Poly(lactid-co-glycolide) nanoparticles loaded with ropivacaine: preparation and in vivo release in animals

doi:10.3969/j.issn.2095-4344.1535

Abstract

Abstract:

BACKGROUND: Synthesis of ropivacaine-loaded poly(lactid-co-glycolide) copolymer microsphere and its pharmacokinetics have been studied preliminarily, and we have confirmed its effectiveness. However, its large size and tissue simulation limit its application.

OBJECTIVE: To prepare poly(lactid-co-glycolide) nanoparticles loaded with ropivacaine and to study their particle characteristics, in vivo release characteristics and toxicity.

METHODS: Poly(lactid-co-glycolide) nanoparticles loaded with ropivacaine were prepared with poly(lactid-co-glycolide) as carriers by the water-in-oil-in-water emulsion solvent evaporation method. The micromeritic characteristics of the nanoparticles, such as the particle size, loading and entrapment efficiency were taken as parameters for evaluating. One hundred Kunming mice provided by the Laboratory Animal Centre of Southern Medical University in China were randomized into experimental and control groups, and then were subcutaneously injected with poly(lactid-co-glycolide) nanoparticles loaded with ropivacaine and 0.5% ropivacaine, respectively. Blood concentration monitoring was performed at 30 minutes, 1, 2, 3, 6, 10, 18, 24, 36 and 48 hours after administration. Drug release was observed in vivo, and pathological examinations were performed on the injection site and main body organs to study its tissue toxicity.

RESULTS AND CONCLUSION: The poly(lactid-co-glycolide) nanoparticles loaded with ropivacaine were prepared. The average particle size was (73.5±16.7) nm, the drug loading efficiency was (6.07±0.22)%, and the encapsulation efficiency was (62.73±4.83)%. The blood drug concentration in the experimental group was significantly lower than that in the control group (P=0.00). The drug retention time in the control and experimental groups was 6 and 48 hours, respectively, indicating the drug release sustained. The mice in the experimental group appeared with mild inflammation in the injection site, and no obvious pathological changes in major organs or necrotic cells occurred. To conclude, poly(lactid-co-glycolide) nanoparticles loaded with ropivacaine can be successfully prepared, and can achieve sustained-release in animals, and have low toxicity.

中国组织工程研究杂志出版内容重点：生物材料；骨生物材料; 口腔生物材料; 纳米材料; 缓释材料; 材料相容性；组织工程

Key words: Amides;, Drug Delivery Systems, Histocompatibility, Tissue Engineering

CLC Number:

R453

R318

Tian Hongju, Chen Zhongqing. Poly(lactid-co-glycolide) nanoparticles loaded with ropivacaine: preparation and in vivo release in animals[J]. Chinese Journal of Tissue Engineering Research, 2019, 23(6): 924-929.

Figures/Tables 5

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