Abstract
Flexible liposomes (FLs) were developed as promising nano-carriers for anticancer drugs. Coating them with chitosan (CS) could improve their drug delivery properties. The aim of this study was to investigate the physicochemical characteristics, pharmacokinetics behavior, and cytotoxic efficacy of docetaxel (DTX)-loaded CS-coated FLs (C-FLs). DTX-loaded FLs and C-FLs were produced via thin-film evaporation and electrostatic deposition methods, respectively. To explore their physicochemical characterization, the particle size, zeta potential, encapsulation efficiency (EE%), morphology, and DTX release profiles were determined. In addition, pharmacokinetic studies were performed, and cytotoxic effect was assessed using colon cancer cells (HT29). Various FLs, dependent on the type of surfactant, were formed with particle sizes in the nano-range, 137.6 ± 6.3 to 238.2 ± 14.2 nm, and an EE% of 59–94%. Moreover, the zeta potential shifted from a negative to a positive value for C-FL with increased particle size and EE%, and the in vitro sustained-release profiles of C-FL compared to those of FL were evident. The optimized C-FL containing sodium deoxycholate (NDC) and dicetyl phosphate (DP) elicited enhanced pharmacokinetic parameters and cytotoxic efficiency compared to those of the uncoated ones and Onkotaxel®. In conclusion, this approach offers a promising solution for DTX delivery.
Highlights
Docetaxel (DTX) is one of the most effective anticancer drugs, and was used over the past several decades against breast, ovarian, lung, colorectal, and head and neck cancers [1,2]
flexible liposomes (FLs) were fabricated to increase drug loading and the flexibility of the membrane depending on their composition (Tables 1 and 2)
These results revealed that the chitosomes had a significantly higher EE% and DL% than liposomes
Summary
Docetaxel (DTX) is one of the most effective anticancer drugs, and was used over the past several decades against breast, ovarian, lung, colorectal, and head and neck cancers [1,2]. Many studies reported that flexible liposomes (FLs) are better carriers of drugs than conventional liposomes (CLs) [7]. FLs have flexible membranes due to the existence of edge activators such as Tween-80 and sodium deoxycholate [8,9]. These vesicles have the ability to cross pores that are smaller in size than their size, because lipid bilayers possess a higher curvature than CLs [10]. Positive surface-coated liposomes were designed to improve liposomal characterizations such as stability, sustained drug release, and effective targetability [11]
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