title: The effects of particle properties on nanoparticle drug retention and release in dynamic minoxidil foams.
abstract: Nanocarriers may act as useful tools to deliver therapeutic agents to the skin. However, balancing the drug-particle interactions; to ensure adequate drug loading, with the drug-vehicle interactions; to allow efficient drug release, presents a significant challenge using traditional semi-solid vehicles. The aim of this study was to determine how the physicochemical properties of nanoparticles influenced minoxidil release pre and post dose application when formulated as a simple aqueous suspension compared to dynamic hydrofluoroalkane (HFA) foams. Minoxidil loaded lipid nanoparticles (LN, 1.4 mg/ml, 50 nm) and polymeric nanoparticles with a lipid core (PN, 0.6 mg/ml, 260 nm) were produced and suspended in water to produce the aqueous suspensions. These aqueous suspensions were emulsified with HFA using pluronic surfactant to generate the foams. Approximately 60% of the minoxidil loaded into the PN and 80% of the minoxidil loaded into the LN was released into the external aqueous phase 24h after production. Drug permeation was superior from the PN, i.e. it was the particle that retained the most drugs, irrespective of the formulation method. Premature drug release, i.e. during storage, resulted in the performance of the topical formulation being dictated by the thermodynamic activity of the solubilised drug not the particle properties.
authors.affiliation: Pharmaceutical Science Division, King's College London, 150 Stamford Street, London SE1 9NH, UK.
authors.forename: Yanjun
authors.initials: Y
authors.lastname: Zhao
authors.forename: Marc B
authors.initials: MB
authors.lastname: Brown
authors.forename: Stuart A
authors.initials: SA
authors.lastname: Jones
mesh_terms: D003692:Delayed-Action Preparations / Q000737:chemistry / Q000378:metabolism; D004337:Drug Carriers / Q000737:chemistry / Q000378:metabolism*; D006845:Hydrocarbons, Fluorinated / Q000737:chemistry / Q000378:metabolism*; D008914:Minoxidil / Q000737:chemistry / Q000378:metabolism*; D053758:Nanoparticles / Q000737:chemistry; D010316:Particle Size; D013535:Suspensions; D005466:Fluorocarbons
chemical_list: D003692:Delayed-Action Preparations; D004337:Drug Carriers; D006845:Hydrocarbons, Fluorinated; D008914:Minoxidil; D013535:Suspensions; C094049:apaflurane; D005466:Fluorocarbons