An Injectable Oil-Based Depot Formulation of N-Acyloxymethyl Prodrug of Ropivacaine for Long-Acting Local Analgesia: Formulation Development and In Vitro/In Vivo Evaluation DOI Creative Commons
Xiaowei Liu,

Ruihan Zhao,

Peijie Xu

et al.

Pharmaceutics, Journal Year: 2024, Volume and Issue: 17(1), P. 37 - 37

Published: Dec. 30, 2024

Objectives: The development of novel long-acting injectables for local anesthetics is necessary to effectively manage the acute postoperative pain. aim this study was prepare an injectable oil-based formulation ropivacaine (ROP) prodrug (ropivacaine stearoxil, ROP-ST) and investigate pharmacokinetics pharmacodynamics after administration. Methods: A N-acyloxymethyl ROP, i.e., ROP-ST, synthesized its physicochemical properties such as log P, solubility stability characterized. soybean depot ROP-ST prepared, in-vitro release evaluated using “inverted-cup” method. Pharmacokinetic profiles tissue retention were investigated intramuscular administration in rats. analgesic efficacy assessed via a von Frey monofilaments test by measuring paw withdrawal thresholds. Results: structure ascertained with clear 1H NMR assignment accurate mass-to-charge ratio. high Log P value (9.16) demonstrated extremely low aqueous solubility, but biolabile when contact plasma or liver esterase. Intramuscular injection oil solution rats provided significantly higher mean residence time without very peak ROP. In pain model rats, into vicinity sciatic nerve right ankle controlled at least 72 h. Conclusions: ROP may provide new opportunity analgesia

Language: Английский

Latest advancements and trends in biomedical polymers for disease prevention, diagnosis, treatment, and clinical application DOI

Mingxia Jiang,

Huapan Fang, Huayu Tian

et al.

Journal of Controlled Release, Journal Year: 2025, Volume and Issue: 380, P. 138 - 174

Published: Feb. 5, 2025

Language: Английский

Citations

2
Long-acting injectables for the treatment of substance use disorder: a look ahead DOI

Sohyung Lee,

Nitin Joshi

Expert Opinion on Drug Delivery, Journal Year: 2025, Volume and Issue: unknown

Published: April 12, 2025

Language: Английский

Citations

0
Drug-caged drug: photoredox catalysis-enabled dual decaging of nitric oxide and local anesthetics for simultaneous antibacterial treatment and pain relief DOI Creative Commons
Jinming Hu, Jiqian Zhang,

Guihai Gan

et al.

Research Square (Research Square), Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 4, 2024

Abstract Bacterial infections often result in significant pain, negatively impacting patient outcomes and quality of life. Conventional therapies primarily focus on pathogen eradication but frequently overlook the associated thereby limiting their overall clinical effectiveness. Herein, we propose a 'drug-caged drug' strategy which secondary amine group local anesthetic tetracaine (TTC) is selectively caged by nitric oxide (NO), forming TTC-NO prodrug. The prodrug co-loaded with photocatalyst fac-Ir(ppy)3 into poly(ethylene glycol)-b-poly(ε-caprolactone) (PEG-b-PCL) micellar nanoparticles (TTC-NO@M), enabling dual uncaging TTC NO under mild visible light irradiation through photocatalytic mechanism. We demonstrate that TTC-NO@M exhibits combined antibacterial, anti-inflammatory, analgesic activities simultaneously releasing TTC. This effectively treats MRSA-infected mice both cutaneous wound septic arthritis models while alleviating infection-associated pain. work offers promising approach to address challenges bacterial

Language: Английский

Citations

0
An Injectable Oil-Based Depot Formulation of N-Acyloxymethyl Prodrug of Ropivacaine for Long-Acting Local Analgesia: Formulation Development and In Vitro/In Vivo Evaluation DOI Creative Commons
Xiaowei Liu,

Ruihan Zhao,

Peijie Xu

et al.

Pharmaceutics, Journal Year: 2024, Volume and Issue: 17(1), P. 37 - 37

Published: Dec. 30, 2024

Objectives: The development of novel long-acting injectables for local anesthetics is necessary to effectively manage the acute postoperative pain. aim this study was prepare an injectable oil-based formulation ropivacaine (ROP) prodrug (ropivacaine stearoxil, ROP-ST) and investigate pharmacokinetics pharmacodynamics after administration. Methods: A N-acyloxymethyl ROP, i.e., ROP-ST, synthesized its physicochemical properties such as log P, solubility stability characterized. soybean depot ROP-ST prepared, in-vitro release evaluated using “inverted-cup” method. Pharmacokinetic profiles tissue retention were investigated intramuscular administration in rats. analgesic efficacy assessed via a von Frey monofilaments test by measuring paw withdrawal thresholds. Results: structure ascertained with clear 1H NMR assignment accurate mass-to-charge ratio. high Log P value (9.16) demonstrated extremely low aqueous solubility, but biolabile when contact plasma or liver esterase. Intramuscular injection oil solution rats provided significantly higher mean residence time without very peak ROP. In pain model rats, into vicinity sciatic nerve right ankle controlled at least 72 h. Conclusions: ROP may provide new opportunity analgesia

Language: Английский

Citations

0