用于乳腺癌治疗的可生物降解硫代壳聚糖水凝胶的合成及体外研究。

Synthesis and in vitro studies of biodegradable thiolated chitosan hydrogels for breast cancer therapy.

机构信息

Nanostructured Materials Synthesis Laboratory, International Research Institute of Arian Chemie Gostar, Tabriz, Iran.

出版信息

Int J Biol Macromol. 2011 Jun 1;48(5):747-52. doi: 10.1016/j.ijbiomac.2011.02.020. Epub 2011 Mar 4.

DOI:10.1016/j.ijbiomac.2011.02.020

Abstract

Local drug delivery strategies have gained momentum recently as a promising modality in cancer therapy. In order to deliver Letrozole (LTZ) at the tumor site in therapeutically relevant concentrations, acetyl-polyamidoamine (Ac-PAMAM)-thiolated chitosan (TCS) films were fabricated. LTZ could be loaded at 31% wt/wt in films, which were translucent and flexible. Physicochemical characterization of LTZ via thermal technique revealed information on solid-state properties of LTZ as well as thiolated chitosan in films. While thiolated chitosan was in amorphous form, LTZ seemed to be present in both amorphous and crystalline forms in film. The lack of formulation-induced local inflammatory responses of LTZ-acetyl-polyamidoamine (Ac-PAMAM)-thiolated chitosan (TCS) films a new paradigm for localized chemotherapy based on breast delivery systems.

摘要

局部给药策略最近作为癌症治疗的一种有前途的方式得到了发展。为了在治疗相关浓度下将来曲唑（LTZ）递送到肿瘤部位，制备了乙酰化聚酰胺胺（Ac-PAMAM）-巯基化壳聚糖（TCS）薄膜。LTZ 可以以 31%wt/wt 的比例负载在薄膜中，薄膜为半透明且具有柔韧性。通过热技术对 LTZ 进行的物理化学表征揭示了薄膜中 LTZ 以及巯基化壳聚糖的固态特性信息。虽然巯基化壳聚糖呈无定形态，但 LTZ 在薄膜中似乎同时以无定形和结晶形式存在。LTZ-乙酰化聚酰胺胺（Ac-PAMAM）-巯基化壳聚糖（TCS）薄膜缺乏制剂诱导的局部炎症反应，为基于乳腺递药系统的局部化疗开创了一个新的范例。