International journal of pharmaceutics
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Local anesthetics are substances able to induce pain relief by binding to the sodium channel of excitable membranes, blocking the influx of sodium ions and the propagation of nervous impulses. S(--) bupivacaine (S(--) bvc) is an amide type local anesthetic widely used in surgery and obstetrics for sustained peripheral and central nerve blockade. The present work focuses on the characterization of an inclusion complex of S(--) bvc in 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CD). ⋯ In addition, the study of the apparent stability constant by HPLC and solubility isotherm gives thermodynamics information about the interaction between S(--) bvc and HP-beta-CD. The application of the continuous variation method indicated the presence of a complex with 1:1 S(--) bvc:HP-beta-CD stoichiometry. This is an important study for the characterization of potential formulations to be used as therapeutic options for the treatment of pain.