The microfluidity and dissolution of hydrogenated PC liposome anchored with alkyl grafted poly(amino acid)s

The stability of a polymer hybridized liposome (PHL) was examined with the microfluidic and thermal state of anchored alkyl chains, and with dissolution against deoxycholate (DOC). Poly(asparagine) grafted with octadecylamine (PAsn-g-C18), poly(aspartic acid) grafted with octadecylamine (PAsp-g-C18), and poly(aspartic acid) grafted with phytosphingosine (PAsp-g-PHS) were synthesized. The microfluidity of the membrane of the PHL was evaluated by fluorescence polarization of 1,6-diphenyl-1,3,5-hexatriene (DPH) and the phase transition temperature (Tc) was measured by differential scanning calorimetry (DSC). The membrane fluidity of liposomes was increased by the inclusion of amphiphilic graft polymers. The phase transition temperature of liposomes increased by the anchoring of PAsn-g-C18, while the inclusion of PAsp-g-C18 or PAsp-g-PHS lowered the Tc. The surface charge of PHL of PAsn-g-C18 was changed by the cationic lipid content. The structural stability of the PHL was affected by variation of the hydrophilic backbone or the hydrophobic moiety of the polymer and PHL of PAsn-g-C18 was most stable against DOC. An increased degree of substitution of the graft copolymer led to better stability of the PHL. It was found that the polymer characteristics affect the physicochemical strength of the PHL structure, resulting in different degrees of stability enhancement.

Polymer-hybridized liposomes of saturated lecithin were formed by association of amphiphilic poly(amino acid) derivatives. The membrane fluidity and stability of vesicles were evaluated for their use as a potential drug carrier system.Figure optionsDownload as PowerPoint slideHighlights
► The membrane fluidity of PHL-PAsp-C18 was higher than that of PHL-PAsn-C18.
► The Tc of liposomes was lowered by the inclusion of PAsp-g-C18 or PAsp-g-PHS.
► The zeta potential of PHL-PAsn-C18 increased with cationic lipid content.
► The stability of PHLs against DOC was influenced by polymer characteristics.