Size, shape, charge and “stealthy” surface: Carrier properties affect the drug circulation time in vivo

Abstract

The present review sets out to discuss recent developments of the effects and mechanisms of carrier properties on their circulation time. For most drugs, sufficient in vivo circulation time is the basis of high bioavailability. Drug carrier plays an irreplaceable role in helping drug avoid being quickly recognized and cleared by mononuclear phagocyte system, to give drug enough time to arrive at targeted organ and tissue to play its therapeutic effect. The physical and chemical properties of drug carriers, such as size, shape, surface charge and surface modification, would affect their in vivo circulation time, metabolic behavior and biodistribution. The final circulation time of carriers is determined by the balance between macrophage recognitions, blood vessel penetration and urine excretion. Therefore, when designing the drug delivery system, we should pay much attention to the properties of drug carriers to get enough in vivo circulation time to arrive at target site eventually. This article mainly reviews the effect of carrier size, size, surface charge and surface properties on its circulation time in vivo , and discusses the mechanism of these properties affecting circulation time. This review has reference significance for the research of long-circulation drug delivery system.

Poly(lactic-co-glycolic acid) microsphere production based on quality by design: a review

“…Drug loading and encapsulation efficiency are important indicators of drug content in microspheres (Di et al, 2020). Drug loading not only affects the drug release characteristics, but is also reflective of the inter-batch stability, which is an important indicator of process maturity.…”

“…Particle size affects the needle penetration and drug distribution (Di et al, 2020). Moreover, a linear relationship exists between the particle size and degradation rate.…”

Liver Targeting of Daclatasvir via Tailoring Sterically Stabilized Bilosomes: Fabrication, Comparative In Vitro/In Vivo Appraisal and Biodistribution Studies

“…When opsonin attracts PEGylated vesicles, the PEG chains will be compressed and condensed, resulting in the conversion of their original conformation to a steric hindered state, thus preventing the attraction between opsonin and the particles and, hence, avoiding their uptake by the MPS. 13 …”

“…To address this problem, various hydrophilic polymers, including poly(vinyl alcohol), poly(N-vinylpyrrolidone), poly(2-oxazoline), and poly(ethylene glycol) (PEG), and zwitterionic polymers, such as poly(carboxybetaine methacrylate), 12 have been introduced to yield more hydrophilic nanoparticles and to decrease MPS reuptake. [12][13][14] PEG is one of the most hydrophilic molecules that is commonly used as an example of a stealthy polymer. The PEGylation of nanovesicles results in a reduction in their electrostatic charge, by forming an aqueous layer surrounding them, thus avoiding their renal clearance.…”

“…When opsonin attracts PEGylated vesicles, the PEG chains will be compressed and condensed, resulting in the conversion of their original conformation to a steric hindered state, thus preventing the attraction between opsonin and the particles and, hence, avoiding their uptake by the MPS. 13 To the best of our knowledge, the previous literature lacks satisfactory data about any targeting drug delivery of DAC to the liver. Thus, this investigation was established to achieve two major goals.…”