Development of a novel probe sonication assisted enhanced loading of 5-FU in SPION encapsulated pectin nanocarriers for magnetic targeted drug delivery system.
A novel probe sonication method is developed to enhance loading of 5-fluorouracil (5-FU) in SPION encalsulated pectin nanocarriers of 100-150 nm size (referred here as MP-5FU nanocarriers). Probe sonication at 20 kHz for 60 min resulted in 5-FU loading efficiency of 33.2 ± 2.5%w/w and corresponding drug loading content of 18.2 ± 1.1 wt%. These are two folds higher than literature report of 5-FU loading in pectin. The enhanced loading is attributed to increase in the rate of dissolution of 5-FU in pectin due to transmission of kHz order sonic waves which increases temperature and pressure in the medium due to formation and collapsing of cavitation bubbles. The fabricated MP-5FU nanocarriers with saturation magnetization (43.13 emu/g) exhibited pH responsive, swelling controlled in vitro release of 5-FU in simulated gastric fluid at pH 1.2, in simulated intestinal fluid at pH 6.8, in simulated colonic fluid at pH 5.5, and in phosphate buffer solution at pH 7.4. The cytotoxicity of MP-5FU was measured by sulforhodamine B (SRB) assay and its GI(50) was more than 5mg/mL for cancer cells of HT-29 (colon) and Hep G2 (liver), while it was 3.7 mg/mL for cancer cells of MIA-PaCa-2 (Pancreas).
Department of Chemistry, Indian Institute of Technology Roorkee, Roorkee, India. duttafcy@iitr.ernet.in
Raj Kumar
RK
Dutta
Saurabh
S
Sahu
D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage / Q000494:pharmacology; D001826:Body Fluids / Q000737:chemistry / Q000378:metabolism; D045744:Cell Line, Tumor; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D005472:Fluorouracil / Q000008:administration & dosage / Q000494:pharmacology*; D019073:HT29 Cells; D056945:Hep G2 Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D058185:Magnetite Nanoparticles; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D010316:Particle Size; D010368:Pectins / Q000737:chemistry; D011312:Pressure; D012995:Solubility; D013010:Sonication; D013696:Temperature
D000964:Antimetabolites, Antineoplastic; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D058185:Magnetite Nanoparticles; D010368:Pectins; D005472:Fluorouracil