Development of Hydrophilic Drug Encapsulation and Controlled Release Using a Modified Nanoprecipitation Method

Abstract

The improvement of the loading content of hydrophilic drugs by polymer nanoparticles (NPs) recently has received increased attention from the field of controlled release. We developed a novel, simply modified, drop-wise nanoprecipitation method which separated hydrophilic drugs and polymers into aqueous phase (continuous phase) and organic phase (dispersed phase), both individually and involving a mixing process. Using this method, we produced ciprofloxacin-loaded NPs by Poly (d,l-lactic acid)-Dextran (PLA-DEX) and Poly lactic acid-co-glycolic acid-Polyethylene glycol (PLGA-PEG) successfully, with a considerable drug-loading ability up to 27.2 wt% and an in vitro sustained release for up to six days. Drug content with NPs can be precisely tuned by changing the initial drug feed concentration of ciprofloxacin. These studies suggest that this modified nanoprecipitation method is a rapid, facile, and reproducible technique for making nano-scale drug delivery carriers with high drug-loading abilities

Design and Characterization of Spray-Dried Chitosan-Naltrexone Microspheres for Microneedle-Assisted Transdermal Delivery

“…Chitosan molecular weight (MW), polymer concentration, chitosan-NTX ratio, and spray-dryer feed flow rate were selected as critical formulation and process variables that may influence microsphere properties. Chitosan MW and concentration were selected because increased polymer MW and concentration have been shown to influence particle size and drug encapsulation efficiency [ 20 ], chitosan-NTX ratio was chosen as it impacts drug-loading capacity [ 21 , 22 ], and feed flow rate was selected for its proven influence on parameters such as yield and particle size in a spray-drying process [ 23 ]. Each variable was tested at 3 levels in a randomized 27-experiment Box Behnken design ( Table 1 ), with variables at level −1, 0, and +1 depicting low, medium, and high levels, respectively ( Table 2 ).…”

PLGA-based drug delivery system for combined therapy of cancer: research progress

“…Phase separation technology and nano-precipitation method are also methods to obtain PLGA micro/ nanoparticle with controllable release ability by simple preparation process [40,41]. In addition, the nanoprecipitation method can complete the preparation of particles in one step, and it is simpler and more effective than emulsification method to encapsulate drugs [42].The salting-out method is an improved emulsification technique, which is suitable for high-concentration polymer solutions and is beneficial to the encapsulation of heat-sensitive drugs [43]. Another spray drying method is also suitable for packaging heat-sensitive substances, and it is the preferred method for removing organic solvents [44][45][46].…”

The Synthesis, Characterization and Applications of Polyhydroxyalkanoates (PHAs) and PHA-Based Nanoparticles

“…Anesthetics, antibiotics, anti-inflammatory agents, anticancer agents, antineoplastic agents, hormones, hydrogels, steroids, and vaccines have all been delivered using PHA-based nanoparticles ( Table 2 ) [ 246 , 247 ]. Hydrophobic PHA nanoparticles can be modified to encapsulate hydrophobic drugs as well as hydrophilic drugs [ 248 ]. Curcumin, a hydrophobic compound, was successfully loaded onto PHA-based nanoparticles, which were smooth and spherically shaped with sizes ranging from 300 to 500 nm.…”