A thermosensitive vaginal gel formulation with HPγCD for the pH-dependent release and solubilization of amphotericin B

Kim, Ye-Tae; Shin, Baek-Ki; Garripelli, Vivek Kumar; Kim, Jin‐Ki; Davaa, Enkhzaya; Jo, Seong Mu; Park, Jeong Sook

doi:10.1016/j.ejps.2010.07.009

Cited by 71 publications

(62 citation statements)

References 31 publications

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“…Aiming to confirm the formation of inclusion complexes and gain insight into the TSC/CD interactions, samples of different complexes were studied by ATR/FT-IR spectroscopy and compared to pure TSCs and PMs (41,42). The characteristic bands of -NH streching of the terminal -NH 2 group for TSC1, TSC2 and TSC3 were found at 3375.4-3371.4 and 3263.3-3259.3 cm −1 , and the band of -NH-C (S)-NH 2 streching at 3153.4-3149.4 cm −1 , respectively.…”

Section: Tsc/cd Interactionmentioning

confidence: 99%

Novel 1-indanone Thiosemicarbazone Antiviral Candidates: Aqueous Solubilization and Physical Stabilization by Means of Cyclodextrins

2011

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Section: Tsc/cd Interactionmentioning

confidence: 99%

Novel 1-indanone Thiosemicarbazone Antiviral Candidates: Aqueous Solubilization and Physical Stabilization by Means of Cyclodextrins

2011

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“…In 1009 vivo local drug residence experiments were performed on female ICR mice. Carrageenan resulted to prolong significantly local residence of acyclovir and to have a synergistic bioadhesive effect with Carbopol.Other authors[120] studied a vaginal gel using a novel pluronic-based multiblock copolymer derivative (MBCP-2) for the vaginal delivery of…”

mentioning

confidence: 99%

“…The changes in hormonal 115 levels are responsible for the decrease in vaginal fluids and glycogen 116 concentration, so that the environment becomes hostile to the protec- 117 tive lactobacilli that are responsible for lactic acid production and, as a 118 consequence, vaginal pH increases. The environment faced by drug 119 delivery systems can therefore vary depending on hormonal changes, 120 but also on sexual intercourses or pathological conditions, with possible 121 consequences in their performance. 122 3.…”

mentioning

confidence: 99%

Mucoadhesive and thermogelling systems for vaginal drug delivery

Caramella

Rossi

Ferrari

et al. 2015

Advanced Drug Delivery Reviews

217

148

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“…There was no evidence of melting in AmB up to 250°C, because this antibiotic has already decomposed, which could be observed in the DSC thermogram for AmB (double broad endotherms at ~170 and 210°C) and was identical to that of the previous report. 42 MPEG-PCL-g-PEI showed a broad endothermic peak at ~47°C, while the DSC scan of AmB/MPEG-PCL-g-PEI micelles did not show any signs of AmB endothermic peak, indicating the formation of an amorphous state and the molecular encapsulation of the drug inside the core-shell structure.…”

mentioning

confidence: 99%

Preparation, characterization, and evaluation of amphotericin B-loaded MPEG-PCL-g-PEI micelles for local treatment of oral <em>Candida albicans</em>

Zhou¹,

Zhang²,

Chen³

et al. 2017

IJN

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Fatal Candida albicans infections in the mucosal system can occur in association with immune-compromised diseases and dysbacteriosis. Currently, amphotericin B (AmB) is considered to be the most effective antibiotic in the treatment of C. albicans infections, but its clinical application is limited by side effects and poor bioavailability. In order to use AmB in the local treatment of oral C. albicans infections, AmB/MPEG-PCL-g-PEI (monomethoxy poly(ethylene glycol)-poly(epsilon-caprolactone)-graft-polyethylenimine, MPP) micelles were prepared. A series of characterizations were performed. The micelles allowed a sustained in vitro release in both normal oral conditions (pH 6.8) and C. albicans infection conditions (pH 5.8). Then, buccal tablets containing freeze-dried powder of AmB/MPP micelles were produced by direct compression process and evaluated as regards to weight variation, hardness, and friability. In vitro drug release of the buccal tablets was measured in both the United States Pharmacopeia dissolution apparatus and the dissolution rate test apparatus, which was previously designed for simulating in vivo conditions of the oral cavity. The buccal tablets could sustainably release within 8 h and meet the antifungal requirements. Regarding safety assessment of AmB/MPP micelles, in vivo histopathological data showed no irritation toward buccal mucosa of the rats in both optical microscopy and ultrastructure observation of the tissues. MTT experiment proved that AmB/MPP micelles reduced the cytotoxicity of AmB. The micelles delivered through the gastrointestinal route were also found to be non-systemic toxicity by liquid chromatography-mass spectrometry analysis. Furthermore, the antifungal action of AmB/MPP micelles was evaluated. Although AmB/MPP had no obvious improvement as compared to AmB alone in the antifungal effect on planktonic C. albicans , the micelles significantly enhanced the antifungal activity against the biofilm state of C. albicans . Thus, it was concluded that AmB/MPP micelles represent a promising novel drug delivery system for the local treatment of oral C. albicans infections.

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A thermosensitive vaginal gel formulation with HPγCD for the pH-dependent release and solubilization of amphotericin B

Cited by 71 publications

References 31 publications

Novel 1-indanone Thiosemicarbazone Antiviral Candidates: Aqueous Solubilization and Physical Stabilization by Means of Cyclodextrins

Novel 1-indanone Thiosemicarbazone Antiviral Candidates: Aqueous Solubilization and Physical Stabilization by Means of Cyclodextrins

Mucoadhesive and thermogelling systems for vaginal drug delivery

Preparation, characterization, and evaluation of amphotericin B-loaded MPEG-PCL-g-PEI micelles for local treatment of oral <em>Candida albicans</em>

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