Development of High‐Drug‐Loading Nanoparticles

Abstract

research on developing nanoparticles with high drug loading (> 10 wt%) from the perspective of synthesis strategies, including post-loading, co-loading, and pre-loading. Based on these three different strategies, various nanoparticle systems with different materials and drugs are summarized and discussed in terms of their synthesis methods, drug loadings, encapsulation efficiencies, release profiles, stabilities, and their applications in drug delivery. The advantages and disadvantages of these strategies are presented with an objective of providing useful design rules for future development of high-drug-loading nanoparticles.

Bare Iron Oxide Nanoparticles as Drug Delivery Carrier for the Short Cationic Peptide Lasioglossin

“…For BION@LL complexes, this effect is more distinct: the determined hydrodynamic diameters are 1302 nm in PBS, 1070 nm in water, and 470 nm in HS. Therefore, in HS, the particles show diameters in the nanoscale <1000 nm and are better comparable with sizes of other iron-based drug carriers [46][47][48]. Still, the size is not in the ideal range of 10-100 nm.…”

“…The maximal reached drug loading after one washing step in both experiments is 15.2% ( Equation (S3) ). Other post-loaded nanocarriers where the interaction is also based on hydrophobic, electrostatic interactions, π-π stacking, or hydrogen bonding show drug loading between 11.8% and 68.1% depending on the drug and the material [ 46 ]. For iron-based systems, Qu et al achieved a loading of 9.8% to 11.8% of 10-Hydroxycamptothecin on polyethylene glycol-chitosan coated IONs [ 47 ].…”

“…In contrast, at pH 9 smaller agglomerates were formed, so at 0.25 g/L peptide the hydrodynamic diameter is between 0.50 and 1.70 µm ( Figure 4 b,c). Other iron post-loaded carriers show sizes between 100 and 600 nm [ 46 , 47 , 48 ]. In general, the ideal size for a nanoparticle-based drug delivery system is between 10 and 100 nm to achieve long blood circulation times and make cellular uptake possible [ 18 ].…”

“…Pharmaceuticals 2021, 14, x FOR PEER REVIEW 8 of 17 of other iron-based drug carriers [46][47][48]. Still, the size is not in the ideal range of 10-100 nm.…”

Green, scalable, low cost and reproducible flow synthesis of biocompatible PEG-functionalized iron oxide nanoparticles

“…5a). Based on the fluorescein absorbance peak height, the drug loading efficiency was estimated at 21% and the drug loading capacity was calculated at 15 wt% which is considered a high drug loading (>10%) 51 suitable for drug delivery applications. Fluorescein serves here as a proof-of-concept, illustrating that the Fe 3 O 4 NP-NDA-PEG-COOH can act as a flexible nanoparticle platform to which any molecule of interest with an amine group can be coupled to.…”