دورية أكاديمية

DoE development of ionic gradient liposomes: A successful approach to improve encapsulation, prolong anesthesia and decrease the toxicity of etidocaine.

التفاصيل البيبلوغرافية
العنوان: DoE development of ionic gradient liposomes: A successful approach to improve encapsulation, prolong anesthesia and decrease the toxicity of etidocaine.
المؤلفون: Oliveira JD; Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas (Unicamp), Campinas, SP, Brazil., Rodrigues da Silva GH; Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas (Unicamp), Campinas, SP, Brazil., de Moura LD; Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas (Unicamp), Campinas, SP, Brazil., Göethel G; Toxicology Laboratory, Pharmacy Faculty, Federal University of Rio Grande do Sul (UFRGS), Porto Alegre, RS, Brazil., Papini JZB; São Leopoldo Mandic Institute and Research Center, Campinas-São Paulo, Brazil., Casadei BR; Physics Institute, University of São Paulo, Brazil., Ribeiro LNM; Institute of Biotechnology Federal University of Uberlândia (UFU), Uberlândia, MG, Brazil., Cabeça LF; Department of Chemistry, Federal Technological University of Parana, Londrina, PR, Brazil., Garcia SC; Toxicology Laboratory, Pharmacy Faculty, Federal University of Rio Grande do Sul (UFRGS), Porto Alegre, RS, Brazil., Martinez EF; São Leopoldo Mandic Institute and Research Center, Campinas-São Paulo, Brazil., Tofoli GR; São Leopoldo Mandic Institute and Research Center, Campinas-São Paulo, Brazil., de Paula E; Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas (Unicamp), Campinas, SP, Brazil. Electronic address: depaula@unicamp.br.
المصدر: International journal of pharmaceutics [Int J Pharm] 2023 Mar 05; Vol. 634, pp. 122672. Date of Electronic Publication: 2023 Feb 02.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Elsevier/North-Holland Biomedical Press Country of Publication: Netherlands NLM ID: 7804127 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1873-3476 (Electronic) Linking ISSN: 03785173 NLM ISO Abbreviation: Int J Pharm Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Amsterdam, Elsevier/North-Holland Biomedical Press.
مواضيع طبية MeSH: Liposomes*/chemistry , Anesthesia*, Rats ; Animals ; Etidocaine ; Anesthetics, Local ; Ions/chemistry
مستخلص: Etidocaine (EDC) is a long-acting local anesthetic of the aminoamide family whose use was discontinued in 2008 for alleged toxicity issues. Ionic gradient liposomes (IGL) are nanostructured carriers for which an inner/outer gradient of ions increases drug upload. This work describes IGL EDC , a formulation optimized by Design of Experiments, composed of hydrogenated soy phosphatidylcholine:cholesterol:EDC, and characterized by DLS, NTA, TEM/Cryo-TEM, DSC and 1 H NMR. The optimized IGL showed significant encapsulation efficiency (41 %), good shelf stability (180 days) and evidence of EDC interaction with the lipid bilayer (as seen by DSC and 1 H NMR results) that confirms its membrane permeation. In vitro (release kinetics and cytotoxicity) tests showed that the encapsulation of EDC into the IGL promoted sustained release for 24 h and decreased by 50 % the intrinsic toxicity of EDC to Schwann cells. In vivo IGL EDC decreased the toxicity of EDC to Caenorhabditis elegans by 25 % and extended its anesthetic effect by one hour, after infiltrative administration, at clinically used (0.5 %) concentration, in rats. Thus, this novel drug delivery system is a promise for the possible reintroduction of EDC in clinics, aiming at the control of operative and postoperative pain.
Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2023 Elsevier B.V. All rights reserved.)
فهرسة مساهمة: Keywords: Drug delivery; Etidocaine; Ionic gradient liposomes; Local anesthetics; Toxicity
المشرفين على المادة: 0 (Liposomes)
I6CQM0F31V (Etidocaine)
0 (Anesthetics, Local)
0 (Ions)
تواريخ الأحداث: Date Created: 20230204 Date Completed: 20230224 Latest Revision: 20230224
رمز التحديث: 20230224
DOI: 10.1016/j.ijpharm.2023.122672
PMID: 36738810
قاعدة البيانات: MEDLINE
الوصف
تدمد:1873-3476
DOI:10.1016/j.ijpharm.2023.122672