Polymeric micelles for oral drug administration enabling locoregional and systemic treatments

Abstract

Each therapeutic purpose demands micelles with different performance regarding stability in the GI tract, ability to overcome physiological barriers and drug release patterns. Depending on the block copolymer composition and structure, a wealth of self-assembled micelles with different morphologies and stability can be prepared. Moreover, copolymer unimers can play a role in improving drug absorption through the GI mucosa, either by increasing membrane permeability to the drug and/or the carrier or by inhibiting drug efflux transporters or first-pass metabolism. Therefore, polymeric micelles can be pointed out as versatile vehicles to increase oral bioavailability of drugs that exhibit poor solubility or permeability and may even be an alternative to parenteral carriers when targeting is pursued.

Intranasal delivery of nanomicelle curcumin promotes corneal epithelial wound healing in streptozotocin-induced diabetic mice

“…Recent studies show that polymeric micelle is one of the most attractive nanocarriers for hydrophobic drugs and its use improves drug’s bioavailability1617. Amphiphilic block copolymers can form nano-sized aggregates with core-shell structures, which can solubilize poorly water-soluble drugs.…”

Oral Delivery of Multicompartment Nanomedicines for Colorectal Cancer Therapeutics: Combining Loco‐Regional Delivery with Cell‐Target Specificity

“…Additionally, the majority of nanomedicines to date focus on intravenous formulations, which is an undesirable delivery route due to patient perception, personnel requirements, and associated cost, resulting in low compliance and in the case of gastrointestinal (GI) disease, an ineffective delivery route to the disease site . Oral administration of drugs offers a more convenient and patient‐compatible approach, and in the case of GI diseases, better availability at the disease site . Colon‐discriminate oral delivery systems that utilize specific mechanisms for drug release such as pH‐dependence, time dependence, microbiologically‐triggered, and prodrug‐based systems have been reported, with varying degrees of success achieved .…”

“…[7] Oral administration of drugs offers a more convenient and patientcompatible approach, and in the case of GI diseases, better availability at the disease site. [8] Colon-discriminate oral delivery systems that utilize specific mechanisms for drug release such as pH-dependence, time dependence, microbiologically-triggered, and prodrug-based systems have been reported, with varying degrees of success achieved. [9] Recently, our group has shown that chitosan nanoparticles encapsulated into commercially available Eudragit RS100 microcapsules show substantial accumulation of chitosan nanoparticles in the colonic region.…”

Interaction of poloxamine block copolymers with lipid membranes: Role of copolymer structure and membrane cholesterol content

“…Compared to common surfactants, most block copolymers exhibit improved capability to self-assemble into micelle-like or more complex structures (vesicles and polymersomes) that can host a variety of drugs, leading to higher apparent solubility, stability and capability to target the payload to specific tissues or cells [3,4]. Suitability for being decorated with a variety of ligands and/or prepared with stimuli-responsive components makes block copolymers-based nanocarriers attractive to face up to a variety of therapeutic demands [5].…”