Development of Lipid-Based Gastroretentive Delivery System for Gentian Extract by Double Emulsion–Melt Dispersion Technique
Gentian (gentiana luteaL.，Gentianaceae）根提取物（GRE）用于治疗胃肠道疾病。然而，由于生物利用度较低和优势生物活性化合物绅士甲基肽的生物利用度低下，其生物活性潜力在常规形式中受到限制。研究的目的是将GRE封装在基于脂质的胃肠道递送系统中，该系统可以提供高产量和封装效率，以及通过直接压缩获得的片剂的双相释放。
Solid lipid microparticles (SLM) loaded with GRE were prepared by freeze-drying double (W/O/W) emulsions, which were obtained by a multiple emulsion–melt dispersion technique, with GRE as the inner water phase, Gelucire®39/01或43/01作为脂质成分，有或不添加多孔二氧化硅（Sylysia）®350）在外水相。通过SEM和汞侵入孔隙法检查配制的SLM粉末，以及确定产量，封装效率和流量性能。此外，还研究了通过直接压缩获得的绅士固醇的体外溶解，分散系统的大小，机械性能和片剂的粘膜粘附。
The results have revealed that SLM with the macroporous structure were formulated, and, consequently, the powders floated immediately in the acidic medium. Formulation with porous silica (Sylysia®350）和胶状®43/01作为固体脂质的特征是高产末端封装效率。此外，通过直接压缩该制剂获得的片剂的粘膜特性，以及在溶解培养基中存在甲状腺素的双相释放，纳米共聚物的存在以及最佳的机械性能表明，开发了一种有希望的基于脂质的脂质基于GRE的脂质胃系统。
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材料：Gentiana（Gentiana Lutea，Gentianaceae）的根是从药用植物研究所购买的“博士”JosifPančić”（塞尔维亚贝尔格莱德）。Gelucire®43/01Gelucire®39/01作为礼品样本从Gattefossé®（法国圣普里斯特）。从Palsgaard®（Denmark Juelsminde）作为礼品样品获得了聚甘油多乙醇。Trehalose dihydrate购自TCI化学品（日本东京）。Span®80（山梨省oleate），Tween®80（多氧化物80), Tween® 20 (polysorbate 20）和氯化钠从默克公司., Germany, while sodium alginate was purchased from Fisher Scientific, soybean lecithin was obtained from Serva Chemical Co. (Heidelberg, Germany), Sylysia® 350 was obtained from Fuji Silysia chemical ltd. (Kasugai Aichi, Japan). For the mucoadhesion evaluation, the mucin from a porcine stomach, Type II (Sigma-Aldrich, Shanghai, China) was used. All other chemicals were of analytical grade, including orthophosphoric acid (Sigma-Aldrich Chemie GmbH, Münich, Germany), acetonitrile (Merck, Darmstadt, Germany). Ultra-pure water was prepared using a Milli-Q purification system (Millipore, Guyancourt, France). Gentiopicroside standard was obtained from ChromaDex (Los Angeles, CA, USA).
Article information: Mudrić, J.; Šavikin, K.; Đekić, L.; Pavlović, S.; Kurćubić, I.; Ibrić, S.; Đuriš, J. Development of Lipid-Based Gastroretentive Delivery System for Gentian Extract by Double Emulsion–Melt Dispersion Technique.Pharmaceutics2021，，，，13，，，，2095. https://doi.org/10.3390/pharmaceutics13122095