2014
Paclitaxel isomerisation in polymeric micelles based on hydrophobized hyaluronic acid
SMEJKALOVA, D; Kristina NEŠPOROVÁ; M HERMANNOVA; G HUERTA-ANGELES; D COZIKOVA et al.Základní údaje
Originální název
Paclitaxel isomerisation in polymeric micelles based on hydrophobized hyaluronic acid
Autoři
SMEJKALOVA, D; Kristina NEŠPOROVÁ; M HERMANNOVA; G HUERTA-ANGELES; D COZIKOVA; Lucie VIŠTEJNOVÁ; B SAFRANKOVA; J NOVOTNY; Jindra KUČEŘÍKOVÁ a V VELEBNY
Vydání
International Journal of Pharmaceutics, AMSTERDAM, ELSEVIER SCIENCE BV, 2014, 0378-5173
Další údaje
Jazyk
angličtina
Typ výsledku
Článek v odborném periodiku
Utajení
není předmětem státního či obchodního tajemství
Impakt faktor
Impact factor: 3.650
Označené pro přenos do RIV
Ne
UT WoS
Klíčová slova anglicky
Polymeric micelle; Hyaluronan; Paclitaxel; Stability; Isomer
Změněno: 4. 7. 2014 16:20, Mgr. Kristina Nešporová, Ph.D.
Anotace
V originále
Physical and chemical structure of paclitaxel (PTX) was studied after its incorporation into polymeric micelles made of hyaluronic acid (HA) (M-w = 15 kDa) grafted with C6 or C18:1 acyl chains. PTX was physically incorporated into the micellar core by solvent evaporation technique. Maximum loading capacity for HAC6 and HAC18:1 was determined to be 2 and 14 wt.%, respectively. The loading efficiency was higher for HAC18:1 and reached 70%. Independently of the derivative, loaded HA micelles had spherical size of approximately 60-80 nm and demonstrated slow and sustained release of PTX in vitro. PTX largely changed its form from crystalline to amorphous after its incorporation into the micelle's interior. This transformation increased PTX sensitivity towards stressing conditions, mainly to UV light exposure, during which the structure of amorphous PTX isomerized and formed C3-C11 bond within its structure. In vitro cytotoxicity assay revealed that polymeric micelles loaded with PTX isomer had higher cytotoxic effect to normal human dermal fibroblasts (NHDF) and human colon carcinoma cells (HCT-116) than the same micelles loaded with non-isomerized PTX. Further observation indicated that PTX isomer influenced in different ways cell morphology and markers of cell cycle. Taken together, PTX isomer loaded in nanocarrier systems may have improved anticancer activity in vivo than pure PTX. (C) 2014 Elsevier B.V. All rights reserved.