Amphiphilic poly(hydroxyethylaspartamide) derivative-based micelles as drug delivery systems for ferulic acid.
Self-assembling micelles, potentially useful as drug delivery systems for ferulic acid (FA), were obtained in aqueous media from amphiphilic alpha,beta-poly(N-2-hydroxyethyl)-dl-aspartamide (PHEA) copolymers bearing at the polyamino acidic backbone both poly(ethyleneglycol) (2000 or 5000 Da) and hexadecylamine (C(16)) moieties, at a concentration of 7 x 10(- 3) and 4 x 10(- 3) g/l, respectively, with nanometre size and negative zeta potential. These micelles were able to entrap FA and to release it in a prolonged way in phosphate buffer solution at pH 7.4 and human plasma. These systems were also stable in storage conditions and have no cytotoxic effects on Caco-2, 16 HBE, HuDe and K562 cell lines. Moreover, PHEA-PEG(2000)-C(16) and PHEA-PEG(5000)-C(16) micelles were able to escape from phagocytosis by murine macrophages as a function of the surface PEGylation.
Craparo
Emanuela Fabiola
EF
Dipartimento di Chimica e Tecnologie Farmaceutiche, Università di Palermo, Palermo, Italy. ema.craparo@unipa.it
Gennara
Cavallaro
C
Chiara
Ognibene Maria
OM
Girolamo
Teresi
T
Luisa
Bondi Maria
BM
Gaetano
Giammona
G
D000200:Action Potentials / Q000187:drug effects / Q000502:physiology; D000818:Animals; D002021:Buffers; D018938:Caco-2 Cells; D003373:Coumaric Acids / Q000737:chemistry* / Q000378:metabolism; D016503:Drug Delivery Systems / Q000379:methods*; D005456:Fluorescent Dyes; D006801:Humans; D006863:Hydrogen-Ion Concentration; D020014:K562 Cells; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D008823:Micelles; D010455:Peptides / Q000737:chemistry*; D010587:Phagocytosis / Q000187:drug effects; D010936:Plant Extracts / Q000737:chemistry / Q000378:metabolism; D012235:Rhodamines; D013678:Technology, Pharmaceutical
D002021:Buffers; D003373:Coumaric Acids; D005456:Fluorescent Dyes; D008823:Micelles; D010455:Peptides; D010936:Plant Extracts; D012235:Rhodamines; C008965:alpha,beta-poly((2-hydroxyethyl)-aspartamide); C004999:ferulic acid; C029773:rhodamine B