Anhydrous nanoprecipitation for the preparation of nanodispersions of tenofovir disoproxil fumarate in oils as candidate long-acting injectable depot formulations

Hobson, James J.; Curley, Paul; Savage, Alison C.; Al-khouja, Amer; Siccardi, Marco; Flexner, Charles; Meyers, Caren L. Freel; Owen, Andrew; Rannard, Steve

doi:10.1039/c9na00529c

“…This drug is only used in veterinary medicine, but the system might be applicable for other drugs used in humans. With the aim of preventing moisture contact to hydrophilic APIs during formulation, a complete anhydrous nanoprecipitation method for the hydrophilic drug disoproxil fumarate was recently reported by Hobson and coworkers [45]. The nanoprecipitates were subsequently dispersed in different oils intended for i.m.…”

Section: Oil-based Solutionsmentioning

confidence: 99%

Injectable Lipid-Based Depot Formulations: Where Do We Stand?

Rahnfeld

¹

,

Luciani

²

2020

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The remarkable number of new molecular entities approved per year as parenteral drugs, such as biologics and complex active pharmaceutical ingredients, calls for innovative and tunable drug delivery systems. Besides making these classes of drugs available in the body, injectable depot formulations offer the unique advantage in the parenteral world of reducing the number of required injections, thus increasing effectiveness as well as patient compliance. To date, a plethora of excipients has been proposed to formulate depot systems, and among those, lipids stand out due to their unique biocompatibility properties and safety profile. Looking at the several long-acting drug delivery systems based on lipids designed so far, a legitimate question may arise: How far away are we from an ideal depot formulation? Here, we review sustained release lipid-based platforms developed in the last 5 years, namely oil-based solutions, liposomal systems, in situ forming systems, solid particles, and implants, and we critically discuss the requirements for an ideal depot formulation with respect to the used excipients, biocompatibility, and the challenges presented by the manufacturing process. Finally, we delve into lights and shadows originating from the current setups of in vitro release assays developed with the aim of assessing the translational potential of depot injectables.

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Stable Polymer Nanoparticles with Exceptionally High Drug Loading by Sequential Nanoprecipitation

Liu

¹

,

Yang

²

,

Baby

³

et al. 2020

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Poor solubility often leads to low drug efficacy. Encapsulation of water‐insoluble drugs in polymeric nanoparticles offers a solution. However, low drug loading remains a critical challenge. Now, a simple and robust sequential nanoprecipitation technology is used to produce stable drug‐core polymer‐shell nanoparticles with high drug loading (up to 58.5 %) from a wide range of polymers and drugs. This technology is based on tuning the precipitation time of drugs and polymers using a solvent system comprising multiple organic solvents, which allows the formation of drug nanoparticles first followed by immediate precipitation of one or two polymers. This technology offers a new strategy to manufacture polymeric nanoparticles with high drug loading having good long‐term stability and programmed release and opens a unique opportunity for drug delivery applications.

show abstract

Stable Polymer Nanoparticles with Exceptionally High Drug Loading by Sequential Nanoprecipitation

Liu

¹

,

Yang

²

,

Baby

³

et al. 2020

View full text Add to dashboard Cite

Poor solubility often leads to low drug efficacy. Encapsulation of water‐insoluble drugs in polymeric nanoparticles offers a solution. However, low drug loading remains a critical challenge. Now, a simple and robust sequential nanoprecipitation technology is used to produce stable drug‐core polymer‐shell nanoparticles with high drug loading (up to 58.5 %) from a wide range of polymers and drugs. This technology is based on tuning the precipitation time of drugs and polymers using a solvent system comprising multiple organic solvents, which allows the formation of drug nanoparticles first followed by immediate precipitation of one or two polymers. This technology offers a new strategy to manufacture polymeric nanoparticles with high drug loading having good long‐term stability and programmed release and opens a unique opportunity for drug delivery applications.

show abstract

Anhydrous nanoprecipitation for the preparation of nanodispersions of tenofovir disoproxil fumarate in oils as candidate long-acting injectable depot formulations

Abstract: The facile formation of drug nanoparticles in injectable/ingestible oils, of water-soluble antiretroviral tenofovir disoproxil fumarate, using a novel nanoprecipitation is presented with studies showing drug release into relevant aqueous media.

Cited by 5 publications

References 39 publications

Injectable Lipid-Based Depot Formulations: Where Do We Stand?

Injectable Lipid-Based Depot Formulations: Where Do We Stand?

Stable Polymer Nanoparticles with Exceptionally High Drug Loading by Sequential Nanoprecipitation

Stable Polymer Nanoparticles with Exceptionally High Drug Loading by Sequential Nanoprecipitation

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