Provided is a pharmaceutical preparation composition comprising a polymerized camptothecin derivative which is obtained by bonding a camptothecin derivative to a polymer carrier, and has nanoparticle-forming properties of associating in an aqueous solution, the pharmaceutical preparation composition having enhanced preparation stability. Particularly, a pharmaceutical preparation maintaining nanoparticle-forming properties, which are an important factor, and having an excellent storage stability is provided.

Disclosed is a pharmaceutical preparation comprising a block copolymer in which a polyethylene glycol segment is linked to a polyglutamic acid segment containing a glutamic acid unit having a camptothecin derivative bonded thereto, the pharmaceutical preparation capable of forming associates in an aqueous solution. When the pharmaceutical preparation is made into an aqueous solution containing the camptothecin derivative at a concentration of 1 mg/mL, the pH of the aqueous solution is 2.4 to 7.0, and the change ratio of the associate-forming ability of the pharmaceutical preparation after storage at 40° C. for one week under light-blocked conditions is 50% or less.

Provided is a pharmaceutical preparation composition comprising a polymerized camptothecin derivative which is obtained by bonding a camptothecin derivative to a polymer carrier, and has nanoparticle-forming properties of associating in an aqueous solution, the pharmaceutical preparation composition having enhanced preparation stability. Particularly, a pharmaceutical preparation maintaining nanoparticle-forming properties, which are an important factor, and having an excellent storage stability is provided.

Disclosed is a pharmaceutical preparation comprising a block copolymer in which a polyethylene glycol segment is linked to a polyglutamic acid segment containing a glutamic acid unit having a camptothecin derivative bonded thereto, the pharmaceutical preparation capable of forming associates in an aqueous solution. When the pharmaceutical preparation is made into an aqueous solution containing the camptothecin derivative at a concentration of 1 mg/mL, the pH of the aqueous solution is 2.4 to 7.0, and the change ratio of the associate-forming ability of the pharmaceutical preparation after storage at 40° C. for one week under light-blocked conditions is 50% or less.

Some variations provide a low-adhesion coating comprising a continuous matrix containing a first component, a plurality of inclusions containing a second component, and a solid-state lubricant distributed within the coating, wherein one of the first component or the second component is a low-surface-energy polymer, and the other of the first component or the second component is a hygroscopic material. The solid-state lubricant may be selected from graphite, graphene, molybdenum disulfide, tungsten disulfide, hexagonal boron nitride, or poly(tetrafluoroethylene) or other fluoropolymers. The solid-state lubricant particles may be coated with a metal selected from cadmium, lead, tin, zinc, copper, nickel, or alloys containing one or more of these metals. The solid-state lubricant is typically characterized by an average particle size from about 0.1 μm to about 500 μm. The solid-state lubricant is preferably distributed throughout the coating.

Methods for efficient preparation of drug-polymer (or oligomer) conjugates useful in the preparation of particles, including microparticles and nanoparticles, for delivery of the drug in vivo for therapeutic applications are provided. The invention also provides nanoparticles prepared by nanoprecipitation using drug-polymer/oligomer conjugates of the invention. The drug conjugates are formed during polymerization of the polymer or oligomer in which the drug is employed as an initiator of the polymerization of the monomers which form the polymer and/or oligomer. More specifically, the drug conjugates are formed by ring-opening polymerization of cyclic monomers in the presence of an appropriate ring-opening polymerization catalyst and the initiator (the drug). The method is particularly useful for formation of polymer/oligomer conjugates with drugs and other chemical species containing one or more hydroxyl groups or thiol groups.

Methods for efficient preparation of drug-polymer (or oligomer) conjugates useful in the preparation of particles, including microparticles and nanoparticles, for delivery of the drug in vivo for therapeutic applications are provided. The invention also provides nanoparticles prepared by nanoprecipitation using drug-polymer/oligomer conjugates of the invention. The drug conjugates are formed during polymerization of the polymer or oligomer in which the drug is employed as an initiator of the polymerization of the monomers which form the polymer and/or oligomer. More specifically, the drug conjugates are formed by ring-opening polymerization of cyclic monomers in the presence of an appropriate ring-opening polymerization catalyst and the initiator (the drug). The method is particularly useful for formation of polymer/oligomer conjugates with drugs and other chemical species containing one or more hydroxyl groups or thiol groups.

This document relates to functionalized (e.g., mono- or bi-functional) polymers (e.g., polyethylene glycol and related polymers) as well as methods and materials for making and using such functionalized polymers.

The present invention relates to a method for producing polyethercarbonate-polyoxymethylene block copolymers, comprising the step of polymerizing formaldehyde, wherein formaldehyde is polymerized in the presence of a polyethercarbonate having at least one Zerewitinoff-active H atom, obtaining an intermediate product. The obtained intermediate product can be further reacted with a cyclic carboxylic acid ester or carbonic acid ester, a cyclic anhydride, an epoxide, and/or an isocyanate, wherein a hydroxyl- or carboxy-functional or NCO-modified polyethercarbonate-polyoxymethylene block copolymer is obtained. The present invention further relates to polyethercarbonate-polyoxymethylene block copolymers that can be obtained by means of such a method and to the use of same to produce polyurethane polymers.

The present invention relates to a method for producing polyethercarbonate-polyoxymethylene block copolymers, comprising the step of polymerizing formaldehyde, wherein formaldehyde is polymerized in the presence of a polyethercarbonate having at least one Zerewitinoff-active H atom, obtaining an intermediate product. The obtained intermediate product can be further reacted with a cyclic carboxylic acid ester or carbonic acid ester, a cyclic anhydride, an epoxide, and/or an isocyanate, wherein a hydroxyl- or carboxy-functional or NCO-modified polyethercarbonate-polyoxymethylene block copolymer is obtained. The present invention further relates to polyethercarbonate-polyoxymethylene block copolymers that can be obtained by means of such a method and to the use of same to produce polyurethane polymers.

This invention relates to shape memory block copolymers comprising: at least one switching segment having a T.sub.trans from 10 to 70° C.; and at least one soft segment, wherein at least one of the switching segments in linked to at least one of the soft segments by at least one linkage, and wherein the copolymer transforms from a first shape to a second shape by application of a first stimulus and the copolymer transforms back to the first shape from the second shape by application of a second stimulus. The shape memory block copolymers may be biocompatible and biodegradable.

This invention relates to shape memory block copolymers comprising: at least one switching segment having a T.sub.trans from 10 to 70° C.; and at least one soft segment, wherein at least one of the switching segments in linked to at least one of the soft segments by at least one linkage, and wherein the copolymer transforms from a first shape to a second shape by application of a first stimulus and the copolymer transforms back to the first shape from the second shape by application of a second stimulus. The shape memory block copolymers may be biocompatible and biodegradable.