Elsevier

Pharmacological Reports

Volume 64, Issue 5, September–October 2012, Pages 1020-1037
Pharmacological Reports

Nanoparticles as drug delivery systems

https://doi.org/10.1016/S1734-1140(12)70901-5Get rights and content

Abstract

Controlled drug delivery systems (DDS) have several advantages compared to the traditional forms of drugs. A drug is transported to the place of action, hence, its influence on vital tissues and undesirable side effects can be minimized. Accumulation of therapeutic compounds in the target site increases and, consequently, the required doses of drugs are lower. This modern form of therapy is especially important when there is a discrepancy between the dose or the concentration of a drug and its therapeutic results or toxic effects. Cell-specific targeting can be accomplished by attaching drugs to specially designed carriers. Various nanostructures, including liposomes, polymers, dendrimers, silicon or carbon materials, and magnetic nanoparticles, have been tested as carriers in drug delivery systems. In this review, the aforementioned nanocarriers and their connections with drugs are analyzed. Special attention is paid to the functionalization of magnetic nanoparticles as carriers in DDS. Then, the advantages and disadvantages of using magnetic nanoparticles as DDS are discussed.

Introduction

Delivering therapeutic compound to the target site is a major problem in treatment of many diseases. A conventional application of drugs is characterized by limited effectiveness, poor biodistribution, and lack of selectivity [111]. These limitations and drawbacks can be overcome by controlling drug delivery. In controlled drug delivery systems (DDS) the drug is transported to the place of action, thus, its influence on vital tissues and undesirable side effects can be minimized. In addition, DDS protects the drug from rapid degradation or clearance and enhances drug concentration in target tissues, therefore, lower doses of drug are required [111]. This modern form of therapy is especially important when there is a discrepancy between a dose or concentration of a drug and its therapeutic results or toxic effects.

Cell-specific targeting can be achieved by attaching drugs to individually designed carriers. Recent developments in nanotechnology have shown that nano-particles (structures smaller than 100 nm in at least one dimension) have a great potential as drug carriers. Due to their small sizes, the nanostructures exhibit unique physicochemical and biological properties (e.g., an enhanced reactive area as well as an ability to cross cell and tissue barriers) that make them a favorable material for biomedical applications.

Section snippets

Nanocarriers used in drug delivery system

According to the definition from NNI (National Nanotechnology Initiative), nanoparticles are structures of sizes ranging from 1 to 100 nm in at least one dimension. However, the prefix “nano” is commonly used for particles that are up to several hundred nanometers in size.

Nanocarriers with optimized physicochemical and biological properties are taken up by cells more easily than larger molecules, so they can be successfully used as delivery tools for currently available bioactive compounds [145

Liposomes

Liposomes have been the first to be investigated as drug carriers. They are nano/micro-particular or colloidal carriers, usually with 80–300 nm size range [144]. They are spherical vesicles composed of phospholipids and steroids (e.g., cholesterol), bilayers, or other surfactants and form spontaneously when certain lipids are dispersed in aqueous media where liposomes can be prepared, e.g., by sonication [139]. Liposomes have been reported to increase the solubility of drugs and improve their

Nanoparticles based on solid lipids

SLN (solid lipid nanoparticles), NLC (nanostructured lipid carriers) and LDC (lipid drug conjugates) are types of carrier systems based on solid lipid matrix, i.e., lipids solid at the body temperature [165]. They have been exploited for the dermal [1], peroral [100], parenteral [109], ocular [13], plumonary [83], and rectal [147] delivery.

SLN are particles made of solid lipids, e.g., highly purified triglycerides, complex glyceride mixtures or waxes stabilized by various surfactants [76]. The

Polymeric nanoparticles

Polymeric nanoparticles (PNPs) are structures with a diameter ranging from 10 to 100 nm. The PNPs are obtained from synthetic polymers, such as poly-ε-caprolactone [20], polyacrylamide [14] and polyacrylate [156], or natural polymers, e.g., albumin [94], DNA [93], chitosan [93, 128] gelatin [131]. Based on in vivo behavior, PNPs may be classified as biodegradable, i.e., poly(L-lactide) (PLA) [91], polyglycolide (PGA) [118], and non-biodegradable, e.g., polyurethane [55].

PNPs are usually coated

Dendrimer nanocarriers

Dendrimers are unique polymers with well-defined size and structure. Dendritic architecture is one of the most popular structures observed throughout all biological systems. Some of the examples of nanometric molecules possessing dendritic structure include: glycogen, amylopectin, and proteoglycans [146].

In the structure of dendrimer, in contrast to the linear polymer, the following elements can be distinguished: a core, dendrons, and surface active groups. The core is a single atom or molecule

Silica materials

Silica materials used in controlled drug delivery systems are classified as xerogels [36] and mesoporous silica nanoparticles (MSNs), e.g., MCM-41 (Mobil Composition of Matter) and SBA-15 (Santa Barbara University mesoporous silica material) [163]. They exhibit several advantages as carrier systems, including biocompatibility, highly porous framework and an ease in terms of functionalization [7]. Among inorganic nanoparticles, silica materials are the carriers which most often are chosen for

Carbon nanomaterials

Carbon nanocarriers used in DDS are differentiated into nanotubes (CNTs) and nanohorns (CNH).

CNTs are characterized by unique architecture formed by rolling of single (SWNCTs – single walled carbon nanotubes) or multi (MWCNTs – multi walled carbon nanotubes) layers of graphite with an enormous surface area and an excellent electronic and thermal conductivity [17]. Biocompatibility of nanotubes may be improved by chemical modification of their surface [54]. Such adjustment can be implemented by

Magnetic nanoparticles

Magnetic nanoparticles exhibit a wide variety of attributes, which make them highly promising carriers for drug delivery. In particular, these are: easy handling with the aid of an external magnetic field, the possibility of using passive and active drug delivery strategies, the ability of visualization (MNPs are used in MRI), and enhanced uptake by the target tissue resulting in effective treatment at the therapeutically optimal doses [10].

However, in most of the cases where magnetic

Conclusion

Nanocarriers as drug delivery systems are designed to improve the pharmacological and therapeutic properties of conventional drugs. The incorporation of drug molecules into nanocarrier can protect a drug against degradation as well as offers possibilities of targeting and controlled release. Due to small dimensions, nanocarriers are able to cross the blood-brain-barrier (BBB) and operate on cellular level. In comparison with the traditional form of drugs, nanocarrier-drug conjugates are more

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