Implantable drug delivery devices for localized drug delivery
Inventors
Rairkar, Maithili • Desai, Pujan • Schuler, Carlos • Daud, Maxime • Rappaport, Maxime D. • Munster, Pamela • Maroney, John • McLaughlin, Margaret • Casab, Tobias H. • Hall, Keith • Thomas, Scott
Assignees
University of California San Diego UCSD • Alessa Therapeutics Inc
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Publication Number
US-11338119-B2
Publication Date
2022-05-24
Expiration Date
Abstract
Provided herein are drug implants comprising a therapeutically active agent for the treatment of disease in a subject. In some cases, the drug implant may comprise a polymer matrix and a therapeutically active agent disposed therein. Additionally provided are methods for manufacturing the drug implants and methods of treating diseases with the implants. In some cases, the drug implant may comprise bicalutamide, e.g., for use in the treatment of prostate cancer.
Core Innovation
An implant for insertion in or adjacent a human prostate is provided that includes bicalutamide dispersed in a liquid silicone rubber matrix. The liquid silicone rubber matrix has a Shore A hardness of at least 30 durometer, and the implant includes the bicalutamide in an amount of at least 30% w/w. The bicalutamide is characterized by a D90 of less than 15 microns.
The implant is configured to release bicalutamide at a rate between 1.2 μg/day and 95 μg/day following any initial burst of release. This release is maintained for at least 6 months after implantation of the implant in prostate tissue or in a tissue near a prostate.
Claims Coverage
The independent claim set centers on a prostate implant defined by a specific drug/polymer composition, particle-size constraint, mechanical hardness, high drug loading, and a bounded bicalutamide release profile for a minimum post-implantation period. The inventive features in the dependents further refine particle size, delivery configuration, and additional release constraints or extended duration.
Prostate implant comprising bicalutamide in liquid silicone rubber matrix
An implant for insertion in or adjacent a human prostate comprising bicalutamide dispersed in a liquid silicone rubber matrix.
Matrix hardness of at least 30 durometer
The liquid silicone rubber matrix has a Shore A hardness of at least 30 durometer.
At least 30% w/w bicalutamide loading
The implant comprises the bicalutamide in an amount of at least 30% w/w.
Bicalutamide D90 less than 15 microns
The bicalutamide has a D90 of less than 15 microns.
Sustained bicalutamide release rate for at least 6 months after implantation
The liquid silicone rubber matrix releases bicalutamide at a rate of between 1.2 μg/day and 95 μg/day, following any initial burst of release, for at least 6 months after implantation of the implant in a prostate tissue or a tissue near a prostate.
Median particle size of bicalutamide less than 10 microns
The bicalutamide in the implant has a median particle size of less than 10 microns.
Delivery through needle or catheter lumen
The implant is configured for delivery to the prostate tissue or the tissue near the prostate through a lumen of a needle or a catheter.
Cumulative release limit in 1% w/w SDS at day 60
The implant includes bicalutamide at about 30% w/w, with cumulative bicalutamide release in a 1% w/w sodium lauryl sulfate (SDS) solution being less than 500 μg at day 60.
Extended minimum duration release for at least 2 years
The implant includes a liquid silicone rubber matrix that releases bicalutamide at a rate between 0.6 μg/day and 95 μg/day after any initial burst, for at least 2 years after implantation in prostate tissue or tissue near a prostate.
Implant lacking a sheath
The implant is characterized by lacking a sheath.
Overall, the claims cover a bicalutamide-in-liquid-silicone-rubber prostate implant where key constraints are Shore A hardness, high bicalutamide loading, controlled particle size (D90 <15 microns and optionally median <10 microns), and a bounded bicalutamide release rate after initial burst for at least 6 months, with refinements for delivery configuration, additional cumulative release limitations in SDS at day 60, and extension to at least 2 years.
Stated Advantages
Sustained local release of bicalutamide for at least 6 months after implantation in prostate tissue or tissue near the prostate.
Bounded bicalutamide release rate between 1.2 μg/day and 95 μg/day following any initial burst of release.
Optionally extended sustained release for at least 2 years after implantation.
Controlled mechanical hardness of the liquid silicone rubber matrix (Shore A at least 30 durometer).
Controlled bicalutamide particle size (D90 less than 15 microns; median particle size less than 10 microns in dependent embodiments).
High bicalutamide loading (at least 30% w/w; about 30% w/w in some dependents).
Documented Applications
Implantable localized bicalutamide delivery by an implant inserted in or adjacent a human prostate, including delivery to prostate tissue or tissue near the prostate.
Sustained bicalutamide delivery for at least 6 months after implantation in prostate tissue or a tissue near a prostate.
Extended-duration delivery embodiments for at least 2 years after implantation in prostate tissue or tissue near a prostate.
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