Dsm IP Assets B.v.

George Mihov

Guy Draaisma

Jens Christoph Thies

Silvana Rensina Antonnietta Di Silvestre

Tristan Handels

John Andrew Zupancich

Mirian Hendrika Jacoba Gillissen-Van Der Vight

Astrid Franken

Silvana Rensina Silvestre Di

Kenneth Alan Messier

Julien Francois Berard

Detlef Olaf Schumann

Soazig Claude Marie Delamarre

Di Silvana Rensina Antonnietta Silvestre

Detlef Olaf Alexander Schumann

The present invention relates to a drug delivery system comprising a core and a shell in which the core comprises a hydrolytically degradable polymer X which polymer backbone comprises pendant ester and acid functionalities and in which the shell comprises a hydrolytic degradable polymer Y. The hydrolytic degradable polymers X and Y are different polymers. Polymer X further comprises amino-acids in the polymer backbone and degrades via zero order degradation kinetics for a period of at least 3 months. Polymer Y degrades via auto-acceleration degradation kinetics.

Drug delivery system for delivery of acid sensitivity drugs

The present inventioN relates to fibers comprising a polyesteramide (PEA) having a chemical formula described by structural formula (IV), wherein &#x2212;m+p varies from 0.9-0.1 and q varies from 0.1 to 0.9, &#x2212;m+p+q=1 whereby m or p could be 0, &#x2212;n is about 5 to about 300; (pref. 50-200), &#x2014;Ris independently selected from the group consisting of (C-C) alkylene or (C-C) alkenylene and combinations thereof; &#x2014;Rand Rin a single backbone unit m or p, respectively, are independently selected from the group consisting of hydrogen, (C-C)alkyl, (C-C)alkenyl, (C-C)alkynyl, (C-C)aryl, &#x2014;(CH)SH, &#x2014;(CH)S(CH), &#x2014;CHOH, &#x2014;CH(OH)CH, &#x2014;(CH)NH+, &#x2014;(CH)NHC(&#x2550;NH+)NH, &#x2014;CHCOOH, &#x2014;(CH)COOH, &#x2014;CH&#x2014;CO&#x2014;NH, &#x2014;CHCH&#x2014;CO&#x2014;NH, &#x2014;CHCHCOOH, CH&#x2014;CH&#x2014;CH(CH)&#x2014;, (CH)&#x2014;CH&#x2014;CH&#x2014;, HN&#x2014;(CH)&#x2014;, Ph-CH&#x2014;, CH&#x2550;C&#x2014;CH&#x2014;, HO-p-Ph-CH&#x2014;, (CH)&#x2014;CH&#x2014;, Ph-NH&#x2014;, NH&#x2014;(CH)&#x2014;C&#x2014;, NH&#x2014;CH&#x2550;N&#x2014;CH&#x2550;C&#x2014;CH&#x2014;. &#x2014;Ris selected from the group consisting of (C-C)alkylene, (C-C)alkenylene, alkyloxy or oligoethyleneglycol, &#x2014;Ris selected from bicyclic-fragments of 1,4:3,6-dianhydrohexitols of structural formula (III); &#x2014;Ris selected from the group consisting of (C-C)aryl (CC)alkyl, &#x2014;Ris &#x2014;(CH)4-; whereby a is at least 0.05 and b is at least 0.05 and a+b=1. 

Fibers comprising polyesteramide copolymers for drug delivery

The present disclosure relates to fibers implantable in the body of a human or animal and processes for manufacturing such a fiber. The fiber undergoes a reduction in surface area to volume ratio of a factor of 1.05-10 upon injection in the human or animal body. In an embodiment, a process for manufacturing a fiber comprises extruding a biodegradable polymer into a fiber capable of fitting in a syringe needle of at least 25 Gauge, and cooling the fiber below its dry glass transition temperature while the fiber is under tension.

