Gel-microemulsions as vaginal spermicides and intravaginal drug delivery vehicles

D’Cruz, Osmond J.; Uckun, Fatih M.

doi:10.1016/s0010-7824(01)00233-5

Cited by 91 publications

(61 citation statements)

References 45 publications

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“…The incorporated extracts were prepared in accordance with the methods of D'Cruz et al 19 and D'Cruz and Uckun 48 for the purpose of improving the pharmacological properties of the extracts. Thus, the results found in this study confirm the assertion that the incorporation of bioactive compounds into nanostructured lipid systems for drug delivery enhances the action in comparison to the free form of the same bioactive compounds.…”

Section: In Vivo Experiments Of a Urundeuva Leavesmentioning

confidence: 99%

Nanostructured lipid system as a strategy to improve the anti-Candida albicans activity of Astronium sp.

Bonifácio¹,

Ramos²,

Silva³

et al. 2015

IJN

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The genus Astronium (Anacardiaceae) includes species, such as Astronium fraxinifolium , Astronium graveolens , and Astronium urundeuva , which possess anti-inflammatory, anti-ulcerogenic, healing, and antimicrobial properties. Nanostructured lipid systems are able to potentiate the action of plant extracts, reducing the required dose and side effects and improving antimicrobial activity. This work aims to evaluate a nanostructured lipid system that was developed as a strategy to improve the anti- Candida albicans activity of hydroethanolic extracts of stems and leaves from Astronium sp. The antifungal activity against C. albicans (ATCC 18804) was evaluated in vitro by a microdilution technique. In addition to the in vitro assays, the Astronium sp. that showed the best antifungal activity and selectivity index was submitted to an in vivo assay using a model of vulvovaginal candidiasis infection. In these assays, the extracts were either used alone or were incorporated into the nanostructured lipid system (comprising 10% oil phase, 10% surfactant, and 80% aqueous phase). The results indicated a minimal inhibitory concentration of 125.00 µg/mL before incorporation into the nanostructured system; this activity was even more enhanced when this extract presented a minimal inhibitory concentration of 15.62 µg/mL after its incorporation. In vivo assay dates showed that the nanostructure-incorporated extract of A. urundeuva leaves was more effective than both the unincorporated extract and the antifungal positive control (amphotericin B). These results suggest that this nanostructured lipid system can be used in a strategy to improve the in vitro and in vivo anti- C. albicans activity of hydroethanolic extracts of Astronium sp.

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Section: In Vivo Experiments Of a Urundeuva Leavesmentioning

confidence: 99%

Nanostructured lipid system as a strategy to improve the anti-Candida albicans activity of Astronium sp.

Bonifácio¹,

Ramos²,

Silva³

et al. 2015

IJN

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“…16,17 The orientation for oil-in-water (O/W) or water-in-oil (W/O) depends on the surfactant and oil physicochemical properties, on the relation between surfactant/cosurfactant proportions, as well as water/oil proportions. 18,19 Lately, the search for bioactive compounds has increased, and according to the literature the adsorption of extracts and molecules with lipophilic nature or lipids, as well as vegetable oils, can be enhanced when combined to nanocarriers. 20,21 Some vegetable oils obtained from seeds hold interesting amounts of bioactive compounds, and therefore have become an important field of research.…”

Section: Introductionmentioning

confidence: 99%

Microemulsion of Brazil nut oil as a natural product to improve superoxide release in human phagocytes

