Levobupivacaine Thermogel for Long-acting Analgesia

Abstract

The adequate management of analgesia, by pharmacological methods or not, is a great challenge. Local anesthetics are used for pain relief, mainly by parenteral, intramuscular, catheter, and other routes of administration. The use of in situ forming systems becomes an alternative for the control of pain. The present research investigates development of thermogels containing poloxamer and levobupivacaine. All formulations were prepared by the cold method; the compatibilities of the excipients were evaluated by DSC, rheology and viscosities, transition temperature, syringeability, release kinetics, and permeation. The compatibility of the tested excipients with the drug was initially observed; all formulations had a viscosity increase at 37°C. Different delivery rates were observed in both the release and permeation studies. The developed systems maintained the in vitro release of the drug for a long period, likely decreasing side effects in vivo and avoiding the need for supplementary analgesia by other routes.

Long-Acting Gel Formulations: Advancing Drug Delivery across Diverse Therapeutic Areas

“…Not specified [38] Achieving long-acting local analgesia. Intelligent hydrogel with bupivacaine microcrystals and calcium carbonate as a pH regulator.…”

“…These gels are primarily characterized by their temperature-sensitive properties, where they transition from a liquid to a gel state upon reaching body temperature. Notable materials in this category include N-isopropylacrylamide (NIPAm)-based gels, which solidify at body temperature [ 3 ], and Poloxamer 407, a thermosensitive polymer that forms a gel at physiological temperatures [ 8 , 37 , 38 , 61 ].…”

“…In vitro studies assessed the gel formulation for its drug release, permeation, and ease of syringe use. This could introduce a novel method for sustained pain management, potentially reducing the frequency of dosing and enhancing postoperative pain relief [ 38 ].…”

“…Research in neuroendocrine disorders and acromegaly has demonstrated a shift towards long-acting formulations, such as lanreotide Autogel, to ensure consistent and manageable treatment options for patients, with the goal of optimizing therapeutic effectiveness and improving quality of life [ 18 , 19 , 20 , 21 , 22 , 23 , 24 , 25 , 26 , 27 , 28 , 29 ]. The investigation into ophthalmic applications and pain management reveals a significant demand for long-acting gels to improve adherence to treatment, reduce the frequency of administration, and increase patient comfort in managing conditions like glaucoma and chronic pain [ 30 , 31 , 32 , 33 , 34 , 35 , 36 , 37 , 38 , 39 , 40 , 41 ].…”