title: Study on formulation variables of methotrexate loaded mesoporous MCM-41 nanoparticles for dissolution enhancement.
abstract: The aim of this study was to develop methotrexate loaded mesoporous MCM-41 nanoparticles for improved dissolution of methotrexate. The mesoporous MCM-41 nanoparticles act as carrier for drug and increase the solubility of the drug. In order to achieve this objective small pore size MCM-41 nanoparticles have been synthesized followed by drug loading process. The process of drug loading was optimized using full 3³ factorial design. With a view to obtain maximum drug loading three variables, concentration of drug solution, stirring rate, and drug:carrier ratio were optimized using a full 3³ factorial design. Using statistically designed experiments, the inclusion of methotrexate in MCM-41 nanoparticles was successfully carried out to obtain a drug loading of about 48%. X-ray powder diffraction and differential scanning calorimetry revealed the presence of methotrexate in amorphous form and FT-IR spectroscopy showed the presence of light interactions between the silicate silanols and the drug. The decrease of Brunauer, Emmett and Teller specific surface area and pore volume between free MCM-41 and the inclusion compound was the proof of the presence of methotrexate inside the mesopores. The inclusion compound was submitted to in vitro dissolution tests and a remarkable dissolution rate improvement was observed in comparison to the crystalline drug in all tested conditions.
authors: Pharmacy Department, M. S. University of Baroda, Centre of Relevance and Excellence in New Drug Delivery System, Vadodara 390002, Gujarat, India. nasirvadia@rediff.com
authors: Nasir
authors: N
authors: Vadia
authors: Sadhana
authors: S
authors: Rajput
mesh_terms: D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage / Q000032:analysis / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D004337:Drug Carriers / Q000008:administration & dosage / Q000032:analysis / Q000737:chemistry*; D004339:Drug Compounding; D005493:Folic Acid Antagonists / Q000008:administration & dosage / Q000032:analysis / Q000737:chemistry*; D007700:Kinetics; D008727:Methotrexate / Q000008:administration & dosage / Q000032:analysis / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D009994:Osmolar Concentration; D033362:Powder Diffraction; D012822:Silicon Dioxide / Q000737:chemistry*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013223:Statistics as Topic; D013499:Surface Properties
chemical_list: D000964:Antimetabolites, Antineoplastic; D004337:Drug Carriers; D005493:Folic Acid Antagonists; C509968:MCM-41; D012822:Silicon Dioxide; D008727:Methotrexate