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Acetic and Acrylic Acid Molecular Imprinted Model Silicone Hydrogel Materials for Ciprofloxacin-HCl Delivery.

ABSTRACT: Contact lenses, as an alternative drug delivery vehicle for the eye compared to eye drops, are desirable due to potential advantages in dosing regimen, bioavailability and patient tolerance/compliance. The challenge has been to engineer and develop these materials to sustain drug delivery to the eye for a long period of time. In this study, model silicone hydrogel materials were created using a molecular imprinting strategy to deliver the antibiotic ciprofloxacin. Acetic and acrylic acid were used as the functional monomers, to interact with the ciprofloxacin template to efficiently create recognition cavities within the final polymerized material. Synthesized materials were loaded with 9.06 mM, 0.10 mM and 0.025 mM solutions of ciprofloxacin, and the release of ciprofloxacin into an artificial tear solution was monitored over time. The materials were shown to release for periods varying from 3 to 14 days, dependent on the loading solution, functional monomer concentration and functional monomer:template ratio, with materials with greater monomer:template ratio (8:1 and 16:1 imprinted) tending to release for longer periods of time. Materials with a lower monomer:template ratio (4:1 imprinted) tended to release comparatively greater amounts of ciprofloxacin into solution, but the release was somewhat shorter. The total amount of drug released from the imprinted materials was sufficient to reach levels relevant to inhibit the growth of common ocular isolates of bacteria. This work is one of the first to demonstrate the feasibility of molecular imprinting in model silicone hydrogel-type materials.

SUBMITTER: Hui A

PROVIDER: S-EPMC5448947 | biostudies-other | 2012 Jan

REPOSITORIES: biostudies-other

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Project description:BackgroundThe hydrogel based system is found to be rarely reported for the delivery of hydrophobic drug due to the incompatibility of hydrophilicity of the polymer network and the hydrophobicity of drug. This problem can be solved by preparing semi-interpenetrating network of cross-linked polymer for tuning the hydrophilicity so as to entrap the hydrophobic drugs. The current study is to develop a folic acid conjugated cross-linked pH sensitive, biocompatible polymeric hydrogel to achieve a site specific drug delivery. For that, we have synthesized a folic acid conjugated PEG cross-linked acrylic polymer (FA-CLAP) hydrogel and investigated its loading and release of curcumin. The formed polymer hydrogel was then conjugated with folic acid for the site specific delivery of curcumin to cancer cells and then further characterized and conducted the cell uptake and cytotoxicity studies on human cervical cancer cell lines (HeLa).ResultsIn this study, we synthesized folic acid conjugated cross-linked acrylic hydrogel for the delivery of hydrophobic drugs to the cancer site. Poly (ethyleneglycol) (PEG) diacrylate cross-linked acrylic polymer (PAA) was prepared via inverse emulsion polymerization technique and later conjugated it with folic acid (FA-CLAP). Hydrophobic drug curcumin is entrapped into it and investigated the entrapment efficiency. Characterization of synthesized hydogel was done by using Fourier Transform-Infrared spectroscopy (FT-IR), Transmission Electron Microscopy (TEM), Differential Scanning Calorimetry (DSC). Polymerization and folate conjugation was confirmed by FT-IR spectroscopy. The release kinetics of drug from the entrapped form was studied which showed initial burst release followed by sustained release due to swelling and increased cross-linking. In vitro cytotoxicity and cell uptake studies were conducted in human cervical cancer (HeLa) cell lines.ConclusionsResults showed that curcumin entrapped folate conjugated cross-linked acrylic polymer (FA-CLAP) hydrogel showed higher cellular uptake than the non folate conjugated form. So this can be suggested as a better delivery system for site specific release of hydrophobic cancer drugs.

Project description:PurposeTo compare the subjective performances of verofilcon A daily disposable silicone hydrogel contact lenses (CLs) and etafilcon A hydrogel CLs.MethodsSuccessful wearers of spherical soft CLs for distance correction were prospectively randomized to wear verofilcon A or etafilcon A lenses for 1 week and crossed over to the alternative lenses. The primary study objective was a comparison of distance visual acuity (VA). Exploratory endpoints included subjective overall lens preference (5-point scale) and subjective ratings (10-point scales) of end-of-day (EOD) vision, overall handling, insertion comfort, EOD comfort, overall quality of vision, overall comfort, vision throughout the day, lens handling at insertion, and lens handling at removal.ResultsOf 92 subjects (184 eyes), 46 each were randomized to verofilcon A or etafilcon A lenses and subsequently crossed over to the other lenses. Evaluation of distance VA showed that verofilcon A lenses were noninferior to etafilcon A lenses. Comparison of lens preference showed that 68 (73.9%) subjects somewhat or strongly preferred verofilcon A lenses, whereas 21 (22.9%) somewhat or strongly preferred etafilcon A lenses (p<0.0001). Mean ± SD ratings of EOD vision (8.6±1.5 vs 7.7±1.9), overall handling (8.7±1.5 vs 6.9±2.3), insertion comfort (9.2±1.0 vs 7.7±1.9), and EOD comfort (8.0±1.9 vs 7.0±2.2) were all significantly (p≤0.0001 each) higher for verofilcon A than for etafilcon A lenses. Mean ± SD ratings of overall quality of vision (8.9±1.2 vs 8.2±1.8), overall comfort (8.6±1.5 vs 7.4±1.8), vision throughout the day (8.9±1.3 vs 8.1±1.8), lens handling at insertion (9.0±1.4 vs 6.9±2.5), and lens handling at removal (8.3±2.1 vs 7.7±2.2) were also significantly higher for verofilcon A lenses. No subject experienced any ocular adverse events.ConclusionAfter 1 week of wear, the study population reported that ratings for subjective endpoints were significantly higher for verofilcon A lenses than for etafilcon A lenses.

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Acetic and Acrylic Acid Molecular Imprinted Model Silicone Hydrogel Materials for Ciprofloxacin-HCl Delivery.

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