Poly(d,l-lactide-co-glycolide)/montmorillonite nanoparticles for oral delivery of anticancer drugs.
This research developed a novel bioadhesive drug delivery system, poly(d,l-lactide-co-glycolide)/montmorillonite (PLGA/MMT) nanoparticles, for oral delivery of paclitaxel. Paclitaxel-loaded PLGA/MMT nanoparticles were prepared by the emulsion/solvent evaporation method. MMT was incorporated in the formulation as a matrix material component, which also plays the role of a co-emulsifier in the nanoparticle preparation process. Paclitaxel-loaded PLGA/MMT nanoparticles were found to be of spherical shape with a mean size of around 310 nm and polydispersity of less than 0.150. Adding MMT component to the matrix material appears to have little influence on the particles size and the drug encapsulation efficiency. The drug release pattern was found biphasic with an initial burst followed by a slow, sustained release, which was not remarkably affected by the MMT component. Cellular uptake of the fluorescent coumarin 6-loaded PLGA/MMT nanoparticles showed that MMT enhanced the cellular uptake efficiency of the pure PLGA nanoparticles by 57-177% for Caco-2 cells and 11-55% for HT-29 cells, which was dependent on the amount of MMT and the particle concentration in incubation. Such a novel formulation is expected to possess extended residence time in the gastrointestinal (GI) tract, which promotes oral delivery of paclitaxel.
Dong
Yuancai
Y
Department of Chemical and Biomolecular Engineering, National University of Singapore, 10 Kent Ridge Crescent, Singapore 119260, Singapore.
Feng
Si-Shen
SS
D000284:Administration, Oral; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000494:pharmacology; D001546:Bentonite / Q000737:chemistry*; D001672:Biocompatible Materials / Q000737:chemistry*; D018938:Caco-2 Cells; D003374:Coumarins / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D005456:Fluorescent Dyes / Q000494:pharmacology; D041981:Gastrointestinal Tract / Q000473:pathology; D019073:HT29 Cells; D006801:Humans; D066298:In Vitro Techniques; D019344:Lactic Acid / Q000737:chemistry; D018625:Microscopy, Atomic Force; D018613:Microscopy, Confocal; D036103:Nanotechnology; D017239:Paclitaxel / Q000494:pharmacology; D010316:Particle Size; D011098:Polyglactin 910 / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000737:chemistry; D011142:Polyvinyl Alcohol / Q000737:chemistry; D012997:Solvents / Q000737:chemistry; D013696:Temperature; D013997:Time Factors; D014961:X-Ray Diffraction
D000970:Antineoplastic Agents; D001672:Biocompatible Materials; D003374:Coumarins; D004337:Drug Carriers; D005456:Fluorescent Dyes; D011108:Polymers; D012997:Solvents; D001546:Bentonite; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011098:Polyglactin 910; D011142:Polyvinyl Alcohol; C030123:coumarin; D017239:Paclitaxel