trillion in 2016 and up to $1.5 trillion by 2020. The global demographic, epidemiological and economic changes are transforming the pharmaceutical market. The world population is growing rapidly and is projected to raise from 7 billion in 2011 to 7.7 billion in 2020 and 9.6 billion in 2050, hence an increase in the demand for pharmaceuticals.
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This page was last updated on 10th Sep, 2015
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