Minocycline block copolymer micelles and their anti-inflammatory effects on microglia.

MH, a semisynthetic tetracycline antibiotic with promising neuroprotective properties, was encapsulated into PIC micelles of CMD-PEG as a potential new formulation of MH for the treatment of neuroinflammatory diseases. PIC micelles were prepared by mixing solutions of a Ca(2+)/MH chelate and CMD-PEG copolymer in a Tris-HCl buffer. Light scattering and (1)H NMR studies confirmed that Ca(2+)/MH/CMD-PEG core-corona micelles form at charge neutrality having a hydrodynamic radius approximately 100 nm and incorporating approximately 50 wt.

Enhancement of hydrophilic drug loading and release characteristics through micellization with new carboxymethyldextran-PEG block copolymers of tunable charge density.

The micellization of a model cationic drug, diminazene diaceturate (DIM) and a series of new diblock copolymers, carboxymethyldextran-poly(ethylene glycols) (CMD-PEG), were evaluated as a function of the ionic charge density or degree of substitution (DS) of the carboxymethyldextran block and the molar ratio, [+]/[-], of positive charges provided by the drug to negative charges provided by CMD-PEG. Micelles ([+]/[-]=2) incorporated up to 64% (w/w) DIM and ranged in hydrodynamic radius (R(H)) from 36 to 50 nm, depending on the molecular weight and DS of CMD-PEG. The critical association concentration (CAC) was on the order of 15-50mg/L for CMD-PEG of DS>60%, and ca.