An in vitro and in vivo study of gemcitabine-loaded albumin nanoparticles in a pancreatic cancer cell line

Abstract

Background and objectives Gemcitabine (Gem) is far from satisfactory as the first-line regimen for pancreatic cancer, and the emergence of albumin nanoparticles offers new hope for the delivery of Gem. In this study, Gem-loaded human serum albumin nanoparticles (Gem-HSA-NPs) were successfully synthesized, characterized, and tested on a BxPC-3 cell line both in vitro and in vivo. Materials and methods 4- N -myristoyl-gemcitabine (Gem-C14) was obtained first by coupling myristoyl with the 4-amino group of Gem. The Gem-HSA-NPs were then prepared by nanoparticle albumin-bound technology and characterized for particle size, zeta potential, morphology, encapsulation efficiency, drug-loading efficiency, and release characteristics. Using both in vitro and in vivo studies, Gem-C14 and Gem-HSA-NPs were tested on the human pancreatic cancer cell line BxPC-3. Results Gem-HSA-NPs showed an average particle size of 150±27 nm, and with an encapsulation rate of 82.99%±3.5% and a drug-loading rate of 10.42%±3.5%, they exhibited a favorable controlled- and sustained-release nature. In in vitro, Gem-C14 was equivalent in cytotoxicity to Gem. In in vivo, the Gem-HSA-NPs exhibited the strongest inhibitory effect on tumor growth but the lowest toxicity among the four groups. Conclusion The enhanced in vivo efficacy of Gem-HSA-NPs toward the pancreatic cancer cell line suggests their potential role for use in the clinical field.

Designing Two‐Dimensional Nanosheets for Improving Drug Delivery to Fucose‐Receptor‐Overexpressing Cancer Cells

“…The maximum percent LE and EE values were found to be 36.2±0.7 and 60.4±1.3 %, respectively. In previous works, the LE of GEM was found to be only between about 7–10 % . The high amount of GEM loaded onto the FGONS was via noncovalent interactions.…”

Antitumor Features of Vegetal Protein-Based Nanotherapeutics

“…Proteins, cellulose and starch or polysaccharides, such as alginates, are all natural polymers extracted from plants, microbes and animals [66,67]; while polyesters, polyanhydrides or polyamides are synthetic compounds that can be customized to provide the required mechanical and chemical properties for various applications [68]. Among natural polymers, proteins such as casein, albumin and silk are currently being used for anticancer purposes [69][70][71]. Plant proteins, such as zein and gliadins, have drawn great interest in the last decade because they have been used to develop various biocompatible nanocarriers for anticancer purposes [19].…”

Triple-functional albumin-based nanoparticles for combined chemotherapy and photodynamic therapy of pancreatic cancer with lymphatic metastases

“…21 Briefly, P@-HSA was mixed with pure water. Separately, Gem-C14 was dissolved in chloroform saturated with pure water.…”

“…19,20 However, due to low molecular weight and high solubility in water, the clinical benefits of Gem are compromised by its short plasma half-life and relative low concentration around tumor sites. 20 In previous work, 21 we have reported using NP albumin-bound (Nab) technique to prepare Gem-loaded human serum albumin (HSA) NPs (Gem-HSA-NPs), which exhibited satisfied inhibition effect with moderate toxicity both in vitro and in vivo. However, this single therapeutic approach remains compromising for completely curing cancer.…”