Electrospun cellulose acetate phthalate fibers for semen induced anti-HIV vaginal drug delivery

Huang, Chaobo; Soenen, Stefaan J.; Gulck, Ellen Van; Vanham, Guido; Rejman, Joanna; Calenbergh, Serge Van; Vervaet, Chris; Coenye, Tom; Verstraelen, Hans; Temmerman, Marleen; Demeester, Jo; Smedt, Stefaan C. De

doi:10.1016/j.biomaterials.2011.10.004

Cited by 151 publications

(92 citation statements)

References 29 publications

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“…Figure 6 shows a schematic illustration of the inhibitory action of CAP nanofibers containing the antiviral drugs. 120 Besides the commonly known implantable nanofibrous drug-delivery systems, few studies 84,123 have been published on the application of drug-loaded nanofibers as oral drug-delivery systems, which is the preferred route of drug administration from the aspects of convenience, patient compliance, and cost-effectiveness. Eudragit L 100-55 nanofibers containing diclofenac sodium, a nonsteroidal anti-inflammatory drug, were fabricated for oral drug-delivery purposes.…”

Section: Most Innovative Applicationsmentioning

confidence: 99%

Advances in drug delivery via electrospun and electrosprayed nanomaterials

Zamani¹,

Prabhakaran²,

Ramakrishna³

2013

IJN

204

104

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Electrohydrodynamic (EHD) techniques refer to procedures that utilize electrostatic forces to fabricate fibers or particles of different shapes with sizes in the nano-range to a few microns through electrically charged fluid jet. Employing different techniques, such as blending, surface modification, and coaxial process, there is a great possibility of incorporating bioactive such molecules as drugs, DNA, and growth factors into the nanostructures fabricated via EHD techniques. By careful selection of materials and processing conditions, desired encapsulation efficiency as well as preserved bioactivity of the therapeutic agents can be achieved. The drug-loaded nanostructures produced can be applied via different routes, such as implantation, injection, and topical or oral administration for a wide range of disease treatment. Taking advantage of the recent developments in EHD techniques like the coaxial process or multilayered structures, individually controlled delivery of multiple drugs is achievable, which is of great demand in cancer therapy and growth-factor delivery. This review summarizes the most recent techniques and postmodification methods to fabricate electrospun nanofibers and electrosprayed particles for drug-delivery applications.

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Section: Most Innovative Applicationsmentioning

confidence: 99%

Advances in drug delivery via electrospun and electrosprayed nanomaterials

Zamani¹,

Prabhakaran²,

Ramakrishna³

2013

IJN

204

104

View full text Add to dashboard Cite

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“…Moreover, microbicide films reported in literature have low drug loadings (less than 1.5 wt%) (6,7), which when coupled with their small dosage size limits their application to only highly potent antiretroviral (ARV) drugs. Recently, Ball et al and Huang et al demonstrated that electrospun fibers could release a range of active ARV drugs and spermicides (8) and that such release could occur in response to stimuli, such as a semen-induced rise in pH (9). Furthermore, Huang et al demonstrated high loading (15 wt%) of tenofovir disoproxil into electrospun fibers (9), which would reduce the required dosage size.…”

mentioning

confidence: 99%

“…Recently, Ball et al and Huang et al demonstrated that electrospun fibers could release a range of active ARV drugs and spermicides (8) and that such release could occur in response to stimuli, such as a semen-induced rise in pH (9). Furthermore, Huang et al demonstrated high loading (15 wt%) of tenofovir disoproxil into electrospun fibers (9), which would reduce the required dosage size.…”

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confidence: 99%

Electrospun Solid Dispersions of Maraviroc for Rapid Intravaginal Preexposure Prophylaxis of HIV

