In-situ phase transition from microemulsion to liquid crystal with the potential of prolonged parenteral drug delivery

Ren, Xiazhong; Svirskis, Darren; Alany, Raid G.; Zargar‐Shoshtari, Sara; Wu, Zimei

doi:10.1016/j.ijpharm.2012.04.020

Cited by 41 publications

(18 citation statements)

References 18 publications

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“…Therefore, the inhibitory profile in relation to the mucoadhesive properties was presented by S. Infected animals produced excess vaginal discharge that came into contact with the system and promoted membership in the vaginal mucosa, there by stimulating a direct interaction of the active principle with the mucous membranes and triggering a direct release at the desired site of action [29,30,31]. …”

Section: Discussionmentioning

confidence: 99%

Syngonanthus nitens Bong. (Rhul.)-Loaded Nanostructured System for Vulvovaginal Candidiasis Treatment

Ramos

Toledo

Calixto

et al. 2016

IJMS

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Herbal-loaded drug delivery nanotechnological systems have been extensively studied recently. The antimicrobial activity of medicinal plants has shown better pharmacological action when such plants are loaded into a drug delivery system than when they are not loaded. Syngonanthus nitens Bong. (Rhul.) belongs to the Eriocaulaceae family and presents antiulcerogenic, antioxidant, antibacterial, and antifungal activity. The aim of this study was to evaluate the antifungal activity of Syngonanthus nitens (S. nitens) extract that was not loaded (E) or loaded (SE) into a liquid crystal precursor system (S) for the treatment of vulvovaginal candidiasis (VVC) with Candida albicans. The minimal inhibitory concentration (MIC) was determined by the microdilution technique. Additionally, we performed hyphae inhibition and biofilm tests. Finally, experimental candidiasis was evaluated in in vivo models with Wistar female rats. The results showed effective antifungal activity after incorporation into S for all strains tested, with MICs ranging from 31.2 to 62.5 μg/mL. Microscopic observation of SE revealed an absence of filamentous cells 24 h of exposure to a concentration of 31.2 μg/mL. E demonstrated no effective action against biofilms, though SE showed inhibition against biofilms of all strains. In the in vivo experiment, SE was effective in the treatment of infection after only two days of treatment and was more effective than E and amphotericin B. The S. nitens is active against Candida albicans (C. albicans) and the antifungal potential is being enhanced after incorporation into liquid crystal precursor systems (LCPS). These findings represent a promising application of SE in the treatment of VVC.

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Section: Discussionmentioning

confidence: 99%

Syngonanthus nitens Bong. (Rhul.)-Loaded Nanostructured System for Vulvovaginal Candidiasis Treatment

Ramos

Toledo

Calixto

et al. 2016

IJMS

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“…The bag was immersed into a flask containing 200 ml dissolution medium (PBS/propylene glycol, 60:40) that was placed in an agitating water bath. We used 40 % propylene glycol in the receptor phase since previous studies used receptor phases containing up to 50 % propylene glycol for in vitro release and ex vivo penetration experiments (10)(11)(12). The system was maintained at 37 ± 0.5 o C and agitated at 60 rpm.…”

Section: In Vitro Drug Releasementioning

confidence: 99%

Solid Lipid Nanoparticles and Nanostructured Lipid Carriers of Loratadine for Topical Application: Physicochemical Stability and Drug Penetration through Rat Skin

Üner¹,

Karaman²,

Aydoğmuş³

2014

Trop. J. Pharm Res

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Purpose: To prepare solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) of loratadine (LRT) for the treatment of allergic skin reactions. (> 90.67 %). LRT was compatible with the other excipients after 6 months. Particle size did not significantly alter particularly at RT. The highest release rate was obtained with NE (1.339 ± 0.026 mcg/ml/h) followed by NLC (1.007 ± 0.011 mcg/ml/h) and SLN (0.821 ± 0.012 mcg/ml/h), indicating anomalous transport (p < 0.05). Penetration profiles of LRT through skin were statistically similar for SLN and NLC (p > 0.05

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“…[23][24][25][26][27] Depending on the amount of water in the mesophase, the properties of the solid and liquid states are combined in different ways to create a phase with 1 of 3 structures: lamellar, hexagonal, or cubic. [28][29][30] This drug delivery technology can control the speed and extension of drug release at the administration site and provide stability against disintegration in the biological environment. 31,32 Although FPS based on MO enable drugs of different polarities and molecular weight to be carry within their compartments, 33 the release efficiency of poorly water-soluble drugs is low.…”

Section: Introductionmentioning

confidence: 99%

The Monoglyceride Content Affects the Self-Assembly Behavior, Rheological Properties, Syringeability, and Mucoadhesion of In Situ–Gelling Liquid Crystalline Phase

Nunes

Teixeira

Kaminski

et al. 2016

Journal of Pharmaceutical Sciences

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This article reports the development of a precursor liquid crystalline system based on a mixture of monoglycerides (MO) and Cremophor(®) (CREM) that exhibits in situ gelation to a liquid crystalline phase. The effects of different MO/CREM ratios and the water content (WC) on several performance characteristics were investigated with a full factorial design. The formulations were characterized by polarized light microscopy, small-angle X-ray scattering, and water uptake assays. Rheological, syringeability, and mucoadhesion evaluation were also performed. The polarized light microscopy and small-angle X-ray scattering results for average and high MO/CREM ratios (2.1 and 4.0, respectively) indicated the coexistence of phases in transition to the liquid crystalline phase, independently of the WC. These systems became more viscous after taking up water, showing peaks characteristic of a cubic phase. Systems that had average and high MO/CREM ratios also exhibited shear-thinning behavior and high elasticity. Most systems showed suitable mucoadhesion for buccal purposes. Response surface methodology results demonstrated that the relative contribution of MO was the principal factor that affected the performance of the system. Accordingly, these precursor systems with average to high MO/CREM ratios and an average WC (10% w/w) demonstrated physicochemical and mucoadhesive properties that could enable them to be used as an in situ-gelling controlled drug delivery platform.

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In-situ phase transition from microemulsion to liquid crystal with the potential of prolonged parenteral drug delivery

Cited by 41 publications

References 18 publications

Syngonanthus nitens Bong. (Rhul.)-Loaded Nanostructured System for Vulvovaginal Candidiasis Treatment

Syngonanthus nitens Bong. (Rhul.)-Loaded Nanostructured System for Vulvovaginal Candidiasis Treatment

Solid Lipid Nanoparticles and Nanostructured Lipid Carriers of Loratadine for Topical Application: Physicochemical Stability and Drug Penetration through Rat Skin

The Monoglyceride Content Affects the Self-Assembly Behavior, Rheological Properties, Syringeability, and Mucoadhesion of In Situ–Gelling Liquid Crystalline Phase

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