A mucoadhesive, cyclodextrin-based vaginal cream formulation of itraconazole

François, M; Snoeckx, Eric; Putteman, Peter; Wouters, Fons; Proost, Eddy De; Delaet, Urbain; Peeters, Jef; Brewster, Marcus E.

doi:10.1208/ps050105

Cited by 55 publications

(25 citation statements)

References 18 publications

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“…The aqueous solubility of itraconazole at ambient temperature and neutral pH was recoded to be around 1 ng/ml. The solubility was found to undergo significant increase in acidic solution reaching 4 μg/ml in 0.1 N HCl at 25°C [27]. The data in Table 1 revealed an equilibrium solubility value of 12.4 μg/ml when determined in 0.1 N HCl, at 37°C (Table 1).…”

Section: Drug Content and Equilibrium Solubilitymentioning

confidence: 94%

Synergistic Enhancement of Itraconazole Dissolution by Ternary System Formation with Pluronic F68 and Hydroxypropylmethylcellulose

Maghraby

2009

Sci. Pharm.

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Pluronic F68 is a surfactant which can inhibit CYP3A4, an enzyme responsible for hepatic metabolism of many drugs including itraconazole. This study investigated the effect of incorporation of Pluronic F68 as a ternary component in solid dispersions of itraconazole with hydroxypropyl-methylcellulose (HPMC) on the dissolution rate of itraconazole. Binary solid dispersions with HPMC, reduced the drug crystallinity, increased the equilibrium solubility but showed slow dissolution. Binary dispersions with Pluronic produced eutectic systems but the increase in solubility and dissolution was lower than that of HPMC systems. Ternary system comprising optimum proportions of drug with Pluronic and HPMC enhanced the dissolution rate showing dissolution efficiency comparable to that obtained with the marketed product of itraconazole. The study thus presented a system capable of increasing the dissolution rate of itraconazole with a potential for increased oral bioavailability by inhibiting its pre-systemic metabolism as well.

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Section: Drug Content and Equilibrium Solubilitymentioning

confidence: 94%

Synergistic Enhancement of Itraconazole Dissolution by Ternary System Formation with Pluronic F68 and Hydroxypropylmethylcellulose

Maghraby

2009

Sci. Pharm.

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“…Thus, itraconazole appears to be a suitable candidate. Clinical investigations has already indicated that application of 5 g of a 2% itraconazole cream was very well tolerated and the drug was not systemically absorbed (Francois et al, 2003). As per the previous discussion, it was also worthy to use itraconazole for a successful development of VDDS considering its pK a (5.6) and normal vaginal pH (4-5).…”

Section: Selection Of Drug Candidatementioning

confidence: 82%

A vaginal drug delivery model

et al. 2016

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Efficient drug delivery at vaginal cavity is often a challenge owing to its peculiar physiological variations including vast differences in pH. Keeping in view this attribute of the target site, the current work was aimed at developing formulation strategies which could overcome this and successfully deliver molecules like itraconazole through SLNs. Optimized SLNs with the given composition was selected for further development into mucoadhesive and thermosensitive gel. Stearic acid and Compritol 888 (1:1, w/w ratio) as lipid, a mixture of 3% Poloxomer 188 and 0.5% sodium taurocholate as surfactant and organic to aqueous ratio of 10:50 was taken. Carbopol 934 and Pluronic F 127 were taken for the development of gel. Optimized gel exhibited a desired gelling temperature (35 C); viscosity (0.920 PaS) and appreciable in vitro drug release (62.2% in 20 h). MTT assay did not show any cytotoxic effect of the gel. When evaluated in vivo, it did not exhibit any irritation potential despite appreciable bioadhesion. A remarkable decrease in CFUs was also observed in comparison with control and marketed formulation when evaluated in rat infection model. Thus, the proposed study defines the challenges for developing a suitable formulation system overcoming the delivery barriers of the vaginal site.

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“…Then, the required amounts 2%, 4% and 8% w/w of the LPE was added to make a proper formula having the best anti-inflammatory activity. Finally the best percentage of the LPE extract was determined and physicochemical stabilities were evaluated [19].…”

Section: Cream Preparationmentioning

confidence: 99%

Evaluation Effect of Probiotic Cream in Carrageenan-Induced Inflammation Model in Male Rat Hind Paw

Saadatzadeh¹,

Karampour²,

Imari³

et al. 2018

Eurasian J Anal Chem

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Background:Inflammation is the first biological response produced by immune system against any infections or foreign allergen in order to protect the body. The main anti-inflammatory drugs that are used today are Non-steroidal anti-inflammatory drugs (NSAID), opioids, and corticosteroids. Despite the broad range of uses of these drugs, many side effects have been associated with their use such as digestive problems like ulcers and peptic bleeding. It has been suggested that products containing probiotics can be used as an effective anti-inflammatory drug, due to effects of Probiotics on immune responses such as reducing the inflammatory cytokines. In this study, we aim to investigate the anti-inflammatory effects of probiotics and to compare the effect with commonly used drugs such as Piroxicam and Calandula in an animal model. Method:In this experimental study, after preparation of topical probiotic cream, used Wistar male rats weighing 180-200 g were used and randomly divided into 6 groups; negative control, positive control (piroxicam & calandula) and 3 treatment groups (2%, 4% and 8% w/w of LPE). Three groups, each received different doses (2%, 4% and 8% w/w) of LPE cream by topical use was 30 minutes before injecting carrageenan into plantar side of hind paw of the rats. Piroxicam gel and Calandula ointment were studied as positive control for anti-inflammatory activity, respectively. Finally, to observe the anti-inflammatory effect, the rat paw edema was measured every 15 min in the first hour and then hourly for 5 hours. In the end, the volume of intact rat ҆ s paw was measured in all groups by using plethysmometer. In the study, the IL-6 levels was measured by the ELIZA method.Result: All groups under the administration of the probiotic extract of Lactobacillus Casei compared to the negative control group in the rat paw edema show significant difference (P<0.05). Dose 2% LPE (Lyophilized cell free Probiotic Extract), turned out to be less effective than 2% Piroxicam cream in reducing edema during the study. But there was no significant difference between the group receiving doses of 4% and 8% w/w. The 4% dose of LPE cream was selected as the most favorable. These effects may be due, at least in part, to the pro-inflammatory cytokine production of IL-6 and TNFα. Also, all the groups under the administration of probiotic extract of Lactobacillus Casei were compared to the Calandula Officinalis group in the male rat paw and it was seen that there was no significant difference between them. Conclusion:The results of this study showed that LPE cream can improve inflammation effects in hand paw edema. Saadatzadeh et al. / Evaluated Anti-inflammatory Effect of Probiotics Cream / 12

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A mucoadhesive, cyclodextrin-based vaginal cream formulation of itraconazole

Cited by 55 publications

References 18 publications

Synergistic Enhancement of Itraconazole Dissolution by Ternary System Formation with Pluronic F68 and Hydroxypropylmethylcellulose

Synergistic Enhancement of Itraconazole Dissolution by Ternary System Formation with Pluronic F68 and Hydroxypropylmethylcellulose

A vaginal drug delivery model

Evaluation Effect of Probiotic Cream in Carrageenan-Induced Inflammation Model in Male Rat Hind Paw

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