A Strategy in The Design of Micellar Shape for Cancer Therapy

Abstract

For cancer therapy, optimization of carrier features is necessary to effectively deliver the targeting agents to tumor sites. Biodegradable poly(ether-anhydrides) micelles with filamentous, rod-like, and spherical shapes are fabricated. Their size and morphology are characterized by AFM and TEM. The encapsulation of doxorubicin hydrochloride (DOX) into the micelles does not impact their shape. The effect of micellar shape on the drug loading capacity and encapsulation efficiency, as well as in vitro drug release, is investigated. The cellular uptakes are evaluated using fluorescence microscopy, confocal laser scanning microscopy and flow cytometry on co-cultures of human hepatoblastoma cell line (HepG2), lung epithelial cancer cell line (A549), and human nasopharyngeal epidermoid carcinoma cells (KB) and fibroblast normal cells mixed with the different shapes of DOX-loaded micelles. The results show that the spherical DOX-loaded micelles are more readily taken up by all types of cells. The impact of micellar shape on in vivo antitumor function is also assessed from changes of tumor volume, body weight loss, and survival rate of 4T1-bearing mice and the immunostaining of tumor sections for analysis of tumor cell proliferation. The results reveal that the filamentous DOX-loaded micelles possess the highest safety to body and the best therapeutic effects to artificial solid tumors. Therefore, the filamentous shape is deemed the most suitable morphology for design and engineering of drug vehicles for cancer therapy.

Size, Shape, and Protein Corona Determine Cellular Uptake and Removal Mechanisms of Gold Nanoparticles

“…A number of researchers focused on studying the effects of size, shape, protein corona, and surface properties on the uptake of Au NPs . Chithrani et al had observed that the cellular uptake of citric acid ligand‐modified Au nanospheres strongly depended on the size and shape.…”

The Effect of the Hydrophilic/Hydrophobic Ratio of Polymeric Micelles on their Endocytosis Pathways into Cells

“…A better understanding of these endocytosis mechanisms can help us to develop drug delivery carriers with better targeting specificity, higher cellular uptake efficiency, and better bioavailability. Nevertheless, for nanocarriers there are so many factors that can influence the endocytosis pathways, such as particle size,21, 22 morphology,22–25 surface charge,22, 26 and so on. Among these factors, the ratio of hydrophilic and hydrophobic moieties of copolymers as drug carriers cannot be ignored either.…”

Electrospun Micelles/Drug‐Loaded Nanofibers for Time‐Programmed Multi‐Agent Release

“…Then, the Cur‐Ms solution were transferred into dialysis bag (MWCO: 1000) with DI water to remove the unloaded Curcumin before freeze‐drying. Drug loading content (LC) and encapsulation efficiency (EE) were measured with UV‐vis spectrophotometer (UV‐2550, Shimadzu, Japan) and calculated as previous report …”