دورية أكاديمية
أعرض في EDS

Sustained Release from Ionic-Gradient Liposomes Significantly Decreases ETIDOCAINE Cytotoxicity.

التفاصيل البيبلوغرافية
العنوان: Sustained Release from Ionic-Gradient Liposomes Significantly Decreases ETIDOCAINE Cytotoxicity.
المؤلفون: Oliveira JD; Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - Unicamp, P.O. Box - 6109, CEP, Campinas, SP, 13083-862, Brazil., Ribeiro LNM; Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - Unicamp, P.O. Box - 6109, CEP, Campinas, SP, 13083-862, Brazil., Rodrigues da Silva GH; Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - Unicamp, P.O. Box - 6109, CEP, Campinas, SP, 13083-862, Brazil., Casadei BR; Department of Biophysics, Federal University of São Paulo - UNIFESP, São Paulo, São Paulo, Brazil., Couto VM; Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - Unicamp, P.O. Box - 6109, CEP, Campinas, SP, 13083-862, Brazil., Martinez EF; Department of Oral Pathology, 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, P.O. Box - 6109, CEP, Campinas, SP, 13083-862, Brazil. depaula@unicamp.br.
المصدر: Pharmaceutical research [Pharm Res] 2018 Oct 10; Vol. 35 (12), pp. 229. Date of Electronic Publication: 2018 Oct 10.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Kluwer Academic/Plenum Publishers Country of Publication: United States NLM ID: 8406521 Publication Model: Electronic Cited Medium: Internet ISSN: 1573-904X (Electronic) Linking ISSN: 07248741 NLM ISO Abbreviation: Pharm Res Subsets: MEDLINE
أسماء مطبوعة: Publication: 1999- : New York, NY : Kluwer Academic/Plenum Publishers
Original Publication: Stuttgart ; New York : Thieme, c1984-
مواضيع طبية MeSH: Anesthetics, Local/*administration & dosage , Anesthetics, Local/*toxicity , Cell Survival/*drug effects , Delayed-Action Preparations/*chemistry , Etidocaine/*administration & dosage , Etidocaine/*toxicity , Liposomes/*chemistry, Anesthetics, Local/pharmacokinetics ; Cell Line ; Cholesterol/chemistry ; Drug Liberation ; Etidocaine/pharmacokinetics ; Fibroblasts/cytology ; Fibroblasts/drug effects ; Humans ; Ions/chemistry ; Phosphatidylcholines/chemistry
مستخلص: Purpose: Etidocaine (EDC) is a long lasting local anesthetic, which alleged toxicity has restricted its clinical use. Liposomes can prolong the analgesia time and reduce the toxicity of local anesthetics. Ionic gradient liposomes (IGL) have been proposed to increase the upload and prolong the drug release, from liposomes.
Methods: First, a HPLC method for EDC quantification was validated. Then, large unilamellar vesicles composed of hydrogenated soy phosphatidylcholine:cholesterol with 250 mM (NH 4 ) 2 SO 4 - inside gradient - were prepared for the encapsulation of 0.5% EDC. Dynamic light scattering, nanotracking analysis, transmission electron microscopy and electron paramagnetic resonance were used to characterize: nanoparticles size, polydispersity, zeta potential, concentration, morphology and membrane fluidity. Release kinetics and in vitro cytotoxicity tests were also performed.
Results: IGL EDC showed average diameters of 172.3 ± 2.6 nm, low PDI (0.12 ± 0.01), mean particle concentration of 6.3 ± 0.5 × 10 12 /mL and negative zeta values (-10.2 ± 0.4 mV); parameters that remain stable during storage at 4°C. The formulation, with 40% encapsulation efficiency, induced the sustained release of EDC (ca. 24 h), while reducing its toxicity to human fibroblasts.
Conclusion: A novel formulation is proposed for etidocaine that promotes sustained release and reduces its cytotoxicity. IGL EDC can come to be a tool to reintroduce etidocaine in clinical use.
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معلومات مُعتمدة: 2014/14457-5 Fundação de Amparo à Pesquisa do Estado de São Paulo
فهرسة مساهمة: Keywords: drug-delivery; etidocaine; ionic gradient liposomes; local anesthesia
المشرفين على المادة: 0 (Anesthetics, Local)
0 (Delayed-Action Preparations)
0 (Ions)
0 (Liposomes)
0 (Phosphatidylcholines)
97C5T2UQ7J (Cholesterol)
I6CQM0F31V (Etidocaine)
تواريخ الأحداث: Date Created: 20181012 Date Completed: 20181113 Latest Revision: 20181114
رمز التحديث: 20231215
DOI: 10.1007/s11095-018-2512-4
PMID: 30306273
قاعدة البيانات: MEDLINE
الوصف
تدمد:1573-904X
DOI:10.1007/s11095-018-2512-4