Interplay of stimuli-responsiveness, drug loading and release for a surface-engineered dendrimer delivery system.

Abstract:

:The objectives of this study were to generate novel thermo and pH dual responsive poly(amidoamine) (PAMAM) via precise surface engineering, and investigate the interplay of dendrimer stimuli-responsiveness and the loading and release properties of a model agent, vitamin E acetate (VEAc). A higher dendrimer generation and maximized VEAc loading at elevated pH all contributed to a lower cloud point (CP) of the dendrimer-VEAc complex. The drug loading in G3.5 surface-engineered PAMAM was 22 mol/mol (pH 7.0) and 10 mol/mol (pH 5.0), which corresponded to a complex CP value at ca. 13 °C (pH 7.0) and 46 °C (pH 5.0), respectively. At physiological conditions, only less than 40% of VEAc was liberated when reaching the plateau, whilst more than 90% of VEAc was released from such system within 6 h at pH 5.0. This was due to the transition of dendrimer surface from dehydrated state to hydrated state upon pH dropping, enabling rapid drug release for therapeutic action. This smart stimuli-responsive dendritic delivery system holds promise for the efficient drug delivery to tissues with pH abnormality such as tumor.

journal_name

Int J Pharm

authors

Liu R,Sun M,Liu X,Fan A,Wang Z,Zhao Y

doi

10.1016/j.ijpharm.2013.12.031

subject

Has Abstract

pub_date

2014-02-28 00:00:00

pages

103-7

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(13)01099-5

journal_volume

462

pub_type

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