Sie sind auf Seite 1von 1

NANOSYSTEMS IN DRUG TARGETING Kapil Bhalla & Saurabh Arjariya

Sagar Institute of Pharmaceutical Sciences, Sagar (M.P.) India

The long cherished goal of targeting drugs to specific sites in the body, where the pharmacological action is desired and sparing other tissues has been actively pursued all these years. The concept of magic bullets given by Ehrlich has now seen a metamorphosis to magic wands, in the form of targeted drug delivery systems. The magic, all due to the specific targeting ligands which guide the drug carriers to the molecular targets be it on cell surface or nuclear membranes. Nanosystems including the nano-sized (<1000 nm) drug carrier systems, such as polymeric nanoparticles, liposomes, micelles and polymerdrug conjugates are the vanguards of this ever-evolving field. Targeting drugs to specific sites, and maintaining pharmacologically relevant drug levels at the site for a period required for desired therapeutic action is what makes the nanosystems the burgeoning magic wands. Substantial challenges still exist in terms of biological barriers. Nevertheless, the approaches like directly reaching the target using catheters, or using exogenous guiding mechanisms (magnetic fields and ultrasound), and exploiting the accessible targets on vascular endothelium are emerging as new and promising trends. It is conceivable, that despite all the formidable challenges, interplay of different disciplines ranging from engineering to biology will make the dream of drug targeting come true.

In the past few decades, rapid advances in cell and molecular biology have allowed us to develop a better understanding of the pathophysiology of various diseases. This has cast a floodlight on the possible cellular and molecular targets which can be exploited not only for drug discovery but also for imaging and therapy. drug targeting has evolved as the most desirable but elusive goal in drug delivery science. It can potentially increase efficacy and reduce toxicity of new and pre-existing drugs by altering their pharmacokinetics and biodistribution and restricting the action of drugs to the treated tissue.


A better understanding of the physiological barriers which a drug needs to overcome should enable the pharmaceutical scientists to develop successful design of targeted drug delivery systems.The challenge in drug targeting is not only the targeting of drug to a specific site but also retaining it for the desired duration to elicit pharmacological action. For a nanosystem administered intravenously, the first and foremost barrier is that of the vascular endothelium and the basement membrane.

Fig: Barriers to drug targeting and the role of nanosystems in overcoming these barriers.

PASSIVE TARGETING 1.Pathophysiological factors Inflammation EPR effect 2. Physicochemical factors Size Molecular weight 3. Anato. opportunities Catheterization Direct injection 4. Chemical approaches Prodrugs ACTIVE TARGETING 1. Biochemical targets Organs Cellular Organelles Intracellular 2. Physical/External stimuli Ultrasound Magnetic field 3. Pretargeting/ 4. Promoter/Transcription targeting

(A) Receptor Folic Acid Receptor LDL Receptors Peptide Receptors (B) Lipid Components of Cell Membranes (C) Surface Antigens/ Proteins Active targeting of drugs can be realized by the use of active agents or ligands which interact with some degree of exclusivity with the specific targets/receptors identified on particular cell types

Nanosystems offer opportunities to achieve drug targeting with newly discovered disease-specific targets, however challenges remain, primarily because of the complexity of the body and the layers of barriers that these systems need to overcome to reach to the target. Effective targeting would require dual focus, a better understanding of the target and a simultaneous development of the targeting system.

Stolnik, S.; Illum, L.; Davis, S.S. Adv. Drug Deliv. Rev., 1995, 16,195-214..