Characterization of the Rheological, Mucoadhesive, and Drug Release Properties of Highly Structured Gel Platforms for Intravaginal Drug Delivery

被引:61
作者
Andrews, Gavin P. [1 ]
Donnelly, Louise [1 ]
Jones, David S. [1 ]
Curran, Rhonda M. [1 ]
Morrow, Ryan J. [1 ]
Woolfson, A. David [1 ]
Malcolm, R. Karl [1 ]
机构
[1] Queens Univ Belfast, Sch Pharm, Drug Delivery & Biomat Grp, Ctr Med Biol, Belfast BT9 7BL, Antrim, North Ireland
基金
英国惠康基金;
关键词
VAGINAL FLUID; PHYSIOLOGICAL CONDITIONS; UROGENITAL ATROPHY; BIOADHESIVE; SYSTEMS; POLYMERS; FORMULATIONS; SEMEN; CREAM; RING;
D O I
10.1021/bm9003332
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
This investigation describes the formulation and characterization of theologically 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 theological 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 theologically 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 delta < 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.
引用
收藏
页码:2427 / 2435
页数:9
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