et al. 2017

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The aim of this study was to develop and characterize a Brazil nut oil microemulsion system and determine the effect of this microemulsion on the superoxide release in human phagocytes. The microemulsion was formulated using distilled water, Brazil nut as the oily phase, Sorbitan monooleate, Polysorbate 80, and butan-1-ol. Hydrophile-lipophile balance of Brazil nut oil was determined, pseudoternary diagrams were prepared, and microemulsion diagram regions were preselected. Preliminary and accelerated stability tests, rheological characterization and dynamic light scattering were performed. The immunomodulatory effect of the microemulsion on the interactions with leukocytes was determined by superoxide release. The developed formulations were classified as oil-in-water, showed a Newtonian profile, with linear viscosity and droplet sizes of 46.9; 66.5 and 34.3 nm. When we assessed the interaction of the microemulsion of Brazil nut oil with phagocytes, we observed an increase in superoxide release. Our findings indicate that the developed formulation improved the immunomodulatory activity of the Brazil nut oil, proving to be a natural product option for future applications, in particular for infectious diseases.

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“…13,26 The ingredients selected included drug solubilizers and stabilizers (PEG, polysorbate 80, and Sorbitol), and a preservative (sodium benzoate). A polymer suspension of microcrystalline cellulose (Avicel) and xanthan gum (Xantural 75) were selected as a thickening agent additive to the lipid-based system to obtain a gel with desirable viscosity and compatibility with vaginal mucosa.…”

Section: Gel Formulationmentioning

confidence: 99%

Conceival, a novel noncontraceptive vaginal vehicle for lipophilic microbicides

2005

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The objective of this study was to develop a nontoxic and noncontraceptive vaginal drug delivery vehicle for lipophilic anti-human immunodeficiency virus (HIV) microbicides. Three representative poorly water-soluble novel broad-spectrum anti-HIV microbicides, PHI-113, PHI-346, and PHI-443, were evaluated in 11 different solvent systems. Based on their solubility profiles, a novel nonspermicidal self-emulsifying gel (viz Conceival) composed of pharmaceutical excipients, sorbitol, polyethylene glycol 400, polysorbate 80, microcrystalline cellulose, xanthan gum, and water was optimized. Conceival enhanced the solubility of these poorly water-soluble (<0.001 mg/mL) anti-HIV drugs by at least 150-to 270-fold. Conceival was evaluated in vivo in the New Zealand white rabbit model for the preservation of sperm function based on pregnancy outcome and the potential for vaginal irritation following single and multiple intravaginal applications, respectively. Conceival administered intravaginally immediately prior to artificial insemination with semen had no adverse effects on subsequent reproductive performance, neonatal survival, or pup development when compared with untreated control group. Histologic evaluation of vaginal tissues of rabbits exposed intravaginally to Conceival for 14 consecutive days revealed lack of epithelial, submucosal, and vascular changes at the gel application site (total irritation score <3 out of a possible 16). These findings indicate that Conceival has potential to become a clinically useful, safe noncontraceptive vaginal vehicle for lipophilic microbicides.

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Gel-microemulsions as vaginal spermicides and intravaginal drug delivery vehicles

Cited by 91 publications

References 45 publications

Nanostructured lipid system as a strategy to improve the anti-Candida albicans activity of Astronium sp.

Nanostructured lipid system as a strategy to improve the anti-Candida albicans activity of Astronium sp.

Microemulsion of Brazil nut oil as a natural product to improve superoxide release in human phagocytes

Conceival, a novel noncontraceptive vaginal vehicle for lipophilic microbicides

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Gel-microemulsions as vaginal spermicides and intravaginal drug delivery vehicles

Cited by 91 publications

References 45 publications

Nanostructured lipid system as a strategy to&nbsp;improve the anti-Candida albicans activity of&nbsp;Astronium sp.

Nanostructured lipid system as a strategy to&nbsp;improve the anti-Candida albicans activity of&nbsp;Astronium sp.

Microemulsion of Brazil nut oil as a natural product to improve superoxide release in human phagocytes

Conceival, a novel noncontraceptive vaginal vehicle for lipophilic microbicides

Contact Info

Product

Resources

About

Nanostructured lipid system as a strategy to improve the anti-Candida albicans activity of Astronium sp.

Nanostructured lipid system as a strategy to improve the anti-Candida albicans activity of Astronium sp.