Preparation Characterization Evaluation of Miconazole-Cyclodextrin Complexes for Improved Oral Topical Delivery

Tenjarla, Srini; Puranajoti, Porranee; Kasina, Ram; Mandal, Tarun K.

doi:10.1021/js970361l

Cited by 89 publications

(33 citation statements)

References 17 publications

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“…The signiˆcant ( p＜0.05) decrease in ‰ux value of BCD-colchicine formulation suggests depot-forming ability of formulation. Similarly, Tenjarla et al 28) and Simeoni et al 29) reported reduced skin permeation and increased skin accumulation of miconazole and oxybenzone by cyclodextrin complexation.…”

Section: Resultsmentioning

confidence: 89%

Preparation and in Vitro, in Vivo Characterization of Elastic Liposomes Encapsulating Cyclodextrin-Colchicine Complexes for Topical Delivery of Colchicine

2010

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In the present study, an attempt was made to develop a cyclodextrin-colchicine complex and to study its eŠect on skin permeation and deposition of colchicine. Colchicine b cyclodextrin (BCD) complex was prepared by freeze-drying method and complex formation was conˆrmed by NMR and in vitro drug release study. Formulation containing cyclodextrin-drug complex showed 6-fold increase in transdermal ‰ux in comparison with drug solution. Skin retention studies were carried out with the objective of determining the depot eŠect of elastic liposomes in skin. The amount of drug deposited was 12.4-fold higher in case of elastic liposomes of colchicine-cyclodextrin complex (567±1.5 mg) than drug solution (46±1.1 mg). The biological evaluation of various vesicular formulations and drug solution was carried out using monosodium urate-induced air pouch model. The results of anti-gout activity in rats showed better and sustained biological eŠects over 24 h measured in terms of exudate volume, reduction in leukocyte count, decrease in in‰ammatory cell accumulation, and collagen deposition with colchicine-BCD elastic liposomal formulation than drug solution. Hence the present study reveals that colchicine-cyclodextrin-elastic liposomes approach possesses good potential to enhance skin accumulation, prolong drug release, and improve the site-speciˆcity of colchicine.

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Section: Resultsmentioning

confidence: 89%

Preparation and in Vitro, in Vivo Characterization of Elastic Liposomes Encapsulating Cyclodextrin-Colchicine Complexes for Topical Delivery of Colchicine

2010

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“…The addition of citric acid along with b-cyclodextrin resulted in an increase in solubility of carvedilol to a much greater extent compared to complexation of the drug with b-cyclodextrin alone. This may be attributed to the fact that organic hydroxyl acids such as citric acid are able to enhance the solubility of the basic guest molecule both by forming a salt and by increasing the stability constant of the complex (11). Thus the addition of citric acid results in formation of carvedilol citrate salt (6).…”

Section: Phase Solubility Studiesmentioning

confidence: 99%

Ternary complexation of carvedilol, β-cyclodextrin and citric acid for mouth-dissolving tablet formulation

Patil

Gaikwad

2009

Acta Pharmaceutica

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Carvedilol is a non-selective beta-blocker indicated in the treatment of mild to moderate congestive heart failure. It is a basic, lipophilic compound. Being categorized as Class II compound as per the BCS classification system, it possesses very poor oral bioavailability and shows significant first pass metabolism (1). Thus, a strategy to improve bioavailability should aim at improving its aqueous solubility and overcoming first pass The purpose of this study was to improve the solubility and dissolution rate of carvedilol by forming a ternary complex with b-cyclodextrin and citric acid and to formulate its mouth-dissolving tablets. The rationale for preparing mouth-dissolving tablet of carvedilol was to make the drug available in a soluble form in the mouth, which would facilitate its absorption from the buccal cavity. This would help to overcome its first-pass metabolism and thereby improve bioavailability. Phase solubility studies revealed the ability of b-cyclodextrin and citric acid to complex with carvedilol and significantly increase its solubility. Ternary complexation of carvedilol was carried out with b-cyclodextrin and citric acid by physical mixing, kneading and spray drying methods and the prepared complexes were characterized by Fourier transform infra red spectroscopy, differential scanning calorimetry, powder X-ray diffractometry, scanning electron microscopy and complexation efficiency. The complex obtained by the spray drying method resulted in highest complexation efficiency and a 110-fold increase in the solubility of carvedilol. The mouth-dissolving tablets formulated using the spray dried complex with suitable excipients showed 100 % dissolution within five minutes. Accelerated stability studies of mouth-dissolving tablets carried out as per ICH guidelines revealed that the tablets were stable.

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“…[14][15][16] These systems have been shown to enhance the antifungal activity of miconazole. 4 To date, 17,18 Solid lipid nanoparticles (SLNs) were developed at the beginning of the 1990s as an alternative particulate delivery system to liposomes, emulsions, microparticles, and polymeric nanoparticulate systems. SLNs combine the advantages of those systems, such as controlled release, biodegradability, biocompatibility, and the protection of the incorporated drug against chemical degradation.…”

Section: Introductionmentioning

confidence: 99%

Miconazole-loaded solid lipid nanoparticles: formulation and evaluation of a novel formula with high bioavailability and antifungal activity

Aljaeid¹,

Hosny²

2016

IJN

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Background and objective Miconazole is a broad-spectrum antifungal drug that has poor aqueous solubility (<1 µg/mL); as a result, a reduction in its therapeutic efficacy has been reported. The aim of this study was to formulate and evaluate miconazole-loaded solid lipid nanoparticles (MN-SLNs) for oral administration to find an innovative way to alleviate the disadvantages associated with commercially available capsules. Methods MN-SLNs were prepared by hot homogenization/ultrasonication. The solubility of miconazole in different solid lipids was measured. The effect of process variables, such as surfactant types, homogenization and ultrasonication times, and the charge-inducing agent on the particle size, zeta potential, and encapsulation efficiency were determined. Furthermore, in vitro drug release, antifungal activity against Candida albicans , and in vivo pharmacokinetics were studied in rabbits. Results The MN-SLN, consisting of 1.5% miconazole, 2% Precirol ATO5, 2.5% Cremophor RH40, 0.5% Lecinol, and 0.1% Dicetylphosphate, had an average diameter of 23 nm with a 90.2% entrapment efficiency. Furthermore, the formulation of MN-SLNs enhanced the antifungal activity compared with miconazole capsules. An in vivo pharmacokinetic study revealed that the bioavailability was enhanced by >2.5-fold. Conclusion MN-SLN was more efficient in the treatment of candidiasis with enhanced oral bioavailability and could be a promising carrier for the oral delivery of miconazole.

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Preparation Characterization Evaluation of Miconazole-Cyclodextrin Complexes for Improved Oral Topical Delivery

Cited by 89 publications

References 17 publications

Preparation and <i>in Vitro</i>, <i>in Vivo</i> Characterization of Elastic Liposomes Encapsulating Cyclodextrin-Colchicine Complexes for Topical Delivery of Colchicine

Preparation and <i>in Vitro</i>, <i>in Vivo</i> Characterization of Elastic Liposomes Encapsulating Cyclodextrin-Colchicine Complexes for Topical Delivery of Colchicine

Ternary complexation of carvedilol, β-cyclodextrin and citric acid for mouth-dissolving tablet formulation

Miconazole-loaded solid lipid nanoparticles: formulation and evaluation of a novel formula with high bioavailability and antifungal activity

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