title: Aqueous core nanocapsules: a new solution for encapsulating doxorubicin hydrochloride.
abstract: In this study, we propose a new solution for the nanoencapsulation of hydrophilic anticancer drug, doxorubicin hydrochloride (DOX). The drug molecules are solubilized in the core of aqueous nanoreservoirs, so-called aqueous core nanocapsules (ACN) recently developed by our team, and dispersed in aqueous bulk media. Since it is well acknowledged that the nanoencapsulation of DOX has many advantages, like reducing the sides effects (e.g. cardiac toxicity), we propose through the present study a novel formulation solution for this purpose. After focusing on the formulation process for optimizing the drug encapsulation yield, the DOX-release profiles were followed up and analyzed. Different physicochemical and in vitro characterization were performed, and complement activation experiments. ACN were shown efficient to encapsulate DOX reaching yields as high as 80%, followed by a sustained release governed by a diffusion-controlled mechanism. The loaded nanocarriers showed low levels of complement activation, compatible with stealth properties. To summarize, this study brings out a new tool for the nanoencapsulation of hydrophilic anticancers and could open new doors for the administration of this particular class of drugs.
authors.affiliation: LUNAM Université, Université d'Angers, INSERM U1066-MINT - Micro et Nanomédecines Biomimétiques, IBS-CHU Angers , 4 rue Larrey, F-49933 Angers , France.
authors.forename: Sandy
authors.initials: S
authors.lastname: Vrignaud
authors.forename: Nicolas
authors.initials: N
authors.lastname: Anton
authors.forename: Catherine
authors.initials: C
authors.lastname: Passirani
authors.forename: Jean-Pierre
authors.initials: JP
authors.lastname: Benoit
authors.forename: Patrick
authors.initials: P
authors.lastname: Saulnier
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry* / Q000494:pharmacology; D055598:Chemical Phenomena; D003167:Complement Activation / Q000187:drug effects; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology; D004058:Diffusion; D004317:Doxorubicin / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry* / Q000494:pharmacology; D004339:Drug Compounding; D016503:Drug Delivery Systems / Q000009:adverse effects; D004355:Drug Stability; D004655:Emulsions; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D008899:Mineral Oil / Q000737:chemistry; D053769:Nanocapsules / Q000009:adverse effects / Q000737:chemistry*; D010316:Particle Size; D010420:Pentanes / Q000737:chemistry; D014677:Pharmaceutical Vehicles / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D012995:Solubility; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry
chemical_list: D000903:Antibiotics, Antineoplastic; D003692:Delayed-Action Preparations; D004655:Emulsions; D053769:Nanocapsules; D010420:Pentanes; D014677:Pharmaceutical Vehicles; D013501:Surface-Active Agents; D011092:Polyethylene Glycols; D004317:Doxorubicin; D008899:Mineral Oil; C067038:isopentane