title: Methotrexate loaded self stabilized calcium phosphate nanoparticles: a novel inorganic carrier for intracellular drug delivery.
abstract: Calcium phosphate is considered as a potential biomaterial for drug and gene delivery because of its excellent features. In this study, we reported the formulation and characterization of calcium phosphate nanoparticle containing anticancer drug, methotrexate (MTX). Calcium phosphate nanoparticles containing MTX (CaPi-MTX) were prepared by reverse micelles technique. CaPi-MTX nanoparticles of average size 262 +/- 47.64 nm with entrapment efficiency of 58.04 +/- 4.09% were obtained. The IR spectrum of CaPi-MTX showed characteristics of composite formation of hydroxyapatite with MTX. X-RD analysis revealed that, CaPi-MTX nanoparticles were crystalline and in hydroxyapatite form. TEM studies showed that CaPi-MTX nanoparticles were spherical in shape. In vitro release study of CaPi-MTX nanoparticles showed slow release of MTX at physiological pH (pH 7.4) while > 90% release was observed within 3-4 hours at endosomal pH (pH 5.5 and pH 6.0). Confocal microscopy was performed using CHO cell lines, showed intracellular localization of FITC-Dextran loaded calcium phosphate nanoparticles. Results indicate that prepared CaPi-MTX nanoparticles could serve the purpose for intracellular drug delivery.
authors.affiliation: Pharmacy Department, TIFAC-CORE in NDDS, Faculty of Technology and Engineering, G. H. Patel Building, Fateh Gunj, Vadodara 390002, India.
authors.forename: Ukawala
authors.initials: U
authors.lastname: Mukesh
authors.forename: Vijay
authors.initials: V
authors.lastname: Kulkarni
authors.forename: Rajyaguru
authors.initials: R
authors.lastname: Tushar
authors.forename: R S R
authors.initials: RS
authors.lastname: Murthy
mesh_terms: D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage / Q000737:chemistry; D001826:Body Fluids / Q000737:chemistry; D016466:CHO Cells; D002130:Calcium Phosphates / Q000737:chemistry*; D006224:Cricetinae; D003412:Cricetulus; D004058:Diffusion; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods; D007287:Inorganic Chemicals / Q000737:chemistry; D008422:Materials Testing; D008727:Methotrexate / Q000008:administration & dosage* / Q000737:chemistry*; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry*
chemical_list: D000964:Antimetabolites, Antineoplastic; D002130:Calcium Phosphates; D004337:Drug Carriers; D007287:Inorganic Chemicals; C020243:calcium phosphate; D008727:Methotrexate