Electrospray Encapsulation of Hydrophilic and Hydrophobic Drugs in Poly(L‐lactic acid) Nanoparticles

Abstract

An electrospray method is developed for preparation of beclomethasone-dipropionate- and salbutamol-sulfate-loaded biodegradable poly(L-lactic acid) nanoparticles. Different set-up parameters for electrospraying are examined on particle size, and preparation conditions are optimized for producing spherical-drug-loaded nanoscale particles by controllable processing parameters. Polylactide (PLA)-drug nanoparticles with average diameters of around 200 nm are achieved in a stable cone-jet mode with a flow rate of 4 microL min(-1), polymer concentration of 1%, and ammonium hydroxide content of 0.05%. Morphology and size of the drug-polymer nanoparticles are analyzed by scanning electron microscopy and transmission electron microscopy. Changes in the crystallinity of the PLA polymer and the model drugs are detected by X-ray powder diffraction, and the absence of molecular interactions are confirmed by thermal analyses. The results indicate clearly that electrospraying is a potential method for producing polymeric nanoparticles and for encapsulating both hydrophilic and hydrophobic drugs efficiently into the nanoparticles.

Electrospraying, a Reproducible Method for Production of Polymeric Microspheres for Biomedical Applications

“…Secondly, the size distributions of particles fabricated by emulsion-based techniques tend to be inhomogeneous and broad, contributing to their lack of reproducibility, which in turn hinders their clinical use. Size distribution is a crucial parameter and it was shown that monodisperse size would enable a better control of release profiles and bioavailability of the loaded drug in the body [12,13]. Particle morphology is also important since it affects the internalization by non-phagocytic cells and the degradation of the polymer matrix which, in turn, determines the release kinetics of the loaded component.…”

“…In the context of drug loading, the bioactive molecule is mixed to the polymer solution before electrospraying and can further be emulsified [21]. Some studies which have been undertaken include encapsulation of hydrophilic and hydrophobic model drugs [12], model proteins [21][22][23][24][25], antibiotics [14,26] and anti-cancer drugs [13] in polylactide (PLA) [12,21], poly(lactic-co-glycolic acid) (PLGA) [24,26], polycaprolactone (PCL) [13,24] and chitosan [14].…”

“…During the electrospraying process, there are several parameters which all have an inter-dependent influence on viscosity, electrical conductivity, particle size, distribution, encapsulation efficiencies, loading capacities and in vitro release profiles [12,14,15,[21][22]24,27]. These parameters include voltage, distance to collector, needle gauge, flow rate, polymer, drug, solvent, surfactant, protein/polymer ratio and organic/aqueous ratio.…”

A one-step electrospray-based technique for modulating morphology and surface properties of poly(lactide-co-glycolide) microparticles using Pluronics®

“…[17][18][19] Poly(lactide-co-glycolide) (PLGA), polyhydroxybutyrate (PHB), poly(lactic acid) (PLA), and polycaprolactone (PCL) are examples of polymers that have been electrosprayed into micro-/nanoparticles for drug delivery applications. [20][21][22][23] While these polymers are biocompatible and biodegradable, their hydrophobicity can lead to the formation of unstable suspensions.…”

Release profile and characteristics of electrosprayed particles for oral delivery of a practically insoluble drug

“…Finally, high drug encapsulation efficiencies of around 90 per cent have been reported using electrospraying [29,30]. Several research groups have studied the use of electrospraying to prepare polymeric particles for drug-delivery purposes (including [31][32][33]). Drug-loaded microparticles have been produced in sizes ranging between 250 nm and 100 mm depending on the materials used and the processing parameters applied but are most often observed between 1 and 10 mm in diameter [34].…”