Solubilization of rapamycin

Simamora, Pahala; Alvarez, Joan M.; Yalkowsky, Samuel H.

doi:10.1016/s0378-5173(00)00617-7

Cited by 183 publications

(147 citation statements)

References 10 publications

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“…After 48 h, only about 60% of the total drug was released from PEG 114 -b-PBC 30 micelles. However, rapamycin release from PEG 114 -b-PBC 8 and PEG 114 -b-PBC 17 micelles was much faster compared with PEG 114 -b-PBC 30 micelles. About 80% …”

Section: Preparation and Characterization Of Micellesmentioning

confidence: 91%

“…18,19 Briefly, 1 mg of rapamycin and 10 mg of PEG 114 -b-PBC 8 , PEG 114 -b-PBC 17 , or PEG 114 -b-PBC 30 were dissolved in 0.4 mL methylene chloride in a glass vial. The mixture was vortexed for 1 min to ensure homogeneity and the solvent was evaporated under N 2 flow to form the film.…”

Section: Preparation Of Rapamycin Micellesmentioning

confidence: 99%

“…All of the polymers showed narrow distribution in their molecular weights as revealed by the small value of PDI (1.03-1.15). A combined plot comparing the GPC chromatograms for PEG 114 -b-PBC 8 , PEG 114 -b-PBC 17 , and PEG 114 -b-PBC 30 was shown in Figure 2. The CMC of PEGb-PBC polymers were determined by fluorescence spectroscopy.…”

Section: Synthesis and Characterization Of Polymersmentioning

confidence: 99%

“…The CMC of PEGb-PBC polymers were determined by fluorescence spectroscopy. PEG 114 -b-PBC 8 , PEG 114 -b-PBC 17 , and PEG 114 -b-PBC 30 had low CMC values of 3.6 × 10 −3 , 7.9 × 10 −4 , and 4.0 × 10 −4 mg/mL, respectively ( Figure 4 and Table 1). The CMC of PEG 114 -b-PBC 30 was around 10-folds lower than those of PEG 114 -b-PBC 8 , indicating better stability of micelles prepared from PEG 114 -b-PBC 30 .…”

Section: Synthesis and Characterization Of Polymersmentioning

confidence: 99%

“…It can only slightly dissolve in some organic solvents such as N,N-dimethylacetamide, propylene glycol, glycerin, ethanol, polysorbate 80, and polyethylene glycol (PEG) 400. 8,9 Most of these solubilizing agents are harmful to the liver and kidney and can cause hemolysis and acute hypersensitivity reactions. 10,11 Therefore, novel approaches are needed to develop clinically acceptable injectable formulations of rapamycin.…”

Section: Introductionmentioning

confidence: 99%

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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: Preparation and Characterization Of Micellesmentioning

confidence: 91%

Section: Preparation Of Rapamycin Micellesmentioning

confidence: 99%

Section: Synthesis and Characterization Of Polymersmentioning

confidence: 99%

Section: Synthesis and Characterization Of Polymersmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

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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Drug‐Eluting Stents

Seidlitz

2019

In Vitro Drug Release Testing of Special Dosage Forms

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Biomimetic Nanotherapies: Red Blood Cell Based Core–Shell Structured Nanocomplexes for Atherosclerosis Management

et al. 2019

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Cardiovascular disease is the leading cause of mortality worldwide. Atherosclerosis, one of the most common forms of the disease, is characterized by a gradual formation of atherosclerotic plaque, hardening, and narrowing of the arteries. Nanomaterials can serve as powerful delivery platforms for atherosclerosis treatment. However, their therapeutic efficacy is substantially limited in vivo due to nonspecific clearance by the mononuclear phagocytic system. In order to address this limitation, rapamycin (RAP)‐loaded poly(lactic‐ co ‐glycolic acid) (PLGA) nanoparticles are cloaked with the cell membrane of red blood cells (RBCs), creating superior nanocomplexes with a highly complex functionalized bio‐interface. The resulting biomimetic nanocomplexes exhibit a well‐defined “core–shell” structure with favorable hydrodynamic size and negative surface charge. More importantly, the biomimetic nature of the RBC interface results in less macrophage‐mediated phagocytosis in the blood and enhanced accumulation of nanoparticles in the established atherosclerotic plaques, thereby achieving targeted drug release. The biomimetic nanocomplexes significantly attenuate the progression of atherosclerosis. Additionally, the biomimetic nanotherapy approach also displays favorable safety properties. Overall, this study demonstrates the therapeutic advantages of biomimetic nanotherapy for atherosclerosis treatment, which holds considerable promise as a new generation of drug delivery system for safe and efficient management of atherosclerosis.

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Solubilization of rapamycin

Cited by 183 publications

References 10 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

Drug‐Eluting Stents

Biomimetic Nanotherapies: Red Blood Cell Based Core–Shell Structured Nanocomplexes for Atherosclerosis Management

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