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In vitro study of the embolic characteristics of imipenem/cilastatin particles
Hiroki Nakamura1, Akira Yamamoto2, Takeshi Fukunaga2
1Departments of Radiology, Kawasaki Medical School, 577 , Matsushima, Kurashiki City, Okayama, Japan. h.nakamura@med.kawasaki-m.ac.jp.
Background:
Imipenem/cilastatin (IPM/CS) has long been administered intravenously as a carbapenem antibiotic. However, since this agent is poorly soluble in liquid, occasional reports have described its use as a short-acting, temporary embolic agent. The purpose of this study was to elucidate the characteristics of IPM/CS particles, which are thought to have pain-relieving effects against osteoarthritis-related pain, as an embolic agent.
Methods:
Three aspects of IPM/CS as an embolic agent were evaluated in vitro: particle size; particle shape; and change in particle size over time. For particle size, the long diameter was measured.
Results:
Mean particle size (n=244) was 29.2±12.0 µm (range, 1-60 µm). Shape (n=109) was round in 18.35%, elliptical in 11.93%, and polygonal in 69.72%, showing that most particles were polygonal. In observations of changes in particle size over time (n=9), particles had decreased to 75% of their original size at 82±10.7 min, 50% at 89.3±9.14 min, 25% at 91.3±8.74 min, complete dissolved at 91.8±9.02 min. A rapid shrinkage in diameter was seen in the final period.
Conclusions:
IPM/CS particles are ultrafine and the majority display a polygonal shape. This substance shows ultra-short embolic activity. This study revealed the characteristics of a substance that demonstrates an embolic effect not found in existing embolic materials.
Insights
Imipenem/cilastatin (IPM/CS) particles, though poorly soluble, show potential as an ultrafine, polygonal embolic agent with ultra-short activity. Their unique characteristics may offer novel therapeutic applications.
Area of Science:
- Pharmacology
- Biomaterials Science
- Interventional Radiology
Background:
- Imipenem/cilastatin (IPM/CS) is an intravenously administered carbapenem antibiotic.
- Poor solubility of IPM/CS has led to investigation as a temporary embolic agent.
- Potential pain-relieving effects for osteoarthritis-related pain are hypothesized.
Purpose of the Study:
- To elucidate the characteristics of imipenem/cilastatin (IPM/CS) particles as an embolic agent.
- To evaluate IPM/CS for its potential in pain management for osteoarthritis.
- To characterize the physical properties of IPM/CS relevant to embolic applications.
Main Methods:
- In vitro evaluation of IPM/CS particle properties.
- Measurement of particle size (long diameter) and shape.
- Assessment of particle size change over time to determine dissolution kinetics.
Main Results:
- Mean particle size was 29.2±12.0 µm, with a range of 1-60 µm.
- The majority of particles (69.72%) were polygonal in shape.
- Particles exhibited ultra-short embolic activity, with complete dissolution occurring around 91.8 minutes.
Conclusions:
- IPM/CS particles are ultrafine and predominantly polygonal.
- The substance demonstrates ultra-short embolic activity, distinguishing it from existing embolic materials.
- These findings suggest novel embolic potential for IPM/CS in therapeutic applications.
