The Potential of Atractylodin-Loaded PLGA Nanoparticles as Chemotherapeutic for Cholangiocarcinoma

Abstract

21 (4), 935-941 northeastern region of Thailand (Bridgewater et al., 2014). Standard chemotherapeutic regimens for the treatment of CCA are 5-fluorouracil (5-FU)-based and gemcitabine-based combination therapies with cytotoxic drugs or targeted therapy (

Enhanced oral bioavailability and biodistribution of atractylodin encapsulated in PLGA nanoparticle in cholangiocarcinoma

“…The increase of %EE from 50% to 84% (1.7‐fold) as well as %LE from 2.22% to 3.4% (1.5‐fold) was observed. The difference in physical properties of the current and the previously reported ATD‐PLGA formulation could be explained by the improved encapsulation capacity (and thus the larger size) 9 …”

“…The positive zeta potential value of ATD‐PLGA‐CS is due to the amino group of the CS over the negative charge of PLGA. Results from our previous study suggest a possible association between the concentration of PLGA and ATD on the particle size 9 . The advantages of the current ATD‐PLGA formulation over the previous formulation are the improvement of both physical and pharmaceutical properties of ATD.…”

“…Higher rate of ATD released from the CS coated formulation during the first 48 hours compared with PLGA‐CS could be due to increased solubility of CS in phosphate buffer and thus, rapid penetration into the polymer matrix. Previously reported studies of free ATD suggest relatively low antiproliferative activity of free ATD against CCA cells 7‐9 . Due to the superiority of physical and pharmaceutical properties of ATD‐PLGA over ATD‐PLGA‐CS, ATD‐PLGA was selected in this study for further evaluation of antiproliferative activity against CCA, as well as pharmacokinetic and biodistribution studies.…”

“…It was also found to suppress the production of heme‐oxygenase‐1(HO‐1), the activation of STAT1/3, and the downregulation of NF‐κB pathway in CCA 8 . However, as a lipid‐soluble compound, ATD is hydrophobic with poor pharmacokinetic properties 9 . Nanotechnology has successfully been applied to encounter this problem.…”

“…It is obtained from chitin by alkali hydrolysis and has a unique feature of adhering to the mucosal surface, stabilizing polymer NPs, and prolonging systemic circulation of the carried drug/compound. In our previous study, ATD‐loaded PLGA NPs with relatively potent antiproliferative activity against CCA were successfully prepared with acceptable physical and pharmaceutical properties 9 . The current study aimed to further optimize and characterize the ATD‐loaded PLGA NPs (ATD‐PLGA) and ATD‐loaded PLGA NPs coated with chitosan (ATD‐PLGA‐CS) to improve their physical (particle size, polydispersity index, and zeta potential) and pharmaceutical properties (encapsulation and loading efficiencies).…”