Scalable process to achieve LA injectable delivery of insoluble medicines

Sponsor(s)

None None

Partnerships

None None

Type of technology

Aqueous drug particle suspension

Administration route

Subcutaneous, Intramuscular

Development state and regulatory approval

Niclosamide

Pre-clinical

Not provided

Description

Nanoprecipitation technology to form redispersible solid drug nanoparticles (SDN) formulations that may be stored as solids, reconstituted with water and utilised as long-acting injectables to provide extended drug exposure, of otherwise highly insoluble drugs.

Technology highlight

This technology broadens the use of a highly insoluble drug molecule and generates high injectable concentrations of particles in an aqueous medium and to achieve extended release of medicines. The drug has very low bioavailability but IM injection leads to prolonged plasma exposure

Technology main components

Polymer (eg. hydroxypropyl methylcellulose), Surfactant (eg. Tween 20, Pluronic (r) F127), Sugar (eg. sucrose) Nanoprecipitation into water from Class3 solvents

Information on the raw materials sourcing, availability and anticipated price

readily available and low-price materials - selected from the FDA CDER list of Inactive Ingredients

Delivery device(s)

No delivery device

API desired features

Water-soluble molecules

Water-insoluble molecules

Small molecules

Niclosamide, nitazoxanide, atovaquone

Additional solubility data

Not provided

Additional stability data

Not provided

API loading: Maximum drug quantity to be loaded

50-75 wt%

API co-administration

1 single API :

LogP

Not provided

Scale-up prospects

The process is highly scalable

Tentative equipment list for manufacturing

spray-dryer

Manufacturing

Not provided

Specific analytical instrument required for characterization of formulation

dynamic light scattering (eg. Malvern Panalytical ZetaSizer Ultra Proton Correlation Spectroscope)

Proprietary excipients used

No proprietary excipient used

Novel excipients or existing excipients at a concentration above Inactive Ingredients Database (IID) for the specified route of administration

No novel excipient or existing excipient used

Residual solvents used

No residual solvent used

Other features of the technology

• Biodegradable
• Non-removable
• Room temperature storage
• At least 1 year shelf life

Release properties

Extended drug exposure for > 1 month from single administration

Injectability

injectable (IM or SC) - reconstitutable solid at the point of need

Safety

No safety issues identified during preclinical work

Stability

Drug substance is stable to terminal sterilisation by irradiation

Storage conditions and cold-chain related features

No cold chain requirement

Therapeutic area(s)

Use case(s)

Use of technology

Description

The present invention relates to solid compositions of pharmaceutically active compounds, aqueous dispersions derived from these compositions and processes for the preparation of these solid compositions and dispersions. The present invention also relates to pharmaceutical compositions derived from these solid compositions and dispersions, and their use in the treatment and/or prophylaxis of helminthic, protozoal, and viral infections.

Brief description

Not provided

Representative patent

WO2022101623 (A1)

Category

Process

Patent holder

University of Liverpool

Exclusivity

No exclusivity or licence in place

Expiration date

May 14, 2034

Status

Filed

Publications

<p><span style="color: rgb(33, 33, 33);">Hobson JJ , Savage AC , Dwyer AB , Unsworth C , Massam J , Arshad U , Pertinez H , Box H , Tatham L , Rajoli RKR , Neary M , Sharp J , Valentijn A , David C , Curley P , Liptrott NJ , McDonald TO , Owen A , Rannard SP . </span><a href="https://pubmed.ncbi.nlm.nih.gov/33885522/" rel="noopener noreferrer" target="_blank" style="color: rgb(33, 33, 33);">Scalable nanoprecipitation of niclosamide and in vivo demonstration of long-acting delivery after intramuscular injection</a><span style="color: rgb(33, 33, 33);">. Nanoscale. 2021 Apr 7;13(13):6410-6416. doi: 10.1039/d1nr00309g. Epub 2021 Mar 25. PMID: 33885522.</span></p>

The control of COVID-19 across the world requires the formation of a range of interventions including vaccines to elicit an immune response and immunomodulatory or antiviral therapeutics. Here, we demonstrate the nanoparticle formulation of a highly insoluble drug compound, niclosamide, with known anti SARS-CoV-2 activity as a cheap and scalable long-acting injectable antiviral candidate.

Additional documents

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Useful links

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	Collaborate for development Consider on a case by case basis, collaborating on developing long acting products with potential significant public health impact, especially for low- and middle-income countries (LMICs), utilising the referred to long-acting technology Not provided
	Share technical information for match-making assessment Provide necessary technical information to a potential partner, under confidentiality agreement, to enable preliminary assessment of whether specific medicines of public health importance in LMICs might be compatible with the referred to long-acting technology to achieve a public health benefit Not provided
	Work with MPP to expand access in LMICs In the event that a product using the referred to long-acting technology is successfully developed, the technology IP holder(s) will work with the Medicines Patent Pool towards putting in place the most appropriate strategy for timely and affordable access in low and middle-income countries, including through licensing Not provided

The CELT team at Liverpool are keen to work with partners who wish to scale and distribute products derived from the technology