Solubilization of poorly water-soluble compounds using amphiphilic phospholipid polymers with different molecular architectures.
Colloids Surf B Biointerfaces
; 158: 249-256, 2017 Oct 01.
Article
em En
| MEDLINE
| ID: mdl-28700969
ABSTRACT
To achieve stable and effective solubilization of poorly water-soluble bioactive compounds, water-soluble and amphiphilic polymers composed of hydrophilic 2-methacryloyloxyethyl phosphorylcholine (MPC) units and hydrophobic n-butyl methacrylate (BMA) units were prepared. MPC polymers having different molecular architectures, such as random-type monomer unit sequences and block-type sequences, formed polymer aggregates when they were dissolved in aqueous media. The structure of the random-type polymer aggregate was loose and flexible. On the other hand, the block-type polymer formed polymeric micelles, which were composed of very stable hydrophobic poly(BMA) cores and hydrophilic poly(MPC) shells. The solubilization of a poorly water-soluble bioactive compound, paclitaxel (PTX), in the polymer aggregates was observed, however, solubilizing efficiency and stability were strongly depended on the polymer architecture; in other words, PTX stayed in the poly(BMA) core of the polymer micelle formed by the block-type polymer even when plasma protein was present in the aqueous medium. On the other hand, when the random-type polymer was used, PTX was transferred from the polymer aggregate to the protein. We conclude that water-soluble and amphiphilic MPC polymers are good candidates as solubilizers for poorly water-soluble bioactive compounds.
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01-internacional
Base de dados:
MEDLINE
Assunto principal:
Fosfolipídeos
/
Polímeros
Idioma:
En
Revista:
Colloids Surf B Biointerfaces
Ano de publicação:
2017
Tipo de documento:
Article