PLGA microspheres for the ocular delivery of a peptide drug, vancomycin using emulsification/spray-drying as the preparation method: in vitro/in vivo studies
PLGA microspheres for the ocular delivery of a peptide drug, vancomycin using emulsification/spray-drying as the preparation method: in vitro/in vivo studies
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DOI：
10.1016/j.ejpb.2003.10.018
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发表时间：
2004-03-01
影响因子：
4.9
通讯作者：
Giunchedi, P
中科院分区：
文献类型：
--
作者：
Gavini, E;Chetoni, P;Giunchedi, P
本研究的目的是体外/体内研究聚乳酸-羟基乙酸酯（PLGA）微球作为一种多肽药物万古霉素（VA）局部眼部递送的癌症。通过乳化/喷雾干燥技术制备微球，可作为制备多肽负载微球的双乳液方法的替代方法。药物包封率接近理论值（84.2 ~ 99.5%）；平均粒径以d（vs）表示，约为11 μ m。微球能够调节VA的体外药物释放，其行为依赖于其组成：最高的药物含量对应于最高的释放率。体内研究是通过评估局部给药微球水混悬液后VA在兔房水中的药代动力学特征进行的。与药物水溶液相比，观察到高且长时间的VA浓度和增加的AUC值（2倍）。通过添加悬浮液粘浆剂（羟丙基纤维素）来增加微球悬浮液的粘度并没有增加眼生物利用度。PLGA微球可以作为多肽药物的眼部递送系统。(C) 2003 Elsevier B.V.版权所有
The aim of this study was an in vitro/in vivo investigation on poly(lactide-co-glycolide) (PLGA) microspheres as cancers for the topical ocular delivery of a peptide drug vancomycin (VA). The microspheres were prepared by an emulsification/spray-drying technique that can be proposed as an alternative to the double emulsion method for preparation of peptide-loaded microparticles. The drug encapsulation efficiencies were close to the theoretical values (84.2-99.5%); the average particle size, expressed as d(vs), was about 11 mum. The microspheres were able to modulate the in vitro drug release of VA with a behavior dependent on their composition: the highest drug content corresponded to the highest release rate. In vivo studies were carried out by assessing the pharmacokinetic profile of VA in the aqueous humor of rabbits after topical administration of aqueous suspensions of microspheres. High and prolonged VA concentrations and increased AUC values (2-fold) with respect to an aqueous solution of the drug were observed. Increasing the viscosity of the microsphere suspension by addition of a suspending-viscosizing agent (hydroxypropylcellulose) did not produce an increase of the ocular bioavailability. PLGA microspheres can be proposed as a system for ocular delivery of peptide drugs. (C) 2003 Elsevier B.V. All rights reserved.