Nanotechnology in Therapeutics

A Focus on Nanoparticles as a Drug Delivery System

Suwussa Bamrungsap; Zilong Zhao; Tao Chen; Lin Wang; Chunmei Li; Ting Fu; Weihong Tan


Nanomedicine. 2012;7(8):1253-1271. 

In This Article

Abstract and Introduction


Continuing improvement in the pharmacological and therapeutic properties of drugs is driving the revolution in novel drug delivery systems. In fact, a wide spectrum of therapeutic nanocarriers has been extensively investigated to address this emerging need. Accordingly, this article will review recent developments in the use of nanoparticles as drug delivery systems to treat a wide variety of diseases. Finally, we will introduce challenges and future nanotechnology strategies to overcome limitations in this field.


Nanotechnology involves the engineering of functional systems at the molecular scale. Such systems are characterized by unique physical, optical and electronic features that are attractive for disciplines ranging from materials science to biomedicine. One of the most active research areas of nanotechnology is nanomedicine, which applies nanotechnology to highly specific medical interventions for the prevention, diagnosis and treatment of diseases.[1,2,401] The surge in nanomedicine research during the past few decades is now translating into considerable commercialization efforts around the globe, with many products on the market and a growing number in the pipeline. Currently, nanomedicine is dominated by drug delivery systems, accounting for more than 75% of total sales.[3]

Nanomaterials fall into a size range similar to proteins and other macromolecular structures found inside living cells. As such, nanomaterials are poised to take advantage of existing cellular machinery to facilitate the delivery of drugs. Nanoparticles (NPs) containing encapsulated, dispersed, absorbed or conjugated drugs have unique characteristics that can lead to enhanced performance in a variety of dosage forms. When formulated correctly, drug particles are resistant to settling and can have higher saturation solubility, rapid dissolution and enhanced adhesion to biological surfaces, thereby providing rapid onset of therapeutic action and improved bioavailability. In addition, the vast majority of molecules in a nanostructure reside at the particle surface,[4] which maximizes the loading and delivery of cargos, such as therapeutic drugs, proteins and polynucleotides, to targeted cells and tissues. Highly efficient drug delivery, based on nanomaterials, could potentially reduce the drug dose needed to achieve therapeutic benefit, which, in turn, would lower the cost and/or reduce the side effects associated with particular drugs. Furthermore, NP size and surface characteristics can be easily manipulated to achieve both passive and active drug targeting. Site-specific targeting can be achieved by attaching targeting ligands, such as antibodies or aptamers, to the surface of particles, or by using guidance in the form of magnetic NPs. NPs can also control and sustain release of a drug during transport to, or at, the site of localization, altering drug distribution and subsequent clearance of the drug in order to improve therapeutic efficacy and reduce side effects.

Nanotechnology could be strategically implemented in new developing drug delivery systems that can expand drug markets. Such a plan would be applied to drugs selected for full-scale development based on their safety and efficacy data, but which fail to reach clinical development because of poor biopharmacological properties, for example, poor solubility or poor permeability across the intestinal epithelium, situations that translate into poor bioavailability and undesirable pharmacokinetic properties.[5] The new drug delivery methods are expected to enable pharmaceutical companies to reformulate existing drugs on the market, thereby extending the lifetime of products and enhancing the performance of drugs by increasing effectiveness, safety and patient adherence, and ultimately reducing healthcare costs.[6–8]

Commercialization of nanotechnology in pharmaceutical and medical science has made great progress. Taking the USA alone as an example, at least 15 new pharmaceuticals approved since 1990 have utilized nanotechnology in their design and drug delivery systems. In each case, both product development and safety data reviews were conducted on a case-by-case basis, using the best available methods and procedures, with an understanding that postmarketing vigilance for safety issues would be ongoing. Some representative examples of therapeutic nanocarriers on the market are briefly described in Table 1.

In this review, we focus mainly on the application of nanotechnology to drug delivery and highlight several areas of opportunity where current and emerging nanotechnologies could enable novel classes of therapeutics. We look at challenges and general trends in pharmaceutical nanotechnology, and we also explore nanotechnology strategies to overcome limitations in drug delivery. However, this article can only serve to provide a glimpse into this rapidly evolving field, both now and what may be expected in the future.