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. 1997 Jun;56(6):369–373. doi: 10.1136/ard.56.6.369

Technetium-99m labelled liposomes to image experimental arthritis

O Boerman 1, W Oyen 1, G Storm 1, M Corvo 1, L van Bloois 1, J W M van der Meer 1, F Corstens 1
PMCID: PMC1752389  PMID: 9227166

Abstract

OBJECTIVES—Liposomes sterically stabilised with polyethylene glycol (PEG) labelled with technetium-99m were tested for their ability to image adjuvant arthritis in a rat model.
METHODS—Adjuvant arthritis was induced in the ankle joint of the left hind foot by injection of Mycobacterium butyricum in Freund's incomplete adjuvant in the foot pad. Seven days later animals received the following radiopharmaceuticals labelled with 99mTc (a) non-PEG-liposomes, (b) PEG-liposomes or (c) non-specific human polyclonal IgG. For each of the radiopharmaceuticals the in vivo distribution of the radiolabel was monitored both scintigraphically as well as by counting the dissected tissues at two, eight, and 24 hours after injection.
RESULTS—The pharmacokinetics of the radiopharmaceuticals differed considerably (half life in the blood: PEG-liposomes (18 hours) > 99mTc-IgG (3 hours) > non-PEG liposomes (1 hour)). The inflamed focus was visualised with each of the agents. The uptake of each of the radiopharmaceuticals in the inflamed ankle region correlated with their residence time in the blood (inflamed joint uptake: PEG liposomes (1.15% injected dose (ID)/g)>99mTc-IgG (0.35% ID/g)>non-PEG-liposomes (0.05% ID/g)). Quantitative analysis of the images showed that the inflamed ankle to background ratio was highest with the PEG-liposomes (7.5 at 24 hours after injection), while with the other two agents this ratio did not exceed 4.
CONCLUSION—This study shows that 99mTc-labelled PEG-liposomes may be an excellent agent to visualise arthritis. Increased label uptake in the inflamed joint and increased target to background ratios can be obtained with PEG-liposomes because of their long circulating properties. In addition to their use as vehicles for scintigraphic imaging of arthritis PEG-liposomes might also be used for the site specific delivery of antirheumatic drugs.



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Figure 1  .

Figure 1  

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Blood concentration (A) and uptake in the inflamed ankle (B) of the 99mTc-labelled non-PEG-liposomes, PEG-liposomes, and 99mTc-IgG in rats with adjuvant arthritis in the left ankle. Five rats per group were used. Error bars represent SD.

Figure 2  .

Figure 2  

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Inflamed ankle to unaffected ankle ratio obtained with non-PEG-liposomes, PEG-liposomes, and 99mTc-IgG two hours, eight hours, and 24 hours after injection. The biodistribution data of five rats per group were used. Error bars represent SD.

Figure 3  .

Figure 3  

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Scintigrams of rats with adjuvant arthritis imaged 24 hours after injection of 99mTc-labelled PEG-liposomes, non-PEG-liposomes, and 99mTc-IgG.

Figure 4  .

Figure 4  

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Quantitative analysis of the scintigraphic images of rats (three rats per group) injected with 99mTc-labelled non-PEG-liposomes, PEG-liposomes, and 99mTc-IgG. The activity in the inflamed foot was assessed. The whole body activity at five minutes after injection was set at 100%ID. Error bars represent SD.

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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