Hydrophobic Molecule-Induced Branched Polymer Aggregates and their Use
AssigneeANP Technologies, Inc.
InventorsDujie Qin, Ray Yin, Jing Pan, Yubei Zhang
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Abstract
Symmetrically and asymmetrically branched homopolymers are modified at the surface level with functional groups that enable forming aggregates with water insoluble or poorly water soluble pharmaceutically active agents (PAA). The aggregates formed are specifically induced by interaction of PAA and homopolymer and are different from aggregates that are formed by the polymer alone in the absence of the PAA or by the PAA alone in the absence of the polymer. Such aggregates can be used to improve drug solubility, stability, delivery and efficacy.
Claims28
A lyophilized aggregate obtained by a method comprising:
- (a) mixing:
- (i) a water insoluble or a poorly water soluble pharmaceutically active agent (PAA) dissolved in a solvent miscible with water or a chloroform/ethanol mixture;
- and
- (ii) a water soluble randomly branched homopolymer modified with a hydrophobic surface group, dissolved in an organic solvent to form an aggregate;
- (b) collecting said aggregate of step (a), wherein said collecting comprises evaporating to remove said solvent miscible with water or said chloroform/ethanol mixture, and to remove said organic solvent to yield a collected aggregate;
- (c) dissolving said collected aggregate of step (b) in an aqueous solution;
- and
- (d) lyophilizing said dissolved, collected aggregate solution of step (c) to form said lyophilized aggregate,
- wherein said PAA is located at or in said hydrophobic surface group;
- said lyophilized aggregate is water soluble;
- and on dilution in an aqueous solution, said PAA is released from said lyophilized aggregate at a controlled rate.
The aggregate of claim 19, wherein said aliphatic chain comprises a branch.
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A composition comprising an aggregate consisting of water, a water insoluble or a poorly water soluble pharmaceutically active agent (PAA) and a water soluble randomly branched homopolymer modified with a hydrophobic surface group.
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Dependencies are inferred from the claim text.