کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
602382 1454317 2009 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Strategic approaches for improving entrapment of hydrophilic peptide drugs by lipid nanoparticles
موضوعات مرتبط
مهندسی و علوم پایه مهندسی شیمی شیمی کلوئیدی و سطحی
پیش نمایش صفحه اول مقاله
Strategic approaches for improving entrapment of hydrophilic peptide drugs by lipid nanoparticles
چکیده انگلیسی

In order to introduce hydrophilic peptide drugs into solid lipid nanoparticles (SLN), a technique of combining hydrophobic ion pairing (HIP) and non-aqueous oil-in-oil (O/O) emulsion-evaporation was developed. Leuprolide (LR) was selected as the model drug, while sodium stearate (SA-Na) was used as the negative charged ion pairing material. The formation of leuprolide-sodium stearate (LR-SA-Na) complex was confirmed by differential scanning calorimetry (DSC). It was observed that when the molar ratio of SA-Na/LR reached 2/1, ca 88.5% LR was incorporated into the hydrophobic ion complexes with SA-Na. Compared with the conventional method of solvent diffusion in an aqueous system, the efficiency of LR drug entrapment with SLN increased from 28.0% to 74.6% by the combined technique of HIP and O/O emulsion-evaporation. In vitro drug release tests revealed that employing technique of HIP obviously reduced the burst release and slowed down the rate of drug release. At meanwhile, applying the method of non-aqueous O/O emulsion-evaporation, the longer time of drug release but relatively higher drug burst release ratio was observed in comparison with those by the solvent diffusion method in an aqueous system. The drug entrapment and release behaviors of LR-SA-Na SLN prepared by the O/O emulsion-evaporation method suggested that it could potentially be exploited as an oral delivery system for leuprolide.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Colloids and Surfaces B: Biointerfaces - Volume 70, Issue 2, 1 May 2009, Pages 248–253
نویسندگان
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