Formulation and in-vitro efficacy of antifungal mucoadhesive polymeric matrices for the delivery of miconazole nitrate

Tejada, Guillermo Martínez de; Piccirilli, Gisela N.; Sortino, Maximiliano; Salomón, Claudio J.; Lamas, María Celina; Leonardi, Darío

doi:10.1016/j.msec.2017.05.034

Cited by 52 publications

(26 citation statements)

References 62 publications

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“…The development of pharmaceutical forms begins with the preformulation process, which establishes the physical and chemical, pharmaceutical and technological, pharmacological and toxicological features of substances [ 1 ]. As an active pharmaceutical ingredient, miconazole nitrate (MN) is a broad spectrum antifungal agent which has already been studied in the form of mucoadhesive tablets, polymeric matrices (chitosan, gelatine, gum arabic, alginate, carbopol or acrylic resins), microgels, nano-lipid gels or nano-vesicles formulated to treat oral or vaginal candidiasis [ 2 , 3 , 4 , 5 , 6 , 7 ]. In addition to its antifungal activity, MN also has an antimicrobial action—the imidazole class, which makes it frequently applied on skin mucosa to heal fungal infections [ 8 ].…”

Section: Introductionmentioning

confidence: 99%

Development of Dermal Films Containing Miconazole Nitrate

et al. 2018

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This study aims to develop new antifungal dermal films based on their mechanical properties (elongation, adhesion, behaviour towards vapour moisture) and the in vitro availability of miconazole nitrate, used as a pharmaceutical active ingredient in various concentrations. The three polymeric films prepared were translucent or shiny, with the surface of 63.585 cm2, 0.20–0.30 mm thickness, and content of miconazole nitrate of 3.931 or 15.726 mg·cm2. The mechanical resistance and elongation tests demonstrated that the two films based on hydroxyethyl cellulose (HEC) polymer were more elastic than the one prepared with hydroxypropyl methylcellulose (HPMC). The vapour water absorption and vapour water loss capacity of the films revealed that the HPMC film did not dry very well in the process of preparation by the evaporation of the solvent technique, unlike the HEC films that jellified more evenly in water and had higher drying capacity at 40 °C. The in vitro availability of miconazole nitrate from dermal films was evaluated using the Franz diffusion cell method, through a synthetic membrane (Ø 25 mm × 0.45 µm) and acceptor media with pH 7.4 (phosphate buffer and sodium lauryl sulphate 0.045%), resulting a release rate of up to 70%.

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Section: Introductionmentioning

confidence: 99%

Development of Dermal Films Containing Miconazole Nitrate

et al. 2018

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“…The patches of respective composition, as shown in Table 1 prepared by the solvent casting method. 8 The buccal mucoadhesive patch was prepared using HPMC K15LV, PVP as polymers and CP as a mucoadhesive polymer, PEG 400 as a plasticizer and permeation enhancer and poloxamer as a surfactant. The solvent system used was 50:50 ratios of methanol.…”

Section: Methods Of Preparationmentioning

confidence: 99%

Formulation and Evaluation of Mucoadhesive Patches of Ivabradine Hydrochloride

Roy¹,

Sowmya²,

Srija³

et al. 2018

Int. Res. J. Pharm.

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The objective of this study was to develop a mucoadhesive buccal patch of Ivabradine hydrochloride using mucoadhesive polymers such as carbopol, poloxamer, and HPMC 15LV. During this study polyvinylpyrrolidone, ethyl cellulose considered as a thickening agent or rate controlling polymer. A total number of five formulations were prepared by a solvent evaporation method. The prepared mucoadhesive patches were evaluated for in-vitro dissolution, drug content, folding endurance, mucoadhesive strength, swelling index, and drug-polymer interaction study. From the present study, it found that the mean thickness of the buccal polymeric patches increased with an increase in the amount of polymer percent. Percent swelling index determined at 2, 4, 6 and 8 hrs increased with time and with an increase in the polymer. The in-vitro study was performed by phosphate buffer PH 6.8 in Franz diffusion cell. During the study, it was also found that an increase in the amount of polymer retarded the release of the drug. Formulation F3 released 100% of the drug in 10 hrs of time. There was no such interaction found between drug and excipients.

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“…The ATR-FTIR spectrum of CH ( Figure 2Ab) showed a typical band between 3000-3600 cm -1 , concerned with -OH groups, which is broad due to overlapping with the stretching band of -NH (Pawlak and Mucha, 2003). Other bands were also observed centered at: 2925 cm -1 (stretching vibration of C─H bond); 1643cm -1 (amide I); 1595 cm -1 (NH 2 bending) (Tejada et al, 2017b); 1418 cm -1 (carboxyl -COOH) (Li et al, 2005); 1326 cm −1 (Amide III) (Kumar et al, 2017); 1150 cm -1 (stretching of the C-O-C bridge); 1060 cm -1 and 1020 cm -1 associated to the C-O stretching vibration (Espinosa-Andrews et al, 2010); and finally the band at 892 cm -1 assigned to the absorption peaks of β-(1,4) glycosidic unions in CH (Yue et al, 2009).…”

Section: Mechanical Propertiesmentioning

confidence: 97%

“…Films (containing 135 mg TCZ) were fixed to the central shaft using cyanoacrylate adhesive (Pharmacopoeia, 2017;Shaker et al, 2018;Tejada et al, 2017b). CFU/mL) and by streaking the plate surface in three directions.…”

Section: Dissolution Studiesmentioning

confidence: 99%

Chitosan-hydroxypropyl methylcellulose tioconazole films: A promising alternative dosage form for the treatment of vaginal candidiasis

Calvo

Svetaz

Álvarez

et al. 2019

International Journal of Pharmaceutics

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Vaginal candidiasis is considered a frequent opportunistic mucosal infection and the second most common cause of vaginitis after bacterial vaginosis. In this work, different vaginal films based on chitosan, hydroxypropyl methylcellulose and blends of these polymers containing tioconazole, were developed and thoroughly characterized to improve the conventional therapeutics of vaginal candidiasis. Mechanical properties, swelling, adhesiveness, morphology, antifungal activity, hemocompatibility and cytotoxicity were evaluated. The drug solid state in the films was analyzed by thermal and X-ray diffraction analysis. Films showed homogeneous surfaces and presented similar mechanical properties and adhesiveness. Time-kill studies displayed that films were more active than both tioconazole pure drug and traditional tioconazole ovule against Candida albicans, which is probably related to the fact that tioconazole is in amorphous state inside the films. Although all formulations proved to be hemocompatible, films based only on chitosan exhibited a certain degree of cytotoxicity and therefore they should be avoided. The system based on chitosan-hydroxypropyl methylcellulose with 40% PEG 400 as plasticizer presented fast antimicrobial activity as well as the lowest swelling. Additionally, this formulation did not produce substantial hemolytic and cytotoxic effects, indicating that films based on chitosan-hydroxypropyl methylcellulose could be a promising alternative dosage form for the treatment of vaginal candidiasis.

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Formulation and in-vitro efficacy of antifungal mucoadhesive polymeric matrices for the delivery of miconazole nitrate

Cited by 52 publications

References 62 publications

Development of Dermal Films Containing Miconazole Nitrate

Development of Dermal Films Containing Miconazole Nitrate

Formulation and Evaluation of Mucoadhesive Patches of Ivabradine Hydrochloride

Chitosan-hydroxypropyl methylcellulose tioconazole films: A promising alternative dosage form for the treatment of vaginal candidiasis

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