Formulation and Evaluation of a Robust Drug Delivery System by Using Levofloxacin-Chitosan/Hydroxypropyl β-Cyclodextrin Nanoparticles

Beny      Baby; N.S.      Harsha; K.N.      Jayaveera; Abin      Abraham

Abstract

A total of six formulations (H1A, H1B, H1C, H1D, H1E and H1F) of Levofloxacin-chitosan/hydroxypropyl β-cyclodextrin nanoparticles were prepared by ionic gelation method. The particle size of the prepared nanoparticles varied between 191 and 623 nm and drug content ranged between 59.12 ± 0.22 and 72.89 ± 0.32 %. The drug entrapment efficiency differed between 60.12 ± 1.2 and 75.82 ± 2.2 %. The particles size of nanoparticles increased with increasing concentration of polymer matrix density and this may be due to the increased viscosity of the inner phase and decreased with increasing concentration of hydroxypropyl β-cyclodextrin. The results of drug entrapment efficiency indicated that, the entrapment efficiency increased with increasing concentration of chitosan. The complexation with the cyclodextrin permits a protection for sensitive drug and in vitro release profile observed for these nanoparticles characterized by an erratic drug release in the beginning and followed by a delayed release phase. Of the above six formulations, three formulations H1B, H1E and H1F followed the drug release in a controlled manner. All the selected formulations were best fitted to super case II transport drug release, according to this drug release mechanism could be due to increased plasticization at the relaxing boundary. Scanning electron microscopy indicated that the prepared nanoparticles were discrete, uniform and spherical with a smooth surface. The surface charge indicated that, the formation of nanoparticle depended dramatically on the concentration of free amino groups, which increase the surface charge of the nanoparticles. At the end of the accelerated stability study, the tested formulation showed almost same drug content, in vitro drug release and no color changes from that observed at the opening of the study.

Keywords: Surface charge, levofloxacin, nanoparticles, korsmeyer-peppas model, chitosan, particle size.

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