Developing micro-/nanoparticulate drug delivery systems using "design of experiments"

Abstract

Of late, micro and nanoparticluate drug delivery systems have been gaining immense importance primarily attributed to their improved drug release controlling and targeting efficiencies. Also, the small particle size and desirable surface charge associated with these delivery systems render them suitable for specific applications like lymphatic uptake, pulmonary uptake, tumor targeting, brain targeting, etc. For decades, micro and nanoparticulate systems have been prepared by the conventional “trial and error” approach of changing One Variable at a Time (OVAT). Using this methodology, the solution of a specific problematic formulation characteristic can certainly be achieved, but attainment of the true optimal composition is never guaranteed. Thus, the present manuscript provides an updated account of the systematic approach “Design of Experiments (DoE)” as applicable to formulation development of microparticles and nanostructured systems. Besides providing a bird's eye view of the various experimental designs and optimization techniques employed for DoE optimization of such systems, the present manuscript also presents a copilation of the major micro/nano-structuctred systems optimized through DoE till date. In a nutshell, the article will act both as a ready reckoner of DoE optimization of micro/nano drug delivery systems and a catalyst in providing an impetus to young pharmaceutical “nano & micro” researchers to venture into the rewarding field of systematic DoE optimization.

Optimized synthesis of glycyrrhetinic acid-modified chitosan 5-fluorouracil nanoparticles and their characteristics

“…The more drugs a nanoparticle can carry, the higher drug loading it will possess. Thus, many studies 18,27,28 have been done to find nanoparticles with high drug loading through rational experimental design and optimization. In this study, we used CCD to optimize the preparation process of nanoparticles, and we obtained optimized nanoparticles with relatively small particle size and high drug loading.…”

Designing polymeric microparticles for biomedical and industrial applications

“…For these reasons, the use of this methodology hardly ever leads to an optimized formulation and production process [49].…”

“…Additionally, this type of experimental design also reveals the possible existence of any interactions between factors. After the identification of the critical factors, and through the implementation of an optimization DoE, the optimum levels of the factors, i.e., the values of the independent variables that lead to an optimum response, can be identified [49,50].…”

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“…[17] The supernatant was collected, and the drug content was estimated using UV-visible (Cary 60, 2100, Agilent technology, Germany) spectrophotometric method at 245 nm, using following equations. …”