In Vitro and In Vivo Evaluation of Drug Release from Semisolid Dosage Forms

Petró, Éva; Csóka, IIdikó; Balogh, Attila; Blazsó, G; Erös, I.

doi:10.3797/scipharm.cespt.8.pdd08

Cited by 5 publications

(4 citation statements)

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“…The release of an active ingredient from dermatological preparations is significantly influenced by the partition coefficient between the vehicle and water, the solubility of the active substance in the acceptor medium and the vehicle, and the type of carrier and its viscosity. It is assumed that the release rate of the active compounds from hydrophobic bases or those in the form of emulsions is lower than that from hydrophilic vehicles and can be classified as follows: lipophilic ointment < O/W cream < hydrogel [ 45 , 46 ].…”

Section: Resultsmentioning

confidence: 99%

The Influence of Tea Tree Oil on Antifungal Activity and Pharmaceutical Characteristics of Pluronic® F-127 Gel Formulations with Ketoconazole

Wróblewska

Szymańska

Winnicka

2021

IJMS

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Fungal skin infections are currently a major clinical problem due to their increased occurrence and drug resistance. The treatment of fungal skin infections is based on monotherapy or polytherapy using the synergy of the therapeutic substances. Tea tree oil (TTO) may be a valuable addition to the traditional antifungal drugs due to its antifungal and anti-inflammatory activity. Ketoconazole (KTZ) is an imidazole antifungal agent commonly used as a treatment for dermatological fungal infections. The use of hydrogels and organogel-based formulations has been increasing for the past few years, due to the easy method of preparation and long-term stability of the product. Therefore, the purpose of this study was to design and characterize different types of Pluronic®F-127 gel formulations containing KTZ and TTO as local delivery systems that can be applied in cases of skin fungal infections. The influence of TTO addition on the textural, rheological, and bioadhesive properties of the designed formulations was examined. Moreover, the in vitro release of KTZ, its permeation through artificial skin, and antifungal activity by the agar diffusion method were performed. It was found that obtained gel formulations were non-Newtonian systems, showing a shear-thinning behaviour and thixotropic properties with adequate textural features such as hardness, compressibility, and adhesiveness. Furthermore, the designed preparations with TTO were characterized by beneficial bioadhesive properties. The presence of TTO improved the penetration and retention of KTZ through the artificial skin membrane and this effect was particularly visible in hydrogel formulation. The developed gels containing TTO can be considered as favourable formulations in terms of drug release and antifungal activity.

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Section: Resultsmentioning

confidence: 99%

The Influence of Tea Tree Oil on Antifungal Activity and Pharmaceutical Characteristics of Pluronic® F-127 Gel Formulations with Ketoconazole

Wróblewska

Szymańska

Winnicka

2021

IJMS

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“…, the nature of the vehicle, the solubility of the drug substance in a vehicle and acceptor medium, drug partition coefficient between the vehicle and the water, and the viscosity of the vehicle. Generally, it is considered that the release rate increases in the following order: lipophilic ointment < cream oil/water < gel [ 32 , 33 ].…”

Section: Resultsmentioning

confidence: 99%

The Effect of Cationic Polyamidoamine Dendrimers on Physicochemical Characteristics of Hydrogels with Erythromycin

Wróblewska

Winnicka

2015

IJMS

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Polyamidoamine dendrimers (PAMAM) represent a new class of hyperbranched, monodisperse, three-dimensional polymers with unique properties, which make them very promising carriers of antimicrobial agents. The present study aimed to evaluate the influence of PAMAM-NH2 dendrimers generation two (G2) or three (G3) on physicochemical characteristics and structure of hydrogels with a model antibacterial lipophilic drug—erythromycin—commonly used in topical applications. From the obtained rheograms, it can be concluded that tested hydrogels were non-Newtonian thixotropic systems with shear-thinning behaviour. The dissolution tests revealed that erythromycin was definitely faster released from formulations containing PAMAM-NH2 in concentration and generation dependent manner. However, the addition of PAMAM-NH2 to hydrogels evoked only slight improvement of their antibacterial activity. It was also shown that the structure of hydrogels changed in the presence of PAMAM-NH2 becoming less compact, diversified and more porous. Designed hydrogels with PAMAM-NH2 G2 or G3 were stable stored up to three months at 40 ± 2 °C and 75% ± 5% RH.

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“…The in vitro drug release data in case of two active agents were measured from different vehicles (hydrogel, organogel, w/o and o/w creams, o/w emulgels and w/o/w multiple emulsions) for dermal use. The presented compositions were developed by our research group earlier [12,13].…”

Section: Aimmentioning

confidence: 99%

The role of dissolution testing in quality control

Kovács

Petró

Erös

et al. 2014

Period. Polytech. Chem. Eng.

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Semisolid systems (creams, gels etc.) for dermal application get more and more importance in pharmaceutical and cosmetic industry. However the number of methodologies for their physico-chemical characterization have been increasing; development of methods for the measurement of the active agent's release onto the skin surface is still a challenging task. Beside measuring the amount of the active agent reaching the skin; dissolution testing (also called release testing) can be also a good indicator of product composition changes, therefore it can be used as quality control methodology. The purpose of this study was to investigate the in vitro drug release of active agents from hydrogels, organogels, o/w and w/o creams, emulgels and w/o/w multiple emulsions for dermal use by means of the vertical diffusion cell methodology, for quality control purposes.

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In Vitro and In Vivo Evaluation of Drug Release from Semisolid Dosage Forms

Cited by 5 publications

References 0 publications

The Influence of Tea Tree Oil on Antifungal Activity and Pharmaceutical Characteristics of Pluronic® F-127 Gel Formulations with Ketoconazole

The Influence of Tea Tree Oil on Antifungal Activity and Pharmaceutical Characteristics of Pluronic® F-127 Gel Formulations with Ketoconazole

The Effect of Cationic Polyamidoamine Dendrimers on Physicochemical Characteristics of Hydrogels with Erythromycin

The role of dissolution testing in quality control

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