Physical properties of nanoparticles do matter

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Journal of Pharmaceutical Investigation https://doi.org/10.1007/s40005-020-00504-w

REVIEW

Physical properties of nanoparticles do matter Tony Mutiso Kiio1 · Soyeun Park1 Received: 3 April 2020 / Accepted: 7 October 2020 © The Korean Society of Pharmaceutical Sciences and Technology 2020

Abstract Background  Nanoparticles (NPs) have been used to enhance pharmaceutical properties of drugs, including cell/tissue penetration, selective biodistribution, circulation half-life, and accumulation at target sites. Rigorous efforts, including chemical modifications using target moieties, have been dedicated to improving their functions. Area covered  Optimization of the physical properties of NPs, including size, shape, charge, and elasticity, is suggested to be an important step in the creation of NPs with desirable pharmacokinetic properties for use as drug delivery systems. In this review, we highlight recent findings on the effect of the physical properties of NPs, including the size, shape, surface charge, and elasticity on pharmaceutical functions. Expert opinion  Many studies have demonstrated that 30–200 nm NPs facilitate cell uptake and do not trigger the immune response due to their relatively large surface area. Compared to spherical NPs, non-spherical NPs are not only advantageous for cell uptake but also for systemic circulation owing to their multivalent interactions with the cell surface. The slightly negative charges carried by NPs have been considered responsible for the reduced electrostatic interactions with plasma proteins. Importantly, soft NPs enhance cellular uptake, reduce immunogenicity, and enhance tumor accumulation compared to their hard counterparts. Nonetheless, it is not easy to offer unequivocal suggestions regarding the physical properties of NPs during their pharmacokinetic journey; this is due to the multifaceted aspects at each step. Smart NPs that can alter their physical properties by responding to environmental stimuli were developed as alternatives to address this issue. Thus, physical properties do play a very important role in determining the pharmaceutical applications of NPs. Keywords  Elasticity · Nanoparticles · Pharmacokinetics · Size · Shape · Surface charge

Introduction Nanomedicine incorporating nanoparticles (NPs) as drug delivery systems has had unprecedented growth in recent years. In fact, substantial efforts have been dedicated to the development of innovative drug carriers that can protect therapeutic agents from degradation, enhance efficacy, and alleviate side effects (Wang and Wang 2014). Numerous NP therapeutics have been approved by the FDA for clinical use, and several others are in late-phase clinical trials (Barenholz 2012; Davis et al. 2008; Jain and Stylianopoulos 2010). The NPs used in nanomedicine are in the range of 10–1000 nm. Several forms of NPs, such as liposomal NPs composed of phospholipids (Han et al. 2018; Lee 2019), polymeric NPs * Soyeun Park [email protected] 1



College of Pharmacy, Keimyung University, 1095 Dalgubeoldaero, Daegu 42601, Re