А Study of Haloperidol Release from Polycomplex Nanoparticles Based on Eudragit^® Copolymers

Introduction. The development of polymer carriers for micro- and nanoscale drug delivery systems is an emerging area of modern pharmaceutical technology. One of the urgent needs in this area is the development of effective methods to study the drug release from these systems.

Aim. This work aimed to study the release of a model drug (MD) haloperidol from polycomplex nanoparticles prepared based on interpolyelectrolyte complexes (IPEC) using various methods.

Materials and methods. IPECs were prepared in the form of nanoparticles based on pharmaceutical polymers (Eudragit^® EPO and Eudragit^® L100-55). Size distribution of these nanoparticles were determined using dynamic light scattering on Zetasizer Nano-ZS equipment (Malvern Instruments, UK). The release of haloperidol was studied in a medium simulating an artificial nasal fluid using a vertical Franz diffusion cell (PermeGear, USA) as well as a modified USP IV method in a flow-through cell apparatus (DFZ II, Erweka, Germany).

Results and discussion. Statistically significant increase in the release of haloperidol from polycomplex nanoparticles in contrast with the control (haloperidol solution) is observed when using a vertical diffusion or Franz cell, after almost 2.5 hours. At the same time, it was not possible to study the release of drug using the flow-through cell method (USP IV), due, apparently, to the effect of crystallization of haloperidol on the surface of dialysis membranes in the Float-A-Lyzer^® G2 nanoadapters. The attempts to eliminate this effect and to improve the membrane permeability to haloperidol by adding surfactants (tween-80) and penetration enhancers (DMSO) were not successful.

Conclusion. Both methods are promising for studying the release of drugs from nanosized carriers; however, in the case of using poorly-soluble drugs, including haloperidol, the diffusion method using a vertical Franz cell is effective.

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