Fiber comprising a biodegradable polymer

The present invention relates to a poly (ester amide) (PEA) having a chemical formula described by structural formula (IV), wherein m+p varies from 0.9-0.1 and q varies from 0.1 to 0.9 m+p+q=1 whereby m or p could be 0 n is about 5 to about 300; (pref. 50-200) Ris independently selected from the group consisting of (C-C) alkylene, (C-C) alkenylene, &#x2014;(R&#x2014;CO&#x2014;O&#x2014;R&#x2014;O&#x2014;CO&#x2014;R)&#x2014;, &#x2014;CHR&#x2014;O&#x2014;CO&#x2014;R&#x2014;COOCR&#x2014; and combinations thereof; Rand Rin a single backbone unit m or p, respectively, are independently selected from the group consisting of hydrogen, (C-C)alkyl, (C-C)alkenyl, (C-C)alkynyl, (C-C)aryl, (C-C)alkyl, &#x2014;(CH)SH, &#x2014;(CH)S(CH), &#x2014;CHOH, &#x2014;CH(OH)CH, &#x2014;(CH)NH+, &#x2014;(CH)NHC(&#x2550;NH+)NH, &#x2014;CHCOOH, &#x2014;(CH)COOH, &#x2014;CH&#x2014;CO&#x2014;NH, &#x2014;CHCH&#x2014;CO&#x2014;NH, &#x2014;CHCHCOOH, CH&#x2014;CH&#x2014;CH(CH)&#x2014;, (CH)&#x2014;CH&#x2014;CH&#x2014;, HN&#x2014;(CH)&#x2014;, Ph-CH&#x2014;, CH&#x2550;C&#x2014;CH&#x2014;, HO-p-Ph-CH&#x2014;, (CH)&#x2014;CH&#x2014;, Ph-NH&#x2014;, NH&#x2014;(CH)&#x2014;C&#x2014;, NH&#x2014;CH&#x2550;N&#x2014;CH&#x2550;C&#x2014;CH&#x2014;. Ris selected from the group consisting of (C-C)alkylene, (C-C)alkenylene, alkyloxy or oligoethyleneglycol Ris selected from bicyclic-fragments of 1,4:3,6-dianhydrohexitols of structural formula (III); Ris selected from the group consisting of (C-C)aryl (C-C)alkyl Ris (CH2)4-; Ror Rare independently selected from C-Calkylene or C-Calkenylene. Ror Rare independently selected from H, methyl, C-Calkylene or C-Calkenylene whereby a is at least 0.05 and b is at least 0.05 and a+b=1. 

Biodegradable polyesteramide copolymers for drug delivery

The present invention relates to a poly (ester amide) (PEA) having a chemical formula described by structural formula (IV), wherein 

The present disclosure relates to microparticles or nanoparticles comprising a polyesteramide (PEA) having a chemical formula described by structural formula (IV), wherein m+p varies from 0.9-0.1 and q varies from 0.1 to 0.9; m+p+q=1 whereby m or p could be 0; n is about 5 to about 300; (pref. 50-200); Ris independently selected from the group consisting of (C-C) alkylene, (C-C) alkenylene, &#x2014;(R&#x2014;CO&#x2014;O&#x2014;R&#x2014;O&#x2014;CO&#x2014;R)&#x2014;, &#x2014;CHR&#x2014;O&#x2014;CO&#x2014;R&#x2014;COOCR&#x2014; and combinations thereof; Rand Rin a single backbone unit m or p, respectively, are independently selected from the group consisting of hydrogen, (C-C)alkyl, (C-C)alkenyl, (C-C)alkynyl, (C-C)aryl, (C-C)alkyl, &#x2014;(CH)SH, &#x2014;(CH)S(CH), &#x2014;CHOH, &#x2014;CH(OH)CH, &#x2014;(CH)NH+, &#x2014;(CH)NHC(&#x2550;NH+)NH, &#x2014;CHCOOH, &#x2014;(CH)COOH, &#x2014;CH&#x2014;CO&#x2014;NH, &#x2014;CHCH&#x2014;CO&#x2014;NH, &#x2014;CHCHCOOH, CH&#x2014;CH&#x2014;CH(CH)&#x2014;, (CH)&#x2014;CH&#x2014;CH&#x2014;, HN&#x2014;(CH)&#x2014;, Ph-CH&#x2014;, CH&#x2550;C&#x2014;CH&#x2014;, HO-p-Ph-CH&#x2014;, (CH)&#x2014;CH&#x2014;, Ph-NH&#x2014;, NH&#x2014;(CH)&#x2014;C&#x2014;, NH&#x2014;CH&#x2550;N&#x2014;CH&#x2550;C&#x2014;CH&#x2014;; Ris selected from the group consisting of (C-C)alkylene, (C-C)alkenylene, alkyloxy or oligoethyleneglycol; Ris selected from bicyclic-fragments of 1,4:3,6-dianhydrohexitols of structural formula (III); Ris (C-C)aryl (C-C)alkyl; Ris &#x2014;(CH)&#x2014;; Ror Rare independently selected from C-Calkylene or C-Calkenylene; and Ror Rare independently selected from H, methyl, C-Calkylene or C-Calkenylene; whereby a is at least 0.05 and b is at least 0.05 and a+b=1.

Particles comprising polyesteramide copolymers for drug delivery

Drug delivery compositions are provided having proteins and biodegradable polymers that may be used for controlled and long term release of proteins into a biological environment. According to some embodiments, the drug delivery composition may be provided with at least a protein and a biodegradable polymer possessing at least two different functional groups selected from the group of chosen among carboxyl, ester, amine, amide, thiol, thioester or hydroxyl groups pendant to the main polymer chain whereby the composition absorbs between 5-10% w/w water when exposed to physiological conditions for at least 20 days. A drug delivery system for controlled protein release which includes the drug delivery composition is also provided whereby the drug delivery system may be in the form of microparticles, films, coatings, fibers, pellets, cylinders, discs, implants, microcapsules, microspheres, nanospheres, wafers, micelles, liposomes or woven or non-woven fabrics.

Growing community of inventors

Echt, Netherlands

George Mihov