Dexmedetomidine and levobupivacaine co-loaded, transcriptional transactivator peptide modified nanostructured lipid carriers or lipid–polymer hybrid nanoparticles, which performed better for local anesthetic therapy?

Autor: Huaixin Xing, Li Min, Feng Shuo, Sun Yingui
Rok vydání: 2020
Předmět:
Transcriptional Activation
BALB 3T3 Cells
Polymers
medicine.drug_class
Skin Absorption
Pharmaceutical Science
Nanoparticle
cell penetrating peptides
Peptide
RM1-950
02 engineering and technology
levobupivacaine
030226 pharmacology & pharmacy
Rats
Sprague-Dawley
Mice
03 medical and health sciences
Transactivation
Organ Culture Techniques
0302 clinical medicine
medicine
Animals
Anesthetics
Local
Dexmedetomidine
chemistry.chemical_classification
Dose-Response Relationship
Drug
Chemistry
Local anesthetic
Chronic pain
dexmedetomidine
General Medicine
021001 nanoscience & nanotechnology
medicine.disease
Lipids
Nanostructures
Rats
Levobupivacaine
Regional anesthesia
Anesthesia
Nanoparticles
local anesthetic
lipids (amino acids
peptides
and proteins)
transdermal delivery
Therapeutics. Pharmacology
0210 nano-technology
Anesthesia
Local
Research Article
medicine.drug
Zdroj: Drug Delivery, Vol 27, Iss 1, Pp 1452-1460 (2020)
Drug Delivery
article-version (VoR) Version of Record
ISSN: 1521-0464
1071-7544
Popis: Local anesthetics (LAs) have been widely applied in clinic for regional anesthesia, postoperative analgesia, and management of acute and chronic pain. Nanostructured lipid carriers (NLCs) and lipid–polymer hybrid nanoparticles (LPNs) are reported as good choices for LA therapy. Transactivated transcriptional activator (TAT) was reported as a modifier for the topical delivery of drugs. In the present study, TAT modified, levobupivacaine (LEV) and dexmedetomidine (DEX) co-delivered NLCs (TAT-LEV&DEX-NLCs, T-L&D-N) and LPNs (TAT-LEV&DEX-LPNs, T-L&D-L) were designed and compared for the LA therapy. T-L&D-L exhibited better efficiency in improving the skin permeation, analgesic time, and pain control intensity than T-L&D-N both in vitro and in vivo. On the other side, T-L&D-N also improved the therapeutic effect of drugs to a large extent. These two systems both exhibited superiority in some respects. TAT modified LPNs are more promising platform for the long-term local anesthesia.
Databáze: OpenAIRE
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