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Preparation Methods for Biodegradable Micro-Particles Containing Polypeptide Drugs – non-organic suspension – encapsulation techniques (08-34)

University of Arkansas for Medical Sciences
drug delivery - a novel and effective method for the microencapsulation of small peptides that allows their use and controlled release over a time frame of several months.

Mechanism of action

suspension-encapsulation technique

Full description

Applications:  drug delivery - a novel and effective method for the microencapsulation of small peptides that allows their use and controlled release over a time frame of several months.

The invention is based on a suspension-encapsulation technique that is readily controllable using a unique non-organic approach and is thus a very attractive drug delivery method for several products currently on the market. 

Currently, injection micro-particle depot formulations are produced using complex water-in-oil-water double emulsion or oil-water emulsion evaporation methods in an aqueous polyvinyl alcohol (87% - 90% hydrolyzed) solution.  These methods produce also produce very fine contaminating biodegradable micro-particles due to the presence of hydrophilic/hydrophobic regions of polyvinyl alcohol which cannot be separated.  Thus, the drug release properties cannot be reproducibly produced batch to batch with the proper release kinetics.  

The process described is simpler than prior art that utilizes organic polymeric materials such as poly (vinyl alcohol).  This process uses inorganic materials (e.g., hydroxyapatite) that can be easily removed after encapsulation has been completed.  The solidified micro-particles produced by this invention lack contaminating micro-particles and can be recovered by centrifuge and filtration much more reproducibility than prior methods.

The encapsulation efficiency and particle size can be varied depending on pH and mixing conditions.   Micro-particles ranging from 10 to 20 µm are suitable for subcutaneous injection.

This new process is simple to operate and reproducible.   It can be used for the encapsulation of LHRH drugs such as euprolide acetate (Lupron) and goserelin acetate (Zoladex), as well as other drugs.  In addition the process can be used to encapsulate octapeptide drugs, such as octreotide acetate (somatostatin analogue) for treating acromegaly and (Sandostatin LAR Depot, monthly) and risperdone for treating schizophrenia (Risperdal Costa, biweekly).

            Patent Pending

            Available for Exclusive Licensing

08-34 KIM

Development status

Early Stage

Patent information

U.S. Patent Application #12/221,096

Type of business relationship sought

Seeking commercial partner to license, further develop and commercialize this novel drug time release delivery technology.

Patent number

U.S. Patent Application #12/221,096

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