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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Poly(D,L-lactide-co-glycolide) protein-loaded nanoparticles prepared by the double emulsion method-processing and formulation issues for enhanced entrapment efficiency
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Poly(D,L-lactide-co-glycolide) protein-loaded nanoparticles prepared by the double emulsion method-processing and formulation issues for enhanced entrapment efficiency

机译:通过双乳液法制备的载有聚(D,L-丙交酯-乙交酯)蛋白质的纳米颗粒-加工和配制问题可提高包封效率

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Although extensive research in the field of biodegradable microparticles containing peptide or protein drugs has greatly advanced production know-how,the effects of critical parameters influencing successful drug entrapment have not yet been sufficiently investigated with nano-scaled carriers.This paper deals with the formulation and processing parameters of the W_1/o/w_2 double emulsion method that can affect nanoparticle size and loading.Fluorescein isothiocyanate-labelled bovine serum albumin (FITC-BSA) was used as a model protein.Results showed that high FITC-BSA entrapment efficiencies were reached (>80%) when sonication was used for the two emulsification steps of the nanoparticle formation,independently of the mixing durations and intensities.By comparison,the use of a vortex mixer for obtaining the primary W_1/o emulsion led to a rather poor entrapment efficiency (~25%).Some inherent properties of the poly(D,L-lactic-co-glycolic acid) polymer,such as,for example,high molecular weight,high hydrophilicity or the presence of free carboxylic end groups,enhanced the drug entrapment efficiency.It was also demonstrated that a low nominal drug loading,a large volume of the inner w,phase or the choice of methylene chloride instead of ethyl acetate as organic solvent favoured the drug entrapment,with entrapment efficiency values often reaching 100%.However,when using mediylene chloride,the mean particle size was substantially increased,due to the presence of larger particles.Mean particle size increased also when the polymer concentration in the organic phase was increased.
机译:尽管在包含肽或蛋白质药物的可生物降解微粒领域中进行了广泛的研究,已经获得了非常先进的生产知识,但是对于纳米级载体,尚未充分研究关键参数对成功诱捕药物的影响。 W_1 / o / w_2双乳化法的工艺参数会影响纳米粒子的大小和载量(> 80%)在将超声处理用于纳米颗粒形成的两个乳化步骤时,与混合持续时间和强度无关。相比之下,使用涡旋混合器获得初级W_1 / o乳液会导致截留效果较差效率(〜25%)。聚(D,L-乳酸-乙醇酸共聚物)聚合物的某些固有特性,例如高分子重量,高亲水性或游离羧基端基的存在提高了药物的包封效率。还证明了标称药物载量低,内相的体积大或选择了二氯甲烷代替乙酸乙酯有机溶剂有利于药物的包封,包封效率值通常达到100%。但是,使用二甲苯氯时,由于存在较大的颗粒,平均粒径大大增加。有机相增加。

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