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首页> 外文期刊>Applied Surface Science >Template-Directed Hydrothermal Synthesis Of Hydroxyapatite As A Drug Delivery System For The Poorly Water-Soluble Drug Carvedilol
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Template-Directed Hydrothermal Synthesis Of Hydroxyapatite As A Drug Delivery System For The Poorly Water-Soluble Drug Carvedilol

机译：模板导向水热合成羟基磷灰石作为水溶性差的卡维地洛的药物递送系统

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摘要

In order to improve the dissolution rate and increase the bioavailability of a poorly water-soluble drug, intended to be administered orally, the biocompatible and bioactive mesoporous hydroxyapatite (HA) was successfully synthesized. In the present study, mesoporous HA nanoparticles were produced using Pluronic block co-polymer F127 and cetyltrimethylammonium bromide (CTAB) as templates by the hydrothermal method. The obtained mesoporous HA was employed as a drug delivery carrier to investigate the drug storage/release properties using carvedilol (CAR) as a model drug. Characterizations of the raw CAR powder, mesoporous HA and CAR-loaded HA were carried out by the scanning electron microscopy (SEM), transmission electron microscopy (TEM), X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), Fourier transform infrared (FT-IR) spectroscopy, N_2 adsorption/desorption, thermogravimetric analysis (TGA), and UV-VIS spectrophotometry. The results demonstrated that CAR was successfully incorporated into the mesoporous HA host. In vitro drug release studies showed that mesoporous HA had a high drug load efficiency and provided immediate release of CAR compared with micronized raw drug in simulated gastric fluid (pH 1.2) and intestinal fluid (pH 6.8). Consequently, mesoporous HA is a good candidate as a drug carrier for the oral delivery of poorly water-soluble drugs.
机译：为了提高旨在口服给药的水溶性差的药物的溶解速度并提高其生物利用度，成功地合成了具有生物相容性和生物活性的介孔羟基磷灰石（HA）。在本研究中，以Pluronic嵌段共聚物F127和十六烷基三甲基溴化铵（CTAB）为模板，通过水热法制备了介孔HA纳米粒子。使用卡维地洛（CAR）作为模型药物，将获得的中孔HA用作药物输送载体，以研究药物的储存/释放特性。通过扫描电子显微镜（SEM），透射电子显微镜（TEM），X射线粉末衍射（XRPD），差示扫描量热法（DSC），傅里叶（Fourier）对粗制CAR粉末，介孔HA和载有CAR的HA进行表征变换红外（FT-IR）光谱，N_2吸附/解吸，热重分析（TGA）和UV-VIS分光光度法。结果表明，CAR已成功整合到中孔HA宿主中。体外药物释放研究表明，与微粉化的原料药相比，在模拟的胃液（pH 1.2）和肠液（pH 6.8）中，介孔HA具有较高的载药效率，并且可以立即释放CAR。因此，中孔HA是用于口服递送水溶性差的药物的药物载体的良好候选者。

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  • 来源
    《Applied Surface Science》 |2011年第23期|p.10126-10133|共8页
  • 作者

    Qinfu Zhao; Tianyi Wang; Jing Wang; Li Zheng; Tongying Jiang; Gang Cheng; Siling Wang;

  • 作者单位

    Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, PR China;

    Department of Clinical Pharmacy, School of Pharmacy, Shenyang Pharmaceutical University, No.103, Wenhua Road, Shenyang 110016, PR China;

    Department of Physical Chemistry, School of Basic Science, Shenyang Pharmaceutical University, No.103, Wenhua Road, Shenyang 110016, PR China;

    Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, PR China;

    Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, PR China;

    Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, PR China;

    Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, PR China;

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  • 正文语种 eng
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  • 关键词

    Mesoporous hydroxyapatite; Drug delivery system; Carvedilol; Poorly water-soluble drugs; In vitro dissolution;

    机译：介孔羟基磷灰石;给药系统;卡维地洛;水溶性差;体外溶出度;

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