Evaluation of rapamycin chemical stability in volatile-organic solvents by HPLC

Ricciutelli, Massimo; Martino, Piera Di; Barboni, Luciano; Martelli, Sante

doi:10.1016/j.jpba.2006.02.009

Cited by 18 publications

(11 citation statements)

References 20 publications

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“…Rapamycin concentration was determined by reversephase high-performance liquid chromatography (RP-HPLC) as previously described with slight modifications, 20 using CLC-ODS-18 column (5 :m, 4.6 × 150 mm; Waters Corporation, Milford, MA) maintained at 25 • C, with an ultraviolet detector at 277 nm. The mixture of 80% methanol and 20% water (v/v) was used as a mobile phase, and delivered at a flow rate of 1.0 mL min −1 .…”

Section: Drug Loading and In Vitro Release Profilesmentioning

confidence: 99%

Poly(ethylene glycol)-Block-Poly(2-methyl-2-benzoxycarbonyl-propylene Carbonate) Micelles for Rapamycin Delivery: In Vitro Characterization and Biodistribution

Mahato

2011

Journal of Pharmaceutical Sciences

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Our objective was to synthesize an amphiphilic diblock copolymer for micellar delivery of rapamycin. Poly(ethylene glycol)-block-poly(2-methyl-2-benzoxycarbonyl-propylene carbonate) (PEG-b-PBC) with different hydrophobic core lengths were synthesized from methoxy poly(ethylene glycol) and 2-methyl-2-benzoxycarbonyl-propylene carbonate through ring-opening polymerization using 1,8-diazabicycloundec-7-ene as a catalyst. The critical micelle concentration of PEG-b-PBC was around 10 −8 M and depends on the hydrophobic core length. Rapamycin was effectively incorporated into micelles and drug loading increased with increasing hydrophobic core length, with maximal drug loading of 10% (w/w, drug/polymer), drug loading efficiency of about 85%, and mean particle size of around 70 nm. The drug release profile was also dependent on the hydrophobic core length and the drug release from PEG 114 -b-PBC 30 micelles was the slowest. We also determined the toxicity of rapamycin micelles on insulinoma (INS-1E) $-cells and human islets. Encapsulation of rapamycin into PEG-b-PBC micelles reduced its toxicity. Biodistribution of rapamycin-loaded PEG-b-PBC micelles was determined after systemic administration into mice. Rapamycin-loaded PEG-b-PBC micelles showed little difference in pharmacokinetics and biodistribution characteristics in mice compared with rapamycin carrying nanosuspension. In conclusion, rapamycin formulated with PEG-b-PBC micelles showed significantly reduced toxicity on INS-1E $-cells and human islets, but had similar biodistribution profiles as those of nanosuspensions.

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Section: Drug Loading and In Vitro Release Profilesmentioning

confidence: 99%

Poly(ethylene glycol)-Block-Poly(2-methyl-2-benzoxycarbonyl-propylene Carbonate) Micelles for Rapamycin Delivery: In Vitro Characterization and Biodistribution

Mahato

2011

Journal of Pharmaceutical Sciences

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“…Sirolimus (rapamycin) is a carboxylic lactone-lactam macrolide derived from an actinomycete (Streptomyces hygroscopicus), and the bulk powder consists of three isomeric forms (-α, -β and -γ). The chemical stability of the drug molecule appears to be sensitive to various factors such as pH (27) and organic solvents (28). Obviously, the fusion process of sirolimus polymeric microparticles using infrared radiation could have an impact on chemical stability and consequently alter the stent's immunosuppressive capability.…”

Section: Edpdt and Fusion Processmentioning

confidence: 99%

“…In this case, bulk sirolimus powder was fused for 1 min under identical conditions to the coated stents (100°C ). Sirolimus decomposition studies have been reported in the literature (28,29) but not under heat stress. In these cases, sirolimus degradation has been related to the trans and cis variations.…”

Section: Edpdt and Fusion Processmentioning

confidence: 99%

The Application of Electrostatic Dry Powder Deposition Technology to Coat Drug-Eluting Stents

et al. 2009

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“…Inhibitors of mTOR were mainly analysed in biological matrices even if some methods were published for their determination in solution or in pharmaceutical formulations, as in the case of stability studies or for quality control purposes. [567][568][569][570] Their narrow therapeutic window and highly variable blood levels (for the same administered dose) make mTOR inhibitors analysis in whole blood essential (mTOR inhibitors are concentrated in the red blood cells). In recent years, many analytical methods have been reported for the analysis of mTOR inhibitors in biological samples.…”

Section: Mtor Inhibitorsmentioning

confidence: 99%

Antineoplastic drugs and their analysis: a state of the art review

Guichard

Guillarme

Bonnabry

et al. 2017

Analyst

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The number of patients suffering from cancer is constantly increasing and, consequently, the number of different chemotherapy treatments administered is increasing. Given the high reactivity and toxicity of antineoplastic drugs, analytical methods are required in all pharmaceutical fields, from drug development to their elimination in wastewater; including formulation quality control, environment and human exposure and therapeutic drug monitoring. The aim of this paper is to provide an overview of the analytical methods available for the determination of antineoplastic drugs in different matrices such as pharmaceutical formulations, biological and environmental samples. The applicability and performance of the reported methods will be critically discussed, with focus on the most commonly used antineoplastic drugs. Only conventional compounds and small molecules for targeted therapy will be considered in the present review.

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Evaluation of rapamycin chemical stability in volatile-organic solvents by HPLC

Cited by 18 publications

References 20 publications

Poly(ethylene glycol)-Block-Poly(2-methyl-2-benzoxycarbonyl-propylene Carbonate) Micelles for Rapamycin Delivery: In Vitro Characterization and Biodistribution

Poly(ethylene glycol)-Block-Poly(2-methyl-2-benzoxycarbonyl-propylene Carbonate) Micelles for Rapamycin Delivery: In Vitro Characterization and Biodistribution

The Application of Electrostatic Dry Powder Deposition Technology to Coat Drug-Eluting Stents

Antineoplastic drugs and their analysis: a state of the art review

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