Characterization of the rheological, mucoadhesive, and drug release properties of highly structured gel platforms for intravaginal drug delivery.
Characterization of the rheological, mucoadhesive, and drug release properties of highly structured gel platforms for intravaginal drug delivery.
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DOI：
10.1021/bm9003332
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发表时间：
2009-09-14
影响因子：
6.2
通讯作者：
Malcolm, R. Karl
中科院分区：
文献类型：
--
作者：
Andrews, Gavin P.;Donnelly, Louise;Jones, David S.;Curran, Rhonda M.;Morrow, Ryan J.;Woolfson, A. David;Malcolm, R. Karl
本调查描述了流变学结构的车辆（RSV）设计用于改善药物输送到阴道的配方和表征。制备了含有羟乙基纤维素（HEC，5%w/w）、聚乙烯吡咯烷酮（PVP，4%w/w）、普朗尼克（PL，0或10%w/w）和作为粘膜粘附剂的聚卡波非（PC，3%w/w）或聚（甲基乙烯基醚-共-马来酸酐）（Gantrez S97，3%w/w）的相互作用的多组分聚合物平台。的流变学（扭转和动态），机械（压缩），和粘膜粘附性能进行了表征，并显示依赖于所使用的粘膜粘附剂和PL的列入/排除。还在用模拟阴道液稀释（以模拟体内稀释）后评估凝胶平台的动态流变学性质。含有PC的RSV比含有GAN的对照制剂具有更高的流变学结构。这一趋势也反映在配方硬度、可压缩性、稠度和崩解性上。此外，含有PL（10%w/w）的制剂比不含PL的制剂更具有流变学结构。用模拟阴道液稀释后，RSV的流变学结构显著降低，但RSV仍保持高弹性结构（G′ > G′′和tan δ < 1）。此外，RSVs表现出持续的药物释放特性，被证明是依赖于其流变结构。据认为，这些半固体药物递送系统可用作将治疗剂持续递送至阴道的位点保持平台。
This investigation describes the formulation and characterization of rheologically structured vehicles (RSVs) designed for improved drug delivery to the vagina. Interactive, multicomponent, polymeric platforms were manufactured containing hydroxyethylcellulose (HEC, 5% w/w) polyvinylpyrrolidone (PVP, 4% w/w), Pluronic (PL, 0 or 10% w/w), and either polycarbophil (PC, 3% w/w) or poly(methylvinylether-co-maleic anhydride) (Gantrez S97, 3% w/w) as a mucoadhesive agent. The rheological (torsional and dynamic), mechanical (compressional), and mucoadhesive properties were characterized and shown to be dependent upon the mucoadhesive agent used and the inclusion/exclusion of PL. The dynamic rheological properties of the gel platforms were also assessed following dilution with simulated vaginal fluid (to mimic in vivo dilution). RSVs containing PC were more rheologically structured than comparator formulations containing GAN. This trend was also reflected in formulation hardness, compressibility, consistency, and syringeability. Moreover, formulations containing PL (10% w/w) were more rheologically structured than formulations devoid of PL. Dilution with simulated vaginal fluids significantly decreased rheological structure, although RSVs still retained a highly elastic structure (G′ > G′′ and tan δ < 1). Furthermore, RSVs exhibited sustained drug release properties that were shown to be dependent upon their rheological structure. It is considered that these semisolid drug delivery systems may be useful as site-retentive platforms for the sustained delivery of therapeutic agents to the vagina.
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影响因子：
3.8
作者：
Kieweg, SL;Geonnotti, AR;Katz, DF
通讯作者：
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影响因子：
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DOI：
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作者：
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DOI：
10.1016/s0301-2115(96)02612-7
发表时间：
1997-01-01
影响因子：
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作者：
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通讯作者：
Schram, JHN