Nanotechnology in Pharmaceutical Design

Current Pharmaceutical Design, 2013, Vol. 19, No. 35

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Editorial
Nanotechnology in Pharmaceutical Design Nanotechnology is an engineering of materials at the nanometer scale so that the materials have at least one dimension sized from 1 to 100 nm. Nanotechnology is a multidisciplinary technology, convergence of basic sciences and applied disciplines, and provides various intelligent systems and materials for better pharmaceutical applications. This special issue therefore presents the most recent development of nanotechnology in pharmaceutical design, as summarized by a multidisciplinary team of international experts in two broad areas, i.e. nanodrug and nanoparticle-drug system for effective delivery. Many marketed drugs have a low solubility and subsequently a low bioavailability. The low bioavailability limits the effectiveness of each dose, and thus requires frequent administration, leading to a high financial burden and high drug wastage. In order to enhance drug bioavailability, various techniques have been developed in the recent decades, and one of the most promising methods is to control the drug particles in the nanometer scale (nano-drugs). The large surface area of nano-drugs thus leads to the faster dissolution and the higher solubility as the smaller drug particles have higher surface energy than the bulky drug particles. In this issue, Cheow et al. (Nanyang Technological University, Singapore) [1], Moribe et al. (Chiba University, Japan; and Mahidol University, Thailand) [2], and Ozeki and Tagami (Nagoya City University, Japan) [3] comprehensively review the recent progresses in the production of nano-drugs by conventional top-down and bottom-up methods, and the enhancement of drugs solubility and availability. In particular, Cheow et al. [1] also review some nonconventional methods to prepare nano-drugs and amorphous drug particles, which both improve in the drug bioavailability. Amorphous drug particles, with respect to the crystalline drug particles, can be regarded as aggregates of very small nano-drugs. In some special cases, in the existence of suitable excipients, the nano-drugs and amorphous drugs could be formed in a controllable way, as reviewed by Ozeki and Tagami [3] and Shen et al. (Institute of Chemical and Engineering Sciences, A*STAR, Singapore) [4] in this special issue. The nano-drugs are either dispersed in the excipient matrix as a nanocomposite [3], or limited in the carrier pores (such as mesoporous silica) [4]. In both cases, as-formed nano-drug particles in the nano-sized spaces possess an enhanced dissolution rate and solubility, and an increased bioavailability in comparison with the bulky drug particles. Moreover, the release of drug molecules can be tailored in some active way. For example, the pore opening could be triggered by environmental changes or other external effects [4]. More or less similarly, drug molecules would also exhibit the improved bioavailability once they are carried by various delivery systems through some particular interactions or structures. Pan et al. (Sun-Yat Sen University, China) [5] have reviewed a particular delivery system cubosome. Cubosomes are fragmented cubic gels that are formed with amphiphilic lipids and water molecules, and can be used for the delivery of hydrophilic, amphiphilic and hydrophobic drugs. On the other hand, Cejkova and Stepanek (Institute of chemical Technology, Czech Republic) [6] extensively review advances in the fabrication and characterization of micro- and nano-particles with a non-uniform internal structure, such as core-shell particles, particles with multiple cores or a multi-layered structure, porous particles with both regular and random pore structure, and complex composite particles with a few above-mentioned features. These nano-structured particles can provide specific benefits for effective drug delivery. Targeting delivery system is always actively pursued in the field of drug delivery and pharmaceutical design. In this special issue, Friedman et al. (University of North Carolina at Chapel Hill, USA) [7] review such smart targeting nanoparticle delivery systems. These nanoparticles require conjugation with targeting ligands to direct selective binding to cell types or states. They present some conventional and nonconventional functionalization approaches currently used and investigated. In this special issue, three papers have reviewed the specific application of nanoparticle-drug systems. Gu et al. (The University of Queensland, Australia) [8] comprehensively review various nanoparticle-drug systems that are currently investigated in the prevention or treatment of a specific cardiovascular disease - restenosis, re-narrowing of a blood vessel after removal of atherosclerotic plaque. Wang et al. (Institute of Process Engineering, Chinese Academy of Sciences, China) [9] review recent progress in formulating therapeutic protein delivery systems - hydrophilic polymer microspheres and hydrophobic polymer microcapsules. This paper emphasizes how to maintain the bioactivity of the therapeutic proteins during the system formation. More interestingly, Liang et al. (the University of Queensland; Macquarie University; University of South Australia, Australia) [10] review recent investigations on the nanoparticle skin penetration into the body which could be potentially harmful (such as ZnO/TiO2 nanoparticles in sunscreen) or useful for topical delivery of drugs and skin health nutrients. In summary, this special issue discusses two relevant areas on pharmaceutical design using nanotechnology. I would like to thank all the contributors to this special issue and wish that this special issue will be helpful for the future application of nanotechnology in pharmaceutical design.

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Nanotechnology in Pharmaceutical Design

REFERENCES
[1] [2] [3] [4] [5] [6] [7] [8] [9] [10] Cheow WS, Xu R, Hadinoto K. Towards sustainability: new approaches to nano-drug preparation. Curr Phar Des 2013; 19(35): 6229-45. Moribe K, Ueda K, Limwikrant W, Higashi K, Yamamoto K. Nano-sized crystalline drug production by milling technology. Curr Phar Des 2013; 19(35): 6246-58. Ozeki T, Tagami T. Functionally engineered nanosized particles in pharmaceutics: Improved oral delivery of poorly water-soluble drugs. Curr Phar Des 2013; 19(35): 6259-69. Shen S-C, Ng WK, Chia L, Dong Y-C, Tan RBH. Applications of mesoporous materials as excipients for innovated drug formulation. Curr Phar Des 2013; 19(35): 6270-89. Pan X, Han K, Peng X, Yang Z, Qin L, Zhu C, Huang X, Shi X, Dian L, Lu M, Wu C. Nanostructured cubosomes as advanced drug delivery system. Curr Phar Des 2013; 19(35): 6290-97. Cejkova J, Stepanek F. Compartmentalised and internally structured nanoparticles for drug delivery-A review. Curr Phar Des 2013; 19(35): 6298-314. Friedman AD, Claypool SE, Liu R. The smart targeting of nanoparticles. Curr Phar Des 2013; 19(35): 6315-29. Gu Z, Rolfe R, Thomas AC, Xu ZP. Restenosis treatments using nanoparticle-based drug delivery systems. Curr Phar Des 2013; 19(35): 6330-39. Wang L, Liu Y, Zhang W, Chen X, Yang T, Ma G. Microspheres and microcapsules for protein delivery: strategies of drug activity retention. Curr Phar Des 2013; 19(35): 6340-52. Liang XW, Xu ZP, Grice J, Zvyagin AV, Roberts MS, Liu X. Penetration of NPs and nanomaterials in human skin: Formulation effect. Curr Phar Des 2013; 19(35): 6353-66.

Zhi Ping (Gordon) Xu (PhD)

ARC Centre of Excellence for Functional Nanomaterials Australian Institute for Bioengineering and Nanotechnology The University of Queensland Brisbane, QLD 4072 Australia E-mail: gordonxu@uq.edu.au