Initial Development and Characterization of PLGA Nanospheres Containing Ropivacaine

Abstract

Local anesthetics are able to induce pain relief by binding to the sodium channels of excitable membranes, blocking the influx of sodium ions and the propagation of the nervous impulse. Ropivacaine (RVC) is an amino amide, enantiomerically pure, local anesthetic largely used in surgical procedures, which present physico-chemical and therapeutic properties similar to those of bupivacaine but decreased toxicity and motor blockade. The present work focuses on the preparation and characterization of nanospheres containing RVC; 0.25% and 0.50% RVC were incorporated in poly(d,l-lactide-co-glycolide (PLGA) 50:50) nanospheres (PLGA-NS), prepared by the nanoprecipitation method. Characterization of the nanospheres was conducted through the measurement of pH, particle size, and zeta potential. The pH of the nanoparticle system with RVC was 6.58. The average diameters of the RVC-containing nanospheres was 162.7 ± 1.5 nm, and their zeta potentials were negative, with values of about −10.81 ± 1.16 mV, which promoted good stabilization of the particles in solution. The cytotoxicity experiments show that RVC-loaded PLGA-NS generate a less toxic formulation as compared with plain RVC. Since this polymer drugdelivery system can effectively generate an even less toxic RVC formulation, this study is fundamental due to its characterization of a potentially novel pharmaceutical form for the treatment of pain with RVC.

Preparation and Characterization of Poly(ε-Caprolactone) Nanospheres Containing the Local Anesthetic Lidocaine

“…Use of the nanoparticle system therefore substantially altered the drug release profile. Similar results have been reported for PLA and PLGA NCs loaded with benzocaine,23,24 ropivacaine‐loaded PLGA NSs,55 and bupivacaine‐loaded alginate/chitosan nanoparticles 56…”

From micro- to nanostructured implantable device for local anesthetic delivery

“…Nanospheres have been produced by O/W emulsion [90][91][92][93] and nanoprecipitation. [94][95][96][97][98][99] The first technique consists of making a solution (oily phase) in which the polymer and the drug are dissolved in organic solvents (typically methylene chloride or chloroform).…”

Poly(<small>DL</small>-lactide-<i>co</i>-glycolic acid) Nanoparticle Design and Payload Prediction: A Molecular Descriptor Based Study

“…Altogether 22 compounds reported in literature [43][44][45][46][47][48][49][50][51][52][53][54][55][56][57][58][59] including those reported from our laboratory were used for generation of analysis models (Table 2). Percentage mass loading was considered the property and used in logarithmic form.…”