Abstract
Preparation of sophisticated delivery systems for nanomedicine applications generally involve multi-step procedures using organic solvents. In this study, we have developed a simple self-assembling process to prepare docetaxel-loaded hyaluronic acid (HA) nanocapsules by using a self-emulsification process without the need of organic solvents, heat or high shear forces. These nanocapsules, which comprise an oily core and a shell consisting of an assembly of surfactants and hydrophobically modified HA, have a mean size of 130 nm, a zeta potential of −20 mV, and exhibit high docetaxel encapsulation efficiency. The nanocapsules exhibited an adequate stability in plasma. Furthermore, in vitro studies performed using A549 lung cancer cells, showed effective intracellular delivery of docetaxel. On the other hand, blank nanocapsules showed very low cytotoxicity. Overall, these results highlight the potential of self-emulsifying HA nanocapsules for intracellular drug delivery.
Highlights
Preparation of sophisticated delivery systems for nanomedicine applications generally involve multistep procedures using organic solvents
Dodecylamide-functionalized sodium hyaluronate (C12-hyaluronic acid (HA)) was synthesized by reacting tetrabutylammonium salt of HA with 1-aminododecane by using 2-bromo-1-ethyl pyridinium tetrafluoroborate as the amide coupling reagent
C12-HA was characterized by 1H NMR spectroscopy using a Bruker Avance 400 MHz NMR spectrometer
Summary
Preparation of sophisticated delivery systems for nanomedicine applications generally involve multistep procedures using organic solvents. We have developed a simple self-assembling process to prepare docetaxel-loaded hyaluronic acid (HA) nanocapsules by using a self-emulsification process without the need of organic solvents, heat or high shear forces These nanocapsules, which comprise an oily core and a shell consisting of an assembly of surfactants and hydrophobically modified HA, have a mean size of 130 nm, a zeta potential of −20 mV, and exhibit high docetaxel encapsulation efficiency. HA derivatives can be prepared with appropriate degree of substitution, without affecting its receptor targeting characteristics[12] These amphiphilic HA derivatives have already been used for the formation of micelles with the help of sonication[13,14,15] or electrostatic interactions[16] for the encapsulation of hydrophobic drugs like doxorubicin. Since these polymeric nanocapsules can be prepared without using organic solvents, heat or mechanical stirring, this offers an attractive method to incorporate thermosensitive molecules including peptides, proteins, and antibodies[17]
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