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

GP Andrews, L Donnelly, DS Jones, Rhonda M Curran, RJ Morrow, AD Woolfson, RK Malcolm

    Research output: Contribution to journalArticle

    43 Citations (Scopus)

    Abstract

    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 weremore 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 fluidssignificantly 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 siteretentiveplatforms for the sustained delivery of therapeutic agents to the vagina.
    LanguageEnglish
    Pages2427-2435
    JournalBiomacromolecules
    Volume10
    DOIs
    Publication statusPublished - 2009

    Fingerprint

    Vagina
    Gels
    Maleic Anhydrides
    Poloxamer
    Povidone
    Hardness
    Drug Delivery Systems
    Pharmaceutical Preparations
    Drug Liberation
    Therapeutics
    polyvinylmethoxyethylene-maleic anhydride copolymer
    hydroxyethylcellulose
    calcium polycarbophil

    Cite this

    Andrews, GP ; Donnelly, L ; Jones, DS ; Curran, Rhonda M ; Morrow, RJ ; Woolfson, AD ; Malcolm, RK. / Characterization of the Rheological, Mucoadhesive, and Drug Release Properties of Highly Structured Gel Platforms for Intravaginal Drug Delivery. In: Biomacromolecules. 2009 ; Vol. 10. pp. 2427-2435.
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    abstract = "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 weremore 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 fluidssignificantly 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 siteretentiveplatforms for the sustained delivery of therapeutic agents to the vagina.",
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    Characterization of the Rheological, Mucoadhesive, and Drug Release Properties of Highly Structured Gel Platforms for Intravaginal Drug Delivery. / Andrews, GP; Donnelly, L; Jones, DS; Curran, Rhonda M; Morrow, RJ; Woolfson, AD; Malcolm, RK.

    In: Biomacromolecules, Vol. 10, 2009, p. 2427-2435.

    Research output: Contribution to journalArticle

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    AB - 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 weremore 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 fluidssignificantly 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 siteretentiveplatforms for the sustained delivery of therapeutic agents to the vagina.

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