Long Circulating Nanoparticles Sustained Drug Release
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Solution Overview
Problem
Current nanoparticle systems for drug delivery have limited effectiveness due to rapid clearance from the body and accumulation in healthy tissues, leading to inadequate targeted delivery and short-lasting plasma concentrations of therapeutic agents.
Innovation Solution
Development of biocompatible long-circulating nanoparticles composed of poly(lactic) acid-poly(ethylene)glycol block copolymer, coupled with a therapeutic agent and a targeting moiety, which provides controlled release of the therapeutic agent for extended periods, enhancing plasma concentrations and reducing volume of distribution.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If conventional nanoparticle systems are used for drug delivery, then the therapeutic agent can be delivered to the body, but the nanoparticles clear from the body quickly and accumulate in healthy tissue, resulting in short plasma concentration duration and inadequate targeted delivery
Solution Approach 1:
The patent uses a composite nanoparticle system combining poly(lactic) acid-poly(ethylene)glycol block copolymer with biocompatible polymers coupled to targeting moieties. This composite structure provides both long circulation time in plasma and active targeting capability, resolving the contradiction between duration of action and targeted delivery effectiveness
Solution Approach 2:
The patent applies local quality by incorporating specific targeting moieties (such as antibodies, peptides, or ligands) at the nanoparticle surface that selectively bind to receptors on target cells. This localized functionalization enables specific targeting to diseased tissue while maintaining long circulation half-life in the bloodstream
2Duration of action of moving object
If nanoparticle systems are used to extend therapeutic delivery, then plasma concentration can be prolonged, but the complexity of the delivery system increases
Solution Approach 1:
The patent employs parameter changes by carefully controlling the molecular weights of the block copolymer components (poly(lactic) acid with number average weight of about 16 kDa and poly(ethylene)glycol with number average molecular weight of about 5 kDa) and their weight percentages (about 80 to about 90 weight percent block copolymer and about 1 to about 4% biocompatible polymer with targeting moiety). These optimized parameters achieve extended therapeutic delivery while managing system complexity
Data Source
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AI summary
The present disclosure is directed in part to a biocompatible nanoparticle composition comprising a plurality of non-colloidal long circulating nanoparticles, each comprising a α-hydroxy polyester-co-polyether and a therapeutic agent, wherein such disclosed compositions provide a therapeutic effect for at least 12 hours.