Lidocaine–Liposomes—A Promising Frontier for Transdermal Pain Management

Author:

Leon Maria Magdalena1,Maștaleru Alexandra1ORCID,Oancea Andra1ORCID,Alexa-Stratulat Teodora2,Peptu Cătălina Anișoara3,Tamba Bogdan-Ionel4ORCID,Harabagiu Valeria5ORCID,Grosu Cristina6,Alexa Anisia Iuliana7,Cojocaru Elena8ORCID

Affiliation:

1. Department of Medical Specialties I, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iaşi, Romania

2. Department of Medical Oncology–Radiotherapy, Faculty of Medicine, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iaşi, Romania

3. Department of Natural and Synthetic Polymers, Faculty of Chemical Engineering and Environmental Protection, “Gheorghe Asachi” Technical University of Iasi, 700050 Iasi, Romania

4. CEMEX Laboratory, “Grigore T. Popa” University of Medicine and Pharmacy, 700259 Iaşi, Romania

5. “Petru Poni” Institute of Macromolecular Chemistry, 700487 Iaşi, Romania

6. Department of Medical Specialties III, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iaşi, Romania

7. Department of Surgery II, Discipline of Ophthalmology, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iasi, Romania

8. Department of Morphofunctional Sciences I, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iaşi, Romania

Abstract

(1) Background: We aim to develop novel gel formulations for transdermal drug delivery systems in acute and inflammatory pain therapy. (2) Methods: We induced inflammation by the injection of λ-carrageenan on the hind paw of 80 Wistar male rats. The animals were randomized into eight groups of 10 rats each: C (placebo gel), E (EMLATM), L (lidocaine 2%), L-CD (lidocaine + cyclodextrin 2.5%), L-LP (lidocaine + liposomes 1.7%), L-CS (lidocaine + chitosan 4%), L-CSh (lidocaine + chitosan hydrochloride), and L-CS-LP (lidocaine + chitosan + liposomes). The behavior response was determined with a hot plate, cold plate, and algesimeter, each being performed at 30, 60, 120, 180, and 240 min after pain induction. At the end of the experiment, tissue samples were collected for histological assessment. (3) Results: L-LP had the greatest anesthetic effects, which was proven on the cold plate test compared to placebo and EMLATM (all p ≤ 0.001). L-CS-LP had a significant effect on cold plate evaluation compared to placebo (p ≤ 0.001) and on hot plate evaluation compared to EMLATM (p = 0.018). (4) Conclusions: L-LP is a new substance with a substantial analgesic effect demonstrated by the cold plate in the first 120 min. Further studies with more animals are needed to determine the maximum doses that can be applied for a better analgesia with minimum side effects.

Funder

Romanian National Authority for Scientific Research

Publisher

MDPI AG

Subject

General Medicine

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