物理化学学报 >> 2012, Vol. 28 >> Issue (04): 897-902.doi: 10.3866/PKU.WHXB201202091

软物质 上一篇    下一篇

微乳液法制备可共载水溶和脂溶药物的壳聚糖季铵盐乙醇脂质体的载药性能表征

梁晓飞1, 胡晶莹2, 陈复华2, 李宗海1, 常津3   

  1. 1. 癌基因及相关基因国家重点实验室, 上海交通大学医学院附属仁济医院上海市肿瘤研究所, 上海 200032;
    2. 上海市肿瘤研究所公共实验平台, 上海交通大学医学院附属仁济医院, 上海 200032;
    3. 天津大学材料科学与工程学院纳米生物技术研究所, 天津市材料复合与功能化重点实验室, 天津 430072
  • 收稿日期:2011-10-20 修回日期:2012-01-16 发布日期:2012-03-21
  • 通讯作者: 梁晓飞, 李宗海, 常津 E-mail:xfliang@shsci.org; zonghaili@gmail.com; jinchang@tju.edu.cn
  • 基金资助:

    国家自然科学基金(51003059)及上海市自然科学基金(10ZR1428900)资助项目

Characterization of Chitosan Polymeric Ethosomes Capable of Encapsulating Hydrophobic and Hydrophilic Drugs Prepared by a Microemulsion Method

LIANG Xiao-Fei1, HU Jing-Ying2, CHEN Fu-Hua2, LI Zong-Hai1, CHANG Jin3   

  1. 1. State Key Laboratory of Oncogenes and Related Genes, Shanghai Cancer Institute, Renji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200032, P. R. China;
    2. Public laboratory platform, Shanghai Cancer Institute, Renji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200032, P. R. China;
    3. Institute of Nanobiotechnology, School of Materials Science and Engineering, Tianjin University and Tianjin Key Laboratory of Composites and Functional Materials, Tianjin 300072, P. R. China
  • Received:2011-10-20 Revised:2012-01-16 Published:2012-03-21
  • Contact: LIANG Xiao-Fei, LI Zong-Hai, CHANG Jin E-mail:xfliang@shsci.org; zonghaili@gmail.com; jinchang@tju.edu.cn
  • Supported by:

    The project was supported by the National Natural Science Foundation of China (51003059) and Natural Science Foundation of Shanghai, China (10ZR1428900).

摘要: 采用微乳液法制备了可包载脂溶性和水溶性药物的羧甲基壳聚糖十八烷基季铵盐(OQCMC)乙醇脂质体, 研究了OQCMC乙醇高分子脂质体的相图、粒径和电位、对药物的包封及释放能力及共载水溶性和脂溶性荧光染料后的细胞内递送能力. 结果表明: OQCMC上长链季铵盐分子的取代度和共乳化剂乙醇的加入量对相图中微乳区域的面积影响不大; 微乳液法可制备包载水溶性长春新碱(VCR)、脂溶性消炎痛(IMC)或二者共载的OQCMC载药微球, 微球粒径为(52.40±0.55) nm, 分布均匀; 微乳液体系对VCR的最大载药率为22.7%, 对IMC的最大载药率为20.1%, 二者共载时, VCR的最大载药率为12.2%, IMC的最大载药率为10.0%; 载药微球对药物具有缓控释功能. OQCMC乙醇高聚物脂质体可有效地包载荧光染料异硫氰酸荧光素FITC (水溶性)和尼罗红(脂溶性), 并将二者递送到卵巢癌HO8901细胞内.

关键词: 壳聚糖, 表面活性剂, 纳米颗粒, 药物递送, 微乳液, 乙醇脂质体

Abstract: Polymeric ethosomes, formed from amphiphilic octadecyl quaternized carboxymethyl chitosan (OQCMC) with different degrees of quaternary substitution (DS), were prepared by the microemulsion (ME) method. These ethosomes could simultaneously encapsulate both the hydrophobic drug indomethacin (IMC) and the hydrophilic drug vincristine (VCR). The effects of the DS of the OQCMC and primary alcohols as cosurfactants on the phase diagram were elucidated. The prepared nanoparticles (NPs) were small ((52.40 ± 0.55) nm) and suitable as drug carriers for different drugs. The maximum drug loading efficiencies of VCR-loaded and IMC-loaded NPs were 22.7% and 20.1%, respectively. The drug loading capacities for co-delivery of VCR and IMC were 12.2% and 10.0% , respectively. OQCMC polymeric ethosomes were stable in aqueous solution and exhibited slow, steady drug release. Hydrophilic fluorescein isothiocyanate (FITC) and hydrophobic Nile Red were encapsulated by the OQCMC ME NPs and simultaneously delivered into HO8901 cells with green and red fluorescence, respectively. This co-delivery system may allow for temporally distinct classes of drugs for cancer therapy.

Key words: Chitosan, Surfactant, Nanoparticle, Drug delivery, Microemulsion, Ethosome

MSC2000: 

  • O648