Ball

Woodrow

2014

Antimicrob Agents Chemother

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The development of topical anti-human immunodeficiency virus (HIV) microbicides may provide women with strategies to protect themselves against sexual HIV transmission. Pericoital drug delivery systems intended for use immediately before sex, such as microbicide gels, must deliver high drug doses for maximal effectiveness. The goal of achieving a high antiretroviral dose is complicated by the need to simultaneously retain the dose and quickly release drug compounds into the tissue. For drugs with limited solubility in vaginal gels, increasing the gel volume to increase the dose can result in leakage. While solid dosage forms like films and tablets increase retention, they often require more than 15 min to fully dissolve, potentially increasing the risk of inducing epithelial abrasions during sex. Here, we demonstrate that water-soluble electrospun fibers, with their high surface area-to-volume ratio and ability to disperse antiretrovirals, can serve as an alternative solid dosage form for microbicides requiring both high drug loading and rapid hydration. We formulated maraviroc at up to 28 wt% into electrospun solid dispersions made from either polyvinylpyrrolidone or poly(ethylene oxide) nanofibers or microfibers and investigated the role of drug loading, distribution, and crystallinity in determining drug release rates into aqueous media. We show here that water-soluble electrospun materials can rapidly release maraviroc upon contact with moisture and that drug delivery is faster (less than 6 min under sink conditions) when maraviroc is electrospun in polyvinylpyrrolidone fibers containing an excipient wetting agent. These materials offer an alternative dosage form to current pericoital microbicides.

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“…Huang et al 13 and Ball et al 14 have used electrospun fabrics with variety of antiretroviral drugs but never in combination. Combination drug delivery from electrospun fabrics can be achieved by the co-delivery of multiple drugs encapsulated within the same fiber or into separate fibers.…”

Section: Introductionmentioning

confidence: 99%

Delivery of multipurpose prevention drug combinations from electrospun nanofibers using composite microarchitectures

Blakney

Krogstad

Jiang

et al. 2014

IJN

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Background Electrospun drug-eluting fabrics have enormous potential for the delivery of physicochemically diverse drugs in combination by controlling the underlying material chemistry and fabric microarchitecture. However, the rationale for formulating drugs at high drug loading in the same or separate fibers is unknown but has important implications for product development and clinical applications. Methods Using a production-scale free-surface electrospinning instrument, we produced electrospun nanofibers with different microscale geometries for the co-delivery of tenofovir (TFV) and levonorgestrel (LNG) – two lead drug candidates for multipurpose prevention of HIV acquisition and unintended pregnancy. We investigated the in vitro drug release of TFV and LNG combinations from composites that deliver the two drugs from the same fiber (combined fibers) or from separate fibers in a stacked or interwoven architecture. For stacked composites, we also examined the role that fabric thickness has on drug-release kinetics. We also measured the cytotoxicity and antiviral activity of the drugs delivered alone and in combination. Results Herein, we report on the solution and processing parameters for the free-surface electrospinning of medical fabrics with controlled microarchitecture and high drug loading (up to 20 wt%). We observed that in vitro release of the highly water-soluble TFV, but not the water-insoluble LNG, was affected by composite microarchitecture, fabric thickness, and drug content. Finally, we showed that the drug-loaded nanofibers are noncytotoxic and that the antiviral activity of TFV is preserved through the electrospinning process and when combined with LNG. Conclusion Electrospun fabrics with high drug loading create multicomponent systems that benefit from the independent control of the nanofibrous microarchitecture. Our findings are significant because they will inform the design and production of composite electrospun fabrics for the co-delivery of physicochemically diverse drugs that may be useful for multipurpose prevention.

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Electrospun cellulose acetate phthalate fibers for semen induced anti-HIV vaginal drug delivery

Cited by 151 publications

References 29 publications

Advances in drug delivery via electrospun and electrosprayed nanomaterials

Advances in drug delivery via electrospun and electrosprayed nanomaterials

Electrospun Solid Dispersions of Maraviroc for Rapid Intravaginal Preexposure Prophylaxis of HIV

Delivery of multipurpose prevention drug combinations from electrospun nanofibers using composite microarchitectures

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